Allergic diseases

HYPOALLERGENIC VARIANTS OF MAL D 1, THE MAJOR ALLERGEN FROM MALUS DOMESTICA (Fri, 03 Oct 2014)
<p id="p-0001" num="0000">Disclosed are hypoallergenic variants of Mal d 1, the major allergen from <i>Malus domestica</i>, and the uses thereof in the treatment of allergic diseases.</p>
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COMPOUND CAPABLE OF BINDING S1P RECEPTOR AND PHARMACEUTICAL USE THEREOF (Fri, 26 Sep 2014)
<p id="p-0001" num="0000">A compound having an ability to bind to an S1P receptor and represented by formula (I), a salt thereof, a solvate thereof or a prodrug thereof is useful for prevention and/or treatment of rejection of transplantation, graft-versus-host disease, autoimmune disease, allergic disease and the like:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="11.43mm" wi="69.85mm" file="US20140288034A1-20140925-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein ring A is a cyclic group; ring B is a cyclic group which may have substituent(s); X is a spacer having 1 to 8 atoms in its main chain, etc.; Y is a spacer having 1 to 10 atoms in its main chain, etc.; n is 0 or 1, wherein when n is 0, m is 1 and R<sup>1 </sup>is a hydrogen atom or a substituent, and wherein when n is 1, m is 0 or an integer of 1 to 7 and R<sup>1 </sup>is a substituent, and wherein m is 2 or more, R<sup>1</sup>s are the same or different.</p>
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COMPOSITION (Fri, 26 Sep 2014)
<p id="p-0001" num="0000">Compound (I), and pharmaceutically acceptable salts thereof, are inducers of human interferon. Certain discrete and particular dosages of Compound (I) may be particularly useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and allergic asthma.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="57.57mm" wi="69.93mm" file="US20140288099A1-20140925-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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NOVEL PYRROLO PYRIMIDINE DERIVATIVES (Fri, 29 Aug 2014)
<p id="p-0001" num="0000">The present invention describes new pyrrolo pyrimidine derivatives and pharmaceutically acceptable salts thereof which appear to interact with Bruton's tyrosine kinase (Btk). Accordingly, the novel pyrrolo pyrimidines may be effective in the treatment of autoimmune disorders, inflammatory diseases, allergic diseases, airway diseases, such as asthma and chronic obstructive pulmonary disease (COPD), transplant rejection, cancers e.g. of hematopoietic origin or solid tumors.</p>
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CHROMENE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Fri, 22 Aug 2014)
<p id="p-0001" num="0000">The present application describes modulators of MCP-1 or CCR-2 of formula</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="36.24mm" wi="57.57mm" file="US20140235672A1-20140821-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W<sup>1</sup>, W<sup>2</sup>, W<sup>3</sup>, Y, Z, R<sup>2</sup>, R<sup>3</sup>, R<sup>3′</sup> and R<sup>4</sup>, are defined in the specification. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.</p>
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PHARMACEUTICAL COMPOSITION FOR INFLAMMATORY DISEASES, ALLERGIC DISEASES AND AUTOIMMUNE DISEASES (Fri, 01 Aug 2014)
<p id="p-0001" num="0000">The present invention relates to methods and pharmaceutical compositions for immunosuppression by using the fatty acid derivative represented by formula (I). The present invention further relates to methods and pharmaceutical compositions for treating inflammatory diseases, allergic diseases and autoimmune diseases by using said fatty acid derivative.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.90mm" wi="55.96mm" file="US20140212441A1-20140731-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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RAPID CLEARANCE OF ANTIGEN COMPLEXES USING NOVEL ANTIBODIES (Fri, 01 Aug 2014)
<p id="p-0001" num="0000">The present invention relates to rapid clearance molecules that bind target antigens and FcγRIIb with increased affinity as compared to parent molecules, said compositions being capable of causing accelerated clearance of such antigens. Such compositions are useful for treating a variety of disorders, including allergic diseases, atherosclerosis, and a variety of other conditions.</p>
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RAPID CLEARANCE OF ANTIGEN COMPLEXES USING NOVEL ANTIBODIES (Fri, 25 Jul 2014)
The present invention relates to rapid clearance molecules that bind target antigens and FcyRMb with increased affinity as compared to parent molecules, said compositions being capable of causing accelerated clearance of such antigens. Such compositions are useful for treating a variety of disorders, including allergic diseases, atherosclerosis, and a variety of other conditions.
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NITROGEN-CONTAINING SPIROCYCLIC COMPOUNDS AND PHARMACEUTICAL USES THEREOF (Fri, 04 Jul 2014)
<p id="p-0001" num="0000">A compound of the following general formula [I]:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="43.01mm" wi="50.97mm" file="US20140187534A1-20140703-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein each symbol has the same meaning as defined herein, or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a pharmaceutical use of the same in treating organ transplant rejection, graft versus host reaction after transplantation, autoimmune disease, allergic disease and chronic myeloproliferative disease.</p>
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NOVEL BIS-CHROMONE DERIVATIVES, METHODS FOR THEIR PREPARATION AND USES THEREOF (Fri, 27 Jun 2014)
The invention relates to novel bis-chromone derivatives, methods for their preparation and their therapeutic application, especially in the treatment or prevention of disease involving mast cell activation, such as allergic disease. Provided is a compound according to the general Formula (I).
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1-PHENYL-2-PYRIDINYL ALKYL ALCOHOL DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS (Fri, 06 Jun 2014)
<p id="p-0001" num="0000">Compounds of formula (I) described herein are inhibitors of the phosphodiesterase 4 (PDE4) enzyme and are useful for the prevention and/or treatment of an allergic disease state or a disease of the respiratory tract characterized by airway obstruction.</p>
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NOVEL COMPOUNDS (Sat, 31 May 2014)
Compounds of formula (I) and salts thereof: wherein R1 is n-C4-6alkyl or C1-2alkoxyC1-2alkyl-; R2 is hydrogen or methyl; each R3 is hydroxy, halo or n-C1-3alkyl; m is an integer having a value of 2 to 4; n is an integer having a value of 0 to 3; and p is an integer having a value of 0 to 2, are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and asthma, infectious diseases and cancer, and may also be useful as vaccine adjuvants.
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NOVEL COMPOUNDS (Sat, 31 May 2014)
Compounds of formula (I) and salts thereof wherein R1 is n-C3-6alkyl; R2 is hydrogen or methyl; R3 is hydrogen or C1-6alkyl, and m is an integer having a value of 1 to 4; are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and asthma, infectious diseases and cancer, and may also be useful as vaccine adjuvants.
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NOVEL COMPOUNDS (Sat, 31 May 2014)
Compounds of formula (I) and salts thereof: wherein R1 is n-C3-6alkyl; R2 is hydrogen or methyl; R3 is hydrogen or C1-6alkyl, and m is an integer having a value of 0 to 3; are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and asthma, infectious diseases and cancer, and may also be useful as vaccine adjuvants.
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NEW MACROLIDES AND THEIR USE (Fri, 23 May 2014)
<p id="p-0001" num="0000">The invention relates to macrolide compounds of formula (I),</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="40.47mm" wi="36.83mm" file="US20140142100A1-20140522-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">the use of said compounds as medicaments, in particular for the treatment or prevention of inflammatory and allergic diseases, pharmaceutical compositions containing said compounds and to processes for their preparation. The invention relates in particular to macrolide compounds with antiinflammatory activity mediated primarily through inhibition of phosphodiesterase 4 (PDE4) which makes them useful for the treatment and/or prevention of inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, atopic dermatitis or inflammatory bowel disease or proliferative diseases such as cancer.</li> </ul> </li> </ul> </p>
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PHARMACEUTICAL COMPOSITION FOR INFLAMMATORY DISEASES, ALLERGIC DISEASES AND AUTOIMMUNE DISEASES (Thu, 15 May 2014)
The present invention relates to methods and pharmaceutical compositions for immunosuppression by using the fatty acid derivative represented by formula (I). The present invention further relates to methods and pharmaceutical compositions for treating inflammatory diseases, allergic diseases and autoimmune diseases by using said fatty acid derivative.
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SUBSTITUTED BENZIMIDAZOLES AND BENZOPYRAZOLES AS CCR(4) ANTAGONISTS (Fri, 02 May 2014)
<p id="p-0001" num="0000">Benzimidazole, benzopyrazole and benzotriazole compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.</p>
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Chemokine receptor antagonists and use thereof (Fri, 14 Mar 2014)
<p id="p-0001" num="0000">The present invention relates to a compound represented by formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="16.51mm" wi="54.36mm" file="US08871210-20141028-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein all symbols are as defined here, a salt thereof, a solvate thereof, or a prodrug thereof. The compound of the present invention has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, rejection of transplanted organ, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy. </p>
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Thienopyrazole derivative having PDE7 inhibitory activity (Fri, 14 Mar 2014)
<p id="p-0001" num="0000">To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="24.13mm" wi="52.15mm" file="US08901315-20141202-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> [wherein, especially, R<sup>1 </sup>is a cyclohexyl, a cycloheptyl group or a tetrahydropyranyl group; R<sup>2 </sup>is methyl; R<sup>3 </sup>is a hydrogen atom; and R<sup>4 </sup>is a group: —CONR<sup>5</sup>R<sup>6 </sup>(in which any one of R<sup>5 </sup>and R<sup>6 </sup>is a hydrogen atom)]. </p>
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NOVEL COMPOUNDS (Fri, 28 Feb 2014)
<p id="p-0001" num="0000">Compounds of formula (I) and salts thereof:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="44.28mm" wi="69.85mm" file="US20140056928A1-20140227-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein R<sub>1 </sub>is n-C<sub>1-6</sub>alkyl or C<sub>1-2</sub>alkoxyC<sub>1-2</sub>alkyl-, R<sub>2 </sub>is halo, OH or C<sub>1-3</sub>alkyl, m is an integer having a value of 4, 5, 6 or 7, n is an integer having a value of 0, 1, 2 or 3, and p is an integer having a value of 0, 1 or 2, are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and asthma, infectious diseases and cancer, and may also be useful as vaccine adjuvants.</p>
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PYRAZOLOPYRIMIDINE COMPOUNDS (Fri, 28 Feb 2014)
Compounds of formula (I) and salts thereof : wherein R1 is n-C1-6alkyl or C1-2alkoxyC1-2alkyl-, R2 is halo, OH or C1-3alkyl, m is an integer having a value of 4, 5, 6 or 7, n is an integer having a value of 0, 1, 2 or 3, and p is an integer having a value of 0, 1 or 2, are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and asthma, infectious diseases and cancer, and may also be useful as vaccine adjuvants.
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Compounds Having CRTH2 Antagonist Activity (Fri, 07 Feb 2014)
<p id="p-0001" num="0000">Compounds of general formula (II)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="48.01mm" wi="69.85mm" file="US20140039012A1-20140206-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000">W is chloro or fluoro;</li> <li id="ul0001-0002" num="0000">R<sup>1 </sup>is phenyl optionally substituted with one or more substituents, selected from halo, —CN, —C<sub>1-</sub>C<sub>6 </sub>alkyl, —SOR<sup>3</sup>, —SO<sub>2</sub>R<sup>3</sup>, —SO<sub>2</sub>N(R<sup>2</sup>)<sub>2</sub>, —N(R<sup>2</sup>)<sub>2</sub>, —NR<sup>2</sup>C(O)R<sup>3</sup>, —CO<sub>2</sub>R<sup>2</sup>, —CONR<sup>2</sup>R<sup>3</sup>, —NO<sub>2</sub>, —OR<sup>2</sup>, —SR<sup>2</sup>, —O(CH<sub>2</sub>)<sub>p</sub>OR<sup>2</sup>, or —O(CH<sub>2</sub>)<sub>p</sub>O(CH<sub>2</sub>)<sub>q</sub>OR<sup>2 </sup>wherein <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">each R<sup>2 </sup>is independently hydrogen, —C<sub>1</sub>-C<sub>6 </sub>alkyl, —C<sub>3</sub>-C<sub>8 </sub>cycloalkyl, aryl or heteroaryl;</li> <li id="ul0002-0002" num="0000">each R<sup>3 </sup>is independently, —C<sub>1</sub>-C<sub>6 </sub>alkyl, —C<sub>3</sub>-C<sub>8 </sub>cycloalkyl, aryl or heteroaryl;</li> <li id="ul0002-0003" num="0000">p and q are each independently an integer from 1 to 3; and</li> </ul> </li> <li id="ul0001-0003" num="0000">R<sup>4 </sup>is hydrogen, C<sub>1</sub>-C<sub>6 </sub>alkyl, C<sub>1</sub>-C<sub>6 </sub>alkyl substituted with aryl, aryl, (CH<sub>2</sub>)<sub>m</sub>OC(═O)C<sub>1</sub>-C<sub>6</sub>alkyl, ((CH<sub>2</sub>)<sub>m</sub>O)<sub>n</sub>CH<sub>2</sub>CH<sub>2</sub>X, (CH<sub>2</sub>)<sub>m</sub>N(R<sup>5</sup>)<sub>2 </sub>or CH((CH<sub>2</sub>)<sub>m</sub>O(C═O)R<sup>6</sup>)<sub>2</sub>; <ul id="ul0003" list-style="none"> <li id="ul0003-0001" num="0000">m is 1 or 2;</li> <li id="ul0003-0002" num="0000">n is 1-4;</li> <li id="ul0003-0003" num="0000">X is OR<sup>5 </sup>or N(R<sup>5</sup>)<sub>2</sub>;</li> <li id="ul0003-0004" num="0000">R<sup>5 </sup>is hydrogen or methyl; and</li> <li id="ul0003-0005" num="0000">R<sup>6 </sup>is C<sub>1</sub>-C<sub>18 </sub>alkyl;</li> </ul> </li> <li id="ul0001-0004" num="0000">and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.</li> </ul> </p>
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AMINOCARBOXYLIC ACID DERIVATIVE AND MEDICINAL USE THEREOF (Fri, 24 Jan 2014)
<p id="p-0001" num="0000">The present invention relates to a compound represented by the formula (I), a salt thereof, an N-oxide form thereof, a solvate thereof, or a prodrug thereof, and a medicament containing the same. The compound represented by the formula (I) has an ability to bind to an S1P receptor (particularly, EDG-1, EDG-6, and/or EDG-8) and is useful for preventing and/or treating for rejection to transplantation, graft-versus-host disease, autoimmune diseases, allergic diseases, neurodegenerating diseases, and the like.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="12.78mm" wi="69.85mm" file="US20140023636A1-20140123-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein all symbols are described in the specification.</p>
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Adenine derivatives (Fri, 24 Jan 2014)
<p id="p-0001" num="0000">Compounds of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.32mm" wi="69.85mm" file="US08802684-20140812-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R<sup>1 </sup>is C<sub>1-6</sub>alkylamino, or C<sub>1-6</sub>alkoxy; R<sup>2 </sup>is a group having the structure: </p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="10.16mm" wi="31.67mm" file="US08802684-20140812-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> n is an integer having a value of 1 to 6; Het is a 6-membered saturated heterocycle containing one nitrogen atom wherein Het is attached to the —(CH<sub>2</sub>)<sub>n</sub>— moiety at any carbon atom of the heterocycle; R<sup>3 </sup>is hydrogen, C<sub>1-8</sub>alkyl, or C<sub>3-7</sub>cycloalkylC<sub>0-6</sub>alkyl; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants. </p>
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3,5,N-TRIHYDROXY-ALKANAMIDE AND DERIVATIVES: METHOD FOR MAKING SAME AND USE THEREOF (Fri, 24 Jan 2014)
The present invention provides novel compounds of Formula (I), and pharmaceutically compositions thereof. Compounds of Formula (I) are inhibitors of histone deacetylases (HDACs) and 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase (HMGR). Also provided are methods of using the compounds and pharmaceutical compositions for inhibiting the activity of HDACs and HMGR, treating diseases associated with HDACs or HMGR (e.g., cancer, hypercholesterolemia, an acute or chronic inflammatory disease, autoimmune disease, allergic disease, pathogen infection, neurodegenerative disease, and a disease associated with oxidative stress), or inhibiting drug resistance of cancer cells.
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CARBOXYLIC ACID COMPOUNDS (Fri, 22 Nov 2013)
The present disclosure concerns at least one entity chosen from compounds of Formula (I) and pharmaceutically acceptable salts thereof: (I) wherein the variable groups X, R1, R2, R3 m, n and p are as defined herein. The present disclosure also relates to methods for the preparation of at least one such entity, and intermediates useful in the preparation thereof, to pharmaceutical compositions containing at least one such entity, to the use of at least one such entity in the preparation of medicaments, and to the use of at least one such entity in the treatment of conditions such as, for example, allergic diseases, autoimmune diseases, viral diseases, and cancer.
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Matrix metalloproteinase inhibitors (Fri, 15 Nov 2013)
<p id="p-0001" num="0000">The present invention relates to β-hydroxy and amino-substituted carboxylic acids, which act as matrix metalloproteinase inhibitors, particularly diastereomerically pure β-hydroxy carboxylic acids, corresponding processes for their synthesis, and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune, and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase.</p>
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Matrix metalloproteinase inhibitors (Fri, 08 Nov 2013)
<p id="p-0001" num="0000">The present invention relates to β-hydroxy and amino-substituted carboxylic acids, which act as matrix metalloproteinase inhibitors, particularly diastereomerically pure β-hydroxy carboxylic acids, corresponding processes for their synthesis, and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune, and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase.</p>
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Compound containing basic group and use thereof (Thu, 31 Oct 2013)
The present invention relates to a compound represented by formula (I): wherein all symbols are as defined here, a salt thereof or a solvate thereof. The compound of the present invention has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, rejection of transplanted organ, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy.
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SUBSTITUTED HETERO-BICYCLIC COMPOUNDS, COMPOSITIONS AND MEDICINAL APPLICATIONS THEREOF (Fri, 25 Oct 2013)
The present disclosure provides hetero-biclyclic compounds of formula (I), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, hydrates, N-oxides, co-crystals, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by Bruton's tyrosine kinase (Btk) activity, The disclosure also relates to the process of preparation of compounds of Formula (I). These compounds are useful in the treatment, prevention, prophylaxis, management, or adjunct treatment of all medical conditions related to inhibition of Bruton's tyrosine kinase (Btk), such as inflammatory and/or autoimmune disorder, cell proliferation, rheumatoid arthritis, psoriasis, psoriatic arthritis, transplant rejection, graft-versus-host disease, multiple sclerosis, inflammatory bowel disease, allergic diseases, asthma, type 1 diabetes, myasthenia gravis, hematopoetic disfunction, B-cell malignancies, systemic lupus, erythematosus or other disorders.
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BICYCLIC COMPOUNDS, COMPOSITIONS AND MEDICINAL APPLICATIONS THEREOF (Fri, 25 Oct 2013)
The present disclosure relates to a class of substituted bicyclic compounds of formula (I), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, hydrates, N-oxides, co-crystals, pharmaceutically acceptable salts and pharmaceutical compositions containing them. The disclosure also relates to the process of preparation of compounds of Formula (I). These compounds are useful in the treatment, prevention, prophylaxis, management, or adjunct treatment of all medical conditions related to inhibition of Bruton's tyrosine kinase (Btk), such as inflammatory and/or autoimmune disorder, cell proliferation, rheumatoid arthritis, psoriasis, psoriatic arthritis, transplant rejection, graft-versus-host disease, multiple sclerosis, inflammatory bowel disease, allergic diseases, asthma, type 1 diabetes, myasthenia gravis, hematopoetic disfunction, B-cell malignancies, systemic lupus, erythematosus or other disorders.
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CLIP INHIBITORS AND METHODS OF MODULATING IMMUNE FUNCTION (Fri, 04 Oct 2013)
<p id="p-0001" num="0000">The invention relates to methods for modulating the immune function through targeting of CLIP molecules. The result is wide range of new therapeutic regimens for treating, inhibiting the development of, or otherwise dealing with, a multitude of illnesses and conditions, including autoimmune disease, allergic disease transplant and cell graft rejection, cancer, bacterial infection, HIV infection, and AIDS.</p>
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Clip inhibitors and methods of modulating immune function (Thu, 05 Sep 2013)
The invention relates to methods for modulating the immune function through targeting of CLIP molecules. The result is wide range of new therapeutic regimens for treating, inhibiting the development of, or otherwise dealing with, a multitude of illnesses and conditions, including autoimmune disease, allergic disease transplant and cell graft rejection, cancer, bacterial infection, HIV infection, and AIDS.
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S1P receptor modulating agent (Fri, 23 Aug 2013)
<p id="p-0001" num="0000">An object of the present invention is to provide a compound having a modulating activity at an S1P receptor which is useful for preventing and treating autoimmune diseases, allergic diseases, and the like. According to the present invention, a compound represented by formula (I) or a pharmaceutically acceptable salt thereof is provided.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="37.08mm" wi="70.27mm" file="US08895753-20141125-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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PURINE DERIVATIVES FOR USE IN THE TREATMENT OF ALLERGIC, INFLAMMATORY AND INFECTIOUS DISEASES (Thu, 01 Aug 2013)
Compounds of formula (I): wherein R<sp>1</sp> is C<sb>1-6</sb>alkylamino, or C<sb>1-6</sb>alkoxy; m is an integer having a value of 3, 4, or 5; n is an integer having a value of 0 to 3; p is an integer having a value of 1 or 2 and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
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PRODRUGS OF A PIPERIDINYL DERIVATIVE AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Fri, 12 Jul 2013)
<p id="p-0001" num="0000">The present application describes prodrugs of the compound of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.77mm" wi="74.85mm" file="US20130178444A1-20130711-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis using the prodrug compounds of the invention are disclosed.</p>
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PURINE COMPOUNDS AS PRODRUGS OF A2B ADENOSINE RECEPTOR ANTAGONISTS, THEIR PROCESS AND MEDICINAL APPLICATIONS (Fri, 05 Jul 2013)
<p id="p-0001" num="0000">The present disclosure relates to purine compounds of formula (I) or formula (II) or its tautomers, polymorphs, stereoisomers, solvates or a pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by thereof as A2B adenosine receptor antagonists.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="66.55mm" wi="65.02mm" file="US20130172249A1-20130704-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by the mediation of adenosine A2B receptor. Such conditions include, but are not limited to, asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders including inflammatory bowel disease, sickle cell disease, and/or autoimmune diseases, and to their use in treating mammals for various disease states, such as gastrointestinal disorders, immunological disorders, hypersensitivity disorders, neurological disorders, and cardiovascular diseases due to both cellular hyperproliferation and apoptosis, and the like. The present disclosure also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.</p>
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Substituted anilines as CCR(4) antagonists (Fri, 05 Jul 2013)
<p id="p-0001" num="0000">Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.</p>
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Substituted benzimidazoles and benzopyrazoles as CCR(4) antagonists (Fri, 28 Jun 2013)
<p id="p-0001" num="0000">Benzimidazole, benzopyrazole and benzotriazole compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.</p>
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PREPARATION OF CONJUGATES COMPRISING ADENINE DERIVATIVES AND ALLERGENIC PROTEINS AND THEIR USE FOR SPECIFIC IMMUNOTHERAPY OF ALLERGENIC DISEASES (Thu, 13 Jun 2013)
The present invention refers to the preparation of adenine derivative active esters of formula (I) and use thereof for the preparation of stable conjugates between adenine derivative and allergenic proteins having general structure (II) for the modulation of T<sb>H</sb>2 response in allergic diseases.(I, II).
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SUBSTITUTED BENZIMIDAZOLES AND BENZOPYRAZOLES AS CCR(4) ANTAGONISTS (Fri, 07 Jun 2013)
Benzimidazole, benzopyrazole and benzotriazole compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.
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SUBSTITUTED ANILINES AS CCR(4) ANTAGONISTS (Fri, 07 Jun 2013)
Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.
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Preparation of conjugates comprising adenine derivatives and allergenic proteins and their use for specific immunotherapy of allengenic diseases (Fri, 31 May 2013)
<p id="p-0001" num="0000">The present invention refers to the preparation of adenine derivative active esters of formula (I) and use thereof for the preparation of stable conjugates between adenine derivative and allergenic proteins having general structure (II) for the modulation of T<sub>H</sub>2 response in allergic diseases. (I, II).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="82.89mm" wi="73.91mm" file="US08822407-20140902-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Aminocarboxylic acid derivative and medical use thereof (Thu, 16 May 2013)
The present invention relates to a compound represented by the formula (I), a salt thereof, an N-oxide form thereof, a solvate thereof, or a prodrug thereof, and a medicament containing the same. The compound represented by the formula (I) has an ability to bind to an S1P receptor (particularly, EDG-1, EDG-6, and/or EDG-8) and is useful for preventing and/or treating for rejection to transplantation, graft-versus-host disease, autoimmune diseases, allergic diseases, neurodegenerating diseases, and the like. wherein all symbols are described in the specification.
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INDOLE COMPOUNDS AND PHARMACEUTICAL USE THEREOF (Fri, 10 May 2013)
<p id="p-0001" num="0000">Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like.</p> <p id="p-0002" num="0000">A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof:</p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.48mm" wi="69.85mm" file="US20130116240A1-20130509-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0004" num="0000">wherein each symbol is as described in the specification.</p>
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Nitrogenous heterocyclic derivative and medicine containing the same as an active ingredient (Fri, 05 Apr 2013)
<p id="p-0001" num="0000">A compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="13.89mm" wi="69.85mm" file="US08604207-20131210-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> (wherein each symbol is as defined in the description.) The compounds represented by formula (I) has the antagonistic activity against CCR5, so they are useful in preventing and/or treating CCR5-related diseases, for example, various inflammatory diseases (asthma, nephritis, nephropathy, hepatitis, arthritis, rheumatoid arthritis, rhinitis, conjunctivitis, inflammatory bowel disease such as ulcerative colitis, etc.), immunological diseases (autoimmune diseases, rejection in organ transplantation (rejection of graft of solid organ, rejection of graft of pancreatic islet cells in therapy for diabetes, graft-versus-host disease, etc.), immunosuppression, psoriasis, multiple sclerosis, etc.), infectious diseases (infection with human immunodeficiency virus, acquired immunodeficiency syndrome, infection with RSV, etc.), allergic diseases (atopic dermatitis, urticaria, allergic bronchopulmonary aspergillosis, allergic eosinophilic gastroenteritis, etc.), cardiovascular diseases (arteriosclerosis, ischemic reperfusion injury, etc.), acute respiratory distress syndrome, shock accompanying bacterial infection, diabetes, cancer metastasis and so on. </p>
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Piperidino-dihydrothienopyrimidine sulfoxides and their use for treating COPD and asthma (Fri, 29 Mar 2013)
<p id="p-0001" num="0000">The invention relates to novel piperidino-dihydrothienopyrimidine sulfoxides of formula I,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="47.41mm" wi="64.43mm" file="US08609670-20131217-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000">wherein Ring A is a 6-membered aromatic ring which may optionally comprise one or two nitrogen atoms and</li> <li id="ul0001-0002" num="0000">wherein R is Cl and</li> <li id="ul0001-0003" num="0000">wherein R may be located either in the para-, meta- or ortho-position of Ring A,</li> <li id="ul0001-0004" num="0000">wherein S* is a sulphur atom that represents a chiral center,</li> <li id="ul0001-0005" num="0000">and all pharmaceutically acceptable salts, enantiomers and racemates, hydrates and solvates thereof and the use of these compounds for the treatment of inflammatory or allergic diseases of the respiratory tract such as COPD or asthma.</li> </ul> </p>
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NOVEL PIPERIDINO-DIHYDROTHIENOPYRIMIDINE SULFOXIDES AND THEIR USE FOR TREATING COPD AND ASTHMA (Fri, 08 Mar 2013)
<p id="p-0001" num="0000">The invention relates to novel piperidino-dihydrothienopyrimidine sulfoxides of formula I,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="44.37mm" wi="63.84mm" file="US20130059866A1-20130307-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000">wherein Ring A is a 6-membered aromatic ring which may optionally comprise one or two nitrogen atoms and</li> <li id="ul0001-0002" num="0000">wherein R is Cl and</li> <li id="ul0001-0003" num="0000">wherein R may be located either in the para-, meta- or ortho-position of Ring A,</li> <li id="ul0001-0004" num="0000">wherein S* is a sulphur atom that represents a chiral center,</li> <li id="ul0001-0005" num="0000">and all pharmaceutically acceptable salts, enantiomers and racemates, hydrates and solvates thereof and the use of these compounds for the treatment of inflammatory or allergic diseases of the respiratory tract such as COPD or asthma.</li> </ul> </p>
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DP2 ANTAGONIST AND USES THEREOF (Fri, 01 Mar 2013)
<p id="p-0001" num="0000">Described herein is the DP<sub>2 </sub>anatgonist 2-(3-(2-((tert-butylthio)methyl)-4-(2,2-dimethyl-propionylamino)phenoxy)-4-methoxyphenyl)acetic acid, or a pharmaceutically acceptable salt thereof. Also described are methods of preparing the DP<sub>2 </sub>anatgonist, or a pharmaceutically acceptable salt thereof. Also described herein are pharmaceutical compositions suitable for administration to a mammal that include the DP<sub>2 </sub>anatgonist, or a pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating respiratory diseases or conditions, allergic diseases or conditions, inflammatory diseases or conditions, as well as other prostaglandin D<sub>2</sub>-dependent or prostaglandin D<sub>2</sub>-mediated diseases or conditions.</p>
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NOVEL PIPERIDINO-DIHYDROTHIENOPYRIMIDINE SULFOXIDES AND THEIR USE FOR TREATING COPD AND ASTHMA (Fri, 01 Mar 2013)
The invention relates to novel piperidino-dihydrothienopyrimidine sulfoxides of formula I, wherein Ring A is a 6-membered aromatic ring which may optionally comprise one or two nitrogen atoms and wherein R is CI and wherein R may be located either in the para-, meta- or ortho-position of Ring A, wherein S* is a sulphur atom that represents a chiral center, and all pharmaceutically acceptable salts, enantiomers and racemates, hydrates and solvates thereof and the use of these compounds for the treatment of inflammatory or allergic diseases of the respiratory tract such as COPD or asthma.
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Pyrimidline derivatives having immune modulating properties that act via TLR7 for the treatment of viral or allergic diseases and cancers (Fri, 22 Feb 2013)
<p id="p-0001" num="0000">The present invention provides compounds of formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.26mm" wi="52.92mm" file="US08765939-20140701-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3 </sup>and R<sup>4 </sup>are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy. </p>
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HYPOALLERGENIC VARIANTS OF MAL D 1, THE MAJOR ALLERGEN FROM MALUS DOMESTICA (Fri, 08 Feb 2013)
Disclosed are hypoallergenic variants of Mal d 1, the major allergen from Malus domestica, and the uses thereof in the treatment of allergic diseases.
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COMPOSITION (Fri, 01 Feb 2013)
Compound (I), and pharmaceutically acceptable salts thereof, are inducers of human interferon. Certain discrete and particular dosages of Compound (I) may be particularly useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and allergic asthma.
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Piperidinyl derivative as a modulator of chemokine receptor activity (Fri, 25 Jan 2013)
<p id="p-0001" num="0000">The present application describes the compound of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.77mm" wi="74.85mm" file="US08633226-20140121-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and arthrosclerosis using the compound of the invention are disclosed. </p>
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NOVEL PYRROLO PYRIMIDINE DERIVATIVES (Fri, 18 Jan 2013)
The present invention describes new pyrrolo pyrimidine derivatives and pharmaceutically acceptable salts thereof which appear to interact with Bruton's tyrosine kinase (Btk). Accordingly, the novel pyrrolo pyrimidines may be effective in the treatment of autoimmune disorders, inflammatory diseases, allergic diseases, airway diseases, such as asthma and chronic obstructive pulmonary disease (COPD), transplant rejection, cancers e.g. of hematopoietic origin or solid tumors.
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Chemokine receptor antagonists and use thereof (Fri, 28 Dec 2012)
<p id="p-0001" num="0000">The present invention relates to a compound represented by formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="16.43mm" wi="69.85mm" file="US08614323-20131224-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein all symbols are as defined here, a salt thereof, a solvate thereof, or a prodrug thereof. The compound of the present invention has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, rejection of transplanted organ, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy. </p>
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BENZYLPYRROLIDINONE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Thu, 20 Dec 2012)
The present application describes modulators of MCP-1 or CCR-2 of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein m, n, W, X, R<sp>1</sp> and R<sp>6</sp>, are defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.
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6-AMINO-2-{[(1S)-1-METHYLBUTYL]OXY}-9-[5-(1-PIPERIDINYL)PENTYL]-7,9-DIHYDRO-8H-PURIN-8-ONE MALEATE (Thu, 20 Dec 2012)
A compound which is 6-amino-2-{[(1S)-1-methylbutyl]oxy}-9-[5-(1-piperidinyl)pentyl]-7,9-dihydro-8<i>H</i>-purin-8-one: Formula (I) in the form of a maleate salt, may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
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Purine derivatives and their pharmaceutical uses (Fri, 14 Dec 2012)
<p id="p-0001" num="0000">The present invention relates to compounds of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.90mm" wi="75.52mm" file="US08575340-20131105-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein; <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">R<sup>1 </sup>represents hydrogen or C<sub>1-3</sub>alkyl;</li> <li id="ul0002-0002" num="0000">n is an integer having a value of 1 to 5;</li> <li id="ul0002-0003" num="0000">X represents O or NH;</li> <li id="ul0002-0004" num="0000">Y represents C or N; <br/> or a pharmaceutically acceptable salt thereof, have been shown to be inducers of human interferon and may possess an improved profile with respect to known inducers of human interferon, for example enhanced potency. The compounds of the invention may therefore be useful in the treatment of various disorders, in particular the treatment of infectious diseases, cancer, allergic diseases and other inflammatory conditions, and their use as vaccine adjuvants. </li> </ul> </li> </ul> </p>
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6-amino-2-{[(1<i>S</i>)-1-methylbutyl]oxy}-9-[5-(1-piperidinyl)-7,9-dihydro-8<i>H</i>-purin-8-one maleate (Fri, 07 Dec 2012)
<p id="p-0001" num="0000">The present invention relates to a compound which is 6-amino-2-{[(1S)-1-methylbutyl]oxy}-9-[5-(1-piperidinyl)pentyl]-7,9-dihydro-8H-purin-8-one:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="54.61mm" wi="49.61mm" file="US08703754-20140422-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> in the form of a maleate salt, may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants. </p>
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BENZYLPYRROLIDINONE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Fri, 23 Nov 2012)
<p id="p-0001" num="0000">The present application describes modulators of MCP-1 or CCR-2 of formula</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.40mm" wi="65.53mm" file="US20120295899A1-20121122-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein m, n, W, X, R<sup>1 </sup>and R<sup>6</sup>, are defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.</p>
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COMPOUNDS (Fri, 09 Nov 2012)
<p id="p-0001" num="0000">The present invention includes novel compounds useful in the treatment of various disorders in particular infectious diseases, cancer, and allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, and as vaccine adjuvants.</p>
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Amiloride analogues substituted on the cyclic guanidine moiety as ENaC blockers for treating respiratory diseases (Thu, 08 Nov 2012)
A compound of Formula I in free or salt or solvate form, where R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 and R 11 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. In particular, airway diseases like COPD and cystic fibrosis are treatable, but also inflammatory and allergic diseases. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
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Macrolides and their use (Fri, 02 Nov 2012)
<p id="p-0001" num="0000">The invention relates to macrolide compounds of formula (I), the use of said compounds as medicaments, in particular for the treatment or prevention of inflammatory and allergic diseases, pharmaceutical compositions containing said compounds and to processes for their preparation. The invention relates in particular to macrolide compounds with antiinflammatory activity mediated primarily through inhibition of phosphodiesterase 4 (PDE4) which makes them useful for the treatment and/or prevention of inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, atopic dermatitis or inflammatory bowel disease or proliferative diseases such as cancer.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="43.35mm" wi="57.83mm" file="US08865662-20141021-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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INDOLE COMPOUND AND PHARMACEUTICAL USE THEREOF (Thu, 04 Oct 2012)
Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as described in the specification.
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Chemokine receptor antagonists and use thereof (Fri, 17 Aug 2012)
<p id="p-0001" num="0000">A compound represented by general formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="14.90mm" wi="69.85mm" file="US08519124-20130827-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> a salt thereof, a solvate thereof, or a prodrug thereof wherein all symbols are as defined in the specification has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, systemic erythematosus, retinopathy, macular degeneration, pulmonary fibrosis, transplanted organ rejection, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiac/vascular disease (for example, arteriosclerosis, myocardial infarction, stenocardia, cerebral infarction, chronic arterial occlusive disease, etc.), metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), a preventive and/or therapeutic agent for cancerous diseases or infections, or an agent for regeneration therapy. </p>
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Spirocyclic compounds as modulators of chemokine receptor activity (Fri, 10 Aug 2012)
<p id="p-0001" num="0000">The present application describes modulators of chemokine receptor activity of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.60mm" wi="75.27mm" file="US08877749-20141104-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Matrix metalloproteinase inhibitors (Thu, 12 Jul 2012)
The present invention relates to ²-hydroxy and amino substituted carboxylic acids, which act as matrix metalloprotease inhibitors, particularly diastereomerically pure ²-hydroxy carboxylic acids, corresponding processes for the synthesis of and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase using the compounds.
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NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS AND MEDICINAL USE THEREOF (Fri, 22 Jun 2012)
<p id="p-0001" num="0000">The compound represented by formulae (I) and (II), the salt thereof, the N-oxide thereof or the solvate thereof, or the prodrug thereof and the pharmaceutical composition comprising thereof have a CXCR4-regulating effect, and they are effective in treatment and prevention of various inflammatory disease, various allergic disease, acquired immunodeficiency syndrome infection with human immunodeficiency virus, or agents for regeneration therapy.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.01mm" wi="69.85mm" file="US20120156219A1-20120621-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">(wherein ring A represents a nitrogen-containing heterocyclic group which may have a substituent(s); ring B represents a homocyclic group which may have a substituent(s) or a heterocyclic group which may have a substituent(s); and Y represents a hydrocarbon group which may have a substituent(s), a heterocyclic group which may have a substituent(s), an amino group which may be protected, a hydroxyl group which may be protected or a mercapto group which may be protected; T represents ring A or an amino group which may be protected.)</p>
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8-Triazolylxanthine derivatives, processes for their production and their use as adenosine receptor antagonists (Thu, 21 Jun 2012)
The invention relates to derivatives of the general formulae I and II to processes for the production thereof, to pharmaceutical preparations containing said compounds and/or physiologically compatible salts, or solvates which can be produced therefrom as well as to the pharmaceutical use of said compounds, the salts, or solvates thereof as adenosine receptor antagonists, in particular for the treatment of neurodegenerative disorders, e.g. stroke, amylotrophic lateral sclerosis, dementia, Alzheimer's disease, Parkinson's disease, ischemia/reperfusion injury, inflammation, and/or neurological disorder. The blockade of adenosine receptors could also be useful for other indications regarding the metabolism, e.g. diabetic retinopathy, diabetes mellitus, hyperbaric oxygen-induced retinopathy and/or obesity. Applications could also be the treatment of allergic diseases and autoimmune diseases, including mast cell degranulation, asthma, bronchoconstriction, pulmonary fibrosis, inflammatory or obstructive airways disease and/or chronic obstructive pulmonary disease (COPD). In addition, they could be used to treat cancer, e.g. proliferating tumor, cell proliferation disorders, angiogenesis, lung cancer, breast cancer, pancreatic cancer, thyroid cancer, skin cancer, vascular endothelial cancer, cancer of the central nervous system, esophageal cancer, cancer of the larynx, gastrointestinal cancer, colon cancer, colorectal cancer, rectal cancer, liver cancer, renal cancer, prostate cancer, bladder cancer, cervical cancer, ovarian cancer, endometrial cancer, melanoma, squamous cell carcinoma, basal cell carcinoma, non-small cell lung cancer selected from squamous cell carcinoma, adenocarcinoma, large cell carcinoma, adenosquam- ous carcinoma and/or undifferentiated carcinoma. The diseases associated with adenosine receptors are also diabetes, diarrhea, inflammatory bowel disease and/or gastrointestinal tract disorders. Adenosine receptor antagonists could be effective for treating a hepatic disease or condition for reducing fat deposition in the liver or fibrosis of the liver. The use of compounds of general formulae I and II can be associated with many applications e.g., scleroderm arthritis, atherosclerosis, urticaria, myocardial infarction, myocardial reperfusion after ischemia, vasodilation, hypertension, hypersensitivity, myocardial ischemia, heart attack and/or retinopathy of prematurity.
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Piperidinyl compound as a modulator of chemokine receptor activity (Fri, 15 Jun 2012)
<p id="p-0001" num="0000">The present application describes the compound of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="33.78mm" wi="73.41mm" file="US08642622-20140204-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and arthrosclerosis using the compound of the invention are disclosed. </p>
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8-TRIAZOLYLXANTHINE DERIVATIVES, PROCESSES FOR THEIR PRODUCTION AND THEIR USE AS ADENOSINE RECEPTOR ANTAGONISTS (Fri, 15 Jun 2012)
The invention relates to derivatives of the general formulae (I) and (II) to processes for the production thereof, to pharmaceutical preparations containing said compounds and/or physiologically compatible salts or solvates or prodrugs which can be produced therefrom as well as to the pharmaceutical use of said compounds, the salts or solvates thereof as adenosine receptor antagonists, in particular for the treatment of neurodegenerative disorders, e.g. stroke, amylotrophic lateral sclerosis, dementia, Alzheimer's disease, Parkinson's disease, ischemia/reperfusion injury, inflammation, and/or neurological disorder. The blockade of adenosine receptors could also be useful for other indications regarding the metabolism, e.g. diabetic retinopathy, diabetes mellitus, hyperbaric oxygen - induced retinopathy and/or obesity. Applications could also be the treatment of allergic diseases and autoimmune diseases, including mast cell degranulation, asthma, bronchoconstriction, pulmonary fibrosis, inflammatory or obstructive airways disease and/or chronic obstructive pulmonary disease (COPD). In addition, they could be used to treat cancer. The diseases associated with adenosine receptors are also diabetes, diarrhea, inflammatory bowel disease and/or gastrointestinal tract disorders. Adenosine receptor antagonists could be effective for treating a hepatic disease or condition for reducing fat deposition in the liver or fibrosis of the liver. The use of compounds of general formulae I or II can be associated with many applications e.g., scleroderm arthritis, atherosclerosis, urticaria, myocardial infarction, myocardial reperfusion after ischemia, vasodilation, hypertension, hypersensitivity, myocardial ischemia, heart attack and/or retinopathy of prematurity.
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Indolecarboxylic acid derivative having PGD2 receptor antagonistic activity (Fri, 08 Jun 2012)
<p id="p-0001" num="0000">The present invention provides an indolecarboxylic acid derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases.</p> <p id="p-0002" num="0000">A compound of the general formula (I):</p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="43.52mm" wi="59.52mm" file="US08623903-20140107-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the formula of —X<sup>1</sup>═X<sup>2</sup>—X<sup>3</sup>═X<sup>4</sup>— is a formula of —C(R<sup>1</sup>)═C(R<sup>2</sup>)—C(R<sup>3</sup>)═C(R<sup>4</sup>)— etc.; X<sup>5 </sup>is C(R<sup>5</sup>) or N; R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4 </sup>and R<sup>5 </sup>is independently a hydrogen atom, a halogen atom etc; R<sup>6 </sup>is a formula of —Z—R<sup>10 </sup>etc. wherein Z is alkylene etc., and R<sup>10 </sup>is carboxy etc.; R<sup>7 </sup>is optionally substituted alkyloxy etc.; R<sup>8 </sup>is independently a halogen atom etc.; R<sup>9 </sup>is independently optionally substituted alkyl etc.; Y is a single bond etc.; n is 0 etc.; q is 0 etc.;</li> <li id="ul0002-0002" num="0000">a pharmaceutically acceptable salt or a solvate thereof.</li> </ul> </li> </ul> </p>
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NITROGEN-CONTAINING SPIRO-RING COMPOUND AND MEDICINAL USE OF SAME (Thu, 07 Jun 2012)
A compound of the following general formula [I]: wherein each symbol has the same meaning as defined herein, or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a pharmaceutical use of the same in treating organ transplant rejection, graft versus host reaction after transplantation, autoimmune disease, allergic disease and chronic myeloproliferative disease.
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METHODS FOR PREVENTING OR TREATING METABOLIC DISEASES, INFLAMMATORY DISEASES, AUTOIMMUNE DISEASES, ALLERGIC DISEASES, CENTRAL NERVOUS SYSTEM DISEASES, CARDIOVASCULAR DISEASES, HOMEOSTASIS-RELATED DISEASES OR GLAUCOMA (Fri, 25 May 2012)
<p id="p-0001" num="0000">A method for preventing or treating a metabolic disorder, an inflammatory disease, an autoimmune disease, an allergic disease, a central nervous system disease, a cardiovascular disease, a homeostasis-related disease or glaucoma, involving administering a compound or a salt thereof, the compound having the following formula (1)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="38.02mm" wi="69.85mm" file="US20120129866A1-20120524-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein R<sup>1 </sup>represents alkyl, cycloalkyl, aryl, heterocyclic or aralkyl; R<sup>7 </sup>represents cycloalkyl, aryl or heterocyclic; W represents oxygen or NR<sup>8</sup>, Y represents alkylene, Z represents oxygen, sulfur, OCO or NR<sup>9</sup>; R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>6</sup>, R<sup>8 </sup>and R<sup>9 </sup>represent hydrogen or alkyl.</p>
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BENZYLAMINE COMPOUNDS AS TOLL -LIKE RECEPTOR 7 AGONISTS (Fri, 25 May 2012)
The invention concerns compounds of Formula (I), and pharmaceutically acceptable salts thereof: where such compounds act as TLR7 agonists and at the same time show advantageous selectivity over TLR8 and hERG, wherein the variable groups R1, R2 and n are as defined herein. The invention also relates to methods for the preparation of such compounds and intermediates useful in the preparation thereof, to pharmaceutical compositions containing such compounds, to the use of such compounds in the preparation of medicaments, and to the use of such compounds in the treatment of conditions mediated by TLR7, such as allergic diseases, autoimmune diseases, viral diseases and, in particular, cancer.
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TETRAZOLE DERIVATIVES (Fri, 11 May 2012)
<p id="p-0001" num="0000">The present invention relates to compounds of formula (I) for use as pharmaceutical active compounds, as well as pharmaceutical formulations containing the same, for the treatment of allergic diseases.</p>
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Substituted fused pyrimidine compounds (Fri, 11 May 2012)
<p id="p-0001" num="0000">The present invention discloses substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, solvates, pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor, such as asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders, and/or autoimmune diseases.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="21.67mm" wi="69.85mm" file="US08859566-20141014-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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TRICYCLIC INDOLE-DERIVED SPIRO DERIVATIVES AS CRTH2 MODULATORS (Fri, 11 May 2012)
<p id="p-0001" num="0000">The present invention relates to compounds of formula (I) for use as pharmaceutical active compounds, as well as pharmaceutical formulations containing the same, for the treatment of allergic diseases. The compounds according to Formula (I) are suitable as modulators of CRTH2. The invention provides Spiro derivatives according to Formula (I) and related formulae that are useful in the treatment and/or prevention of diseases selected from allergic diseases such as allergic asthma, allergic rhinitis, allergic conjunctivitis, and inflammatory dermatoses such as atopic dermatitis, contact hypersensitivity, allergic contact dermatitis, chronic urticaria/chronic idiopathic/autoimmune urticaria, drag-induced exanthems (e.g., toxic epidermal necrolysis or Lyell's syndrome/Stevens-Johnson syndrome/drug hypersensitivity syndrome), photodermatosis or polymorphous light emption (e.g., photoirritant contact dermatitis, photoallergy contact dermatitis, chronic actinic dermatitis), and myositis neurodegenerative disorders such as neuropatic pain and other diseases with an inflammatory component such as rheumatoid arthritis, multiple sclerosis, osteoarthritis, and inflammatory bowel disease (IBD).</p>
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7-phenoxychroman carboxylic acid derivatives (Fri, 27 Apr 2012)
<p id="p-0001" num="0000">Compounds of Formula I: (I) in which A, A<sup>1</sup>, R<sup>1</sup>, R<sup>7a</sup>, R<sup>7b</sup>, R<sup>8 </sup>and R<sup>10 </sup>have the meanings given in the specification, are DP2 receptor inhibitors useful in the treatment of useful in the treatment and prevention of immunologic diseases, allergic diseases such as asthma, allergic rhinitis and atopic dermatitis, and other inflammatory diseases mediated by prostaglandin D<sub>2 </sub>(PGD<sub>2</sub>). The compounds of Formula I may also be useful in treating diseases or medical conditions involving the Th2 T cell via production of IL-4, IL-5 and/or IL-13.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="46.99mm" wi="69.85mm" file="US08785445-20140722-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Intermediates for thienopyrazole derivatives having PDE7 inhibitory activity (Thu, 29 Mar 2012)
To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I): [wherein, especially, R 1 is a cyclohexyl, a cycloheptyl group or a tetrahydropyranyl group; R 2 is methyl; R 3 is a hydrogen atom; and R 4 is a group: -CONR 5 R 6 (in which any one of R 5 and R 6 is a hydrogen atom)].
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PURINE COMPOUNDS AS PRODRUGS OF A2B ADENOSINE RECEPTOR ANTAGONISTS, THEIR PROCESS AND MEDICINAL APPLICATIONS (Fri, 23 Mar 2012)
The present disclosure relates to purine compounds of formula (I) or formula (II) or its tautomers, polymorphs, stereoisomers, solvates or a pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by thereof as A2B adenosine receptor antagonists. {Formulas should be inserted here} The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by the mediation of adenosine A2B receptor. Such conditions include, but are not limited to, asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders including inflammatory bowel disease, sickle cell disease, and/or autoimmune diseases. and to their use in treating mammals for various disease states, such as gastrointestinal disorders, immunological disorders, hypersensitivity disorders, neurological disorders, and cardiovascular diseases due to both cellular hyperproliferation and apoptosis, and the like. The present disclosure also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.
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Compound having S1P receptor binding potency and use thereof (Fri, 16 Mar 2012)
<p id="p-0001" num="0000">Provided are: a compound represented by formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="15.07mm" wi="69.85mm" file="US08653305-20140218-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">(wherein ring A and ring D each represent a cyclic group which may have a substituent(s); E and G each represent a bond or a spacer having 1 to 8 atoms in its main chain; L represents a hydrogen atom or a substituent; X represents amino which may have a substituent(s), or a heterocylcic group which contains at least one nitrogen atom and which may have a substituent(s); n represents 0 to 3, and when n is 2 or more, a plurality of ring A's may be the same or different from one another); a salt, an N-oxide form, a solvate, or a prodrug thereof; and a medicament which includes those. The compound of formula (I) is capable of binding S1P receptors (in particular, EDG-1 and/or EDG-6), and useful for preventing and/or treating rejection in transplantation, autoimmune diseases, allergic diseases, etc.</li> </ul> </li> </ul> </p>
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Compounds exhibiting PGD 2 receptor antagonism (Thu, 01 Mar 2012)
A compound having CRTH2 receptor antagonism, represented by the following formula (I). The compound is useful for the treatment of allergic diseases having a relation to eosinophils and the like. A compound of the formula (I): wherein a group represented by the formula: is a group represented by the formula: and the like, R 1 is carboxy and the like, the other symbols are as defined in claim 1.
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6-AMINO-PURIN-8-ONE COMPOUNDS (Fri, 10 Feb 2012)
<p id="p-0001" num="0000">Compounds of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="38.27mm" wi="69.85mm" file="US20120035193A1-20120209-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein R<sup>1 </sup>is C<sub>1-6</sub>alkylamino, C<sub>1-6</sub>alkoxy, or C<sub>3-7</sub>cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.</p>
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PREPARATION OF CONJUGATES COMPRISING ADENINE DERIVATIVES AND ALLERGENIC PROTEINS AND THEIR USE FOR SPECIFIC IMMUNOTHERAPY OF ALLERGENIC DISEASES (Fri, 10 Feb 2012)
The present invention refers to the preparation of adenine derivative active esters of formula (I) and use thereof for the preparation of stable conjugates between adenine derivative and allergenic proteins having general structure (II) for the modulation of TH2 response in allergic diseases.(I, II).
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SUBSTITUTED FUSED PYRIMIDINE COMPOUNDS (Thu, 19 Jan 2012)
The present invention discloses substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, solvates, pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor, such as asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders, and/or autoimmune diseases.
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Synthetic intermediate in the production of a sulfonamide derivative having PGD2 receptor antagonistic activity (Thu, 19 Jan 2012)
The present invention provides an sulfonamide derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the general formula (V): wherein the ring D is a benzene ring etc.; R 1 is hydroxyalkyl etc.; R 2 is independently a hydrogen atoms etc.; R 8 is a halogen atom etc.; L 3 is independently a single bond etc.; R 7 is independently a hydrogen atom etc.; and p is 1, 2, 3 or 4; provided that the substituting position of the piperidino group and L 3 each other is not an ortho-position in the ring D when the ring D is a benzene ring and -L 3 - is -(O-alkylene)-; a pharmaceutically acceptable salt or hydrate thereof.
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PIPERIDINYL COMPOUND AS A MODULATOR OF CHEMOKINE RECEPTOR ACTIVITY (Fri, 23 Dec 2011)
The present application describes the compound of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and arthrosclerosis using the compound of the invention are disclosed.
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PIPERIDINYL COMPOUND AS A MODULATOR OF CHEMOKINE RECEPTOR ACTIVITY (Fri, 23 Dec 2011)
The present application describes the compound of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and arthrosclerosis using the compound of the invention are disclosed.</p>
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Indole compounds and pharmaceutical use thereof (Fri, 16 Dec 2011)
<p id="p-0001" num="0000">Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like.</p> <p id="p-0002" num="0000">A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof:</p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.40mm" wi="69.85mm" file="US08299070-20121030-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein each symbol is as described in the specification. </p>
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LOW-MOLECULAR POLYSULFATED HYALURONIC ACID DERIVATIVE AND MEDICINE CONTAINING SAME (Thu, 08 Dec 2011)
A low-molecular-weight polysulfated hyaluronic acid derivative useful for prevention and/or treatment of an allergic disease. An agent for prevention and/or treatment of an allergic disease selected from pollinosis, allergic rhinitis, allergic conjunctivitis, atopic dermatitis, and asthma, represented by the following general formula (IA) or (IB); wherein n represents a number of 0 to 15; R's each independently represent a hydrogen atom or an SO 3 H group etc.
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Isoquinoline derivative (Fri, 25 Nov 2011)
<p id="p-0001" num="0000">A compound represented by formula (I) or a pharmaceutically acceptable salt thereof has an effect of inhibiting CRTH2 and, therefore, is useful as a preventive or a remedy for allergic diseases such as asthma, atopic dermatitis and allergic rhinitis.</p>
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LOW-MOLECULAR POLYSULFATED HYALURONIC ACID DERIVATIVE AND MEDICINE CONTAINING SAME (Fri, 18 Nov 2011)
<p id="p-0001" num="0000">A low-molecular-weight polysulfated hyaluronic acid derivative useful for prevention and/or treatment of an allergic disease. An agent for prevention and/or treatment of an allergic disease selected from pollinosis, allergic rhinitis, allergic conjunctivitis, atopic dermatitis, and asthma, represented by the following general formula (IA) or (IB);</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="59.27mm" wi="76.03mm" file="US20110281819A1-20111117-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein n represents a number of 0 to 15; R′s each independently represent a hydrogen atom or an SO<sub>3</sub>H group etc.</p>
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Nitrogen-containing heterocyclic derivatives and drugs containing the same as the active ingredient (Thu, 10 Nov 2011)
A compound represented by the following general formula (I), its salt, solvates thereof or prodrugs thereof: (wherein each symbol is as defined in the description.) The compounds represented by the general formula (I) are useful in preventing and/or treating various inflammatory diseases (asthma, nephritis, nephropathy, hepatitis, arthritis, rheumatoid arthritis, rhinitis, conjunctivitis, ulcerative colitis, etc .), immunological diseases (autoimmune diseases, rejection in organ transplantation, immunosuppression, psoriasis, multiple sclerosis, etc .), infection with human immunodeficiency virus (acquired immunodeficiency syndrome, etc .), allergic diseases (atopic dermatitis, urticaria, allergic bronchoplumonary aspergillosis, allergic eosinophilic gastroenteritis, etc .), ischemic reperfusion injury, acute respiratory distress syndrome, shock accompanying bacterial infection, diabetes, cancer metastasis and so on.
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COMPOUNDS (Fri, 04 Nov 2011)
<p id="p-0001" num="0000">The present invention includes novel compounds useful in the treatment of various disorders in particular infectious diseases, cancer, and allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, and as vaccine adjuvants.</p>
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ISOQUINOLINE DERIVATIVE (Thu, 20 Oct 2011)
A compound represented by formula (I) or a pharmaceutically acceptable salt thereof has an effect of inhibiting CRTH2 and, therefore, is useful as a preventive or a remedy for allergic diseases such as asthma, atopic dermatitis and allergic rhinitis.
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PIPERIDINYL DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Fri, 07 Oct 2011)
<p id="p-0001" num="0000">The present application describes substituted piperidinyl modulators of MIP-1α or CCR-1 or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using said modulators are disclosed.</p>
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Azetidinecarboxylic acid derivative and medicinal use thereof (Thu, 06 Oct 2011)
The present invention relates to a compound represented by the formula (I), a salt thereof, an N-oxide form thereof, a solvate thereof, or a prodrug thereof, and a medicament containing the same. The compound represented by the formula (I) has an ability to bind to an S1P receptor (particularly, EDG-1, EDG-6, and/or EDG-8) and is useful for preventing and/or treating for rejection to transplantation, graft-versus-host disease, autoimmune diseases, allergic diseases, neurodegenerating diseases, and the like. wherein all symbols are described in the specification.
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Purine derivatives for use in the treatment of allergic, inflammatory and infectious diseases (Fri, 23 Sep 2011)
<p id="p-0001" num="0000">The present invention relates to compounds of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="38.18mm" wi="69.93mm" file="US08765772-20140701-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R<sup>1 </sup>is C<sub>1-6</sub>alkylamino, C<sub>1-6</sub>alkoxy, or C<sub>3-7</sub>cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants. </p>
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Spiro-piperidine compounds as chemokine receptor antagonists and medicinal use thereof (Thu, 15 Sep 2011)
The present invention relates to a spiro-piperidine compound represented by formula (I): wherein R 1 represents hydrogen, an aliphatic hydrocarbon group which may have a substituent(s) or a cyclic group which may have a substituent(s); and ring A represents a 5- to 8-membered cyclic group which may have a substituent(s), a salt thereof, an N-oxide thereof, a quaternary ammonium salt thereof or a solvate thereof, or a prodrug thereof. The compounds represented by formula (I) have chemokine antagonistic action, so that they are useful for prevention and/or treatment of various inflammatory diseases, immune diseases such as autoimmune diseases or allergic diseases, or HIV infection.
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PURINE DERIVATIVES AND THEIR PHARMACEUTICAL USES (Fri, 19 Aug 2011)
Compounds of formula (I), wherein; R1 represents hydrogen or C1-3alkyl; n is an integer having a value of 1 to 5; X represents O or NH; Y represents C or N; or a pharmaceutically acceptable salt thereof, have been shown to be inducers of human interferon and may possess an improved profile with respect to known inducers of human interferon, for example enhanced potency. The compounds of the invention may therefore be useful in the treatment of various disorders, in particular the treatment of infectious diseases, cancer, allergic diseases and other inflammatory conditions, and their use as vaccine adjuvants.
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6-AMINO-2-{ [ (1S)-1-METHYLBUTYL] OXY}-9-[5-(1-PIPERIDINYL)-7,9-DIHYDRO-8H-PURIN-8-ONE MALEATE (Fri, 19 Aug 2011)
A compound which is 6-amino-2-{[(1S)-1-methylbutyl]oxy}-9-[5-(1-piperidinyl)pentyl]-7,9-dihydro-8H-purin-8-one: Formula (I) in the form of a maleate salt, may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
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BENZYLPYRROLIDINONE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Fri, 19 Aug 2011)
The present application describes modulators of MCP-1 or CCR-2 of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein m, n, W, X, R1 and R6, are defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.
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6-AMINO-2-{ [ (1S)-1-METHYLBUTYL] OXY}-9-[5-(1-PIPERIDINYL)-7,9-DIHYDRO-8H-PURIN-8-ONE MALEATE (Fri, 19 Aug 2011)
A compound which is 6-amino-2-{[(1S)-1-methylbutyl]oxy}-9-[5-(1-piperidinyl)pentyl]-7,9-dihydro-8H-purin-8-one: Formula (I) in the form of a maleate salt, may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.</p>
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Anionic conjugates of glycosylated bacterial metabolite (Fri, 05 Aug 2011)
<p id="p-0001" num="0000">The invention relates to anionic conjugates of glycosylated bacterial metabolites that may be used to mimic the structure and/or activity of the anionic bioactive molecules known as glycosaminoglycans (GAGs). The invention also relates to processes for the preparation of the conjugates. Such conjugates are useful in the prophylaxis and/or treatment of disease conditions and in particular chronic disease conditions such as inflammatory (including allergic) diseases, metastatic cancers and infection by pathogenic agents including bacteria, viruses or parasites.</p>
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AZABENZIMIDAZOLONES (Fri, 05 Aug 2011)
<p id="p-0001" num="0000">Compounds are provided having the general structure of formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="22.10mm" wi="31.16mm" file="US20110190336A1-20110804-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">In formula I, one member of the group (W, X, Y and Z) is a nitrogen atom and the remaining three members of the group are each independently a carbon atom covalently bonded to a radical, R<sub>4</sub>. The radicals, R<sub>1</sub>, R<sub>2</sub>, R<sub>3 </sub>and R<sub>4 </sub>are each defined herein, and n is an integer from 1 to 4. Also provided are stereoisomers, prodrugs, pharmaceutically acceptable salts, hydrates, salt hydrates, acid salt hydrates, and polymorphs of the compounds having the structure of formula I. The compounds bind the prostaglandin D2 receptor and are useful in the prophylaxis and treatment of prostaglandin D2-mediated diseases and conditions, including pain and inflammation, as well as asthma and allergic diseases and conditions.</p>
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DP2 ANTAGONIST AND USES THEREOF (Fri, 15 Jul 2011)
Described herein is the DP2 anatgonist 2-(3-(2-((tert-butylthio)methyl)-4-(2,2-dimethyl- propionylamino)phenoxy)-4-methoxyphenyl)acetic acid, or a pharmaceutically acceptable salt thereof. Also described are methods of preparing the DP2 anatgonist, or a pharmaceutically acceptable salt thereof. Also described herein are pharmaceutical compositions suitable for administration to a mammal that include the DP2 anatgonist, or a pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating respiratory diseases or conditions, allergic diseases or conditions, inflammatory diseases or conditions, as well as other prostaglandin D2-dependent or prostaglandin D2-mediated diseases or conditions.
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DP2 ANTAGONIST AND USES THEREOF (Fri, 15 Jul 2011)
Described herein is the DP2 anatgonist 2-(3-(2-((tert-butylthio)methyl)-4-(2,2-dimethyl- propionylamino)phenoxy)-4-methoxyphenyl)acetic acid, or a pharmaceutically acceptable salt thereof. Also described are methods of preparing the DP2 anatgonist, or a pharmaceutically acceptable salt thereof. Also described herein are pharmaceutical compositions suitable for administration to a mammal that include the DP2 anatgonist, or a pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating respiratory diseases or conditions, allergic diseases or conditions, inflammatory diseases or conditions, as well as other prostaglandin D2-dependent or prostaglandin D2-mediated diseases or conditions.</p>
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THIENOPYRAZOLE DERIVATIVE HAVING PDE7 INHIBITORY ACTIVITY (Fri, 08 Jul 2011)
<p id="p-0001" num="0000">To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="24.13mm" wi="52.15mm" file="US20110166343A1-20110707-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">[wherein, especially, R<sup>1 </sup>is a cyclohexyl, a cycloheptyl group or a tetrahydropyranyl group; R<sup>2 </sup>is methyl; R<sup>3 </sup>is a hydrogen atom; and R<sup>4 </sup>is a group: —CONR<sup>5</sup>R<sup>6 </sup>(in which any one of R<sup>5 </sup>and R<sup>6 </sup>is a hydrogen atom)].</p>
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Nitrogenous heterocyclic derivative and medicine containing the same as an active ingredient (Fri, 24 Jun 2011)
<p id="p-0001" num="0000">A compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="12.70mm" wi="69.85mm" file="US08410276-20130402-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> (wherein each symbol is as defined in the description.) The compounds represented by formula (I) has the antagonistic activity against CCR5, so they are useful in preventing and/or treating CCR5-related diseases, for example, various inflammatory diseases (asthma, nephritis, nephropathy, hepatitis, arthritis, rheumatoid arthritis, rhinitis, conjunctivitis, inflammatory bowel disease such as ulcerative colitis, etc.), immunological diseases (autoimmune diseases, rejection in organ transplantation (rejection of graft of solid organ, rejection of graft of pancreatic islet cells in therapy for diabetes, graft-versus-host disease, etc.), immunosuppression, psoriasis, multiple sclerosis, etc.), infectious diseases (infection with human immunodeficiency virus, acquired immunodeficiency syndrome, infection with RSV, etc.), allergic diseases (atopic dermatitis, urticaria, allergic bronchopulmonary aspergillosis, allergic eosinophilic gastroenteritis, etc.), cardiovascular diseases (arteriosclerosis, ischemic reperfusion injury, etc.), acute respiratory distress syndrome, shock accompanying bacterial infection, diabetes, cancer metastasis and so on. </p>
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Compound containing basic group and use thereof (Fri, 17 Jun 2011)
<p id="p-0001" num="0000">The present invention relates to a compound represented by formula (I-0):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="14.99mm" wi="69.85mm" file="US08822459-20140902-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein symbols in formula have the same meanings as described in the present specification, a salt thereof, an N-oxide thereof or a solvate thereof or a prodrug thereof, and medical use thereof. </p> <p id="p-0003" num="0000">The compound of the present invention has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, transplanted organ rejection, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy.</p>
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Compounds having CRTH2 antagonist activity (Fri, 17 Jun 2011)
<p id="p-0001" num="0000">Compounds of general formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="48.01mm" wi="69.85mm" file="US08536158-20130917-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein <br/> W is chloro or fluoro; <br/> R<sup>1 </sup>is phenyl optionally substituted with one or more substituents, selected from halo, —CN, —C<sub>1</sub>-C<sub>6 </sub>alkyl, —SOR<sup>3</sup>, —SO<sub>2</sub>R<sup>3</sup>, —SO<sub>2</sub>N(R<sup>2</sup>)<sub>2</sub>, —N(R<sup>2</sup>)<sub>2</sub>, —NR<sup>2</sup>C(O)R<sup>3</sup>, —CO<sub>2</sub>R<sup>2</sup>, —CONR<sup>2</sup>R<sup>3</sup>, —NO<sub>2</sub>, —OR<sup>2</sup>, —SR<sup>2</sup>, —O(CH<sub>2</sub>)<sub>p</sub>OR<sup>2</sup>, or —O(CH<sub>2</sub>)<sub>p</sub>O(CH<sub>2</sub>)<sub>q</sub>OR<sup>2 </sup>wherein <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">each R<sup>2 </sup>is independently hydrogen, —C<sub>1</sub>-C<sub>6 </sub>alkyl, —C<sub>3</sub>-C<sub>8 </sub>cycloalkyl, aryl or heteroaryl;</li> <li id="ul0002-0002" num="0000">each R<sup>3 </sup>is independently, —C<sub>1</sub>-C<sub>6 </sub>alkyl, —C<sub>3</sub>-C<sub>8 </sub>cycloalkyl, aryl or heteroaryl;</li> <li id="ul0002-0003" num="0000">p and q are each independently an integer from 1 to 3; and <br/> R<sup>4 </sup>is hydrogen, C<sub>1</sub>-C<sub>6 </sub>alkyl, C<sub>1</sub>-C<sub>6 </sub>alkyl substituted with aryl, aryl, (CH<sub>2</sub>)<sub>m</sub>OC(═O)C<sub>1</sub>-C<sub>6</sub>alkyl, ((CH<sub>2</sub>)<sub>m</sub>O)<sub>n</sub>CH<sub>2</sub>CH<sub>2</sub>X, (CH<sub>2</sub>)<sub>m</sub>N(R<sup>5</sup>)<sub>2 </sub>or CH((CH<sub>2</sub>)<sub>m</sub>O(C═O)R<sup>6</sup>)<sub>2</sub>; </li> <li id="ul0002-0004" num="0000">m is 1 or 2;</li> <li id="ul0002-0005" num="0000">n is 1-4;</li> <li id="ul0002-0006" num="0000">X is OR<sup>5 </sup>or N(R<sup>5</sup>)<sub>2</sub>;</li> <li id="ul0002-0007" num="0000">R<sup>5 </sup>is hydrogen or methyl; and</li> <li id="ul0002-0008" num="0000">R<sup>6 </sup>is C<sub>1</sub>-C<sub>18 </sub>alkyl; <br/> and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis. </li> </ul> </li> </ul> </p>
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Adenine derivatives (Fri, 17 Jun 2011)
<p id="p-0001" num="0000">The present invention relates to compounds of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.40mm" wi="69.85mm" file="US08563717-20131022-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R<sup>1 </sup>is C<sub>1-6</sub>alkylamino, or C<sub>1-6</sub>alkoxy; R<sup>2 </sup>is a group having the structure: </p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="7.03mm" wi="28.70mm" file="US08563717-20131022-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> n is an integer having a value of 1 to 6; Het is a 6-membered saturated heterocycle containing one nitrogen atom wherein Het is attached to the —(CH<sub>2</sub>)<sub>n</sub>— moiety at any carbon atom of the heterocycle; R<sup>3 </sup>is hydrogen, C<sub>1-8</sub>alkyl, or C<sub>3-7</sub>cycloalkylC<sub>0-6</sub>alkyl; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants. </p>
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PURINE DERIVATIVES FOR USE IN THE TREATMENT OF ALLERGIC, INFLAMMATORY AND INFECTIOUS DISEASES (Fri, 10 Jun 2011)
<p id="p-0001" num="0000">The present invention relates to compounds of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="44.87mm" wi="69.85mm" file="US20110135671A1-20110609-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein R<sup>1 </sup>is C<sub>1-6</sub>alkylamino, C<sub>1-6</sub>alkoxy, or C<sub>3-7</sub>cycloalkyloxy; m is an integer having a value of 2 to 6; R<sup>2 </sup>is hydrogen, C<sub>1-6</sub>alkyl, or C<sub>3-7</sub>cycloalkylC<sub>0-6</sub>alkyl; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.</p>
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Purine derivatives for use in the treatment of allergic, inflammatory and infectious diseases (Fri, 10 Jun 2011)
<p id="p-0001" num="0000">The present invention relates to compounds of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="36.91mm" wi="69.85mm" file="US08575181-20131105-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R<sup>1 </sup>is C<sub>1-6</sub>alkylamino, or C<sub>1-6</sub>alkoxy; m is an integer having a value of 3, 4, or 5; n is an integer having a value of 0 to 3; p is an integer having a value of 1 or 2 and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants. </p>
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Nitrogen-containing spirocyclic compounds and pharmaceutical uses thereof (Fri, 10 Jun 2011)
<p id="p-0001" num="0000">A compound of the following general formula [I]:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="46.74mm" wi="52.49mm" file="US08609647-20131217-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein each symbol has the same meaning as defined herein, or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a pharmaceutical use of the same in treating organ transplant rejection, graft versus host reaction after transplantation, autoimmune disease, allergic disease and chronic myeloproliferative disease. </p>
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INDOLE COMPOUND AND PHARMACEUTICAL USE THEREOF (Sat, 04 Jun 2011)
Disclosed are: a therapeutic or prophylactic agent for inflammatory diseases, allergic diseases and autoimmune diseases; an agent for suppressing rejection in organ transplantation; and the like. Specifically disclosed is a compound represented by general formula (I), a pharmaceutically acceptable salt thereof, or a solvate thereof. (In the formula, the symbols are as defined in the description.)</p>
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Compounds having CRTH2 antagonist activity (Fri, 27 May 2011)
<p id="p-0001" num="0000">Compounds of general formula (II)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="47.41mm" wi="69.85mm" file="US08563536-20131022-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000">W is chloro or fluoro;</li> <li id="ul0001-0002" num="0000">R<sup>1 </sup>is phenyl optionally substituted with one or more substituents, selected from halo, —CN, —C<sub>1</sub>-C<sub>6 </sub>alkyl, —SOR<sup>3</sup>, —SO<sub>2</sub>R<sup>3</sup>, —SO<sub>2</sub>N(R<sup>2</sup>)<sub>2</sub>, —N(R<sup>2</sup>)<sub>2</sub>, —NR<sup>2</sup>C(O)R<sup>3</sup>, —CO<sub>2</sub>R<sup>2</sup>, —CONR<sup>2</sup>R<sup>3</sup>, —NO<sub>2</sub>, —OR<sup>2</sup>, —SR<sup>2</sup>, —O(CH<sub>2</sub>)<sub>p</sub>OR<sup>2</sup>, or —O(CH<sub>2</sub>)<sub>p</sub>O(CH<sub>2</sub>)<sub>q</sub>OR<sup>2 </sup>wherein <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">each R<sup>2 </sup>is independently hydrogen, —C<sub>1</sub>-C<sub>6 </sub>alkyl, —C<sub>3</sub>-C<sub>8 </sub>cycloalkyl, aryl or heteroaryl;</li> <li id="ul0002-0002" num="0000">each R<sup>3 </sup>is independently, —C<sub>1</sub>-C<sub>6 </sub>alkyl, —C<sub>3</sub>-C<sub>8 </sub>cycloalkyl, aryl or heteroaryl;</li> <li id="ul0002-0003" num="0000">p and q are each independently an integer from 1 to 3; and</li> </ul> </li> <li id="ul0001-0003" num="0000">R<sup>4 </sup>is hydrogen, C<sub>1</sub>-C<sub>6 </sub>alkyl, C<sub>1</sub>-C<sub>6 </sub>alkyl substituted with aryl, aryl, (CH<sub>2</sub>)<sub>m</sub>OC(═O)C<sub>1</sub>-C<sub>6</sub>alkyl, ((CH<sub>2</sub>)<sub>m</sub>O)<sub>n</sub>CH<sub>2</sub>CH<sub>2</sub>X, (CH<sub>2</sub>)<sub>m</sub>N(R<sup>5</sup>)<sub>2 </sub>or CH((CH<sub>2</sub>)<sub>m</sub>O(C═O)R<sup>6</sup>)<sub>2</sub>; <ul id="ul0003" list-style="none"> <li id="ul0003-0001" num="0000">m is 1 or 2;</li> <li id="ul0003-0002" num="0000">n is 1-4;</li> <li id="ul0003-0003" num="0000">X is OR<sup>5 </sup>or N(R<sup>5</sup>)<sub>2</sub>;</li> <li id="ul0003-0004" num="0000">R<sup>5 </sup>is hydrogen or methyl; and</li> <li id="ul0003-0005" num="0000">R<sup>6 </sup>is C<sub>1</sub>-C<sub>18 </sub>alkyl; <br/> and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis. </li> </ul> </li> </ul> </p>
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PIPERIDINYL DERIVATIVE AS A MODULATOR OF CHEMOKINE RECEPTOR ACTIVITY (Thu, 26 May 2011)
The present application describes the compound of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and arthrosclerosis using the compound of the invention are disclosed.
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COMPETITIVE INHIBITORS OF INVARIANT CHAIN EXPRESSION AND/OR ECTOPIC CLIP BINDING (Fri, 20 May 2011)
<p id="p-0001" num="0000">The invention relates to methods for modulating the immune function through targeting of CLIP molecules. The result is wide range of new therapeutic regimens for treating, inhibiting the development of, or otherwise dealing with, a multitude of illnesses and conditions, including autoimmune disease, cancer, Alzheimer's disease, allergic disease, transplant and cell graft rejection, HIV infection and other viral, bacterial, and parasitic infection, and AIDS. Methods are also provided for preparing a peptide having the property of being able to displace CLIP by feeding one or more peptide sequences into software that predicts MHC Class II binding regions in an antigen sequence and related products.</p>
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Cyclohexenyl modulators of chemokine receptor activity (Fri, 20 May 2011)
<p id="p-0001" num="0000">The present application describes modulators of MCP-1 or CCR-2 of formula, (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein T, W, X, Y, Z, R<sup>1</sup>, R<sup>2</sup>, R<sup>4 </sup>and R<sup>6</sup>, are defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula, (I) are disclosed.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="36.24mm" wi="57.74mm" file="US08507559-20130813-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Matrix metalloproteinase inhibitors (Thu, 19 May 2011)
The present invention relates to ²-hydroxy and amino substituted carboxylic acids, which act as matrix metalloprotease inhibitors, particularly diastereomerically pure ²-hydroxy carboxylic acids, corresponding processes for the synthesis of and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase using the compounds.
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Chromene modulators of chemokine receptor activity (Fri, 13 May 2011)
<p id="p-0001" num="0000">The present application describes modulators of MCP-1 or CCR-2 of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W<sup>1</sup>, W<sup>2</sup>, W<sup>3</sup>, Y, Z, R<sup>2</sup>, R<sup>3</sup>, R<sup>3</sup>′ and R<sup>4</sup>, are defined in the specification. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="36.24mm" wi="57.66mm" file="US08759390-20140624-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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CYCLOHEXENYL COMPOUNDS AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Thu, 12 May 2011)
The present application describes modulators of MCP-1 or CCR-2 of formula,(I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein T, W, X, Y, Z, R<sp>1</sp>, R<sp>2</sp>, R<sp>4</sp> and R<sp>6</sp>, are defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula, (I) are disclosed.
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Aminocarboxylic acid derivative and medicinal use thereof (Fri, 06 May 2011)
<p id="p-0001" num="0000">The present invention relates to a compound represented by the formula (I), a salt thereof, an N-oxide form thereof, a solvate thereof, or a prodrug thereof, and a medicament containing the same. The compound represented by the formula (I) has an ability to bind to an S1P receptor (particularly, EDG-1, EDG-6, and/or EDG-8) and is useful for preventing and/or treating for rejection to transplantation, graft-versus-host disease, autoimmune diseases, allergic diseases, neurodegenerating diseases, and the like.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="12.28mm" wi="69.93mm" file="US08575134-20131105-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">wherein all symbols are described in the specification.</li> </ul> </li> </ul> </p>
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PRODRUGS OF A PIPERIDINYL DERIVATIVE AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Fri, 15 Apr 2011)
The present application describes prodrugs of the compound of formula (I):or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis using the prodrug compounds of the invention are disclosed.
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SPIROCYCLIC COMPOUNDS AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Fri, 15 Apr 2011)
The present application describes modulators of chemokine receptor activity of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.
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PRODRUGS OF A PIPERIDINYL DERIVATIVE AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Fri, 15 Apr 2011)
The present application describes prodrugs of the compound of formula (I):or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis using the prodrug compounds of the invention are disclosed.</p>
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Prodrugs of a piperidinyl derivative as modulators of chemokine receptor activity (Fri, 08 Apr 2011)
<p id="p-0001" num="0000">The present application describes prodrugs of the compound of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.77mm" wi="73.91mm" file="US08410139-20130402-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis using the prodrug compounds of the invention are disclosed. </p>
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SPIROPIPERIDINE COMPOUND AND MEDICINAL USE THEREOF (Fri, 04 Mar 2011)
<p id="p-0001" num="0000">The present invention relates to a CXCR3 antagonist comprising a compound represented by formula (I) (wherein all the symbols have the same meaning as defined in the description),</p> <p id="p-0002" num="0000">a salt thereof, a quaternary ammonium salt thereof, an N-oxide form thereof or a solvate thereof, or a prodrug thereof.</p> <p id="p-0003" num="0000">This antagonist is useful as a preventive, therapeutic and/or progression-suppressing agent for a CXCR3-mediated disease such as an immune or an allergic disease [e.g., an atopic disease, an autoimmune disease (e.g., multiple sclerosis, rheumatoid arthritis, systemic lupus erythematosus, type I diabetes, glomerulonephritis, Sjogren's syndrome and the like), systemic inflammatory response syndrome (SIRS), a rejection response to transplanted organ, tissue and/or cell or the like], a gastrointestinal disease [e.g., an inflammatory bowel disease or the like], or a respiratory disease [e.g., asthma, a chronic obstructive pulmonary disease or the like].</p> <p id="p-0004" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="12.95mm" wi="69.85mm" file="US20110052612A1-20110303-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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HETEROCYCLIC JANUS KINASE 3 INHIBITORS (Fri, 18 Feb 2011)
<p id="p-0001" num="0000">The present invention provides a compound having an excellent JAK3 inhibition activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases, inflammatory diseases, and allergic diseases.</p> <p id="p-0002" num="0000">As a result of studies on a novel condensed heterocyclic derivative, the inventors have found that a compound having a cross-linked structure has an excellent JAK3 inhibition activity, and have completed the present invention.</p> <p id="p-0003" num="0000">In other words, it is verified that the compound according to the present invention has an inhibition activity against JAK3 and is thus useful as an active ingredient of an agent for treating or preventing diseases caused by undesirable cytokine signal transmission (e.g., rejection during organ/tissue transplantation, autoimmune diseases, multiple sclerosis, rheumatoid arthritis, psoriasis, asthma, atopic dermatitis, Alzheimer's disease, and atherosclerotic disease), or diseases caused by abnormal cytokine signal transmission (e.g., cancer and leukemia).</p>
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NEW MACROLIDES AND THEIR USE (Fri, 18 Feb 2011)
The invention relates to macrolide compounds of formula (I), the use of said compounds as medicaments, in particular for the treatment or prevention of inflammatory and allergic diseases, pharmaceutical compositions containing said compounds and to processes for their preparation. The invention relates in particular to macrolide compounds with antiinflammatory activity mediated primarily through inhibition of phosphodiesterase 4 (PDE4) which makes them useful for the treatment and/or prevention of inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, atopic dermatitis or inflammatory bowel disease or proliferative diseases such as cancer.
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NEW MACROLIDES AND THEIR USE (Fri, 18 Feb 2011)
The invention relates to macrolide compounds of formula (I), the use of said compounds as medicaments, in particular for the treatment or prevention of inflammatory and allergic diseases, pharmaceutical compositions containing said compounds and to processes for their preparation. The invention relates in particular to macrolide compounds with antiinflammatory activity mediated primarily through inhibition of phosphodiesterase 4 (PDE4) which makes them useful for the treatment and/or prevention of inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, atopic dermatitis or inflammatory bowel disease or proliferative diseases such as cancer.</p>
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DP2 antagonist and uses thereof (Fri, 11 Feb 2011)
<p id="p-0001" num="0000">Described herein is the DP<sub>2 </sub>antagonist [2′-(3-benzyl-1-ethyl-ureidomethyl)-6-methoxy-4′-trifluoromethyl-biphenyl-3-yl]-acetic acid, or a pharmaceutically acceptable salt thereof. Also described are methods of preparing the DP2 antagonist, or a pharmaceutically acceptable salt thereof. Also described herein are pharmaceutical compositions suitable for administration to a mammal that include the DP<sub>2 </sub>antagonist, or a pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating respiratory diseases or conditions, allergic diseases or conditions, inflammatory diseases or conditions, as well as other prostaglandin D<sub>2</sub>-dependent or prostaglandin D<sub>2</sub>-mediated diseases or conditions.</p>
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DP2 ANTAGONIST AND USES THEREOF (Fri, 11 Feb 2011)
Described herein is the DP2 antagonist [2'-(3-benzyl-1-ethyl-ureidomethyl)-6-methoxy-4'-trifluoromethyl-biphenyl-3-yl]-acetic acid, or a pharmaceutically acceptable salt thereof. Also described are methods of preparing the DP2 antagonist, or a pharmaceutically acceptable salt thereof. Also described herein are pharmaceutical compositions suitable for administration to a mammal that include the DP2 antagonist, or a pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating respiratory diseases or conditions, allergic diseases or conditions, inflammatory diseases or conditions, as well as other prostaglandin D2-dependent or prostaglandin D2-mediated diseases or conditions.
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DP2 ANTAGONIST AND USES THEREOF (Fri, 11 Feb 2011)
Described herein is the DP2 antagonist [2'-(3-benzyl-1-ethyl-ureidomethyl)-6-methoxy-4'-trifluoromethyl-biphenyl-3-yl]-acetic acid, or a pharmaceutically acceptable salt thereof. Also described are methods of preparing the DP2 antagonist, or a pharmaceutically acceptable salt thereof. Also described herein are pharmaceutical compositions suitable for administration to a mammal that include the DP2 antagonist, or a pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating respiratory diseases or conditions, allergic diseases or conditions, inflammatory diseases or conditions, as well as other prostaglandin D2-dependent or prostaglandin D2-mediated diseases or conditions.</p>
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AZAINDOLE DERIVATIVE HAVING PGD2 RECEPTOR ANTAGONISTIC ACTIVITY (Fri, 04 Feb 2011)
<p id="p-0001" num="0000">The present invention creates an azaindole derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further providing a therapeutic agent for treating allergic diseases.</p> <p id="p-0002" num="0000">A compound of the general formula (I)</p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="31.50mm" wi="65.02mm" file="US20110028717A1-20110203-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a 3- to 8-membered nitrogen-containing non-aromatic heterocyclic ring etc.; the formula of —X<sup>1</sup>═X<sup>2</sup>—X<sup>3</sup>═X<sup>4</sup>— is a formula of —C(R<sup>1</sup>)═C(R<sup>2</sup>)—C(R<sup>3</sup>)═N— etc.; R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4 </sup>and R<sup>5 </sup>are independently a hydrogen atom or a halogen atom etc.; R<sup>6 </sup>is optionally substituted C1-C6 alkyloxy etc.; R<sup>7 </sup>is independently a halogen atom etc.; R<sup>8 </sup>is optionally substituted C1-C6 alky etc.; R<sup>9 </sup>is carboxy etc.; M is sulfonyl etc.; Y is a single bond etc.; L<sup>1</sup>, L<sup>2 </sup>and L<sup>3 </sup>are a single bond or alkylene optionally containing one or two heteroatoms etc.; n is 0 etc.; q is 0 etc.; a pharmaceutically acceptable salt or hydrate thereof.</li> </ul> </li> </ul> </p>
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NITROGEN-CONTAINING SPIRO-RING COMPOUND AND MEDICINAL USE OF SAME (Fri, 04 Feb 2011)
Disclosed are a compound represented by general formula [I], a pharmaceutically acceptable salt thereof or a solvate of the same, and medicinal use thereof for treating rejection in organ transplantation, graft-versus-host reaction after organ transplantation, autoimmune diseases, allergic diseases and chronic myeloproliferative diseases by using these compounds as the active ingredient. In general formula [I], Ra's are the same or different and represent (1) a C1-6 alkyl group, etc.; n1 represents an integer of 0 to 4; Rb's are the same or different and represent (1) a C1-6 alkyl group, etc.; n2 represents an integer of 0 to 4; m1 represents an integer of 0 to 3; m2 represents an integer of 1 to 4; Xa=Xb represents (1) CH=CH, etc.; X represents (1) a nitrogen atom, etc.; and Rc represents (1) a hydrogen atom, etc.</p>
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Compound capable of binding S1P receptor and pharmaceutical use thereof (Fri, 28 Jan 2011)
<p id="p-0001" num="0000">A compound having an ability to bind to an SIP receptor and represented by formula (I), a salt thereof, a solvate thereof or a prodrug thereof is useful for prevention and/or treatment of rejection of transplantation, graft-versus-host disease, autoimmune disease, allergic disease and the like:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="11.60mm" wi="69.85mm" file="US08791159-20140729-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">wherein ring A is a cyclic group; ring B is a cyclic group which may have substituent(s); X is a spacer having 1 to 8 atoms in its main chain, etc.; Y is a spacer having 1 to 10 atoms in its main chain, etc.; n is 0 or 1, wherein when n is 0, m is 1 and R<sup>1 </sup>is a hydrogen atom or a substituent, and wherein when n is 1, m is 0 or an integer of 1 to 7 and R<sup>1 </sup>is a substituent, and wherein m is 2 or more, R<sup>1</sup>s are the same or different.</li> </ul> </li> </ul> </p>
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Macrolides and uses of macrolides (Fri, 28 Jan 2011)
<p id="p-0001" num="0000">Macrolides of Formula (I) or (I-A): and wherein the residues R1, R2, R3, R4, R12, R13 and R14 have certain meanings defined in this application are useful for treating or preventing inflammatory or allergic diseases or, cancer in animals and humans.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="111.59mm" wi="69.85mm" file="US08445451-20130521-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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TETRAZOLE DERIVATIVES (Fri, 21 Jan 2011)
The present invention relates to compounds of formula (I) for use as pharmaceutical active compounds, as well as pharmaceutical formulations containing the same, for the treatment of allergic diseases.
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TRICYCLIC INDOLE-DERIVED SPIRO DERIVATIVES AS CRTH2 MODULATORS (Fri, 21 Jan 2011)
The present invention relates to compounds of formula (I) for use as pharmaceutical active compounds, as well as pharmaceutical formulations containing the same, for the treatment of allergic diseases. The compounds according to Formula (I) are suitable as modulators of CRTH2. The invention provides spiro derivatives according to Formula (I) and related formulae that are useful in the treatment and/or prevention of diseases selected from allergic diseases such as allergic asthma, allergic rhinitis, allergic conjunctivitis, and inflammatory dermatoses such as atopic dermatitis, contact hypersensitivity, allergic contact dermatitis, chronic urticaria/chronic idiopathic/autoimmune urticaria, drag-induced exanthems (e.g. toxic epidermal necrolysis or Lyell's syndrome/Stevens-Johnson syndrome/drug hypersensitivity syndrome), photodermatosis or polymorphous light eruption (e.g. photo-irritant contact dermatitis, photoallergy contact dermatitis, chronic actinic dermatitis), and myositis neurodegenerative disorders such as neuropatic pain and other diseases with an inflammatory component such as rheumatoid arthritis, multiple sclerosis, osteoarthritis, and inflammatory bowel disease (IBD).
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TRICYCLIC INDOLE-DERIVED SPIRO DERIVATIVES AS CRTH2 MODULATORS (Fri, 21 Jan 2011)
The present invention relates to compounds of formula (I) for use as pharmaceutical active compounds, as well as pharmaceutical formulations containing the same, for the treatment of allergic diseases. The compounds according to Formula (I) are suitable as modulators of CRTH2. The invention provides spiro derivatives according to Formula (I) and related formulae that are useful in the treatment and/or prevention of diseases selected from allergic diseases such as allergic asthma, allergic rhinitis, allergic conjunctivitis, and inflammatory dermatoses such as atopic dermatitis, contact hypersensitivity, allergic contact dermatitis, chronic urticaria/chronic idiopathic/autoimmune urticaria, drag-induced exanthems (e.g. toxic epidermal necrolysis or Lyell's syndrome/Stevens-Johnson syndrome/drug hypersensitivity syndrome), photodermatosis or polymorphous light eruption (e.g. photo-irritant contact dermatitis, photoallergy contact dermatitis, chronic actinic dermatitis), and myositis neurodegenerative disorders such as neuropatic pain and other diseases with an inflammatory component such as rheumatoid arthritis, multiple sclerosis, osteoarthritis, and inflammatory bowel disease (IBD).</p>
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TETRAZOLE DERIVATIVES (Fri, 21 Jan 2011)
The present invention relates to compounds of formula (I) for use as pharmaceutical active compounds, as well as pharmaceutical formulations containing the same, for the treatment of allergic diseases.</p>
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Hydroxyalkanyl amides as modulators of chemokine receptor activity (Fri, 14 Jan 2011)
<p id="p-0001" num="0000">The application describes modulators of MIP-1α or CCR-1 of the formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein ring A, T, V, R<sub>1</sub>, R<sub>2 </sub>and R<sub>5</sub>, are defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="19.39mm" wi="62.48mm" file="US08492550-20130723-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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HYDROXYALKANYL AMIDES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Thu, 30 Dec 2010)
The application describes modulators of MIP-1α or CCR-1 of the formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein ring A, T, V, R<sb>1</sb>, R<sb>2</sb> and R<sb>5</sb>, are defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.
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Pyrimidine derivatives useful for the treatment of diseases mediated by CRTH2 (Fri, 24 Dec 2010)
<p id="p-0001" num="0000">The present invention relates to a pyrimidine derivative of the formula (I) and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The pyrimidine derivative of the present invention has excellent CRTH2 (G-protein-coupled chemoattractant receptor, expressed on Th2 cells) antagonistic activity and can be used for the prophylaxis and treatment of diseases associated with CRTH2 activity, in particular for the treatment of allergic diseases, such as asthma, allergic rhinitis, atopic dermatitis, and allergic conjunctivitis; eosinophil-related diseases, such as Churg-Strauss syndrome and sinusitis; basophil-related diseases, such as basophilic leukemia, chronic urticaria and basophilic leukocytosis in human and other mammals; and inflammatory diseases characterized by T lymphocytes and profuse leukocyte infiltrates such as psoriasis, eczema, inflammatory bowel disease, ulcerative colitis, Crohn's disease, COPD (chronic obstructive pulmonary disorder) and arthritis.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="47.50mm" wi="69.85mm" file="US07960393-20110614-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Novel Glucocorticoid Receptor Agonists (Fri, 03 Dec 2010)
<p id="p-0001-en" num="0000">This invention relates to novel glucocorticoid receptor agonists of formula (I):</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="42.67mm" wi="74.00mm" file="US20100303758A1-20101202-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003-en" num="0000">and to processes and intermediates for their preparation. The present invention also relates to pharmaceutical compositions containing these compounds, to their combination with one or more other therapeutic agents, as well as to their use for the treatment of a number of inflammatory and allergic diseases, disorders and conditions.</p>
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NOVEL GLUCOCORTICOID RECEPTOR AGONISTS (Fri, 03 Dec 2010)
This invention relates to novel glucocorticoid receptor agonists of formula (I) and to processes and intermediates for their preparation. The present invention also relates to pharmaceutical compositions containing these compounds, to their combination with one or more other therapeutic agents, as well as to their use for the treatment of a number of inflammatory and allergic diseases, disorders and conditions.
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NOVEL GLUCOCORTICOID RECEPTOR AGONISTS (Fri, 03 Dec 2010)
This invention relates to novel glucocorticoid receptor agonists of formula (I) and to processes and intermediates for their preparation. The present invention also relates to pharmaceutical compositions containing these compounds, to their combination with one or more other therapeutic agents, as well as to their use for the treatment of a number of inflammatory and allergic diseases, disorders and conditions. </p>
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PYRAZOLOPYRIMIDINE COMPOUND (Fri, 26 Nov 2010)
<p id="p-0001-en" num="0000">Disclosed is a novel compound having Syk and/or Abl inhibitory activities, which is useful for prevention/treatment of allergic diseases, autoimmune diseases, arthritides and cancers. Specifically disclosed is a pyrazolopyrimidine compound represented by the formula [I] or [III] below, a tautomer thereof, a stereoisomer thereof, a pharmaceutically acceptable salt thereof, or a solvent of any of them.</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="60.62mm" wi="69.85mm" file="US20100298557A1-20101125-C00001.TIF" img-content="photograph" img-format="png"/> </chemistry> </p>
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COMPOUNDS HAVING CRTH2 ANTAGONIST ACTIVITY (Thu, 18 Nov 2010)
Compounds of general formula (I) wherein W is chloro or fluoro; R<sp>1 </sp>is phenyl optionally substituted with one or more substituents selected from halo, -CN, -C<sb>1</sb>-C<sb>6</sb> alkyl, -SOR<sp>3</sp>, -SO<sb>2</sb>R<sp>3</sp>, -SO<sb>2</sb>N(R<sp>2</sp>)<sb>2</sb>, -N(R<sp>2</sp>)<sb>2</sb>, -NR<sp>2</sp>C(O)R<sp>3</sp>, -CO<sb>2</sb>R<sp>2</sp>, - CONR<sp>2</sp>R<sp>3</sp>, -NO<sb>2</sb>, -OR<sp>2</sp>, -SR<sp>2</sp>, -O(CH<sb>2</sb>)<sb>P</sb>OR<sp>2,</sp> and -O(CH<sb>2</sb>)<sb>p</sb>O(CH<sb>2</sb>)<sb>q</sb>OR<sp>2</sp> wherein each R<sp>2</sp> is independently hydrogen, -C<sb>1</sb>-C<sb>6</sb> alkyl, -C<sb>3</sb>-C<sb>8</sb> cycloalkyl, aryl or heteroaryl; each R<sp>3 </sp>is independently, -C<sb>1</sb>-C<sb>6</sb> alkyl, -C<sb>3</sb>-C<sb>8</sb> cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
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MACROLIDES FOR TREATING DISEASES MEDIATED THROUGH PDE INHIBITION (Thu, 11 Nov 2010)
Macrolides of Formula (I) or (I-A): and wherein the residues R1, R2, R3, R4, R12, R13 and R14 have certain meanings defined in this application are useful for treating or preventing inflammatory or allergic diseases or. cancer in animals and humans.
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Compounds having CRTH2 antagonist activity (Fri, 22 Oct 2010)
<p id="p-0001" num="0000">Compounds of general formula (II)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="46.23mm" wi="69.93mm" file="US07919512-20110405-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein <br/> W is chloro or fluoro; <br/> R<sup>1 </sup>is phenyl optionally substituted with one or more substituents, selected from halo, —CN, —C<sub>1</sub>-C<sub>6 </sub>alkyl, —SOR<sup>3</sup>, —SO<sub>2</sub>R<sup>3</sup>, —SO<sub>2</sub>N(R<sup>2</sup>)<sub>2</sub>, —N(R<sup>2</sup>)<sub>2</sub>, —NR<sup>2</sup>C(O)R<sup>3</sup>, —CO<sub>2</sub>R<sup>2</sup>, —CONR<sup>2</sup>R<sup>3</sup>, —NO<sub>2</sub>, —OR<sup>2</sup>, —SR<sup>2</sup>, —O(CH<sub>2</sub>)<sub>p</sub>OR<sup>2</sup>, or —O(CH<sub>2</sub>)<sub>p</sub>O(CH<sub>2</sub>)<sub>q</sub>OR<sup>2 </sup>wherein <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">each R<sup>2 </sup>is independently hydrogen, —C<sub>1</sub>-C<sub>6 </sub>alkyl, —C<sub>3</sub>-C<sub>8 </sub>cycloalkyl, aryl or heteroaryl;</li> <li id="ul0002-0002" num="0000">each R<sup>3 </sup>is independently, —C<sub>1</sub>-C<sub>6 </sub>alkyl, —C<sub>3</sub>-C<sub>8 </sub>cycloalkyl, aryl or heteroaryl;</li> <li id="ul0002-0003" num="0000">p and q are each independently an integer from 1 to 3; and <br/> R<sup>4 </sup>is hydrogen, C<sub>1</sub>-C<sub>6 </sub>alkyl, C<sub>1</sub>-C<sub>6 </sub>alkyl substituted with aryl, aryl, (CH<sub>2</sub>)<sub>m</sub>OC(═O)C<sub>1</sub>-C<sub>6</sub>alkyl, ((CH<sub>2</sub>)<sub>m</sub>O)<sub>n</sub>CH<sub>2</sub>CH<sub>2</sub>X, (CH<sub>2</sub>)<sub>m</sub>N(R<sup>5</sup>)<sub>2 </sub>or CH((CH<sub>2</sub>)<sub>m</sub>O(C═O)R<sup>6</sup>)<sub>2</sub>; </li> <li id="ul0002-0004" num="0000">m is 1 or 2;</li> <li id="ul0002-0005" num="0000">n is 1-4;</li> <li id="ul0002-0006" num="0000">X is OR<sup>5 </sup>or N(R<sup>5</sup>)<sub>2</sub>;</li> <li id="ul0002-0007" num="0000">R<sup>5 </sup>is hydrogen or methyl; and</li> <li id="ul0002-0008" num="0000">R<sup>6 </sup>is C<sub>1</sub>-C<sub>18 </sub>alkyl; <br/> and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis. </li> </ul> </li> </ul> </p>
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CHEMOKINE RECEPTOR ANTAGONIST AND MEDICAL USE THEREOF (Fri, 22 Oct 2010)
<p id="p-0001-en" num="0000">The present invention relates to a compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof, and medical use thereof (the symbols in the formula are as described in the specification).</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="21.51mm" wi="69.85mm" file="US20100266539A1-20101021-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003-en" num="0000">The compound represented by formula (I) has chemokine receptor (especially in CCR4 and/or CCR5) antagonistic activity. Therefore it is useful for prevention and/or treatment of a chemokine receptor-mediated disease such as inflammatory and/or allergic diseases [systemic inflammatory response syndrome (SIRS), anaphylaxis, anaphylactoid reaction, allergic angiitis, transplant rejection reaction, hepatitis, nephritis, nephropathy, pancreatitis, rhinitis, arthritis, inflammatory ocular disease, inflammatory bowel disease, disease in cerebro and/or circulatory system, respiratory disease, dermatosis, autoimmune disease, and the like], infection [viral disease (human immunodeficiency virus infection, acquired immunodeficiency syndrome, SARS, etc.), and the like], and the like.</p>
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SPIRO-PIPERIDINE COMPOUNDS AND MEDICINAL USE THEREOF (Fri, 15 Oct 2010)
<p id="p-0001-en" num="0000">The present invention relates to a spiro-piperidine compound represented by formula (I):</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="12.45mm" wi="69.93mm" file="US20100261641A1-20101014-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003-en" num="0000">wherein R<sup>1 </sup>represents hydrogen, an aliphatic hydrocarbon group which may have a substituent(s) or a cyclic group which may have a substituent(s); and ring A represents a 5- to 8-membered cyclic group which may have a substituent(s), a salt thereof, an N-oxide thereof, a quaternary ammonium salt thereof or a solvate thereof, or a prodrug thereof. The compounds represented by formula (I) have chemokine antagonistic action, so that they are useful for prevention and/or treatment of various inflammatory diseases, immune diseases such as autoimmune diseases or allergic diseases, or HIV infection.</p>
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8-oxoadenine derivatives acting as modulators of TLR7 (Fri, 24 Sep 2010)
<p id="p-0001" num="0000">The present invention provides 8-oxoadenine derivatives, processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The 8-oxoadenine derivatives act as modulators of Toll-like Receptor (TLR) 7 and thus may be used in the treatment of asthma, hepatitis, allergic diseases, viral and bacterial infection as well as cancer.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.73mm" wi="73.58mm" file="US08138172-20120320-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Amino cyclopentyl heterocyclic and carbocyclic modulators of chemokine receptor activity (Fri, 17 Sep 2010)
<p id="p-0001-en" num="0000">Compounds of the formulae (I) and (II): (wherein Q, X, E, G<sup>1</sup>, G<sup>2</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>6 </sup>and Z are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="48.09mm" wi="59.01mm" file="US20100234409A1-20100916-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p>
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SUBSTITUTED FUSED PYRIMIDINE COMPOUNDS (Fri, 17 Sep 2010)
The present invention discloses substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, solvates, pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor, such as asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders, and/or autoimmune diseases.
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SUBSTITUTED FUSED PYRIMIDINE COMPOUNDS (Fri, 17 Sep 2010)
The present invention discloses substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, solvates, pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor, such as asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders, and/or autoimmune diseases. </p>
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NOVEL GLUCOCORTICOID RECEPTOR AGONISTS (Thu, 09 Sep 2010)
This invention relates to novel glucocorticoid receptor agonists of formula (I) and to processes and intermediates for their preparation. The present invention also relates to pharmaceutical compositions containing these compounds, to their combination with one or more other therapeutic agents, as well as to their use for the treatment of a number of inflammatory and allergic diseases, disorders and conditions.
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QUINOLINE DERIVATIVES USED TO TREAT INFLAMMATORY AND ALLERGIC DISEASES (Fri, 03 Sep 2010)
<p id="p-0001-en" num="0000">The present invention relates to compounds of formula (I)</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="41.06mm" wi="52.32mm" file="US20100222349A1-20100902-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003-en" num="0000">and salts thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various diseases, such as allergic rhinitis.</p>
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Piperidine derivatives as modulators of chemokine receptor activity (Fri, 03 Sep 2010)
<p id="p-0001" num="0000">The present application describes modulators of MIP-1 of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as set forth above. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators are disclosed.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="23.54mm" wi="68.50mm" file="US08536198-20130917-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Nitrogen-containing heterocyclic compounds and medicinal use thereof (Fri, 03 Sep 2010)
<p id="p-0001" num="0000">The compound represented by formulae (I) and (II), the salt thereof, the N-oxide thereof or the solvate thereof, or the prodrug thereof and the pharmaceutical composition comprising thereof have a CXCR4-regulating effect, and they are effective in treatment and prevention of various inflammatory disease, various allergic disease, acquired immunodeficiency syndrome infection with human immunodeficiency virus, or agents for regeneration therapy.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.92mm" wi="69.85mm" file="US08153625-20120410-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> (wherein ring A represents a nitrogen-containing heterocyclic group which may have a substituent(s); ring B represents a homocyclic group which may have a substituent(s) or a heterocyclic group which may have a substituent(s); and Y represents a hydrocarbon group which may have a substituent(s), a heterocyclic group which may have a substituent(s), an amino group which may be protected, a hydroxyl group which may be protected or a mercapto group which may be protected; T represents ring A or an amino group which may be protected.). </p>
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USE OF COMPOUNDS HAVING CCR ANTAGONISM (Fri, 27 Aug 2010)
<p id="p-0001-en" num="0000">It is intended to provide preventives/remedies for graft-versus-host disease and/or rejection in organ or bone marrow transplantation, rheumatoid arthritis, autoimmune diseases, allergic diseases, ischemic cerebral cell injury, myocardial infarction, chronic nephritis and arteriosclerosis. The above object can be achieved by preventives/remedies for graft-versus-host disease and/or rejection in organ or bone marrow transplantation, rheumatoid arthritis, autoimmune diseases, allergic diseases, ischemic cerebral cell injury, myocardial infarction, chronic nephritis and arteriosclerosis characterized by containing a specific compound having a CCR (CC chemokine receptor) antagonism.</p>
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HETERO RING DERIVATIVE (Fri, 20 Aug 2010)
Disclosed is a novel excellent prophylactic or therapeutic method for rejections in various types of organ transplan-tation, allergic diseases, autoimmune diseases, hematologic tumors and others, which relies on a selective inhibitory activity on PI3K.delta. and/or an inhibitory activity on the production of II-2 and/or an inhibitory activity on the proliferation of B cells (includ-ing an inhibitory activity on the activation of B cells). It is found that a tri-substituted triazine derivative or a tri-substituted pyrim-idine derivative has a selective inhibitory activity on PI3K.delta. and/or an inhibitory activity on the production of IL-2 and/or an in-hibitory activity on the proliferation of B cells (including an inhibitory activity on the activation of B cells) and can be used as a prophylactic or therapeutic agent for rejections in various types of organ transplantation, allergic diseases (e.g., asthma, atopic der-matitis), autoimmune diseases (e.g., rheumatoid arthritis, psoriasis, ulcerative colitis, Crohn diseases, systemic lupus erythemato-sus), hematologic tumors (e.g., leukemia) and others. </p>
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Piperidinyl derivatives as modulators of chemokine receptor activity (Fri, 13 Aug 2010)
<p id="p-0001" num="0000">The present application describes modulators of MIP-1α of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R<sub>1</sub>, R<sub>3</sub>, R<sub>4</sub>, R<sub>5</sub>, R<sub>5a </sub>and R<sub>5b</sub>, are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators of formula (I) are disclosed.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="23.20mm" wi="70.95mm" file="US08501782-20130806-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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LOW-MOLECULAR POLYSULFATED HYALURONIC ACID DERIVATIVE AND MEDICINE CONTAINING SAME (Fri, 06 Aug 2010)
A low-molecular-weight polysulfated hyaluronic acid derivative useful for prevention and/or treatment of an allergic disease. An agent for prevention and/or treatment of an allergic disease selected from pollinosis, allergic rhinitis, allergic conjunctivitis, atopic dermatitis, and asthma, represented by the following general formula (IA) or (IB); <img he="0" wi="0" file="" alt="" img-content="undefined" img-format="jpg" inline="yes" orientation="portrait"/> (I A) <img he="0" wi="0" file="" alt="" img-content="undefined" img-format="jpg" inline="yes" orientation="portrait"/> (I B) wherein n represents a number of 0 to 15; R's each independently represent a hydrogen atom or an SO3H group etc. 110 </p>
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CLIP INHIBITORS AND METHODS OF MODULATING IMMUNE FUNCTION (Fri, 02 Jul 2010)
<p id="p-0001-en" num="0000">The invention relates to methods for modulating the immune function through targeting of CLIP molecules. The result is wide range of new therapeutic regimens for treating, inhibiting the development of, or otherwise dealing with, a multitude of illnesses and conditions, including autoimmune disease, allergic disease transplant and cell graft rejection, cancer, bacterial infection, HIV infection, and AIDS.</p>
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Preventative treatment and remission of allergic diseases (Fri, 02 Jul 2010)
<p id="p-0001" num="0000">The invention provides the use of at least one plant selected from plants of the family Zingiberaceae in the preparation of a medicament for use in the treatment or prophylaxis of allergic diseases. The plant is optionally selected from the genera <i>Siphonochilus, Kaempferia, Cienkowskia </i>and <i>Cienkowskiella </i>and the species is optionally selected from <i>Siphonochilus aethiopicus, Siphonochilus natalensis, Kaempferia aethiopica, Kaempferia natalensis, Kaempferia ethelae, Cienkowskia aethiopica </i>and <i>Cienkowskiella aethiopica</i>. The allergic disease is selected from asthma and atopy.</p>
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7-PHENOXYCHROMAN CARBOXYLIC ACID DERIVATIVES (Fri, 02 Jul 2010)
Compounds of Formula I: (I) in which A, A1, R1, R7a, R7b, R8 and R10 have the meanings given in the specification, are DP2 receptor inhibitors useful in the treatment of useful in the treatment and prevention of immunologic diseases, allergic diseases such as asthma, allergic rhinitis and atopic dermatitis, and other inflammatory diseases mediated by prostaglandin D2 (PGD2). The compounds of Formula I may also be useful in treating diseases or medical conditions involving the Th2 T cell via production of IL-4, IL-5 and/or IL-13.
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ISOQUINOLINE DERIVATIVE (Fri, 02 Jul 2010)
A compound represented by formula (I) or a pharmaceutically acceptable salt thereof has an effect of inhibiting CRTH2 and, therefore, is useful as a preventive or a remedy for allergic diseases such as asthma, atopic dermatitis and allergic rhinitis. </p>
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7-PHENOXYCHROMAN CARBOXYLIC ACID DERIVATIVES (Fri, 02 Jul 2010)
Compounds of Formula I: (I) in which A, A', R1, R7a, R7b, R8 and R10 have the meanings given in the specification, are DP2 receptor inhibitors useful in the treatment of useful in the treatment and prevention of immunologic diseases, allergic diseases such as asthma, allergic rhinitis and atopic dermatitis, and other inflammatory diseases mediated by prostaglandin D2 (PGD2). The compounds of Formula I may also be useful in treating diseases or medical conditions involving the Th2 T cell via production of IL-4, IL-5 and/or IL-13. </p>
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NOVEL CRYSTALLINE BEPOTASTINE METAL SALT HYDRATE, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME (Fri, 04 Jun 2010)
<p id="p-0001-en" num="0000">The present invention discloses a non-hygroscopic crystalline bepotastine metal salt hydrate, a method for preparing same, and a pharmaceutical composition comprising same for treating or preventing a histamine-mediated disease or an allergic disease.</p>
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Target protein and target gene in drug designing and screening method (Fri, 04 Jun 2010)
<p id="p-0001" num="0000">The present invention provides a novel target protein and a gene for drug discovery, and a means that enables development of a novel pharmaceutical agent by using the same. More particularly, the present invention provides CARP and genes thereof; screening methods for drugs (e.g., antiallergic drugs); a regulator of diseases (e.g., allergic diseases); a drug derivative production method; a complex comprising a drug and CARP, and a production method thereof; kits comprising a drug or a salt thereof; determination methods for the onset or risk of onset of a specified disease, determination methods for susceptibility to a drug, and determination kits used for said methods, and the like.</p>
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Macrolides useful against inflammatory and allergic diseases (Fri, 14 May 2010)
<p id="p-0001" num="0000">New macrolide general compounds of formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="54.02mm" wi="69.09mm" file="US08173609-20120508-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> with improved activity making them useful for inhibiting human phosphodiesterase 4 and treating chronic obstructive pulmonary disease (COPD). </p>
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PURINE DERIVATIVES AS IMMUNOMODULATORS (Fri, 14 May 2010)
<p id="p-0001-en" num="0000">Compounds of formula (I):</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="25.57mm" wi="69.85mm" file="US20100120799A1-20100513-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003-en" num="0000">wherein <ul id="ul0001-en" list-style="none"><li><ul id="ul0002-en" list-style="none"><li>R<sup>1 </sup>is C<sub>1-8</sub>alkylamino, C<sub>1-8</sub>alkoxy, C<sub>3-7</sub>cycloalkylC<sub>1-6</sub>alkylamino, C<sub>3-7</sub>cycloalkylC<sub>1-6</sub>alkoxy, C<sub>1-3</sub>alkoxyC<sub>2-3</sub>alkoxy, or Het<sup>b</sup>-C<sub>1-3</sub>alkoxy;</li><li>Het<sup>b </sup>is a 5- or 6-membered saturated aliphatic heterocycle containing one oxygen atom;</li><li>R<sup>2 </sup>is —(CH<sub>2</sub>)<sub>n</sub>-Het;</li><li>n is an integer having a value of 1 to 4;</li><li>Het is a 5- or 6-membered saturated aliphatic heterocycle containing one oxygen heteroatom, which heterocycle may be substituted by one or two C<sub>1-4</sub>alkyl groups, and salts and solvates thereof, are inducers of human interferon and may be useful in the treatment of various disorders in particular infectious diseases, cancer, and allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, and as vaccine adjuvants.</li></ul></li></ul></p>
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8-azaprostaglandin derivative compound and agent comprising the compound as active ingredient (Fri, 07 May 2010)
<p id="p-0001" num="0000">An 8-azaprostaglandin represented by formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="19.47mm" wi="69.93mm" file="US08026273-20110927-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> (wherein all symbols have the same meanings as described in the specification), a pharmaceutically acceptable salt thereof or a cyclodextrin clathrate thereof. Since the compound represented by formula (I) binds to EP2 subtype among PGE receptor strongly, it is useful for preventive and/or treatment for immune diseases, allergic diseases, neuronal cell death, dysmenorrhea, premature birth, abortion, baldness, retinal neuropathy such as glaucoma, erectile dysfunction, arthritis, pulmonary injury, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, hepatic injury, acute hepatitis, liver cirrhosis, shock, nephritis, renal failure, circulatory diseases, systemic inflammatory response syndrome, sepsis, hemophagocytosis syndrome, macrophage activation syndrome, still disease, Kawasaki Disease, burn, systemic granuloma, ulcerative colitis, Crohn disease, hypercytokinemia at dialysis, multiple organ failure, or bone diseases etc. </p>
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CONDENSED PYRIDINE COMPOUND (Fri, 30 Apr 2010)
<p id="p-0001-en" num="0000">The present invention provides a compound having excellent JAK3 inhibitory activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases, inflammatory diseases, and allergic diseases.</p> <p id="p-0002-en" num="0000">As a result of investigations with respect to novel condensed heterocyclic derivatives, the inventors have verified that a condensed pyridine compound has excellent JAK3 inhibitory activity, thereby completing the present invention.</p> <p id="p-0003-en" num="0000">More specifically, it has been verified that since the compound according to the present invention has inhibitory activity against JAK3, the compound is useful as an active ingredient of an agent for treating or preventing diseases caused by undesirable cytokine signal transduction (e.g., rejection during live organ/tissue transplantation, autoimmune diseases, asthma, atopic dermatitis, rheumatism, psoriasis and atherosclerotic disease), or diseases caused by abnormal cytokine signal transduction (e.g., cancer and leukemia).</p>
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AZABENZIMIDAZOLONES (Fri, 23 Apr 2010)
Compounds are provided having the general structure of formula I: In formula I, one member of the group (W, X, Y and Z) is a nitrogen atom and the remaining three members of the group are each independently a carbon atom covalently bonded to a radical, R4. The radicals, R1 R2, R3 and R4 are each defined herein, and n is an integer from 1 to 4. Also provided are stereoisomers, prodrugs, pharmaceutically acceptable salts, hydrates, salt hydrates, acid salt hydrates, and polymorphs of the compounds having the structure of formula I. The compounds bind the prostaglandin D2 receptor and are useful in the prophylaxis and treatment of prostaglandin D2-mediated diseases and conditions, including pain and inflammation, as well as asthma and allergic diseases and conditions.
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METHOD OF SCREENING COMPOUND USEFUL IN TREATING ALLERGIC DISEASE (Fri, 16 Apr 2010)
<p id="p-0001-en" num="0000">The present invention provides a method of screening for a compound useful for treatment of an allergic disease by identifying a molecule targeted by Intal upon exertion of its efficacy as an anti-allergic agent (hereinafter referred as a target) and using the target, as well as a new type of anti-allergic agent comprising a compound obtainable by the screening as an active ingredient for treatment of an allergic disease.</p>
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Cyclic modulators of chemokine receptor activity (Fri, 16 Apr 2010)
<p id="p-0001" num="0000">The present application describes modulators of MIP-1α or CCR-1 of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n, ring A, T, V, X, R<sub>1</sub>, R<sub>2 </sub>and R<sub>8</sub>, are defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="12.45mm" wi="65.45mm" file="US08324251-20121204-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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PIPERIDINE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Thu, 15 Apr 2010)
The present application describes modulators of MIP-1 of formula (I) : or stereoisomers or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as set forth above. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators are disclosed.
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ANIONIC CONJUGATES OF GLYCOSYLATED BACTERIAL METABOLITE (Fri, 09 Apr 2010)
The invention relates to anionic conjugates of glycosylated bacterial metabolites that may be used to mimic the structure and/or activity of the anionic bioactive molecules known as glycosaminoglycans (GAGs). The invention also relates to processes for the preparation of the conjugates. Such conjugates are useful in the prophylaxis and/or treatment of disease conditions and in particular chronic disease conditions such as inflammatory (including allergic) diseases, metastatic cancers and infection by pathogenic agents including bacteria, viruses or parasites.
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Novel BLT2-mediated disease, BLT2-binding agent and compound (Thu, 08 Apr 2010)
[PROBLEM] The compound that selectively binds to BLT2 and the preventive and/or therapeutic drug for BLT2-mediated disease such as skin disease are needed. [MEANS] FOR SOLVING THE PROBLEMS] The present invention provides the compound with BLT2 binding activity, salt thereof, solvate thereof or prodrug thereof. Since the compound with BLT2 binding activity, particularly the compound represented by the formula (I) , salt thereof, solvate thereof or prodrug thereof (symbols in formula have the same meanings as specification.) have BLT2 binding activity, it is useful for prevention and/or therapy of BLT2 mediated diseases, e.g., dermatosis, intestinal disease, HIV infection, acquired immunodeficiency syndrome, rejection to transplant, transplant rejection, graft-versus-host disease, autoimmune disease, allergic disease, inflammation, infection, ulcers, lymphoma, malignant tumor, leucaemia, arterial sclerosis, hepatitis, hepatic cirrhosis or cancer, etc.
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Matrix metalloproteinase inhibitors (Fri, 02 Apr 2010)
<p id="p-0001" num="0000">The present invention relates to β-hydroxy and amino substituted carboxylic acids, which act as matrix metalloprotease inhibitors, particularly diastereomerically pure β-hydroxy carboxylic acids, corresponding processes for the synthesis of and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, periodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase using the compounds.</p>
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6-amino-purin-8-one compounds (Fri, 26 Mar 2010)
<p id="p-0001" num="0000">Compounds of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="37.85mm" wi="69.85mm" file="US08067426-20111129-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R<sup>1 </sup>is C<sub>1-6</sub>alkylamino, C<sub>1-6</sub>alkoxy, or C<sub>3-7</sub>cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants. </p>
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Compounds for use in the treatment of autoimmune diseases, immuno-allergical diseases and organ or tissue transplantation rejection (Fri, 19 Mar 2010)
<p id="p-0001" num="0000">The present invention provides compounds, pharmaceutical compositions and methods for treating, immuno-allergical diseases, autoimmune diseases, and organ or tissue rejection following transplantation.</p>
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Sulfonamide derivative having PGD2 receptor antagonistic activity (Fri, 19 Mar 2010)
<p id="p-0001" num="0000">The present invention provides an sulfonamide derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases.</p> <p id="p-0002" num="0000">A compound of the general formula (II):</p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="36.75mm" wi="61.89mm" file="US08153793-20120410-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the ring C is an aromatic carbocyclic ring etc.; R1 is carboxy etc.; R2 is independently a halogen atom etc.; R3 is optionally substituted alkyloxy etc.; R4 is independently a halogen atom etc.; R5 is independently optionally substituted alkyl etc.; M is sulfonyl etc.; Y is a single bond etc.; L1 is a single bond etc.; L2 is a single bond etc.; k is 0, 1, 2, 3 or 4; n is 0, 1 or 2; and q is 0, 1, 2 or 3; provided that a) k is not 0 when the ring B is a 6-membered nitrogen-containing heterocyclic ring containing one or two nitrogen atom(s) and the ring C is a benzene ring, etc.;</li> <li id="ul0002-0002" num="0000">a pharmaceutically acceptable salt or a hydrate thereof.</li> </ul> </li> </ul> </p>
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Sulfonamide Derivative Having PGD2 Receptor Antagonistic Activity (Fri, 12 Mar 2010)
<p id="p-0001-en" num="0000">The present invention provides an sulfonamide derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases.</p> <p id="p-0002-en" num="0000">A compound of the general formula (II):</p> <p id="p-0003-en" num="0000"> <ul id="ul0001-en" list-style="none"> <li> <ul id="ul0002-en" list-style="none"> <li>wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the ring C is an aromatic carbocyclic ring etc.; R1 is carboxy etc.; R2 is independently a halogen atom etc.; R3 is optionally substituted alkyloxy etc.; R4 is independently a halogen atom etc.; R5 is independently optionally substituted alkyl etc.; M is sulfonyl etc.; Y is a single bond etc.; L1 is a single bond etc.; L2 is a single bond etc.; k is 0, 1, 2, 3 or 4; n is 0, 1 or 2; and q is 0, 1, 2 or 3; provided that a) k is not 0 when the ring B is a 6-membered nitrogen-containing heterocyclic ring containing one or two nitrogen atom(s) and the ring C is a benzene ring, etc.;</li> <li>a pharmaceutically acceptable salt or a hydrate thereof.</li> </ul> </li> </ul> </p>
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Compounds having CRTH2 antagonist activity (Fri, 12 Mar 2010)
<p id="p-0001-en" num="0000">Compounds of general formula (I)</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="47.67mm" wi="69.85mm" file="US07750027-20100706-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> wherein <ul id="ul0001-en" list-style="none"><li>W is chloro or fluoro;</li><li>R<sup>1 </sup>is phenyl optionally substituted with one or more substituents, selected from halo, —CN, —C<sub>1</sub>-C<sub>6 </sub>alkyl, —SOR<sup>3</sup>, —SO<sub>2</sub>R<sup>3</sup>, —SO<sub>2</sub>N(R<sup>2</sup>)<sub>2</sub>, —N(R<sup>2</sup>)<sub>2</sub>, —NR<sup>2</sup>C(O)R<sup>3</sup>, —CO<sub>2</sub>R<sup>2</sup>, —CONR<sup>2</sup>R<sup>3</sup>, —NO<sub>2</sub>, —OR<sup>2</sup>, —SR<sup>2</sup>, —O(CH<sub>2</sub>)<sub>p</sub>OR<sup>2</sup>, or —O(CH<sub>2</sub>)<sub>p</sub>O(CH<sub>2</sub>)<sub>q</sub>OR<sup>2 </sup>wherein <ul id="ul0002-en" list-style="none"><li>each R<sup>2 </sup>is independently hydrogen, —C<sub>1</sub>-C<sub>6 </sub>alkyl, —C<sub>3</sub>-C<sub>8 </sub>cycloalkyl, aryl or heteroaryl;</li><li>each R<sup>3 </sup>is independently, —C<sub>1</sub>-C<sub>6 </sub>alkyl, —C<sub>3</sub>-C<sub>8 </sub>cycloalkyl, aryl or heteroaryl;</li><li>p and q are each independently an integer from 1 to 3; and</li></ul></li><li>R<sup>4 </sup>is hydrogen, C<sub>1</sub>-C<sub>6 </sub>alkyl, C<sub>1</sub>-C<sub>6 </sub>alkyl substituted with aryl, aryl, (CH<sub>2</sub>)<sub>m</sub>OC(═O)C<sub>1</sub>-C<sub>6</sub>alkyl, ((CH<sub>2</sub>)<sub>m</sub>O)<sub>n</sub>CH<sub>2</sub>CH<sub>2</sub>X, (CH<sub>2</sub>)<sub>m</sub>N(R<sup>5</sup>)<sub>2 </sub>or CH((CH<sub>2</sub>)<sub>m</sub>O(C═O)R<sup>6</sup>)<sub>2</sub>; <ul id="ul0003-en" list-style="none"><li>m is 1 or 2;</li><li>n is 1-4;</li><li>X is OR<sup>5 </sup>or N(R<sup>5</sup>)<sub>2</sub>;</li><li>R<sup>5 </sup>is hydrogen or methyl; and</li><li>R<sup>6 </sup>is C<sub>1</sub>-C<sub>18 </sub>alkyl; <br/> and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis. </li></ul></li></ul></p>
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CYCLIC DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Fri, 12 Mar 2010)
<p id="p-0001-en" num="0000">The present application describes modulators of MIP-1α of formula (I), or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n, A, T, R<sub>1</sub>, R<sub>2 </sub>and R<sub>8</sub>, are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators of formula (I) are disclosed.</p> <p id="p-0002-en" num="0000"/>
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Thienotriazolodiazepine compound and medicinal use thereof (Fri, 19 Feb 2010)
<p id="p-0001" num="0000">A thienotriazolodiazepine compound of the following formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="47.41mm" wi="56.64mm" file="US08044042-20111025-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> a pharmaceutical agent containing the compound as an active ingredient, and a production intermediate and a production method of the thienotriazolodiazepine compound. </p> <p id="p-0003" num="0000">Since this compound has an inhibitory action on costimulatory signal from CD28 on T cell, it is useful for the prophylaxis or suppression of rejection reaction in transplantation of organ or bone marrow and the like, and the prophylaxis or treatment of autoimmune diseases or allergic diseases.</p>
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Amide derivatives and medicinal use thereof (Fri, 19 Feb 2010)
<p id="p-0001" num="0000">The present invention relates to an amide derivative of the formula (1), having a C5a receptor antagonistic action</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.42mm" wi="69.85mm" file="US08198454-20120612-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein each symbol is as defined in the specification. </p> <p id="p-0003" num="0000">The above-mentioned amide derivative, an optically active form thereof and a pharmaceutically acceptable salt thereof are promising as an agent for the treatment or prophylaxis of diseases or syndromes caused by inflammation caused by C5a [e.g., autoimmune diseases such as rheumatism, systemic lupus erythematosus and the like, sepsis, adult respiratory distress syndrome, chronic obstructive pulmonary disease, allergic diseases such as asthma and the like, atherosclerosis, cardiac infarction, brain infarction, psoriasis, Alzheimer's disease and serious organ injury (e.g., pneumonia, nephritis, hepatitis and pancreatitis and the like) due to activation of leukocytes caused by ischemia reperfusion, trauma, burn, surgical invasion and the like]. Moreover, they are useful as a therapeutic or prophylactic agent for the infectious diseases caused by bacteria and virus that invade via a C5a receptor.</p>
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PURINE DERIVATIVES FOR USE IN THE TREATMENT OF ALLERGIC, INFLAMMATORY AND INFECTIOUS DISEASES (Fri, 19 Feb 2010)
Compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
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COMPOUNDS (Fri, 19 Feb 2010)
Compounds of formula (I): wherein R1 is C1-6alkylamino, or C1-6alkoxy; m is an integer having a value of 2 or 3; n is an integer having a value of 0 to 3; p is an integer having a value of 1 or 2; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
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PURINE DERIVATIVES FOR USE IN THE TREATMENT OF ALLERGIC, INFLAMMATORY AND INFECTIOUS DISEASES (Fri, 19 Feb 2010)
Compounds of formula (I): wherein R1 is C1-6alkylamino, or C1-6alkoxy; m is an integer having a value of 3, 4, or 5; n is an integer having a value of 0 to 3; p is an integer having a value of 1 or 2 and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
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NOVEL ADENINE DERIVATIVES (Fri, 19 Feb 2010)
Compounds of formula (I) wherein R1 is C1-6alkylamino, or C1-6alkoxy; R2 is a group having the structure (II): n is an integer having a value of 1 to 6; Het is a 6-membered saturated heterocycle containing one nitrogen atom wherein Het is attached to the -(CH2)n- moiety at any carbon atom of the heterocycle; R3 is hydrogen, C1-8alkyl, or C3-7cycloalkylC0-6alkyl; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
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PURINE DERIVATIVES FOR USE IN THE TREATMENT OF ALLERGIC, INFLAMMATORY AND INFECTIOUS DISEASES (Fri, 19 Feb 2010)
Compounds of Formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 2 to 6; R2 is hydrogen, C1-6alkyl, or C3-7cycloalkylC0-6alkyl; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
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NOVEL ADENINE DERIVATIVES (Fri, 19 Feb 2010)
Compounds of formula (I) wherein R1 is C1-6alkylamino, or C1-6alkoxy; R1 is a group having the structure (II): n is an integer having a value of 1 to 6; Het is a 6-membered saturated heterocycle containing one nitrogen atom wherein Het is attached to the -(CH2)n-moiety at any carbon atom of the heterocycle; R3 is hydrogen, C1-8alkyl, or C3-7cycloalkylC0-6alkyl; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants. </p>
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PURINE DERIVATIVES FOR USE IN THE TREATMENT OF ALLERGIC, INFLAMMATORY AND INFECTIOUS DISEASES (Fri, 19 Feb 2010)
Compounds of Formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 2 to 6; R2 is hydrogen, C1-6alkyl, or C3-7cycloalkylC0-6alkyl; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants. </p>
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PURINE DERIVATIVES FOR USE IN THE TREATMENT OF ALLERGIC, INFLAMMATORY AND INFECTIOUS DISEASES (Fri, 19 Feb 2010)
Compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants. </p>
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Carboxylic acid compounds and medicinal compositions containing the same as the active ingredient (Fri, 05 Feb 2010)
<p id="p-0001" num="0000">A compound represented by formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="48.43mm" wi="71.46mm" file="US08138335-20120320-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">wherein the symbols in the formula are the same meanings as those in specification, salts thereof, solvates thereof, or prodrugs thereof binds to DP receptor and shows antagonistic activity for DP receptor. Thus, it is useful for prevention and/or treatment of diseases such as allergic disease (e.g., allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, urticaria, eczema, diseases accompanied by itch (e.g., atopic dermatitis and urticaria), diseases (e.g., cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (e.g., scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis, etc. Since it specifically binds to DP receptor and binds weakly to other prostaglandins receptors, they can be pharmaceuticals having little side effect.</li> </ul> </li> </ul> </p>
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Compounds Having CRTH2 Antagonist Activity (Fri, 29 Jan 2010)
<p id="p-0001-en" num="0000">Compounds of general formula (I)</p> <p id="p-0002-en" num="0000"> <ul id="ul0001-en" list-style="none"> <li> <ul id="ul0002-en" list-style="none"> <li>W is chloro or fluoro;</li> <li>Z is a —SO<sub>2</sub>YR<sup>1 </sup>group wherein R<sup>1 </sup>is C<sub>3</sub>-C<sub>8 </sub>heterocyclyl, aryl or heteroaryl any of which may optionally be substituted with one or more substituents selected from halo, —CN, —C<sub>1</sub>-C<sub>6 </sub>alkyl, —SOR<sup>3</sup>, —SO<sub>2</sub>R<sup>3</sup>, —SO<sub>2</sub>N(R<sup>2</sup>)<sub>2</sub>, —N(R<sup>2</sup>)<sub>2</sub>, —NR<sup>2</sup>C(O)R<sup>3</sup>, —CO<sub>2</sub>R<sup>2</sup>, —CONR<sup>2</sup>R<sup>3</sup>, —NO<sub>2</sub>, —OR<sup>2</sup>, —SR<sup>2</sup>, —O(CH<sub>2</sub>)<sub>p</sub>OR<sup>2</sup>, and —O(CH<sub>2</sub>)<sub>p</sub>O(CH<sub>2</sub>)<sub>q</sub>OR<sup>2 </sup>wherein <ul id="ul0003-en" list-style="none"><li>each R<sup>2 </sup>is independently hydrogen, —C<sub>1</sub>-C<sub>6 </sub>alkyl, —C<sub>3</sub>-C<sub>8 </sub>cycloalkyl, aryl or heteroaryl;</li><li>each R<sup>3 </sup>is independently, —C<sub>1</sub>-C<sub>6 </sub>alkyl, —C<sub>3</sub>-C<sub>8 </sub>cycloalkyl, aryl or heteroaryl;</li><li>p and q are each independently an integer from 1 to 3;</li></ul></li> <li>Y is a straight or branched C<sub>1</sub>-C<sub>4 </sub>alkylene chain;</li> <li>and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.</li> </ul> </li> </ul> </p>
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CLIP INHIBITORS AND METHODS OF MODULATING IMMUNE FUNCTION (Fri, 29 Jan 2010)
The invention relates to methods for modulating the immune function through targeting of CLIP molecules. The result is wide range of new therapeutic regimens for treating, inhibiting the development of, or otherwise dealing with, a multitude of illnesses and conditions, including autoimmune disease, allergic disease transplant and cell graft rejection, cancer, bacterial infection, HIV infection, and AIDS.
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CLIP INHIBITORS AND METHODS OF MODULATING IMMUNE FUNCTION (Fri, 29 Jan 2010)
: The invention relates to methods for modulating the immune function through targeting of CLIP molecules. The result is wide range of new therapeutic regimens for treating, inhibiting the development of, or otherwise dealing with, a multitude of illnesses and conditions, including autoimmune disease, allergic disease trans-plant and cell graft rejection, cancer, bacterial infection, HIV infec-tion, and AIDS. </p>
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CYCLOHEXENYL MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Fri, 22 Jan 2010)
The present application describes modulators of MCP-1 or CCR-2 of formula,(I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein T, W, X, Y, Z, R1, R2, R4 and R6, are defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula, (I) are disclosed.
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CHROMENE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Fri, 22 Jan 2010)
The present application describes modulators of MCP-1 or CCR-2 of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W1, W2, W3, Y, Z, R2, R3, R3' and R4, are defined in the specification. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.
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COMPOUND HAVING CYCLIC GROUP BOUND THERETO THROUGH SPIRO BINDING AND USE THEREOF (Fri, 01 Jan 2010)
<p id="p-0001-en" num="0000">A compound represented by general formula (I):</p> <p id="p-0002-en" num="0000"/> <p id="p-0003-en" num="0000">a salt thereof, a solvate thereof, or a prodrug thereof wherein all symbols are as defined in the specification has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, retinopathy, macular degeneration, pulmonary fibrosis, transplanted organ rejection, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, cancerous diseases (for example, cancer, cancer metastasis, etc.), a preventive and/or therapeutic agent for cancerous diseases or infections, or an agent for regeneration therapy.</p>
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Piperidinyl derivative as a modulator of chemokine receptor activity (Fri, 01 Jan 2010)
<p id="p-0001" num="0000">The present application describes the compound of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.43mm" wi="74.93mm" file="US08299098-20121030-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and arthrosclerosis using the compound of the invention are disclosed. </p>
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PYRAZOLO (3, 4-B) PYRIDINE DERIVATIVES AS PDE4 INHIBITORS (Fri, 01 Jan 2010)
<p id="p-0001-en" num="0000">The present invention provides a compound of formula (I) or a salt thereof (in particular, a pharmaceutically acceptable salt thereof):</p> <p id="p-0002-en" num="0000"/> <p id="p-0003-en" num="0000">The invention also provides the use of the compounds or salts as inhibitors of phosphodiesterase type IV (PDE4) for the treatment or prophylaxis of inflammatory or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis, atopic dermatitis or psoriasis, e.g. in a mammal such as a human.</p>
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PIPERIDINYL DERIVATIVE AS A MODULATOR OF CHEMOKINE RECEPTOR ACTIVITY (Thu, 31 Dec 2009)
The present application describes the compound of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and arthrosclerosis using the compound of the invention are disclosed.
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PIPERIDINYL DERIVATIVE AS A MODULATOR OF CHEMOKINE RECEPTOR ACTIVITY (Thu, 31 Dec 2009)
The present application describes the compound of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and arthrosclerosis using the compound of the invention are disclosed. </p>
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Tricyclic spiro derivatives as CRTH2 modulators (Fri, 25 Dec 2009)
<p id="p-0001" num="0000">The present invention is related to the use of spiro derivatives of Formula (I) for the treatment and/or prevention of allergic diseases, inflammatory dermatoses and other diseases with an inflammatory component. Specifically, the present invention is related to the use of spiro derivatives for the modulation of CRTH2 activity.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.85mm" wi="69.85mm" file="US08236963-20120807-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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PHARMACEUTICAL COMPOSITIONS COMPRISING N-[2-((2R)-2-{[4-[(4-CHLOROPHENYL)METHYL]-L-OXO-2(IH)-PHTHALAZ INYL]METHYL}-L- PYRROLIDINYL)ETHYL]-4-(METHYLOXY)BUTANAMIDE (Fri, 18 Dec 2009)
The present invention provides aqueous pharmaceutical compositions which comprise a compound which is Λ/-[2-((2R)-2-{[4-[(4-chlorophenyl)methyl]-1-oxo-2(1H)-phthalazinyl]methyl}-1-pyrrolidinyl)ethyl]-4-(methyloxy)butanamide or a pharmaceutically acceptable salt thereof and to their use in the treatment of various inflammatory and/or allergic diseases such as allergic rhinitis.
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Piperidinyl derivatives as modulators of chemokine receptor activity (Fri, 04 Dec 2009)
<p id="p-0001" num="0000">The present application describes substituted piperidinyl modulators of MIP-1α or CCR-1 or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using said modulators are disclosed.</p>
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PURINE DERIVATIVES AS IMMUNOMODULATORS (Thu, 03 Dec 2009)
Compounds of formula (I) wherein R<sp>1</sp> is C<sb>1-8</sb>alkylamino, C<sb>1-8</sb>alkoxy, C<sb>3-7</sb>cycloalkylC<sb>1-6</sb>alkylamino, C<sb>3-7</sb>cycloalkylC<sb>1-6</sb>alkoxy, C<sb>1-3</sb>alkoxyC<sb>2-3</sb>alkoxy, or Het<sp>b</sp>-C<sb>1-3</sb>alkoxy; Het<sp>b</sp> is a 5- or 6-membered saturated aliphatic heterocyle containing one oxygen atom; R<sp>2</sp> is -(CH<sb>2</sb>)<sb>n</sb>-Het; n is an integer having a value of 1 to 4; Het is a 5- or 6-membered saturated aliphatic heterocycle containing one oxygen heteroatom, which heterocycle may be substituted by one or two C<sb>1-4</sb>alkyl groups, and salts and solvates thereof, are inducers of human interferon and may be useful in the treatment of various disorders in particular infectious diseases, cancer, and allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, and as vaccine adjuvants.
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CRYSTAL, AMORPHOUS FORM AND SALT OF METHYL N-Ý3-(6,7-DIMETHOXY- 2-METHYLAMINOQUINAZOLIN-4-YL)PHENYL¨TEREPHTHALAMIC ACID (Thu, 26 Nov 2009)
Crystals, amorphous substances, salts, and hydrates of salt of methyl N-[3-(6,7-dimethoxy-2-methylaminoquinazolin-4-yl)phenyl]terephthalamic acid have PDE4 inhibitory action and are useful for treating allergic diseases such as atopic dermatitis.
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PYRAZOLOPYRIMIDINE COMPOUND (Thu, 26 Nov 2009)
Disclosed is a novel compound having Syk and/or Abl inhibitory activities, which is useful for prevention/treatment of allergic diseases, autoimmune diseases, arthritides and cancers. Specifically disclosed is a pyrazolopyrimidine compound represented by the formula [I] or [III] below, a tautomer thereof, a stereoisomer thereof, a pharmaceutically acceptable salt thereof, or a solvent of any of them.
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CONDENSED PYRIDINE COMPOUND (Thu, 26 Nov 2009)
The present invention provides a compound having excellent JAK3 inhibitory activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases, inflammatory diseases, and allergic diseases. As a result of investigations with respect to novel condensed heterocyclic derivatives, the inventors have verified that a condensed pyridine compound has excellent JAK3 inhibitory activity, thereby completing the present invention. More specifically, it has been verified that since the compound according to the present invention has inhibitory activity against JAK3, the compound is useful as an active ingredient of an agent for treating or preventing diseases caused by undesirable cytokine signal transduction (e.g., rejection during live organ/tissue transplantation, autoimmune diseases, asthma, atopic dermatitis, rheumatism, psoriasis and atherosclerotic disease), or diseases caused by abnormal cytokine signal transduction (e.g., cancer and leukemia).
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Aminocarboxylic acid derivative and medicinal use thereof (Fri, 06 Nov 2009)
<p id="p-0001" num="0000">The present invention relates to a compound represented by the formula (I), a salt thereof, an N-oxide form thereof, a solvate thereof, or a prodrug thereof, and a medicament containing the same. The compound represented by the formula (I) has an ability to bind to an S1P receptor (particularly, EDG-1, EDG-6, and/or EDG-8) and is useful for preventing and/or treating for rejection to transplantation, graft-versus-host disease, autoimmune diseases, allergic diseases, neurodegenerating diseases, and the like.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="13.21mm" wi="69.85mm" file="US07906549-20110315-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">wherein all symbols are described in the specification.</li> </ul> </li> </ul> </p>
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Heterocyclic janus kinase 3 inhibitors (Fri, 30 Oct 2009)
<p id="p-0001" num="0000">The present invention provides a compound of formula (I) having an excellent JAK3 inhibition activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases inflammatory diseases, and allergic diseases. The compound according to the present invention has an inhibition activity against JAK3 and is thus useful as an active ingredient of an agent for treating or preventing diseases caused by undesirable cytokine signal transmission (e.g., rejection during organ/tissue transplantation, autoimmune diseases, multiple sclerosis, rheumatoid arthritis, psoriasis, asthma, atopic dermatitis, Alzheimer's disease, and atherosclerotic disease), or diseases caused by abnormal cytokine signal transmission (e.g., cancer and leukemia).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="28.36mm" wi="55.46mm" file="US07879844-20110201-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Fused azole-pyrimidine derivatives (Fri, 30 Oct 2009)
<p id="p-0001" num="0000">The present invention relates to novel fused azolepyrimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-γ inhibition and can be used for the prophylaxis and treatment of diseases associated with PI3K and particularly with PI3K-γ activity.</p> <p id="p-0002" num="0000">More specifically, the azole derivatives of the present invention are useful for treatment and prophylaxis of diseases as follows: inflammatory and immunoregulatory disorders, such as asthma, atopic dermatitis, rhinitis, allergic diseases, chronic obstructive pulmonary disease (COPD), septic shock, joint diseases, autoimmune pathologies such as rheumatoid arthritis, and Graves' disease, cancer, myocardial contractility disorders, heart failure, thromboembolism, ischemia, and atherosclerosis.</p> <p id="p-0003" num="0000">The compounds of the present invention are also useful for pulmonary hypertension, renal failure, cardiac hypertrophy, as well as neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease, diabetes and focal ischemia, since the diseases also relate to PI3K activity in a human or animal subject.</p>
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COMPOUND EXHIBITING PGD2 RECEPTOR ANTAGONIST (Fri, 16 Oct 2009)
<p id="p-0001-en" num="0000">A compound having CRTH2 receptor antagonism, represented by the following formula (I). The compound is useful for the treatment of allergic diseases having a relation to eosinophils and the like.</p> <p id="p-0002-en" num="0000">A compound of the formula (I):</p> <p id="p-0003-en" num="0000"/> <p id="p-0004-en" num="0000">wherein <br/> a group represented by the formula: </p> <p id="p-0005-en" num="0000"/> <p id="p-0006-en" num="0000">is a group represented by the formula:</p> <p id="p-0007-en" num="0000"/> <p id="p-0008-en" num="0000">and the like, R<sup>1 </sup>is carboxy and the like, R<sup>3 </sup>is —(CH<sub>2</sub>)n-N(—Y)—SO<sub>2</sub>—Ar and the like, the other symbols are as defined in claim <b>1. </b></p>
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Nitrogenous heterocyclic compound and medicinal use thereof (Fri, 18 Sep 2009)
<p id="p-0001" num="0000">A compound represented by formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="16.59mm" wi="69.93mm" file="US08680092-20140325-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> (wherein the symbols are the same as defined in the description), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof, and medicinal use thereof. </p> <p id="p-0003" num="0000">The compound represented by formula (I) has CXCR4 antagonistic activity. It is hence useful as, e.g., a preventive and/or therapeutic agent for CXCR4-mediated diseases such as inflammatory/immunologic diseases (e.g., rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, and rejection reactions of transplanted organs), allergic diseases, infections diseases (e.g., human immunodeficiency virus infection and acquired immunologic deficiency syndrome), psychoneurotic diseases, cerebral diseases, cardiac/vascular disease, metabolic diseases, cancer diseases (e.g., cancer, cancer metastasis) or as an agent for regeneration therapy.</p>
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HYDROXYALKANYL AMIDES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Sat, 12 Sep 2009)
The application describes modulators of MIP-1α or CCR-1 of the formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein ring A, T, V, R1, R2 and R5, are defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.
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Glucocorticoid receptor agonists (Fri, 11 Sep 2009)
<p id="p-0001" num="0000">This invention relates to novel glucocorticoid receptor agonists of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="45.97mm" wi="69.93mm" file="US08822439-20140902-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> and to processes and intermediates for their preparation. The present invention also relates to pharmaceutical compositions containing these compounds, to their combination with one or more other therapeutic agents, as well as to their use for the treatment of a number of inflammatory and allergic diseases, disorders and conditions. </p>
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Glycolipid Derivative and Drug Containing the Same as Active Component (Fri, 11 Sep 2009)
<p id="p-0001-en" num="0000">Glycolipid derivatives having the formula (I):</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="21.93mm" wi="66.80mm" file="us20090227781a1-20090910-c00001.tif" img-content="photograph" img-format="png"/> </chemistry> </p> <p id="p-0003-en" num="0000">wherein R<sup>1 </sup>indicates an aldopyranose residue, R<sup>2 </sup>indicates a hydrogen atom or hydroxyl group, A indicates —CH<sub>2</sub>—, —CH(OH)—CH<sub>2</sub>— or —CH═CHCH<sub>2</sub>—, Z indicates —O— or —CH<sub>2</sub>—, when Z is —O— and x is an integer of 4 to 16, y indicates an integer of 26 to 35, when Z is —O— and x indicates an integer of 17 to 25, y indicates an integer of 0 to 35, when Z is —CH<sub>2</sub>— and x indicates an integer of 4 to 15, y indicates an integer of 26 to 35, and when Z is —CH<sub>2</sub>— and x indicates an integer of 16 to 25, y indicates an integer of 0 to 35 and a drug containing the glycolipid derivative for treatment of autoimmune arthritis and other autoimmune disease, bronchial asthma and other allergic diseases or diseases in which NKT cells or stimulation of NKT cells is known to be participating in the deterioration of conditions.</p>
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NEW MACROLIDES AND THEIR USE (Fri, 04 Sep 2009)
The invention relates to macrolide compounds of formula (I),the use of said compounds as medicaments, in particular for the treatment or prevention of inflammatory and allergic diseases, pharmaceutical compositions containing said compounds and to processes for their preparation. The invention relates in particular to macrolide compounds with anti-inflammatory activity mediated primarily through inhibition of phosphodiesterase 4 (PDE4) which makes them useful for the treatment and/or prevention of inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, atopic dermatitis or inflammatory bowel disease or proliferative diseases such as cancer.
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NEW MACROLIDES AND THEIR USE (Fri, 04 Sep 2009)
The invention relates to macrolide compounds of formula (1),the use of said compounds as medicaments, in particular for the treatment or prevention of inflammatory and allergic diseases, pharmaceutical compositions containing said compounds and to processes for their preparation. The invention relates in particular to macrolide compounds with anti-inflammatory activity mediated primarily through inhibition of phosphodiesterase 4 (PDE4) which makes them useful for the treatment and/or prevention of inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, atopic dermatitis or inflammatory bowel disease or proliferative diseases such as cancer. </p>
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Dual pharmacophores—PDE4-muscarinic antagonistics (Fri, 14 Aug 2009)
<p id="p-0001" num="0000">The present invention relates to novel compounds of Formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="22.61mm" wi="74.42mm" file="US08071588-20111206-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> and their use in the treatment of respiratory diseases, including anti-inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis. </p>
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MACROLIDES FOR TREATING DISEASES MEDIATED THROUGH PDE INHIBITION (Fri, 14 Aug 2009)
Macrolides of Formula (I) or (I-A): and wherein the residues R1, R2, R3, R4, R12, R13 and R14 have certain meanings defined in this application are useful for treating or preventing inflammatory or allergic diseases or. cancer in animals and humans.
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DUAL PHARMACOPHORES - PDE4-MUSCARINIC ANTAGONISTICS (Fri, 14 Aug 2009)
The present invention is directed to novel compounds of Formula (I), for treating an inflammatory or allergic diseases such as chronic obstructive pulmonary disease (COPD).
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DUAL PHARMACOPHORES - PDE4-MUSCARINIC ANTAGONISTICS (Fri, 14 Aug 2009)
The present invention is directed to novel compounds of Formula's (I) - (VI), and pharmaceutically acceptable salts thereof, pharmaceutical compositions and their use in therapy, for example as inhibitors of phosphodiesterase type IV (PDE4) and as antagonists of muscarinic acetylcholine receptors (mAChRs), in the treatment of and/or prophylaxis of respiratory diseases, including inflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis.
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DUAL PHARMACOPHORES-PDE4-MUSCARINIC ANTAGONISTICS (Fri, 14 Aug 2009)
The present invention relates to novel compounds of Formula (I) and their use in the treatment of respiratory diseases, including anti-inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis.
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DUAL PHARMACOPHORES - PDE4-MUSCARINIC ANTAGONISTICS (Fri, 14 Aug 2009)
The present invention is directed to novel compounds of Formula (I), pharmaceutical compositions and their use in therapy, for example as inhibitors of phosphodiesterase type IV (PDE4) and as antagonists of muscarinic acetylcholine receptors (mAChRs), in the treatment of/ and or prophylaxis of respiratory diseases, including antiinflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis.
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DUAL PHARMACOPHORES - PDE4 -MUSCARINIC ANTAGONISTICS (Fri, 14 Aug 2009)
The present invention relates to novel compounds of Formula (I) and their use in the treatment of respiratory diseases, including anti-inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis. </p>
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MACROLIDES AND USES OF MACROLIDES (Fri, 14 Aug 2009)
Macrolides of Formula (I) or (I-A): and wherein the residues R1, R2, R3, R4, R12, R13 and R14 have certain meanings defined in this application are useful for treating or preventing inflammatory or allergic diseases or. cancer in animals and humans. </p>
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DUAL PHARMACOPHORES - PDE4-MUSCARINIC ANTAGONISTICS (Fri, 14 Aug 2009)
The present invention is directed to novel compounds of Formula (I), pharmaceutical compositions and their use in therapy, for example as inhibitors of phosphodiesterase type IV (PDE4) and as antagonists of muscarinic acetylcholine receptors (mAChRs), in the treatment of/ and or prophylaxis of respiratory diseases, including antiinflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis. </p>
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Azaindole derivative having PGD2 receptor antagonistic activity (Fri, 07 Aug 2009)
<p id="p-0001-en" num="0000">The present invention creates an azaindole derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further providing a therapeutic agent for treating allergic diseases.</p> <p id="p-0002-en" num="0000">A compound of the general formula (I)</p> <p id="p-0003-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="32.26mm" wi="66.29mm" file="US07842692-20101130-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001-en" list-style="none"> <li> <ul id="ul0002-en" list-style="none"> <li>wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a 3- to 8-membered nitrogen-containing non-aromatic heterocyclic ring etc.; the formula of —X<sup>1</sup>═X<sup>2</sup>—X<sup>3</sup>═X<sup>4</sup>— is a formula of —C(R<sup>1</sup>)═C(R<sup>2</sup>)—C(R<sup>3</sup>)═N— etc.; R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4 </sup>and R<sup>5 </sup>are independently a hydrogen atom or a halogen atom etc.; R<sup>6 </sup>is optionally substituted C1-C6 alkyloxy etc.; R<sup>7 </sup>is independently a halogen atom etc.; R<sup>8 </sup>is optionally substituted C1-C6 alkyl etc.; R<sup>9 </sup>is carboxy etc.; M is sulfonyl etc.; Y is a single bond etc.; L<sup>1</sup>, L<sup>2 </sup>and L<sup>3 </sup>are a single bond or alkylene optionally containing one or two heteroatoms etc.; n is 0 etc.; q is 0 etc.; a pharmaceutically acceptable salt or hydrate thereof.</li> </ul> </li> </ul> </p>
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Dual pharmacophores—PDE4-muscarinic antagonistics (Fri, 07 Aug 2009)
<p id="p-0001" num="0000">The present invention is directed to novel compounds of Formula (I), pharmaceutical compositions and their use in therapy, for example as inhibitors of phosphodiesterase type IV (PDE4) and as antagonists of muscarinic acetylcholine receptors (mAChRs), in the treatment of/and or prophylaxis of respiratory diseases, including antiinflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis.</p>
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CYCLIC DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Thu, 06 Aug 2009)
The present application describes modulators of MIP-1α of formula (I), or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n, A, T, R<sb>1</sb>, R<sb>2</sb> and R<sb>8</sb>, are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators of formula (I) are disclosed.
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COMPOUND HAVING ACIDIC GROUP WHICH MAY BE PROTECTED, AND USE THEREOF (Fri, 31 Jul 2009)
<p id="p-0001-en" num="0000">A compound represented by general formula (I):</p> <p id="p-0002-en" num="0000"/> <p id="p-0003-en" num="0000">a salt thereof, a solvate thereof, or a prodrug thereof wherein all symbols are as defined in the specification. The compound of the present invention has antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, systemic erythematosus, retinopathy, macular degeneration, pulmonary fibrosis, transplanted organ rejection, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy.</p>
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Compounds having CRTH2 antagonist activity (Fri, 31 Jul 2009)
<p id="p-0001" num="0000">Compounds of general formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="42.76mm" wi="69.85mm" file="US08168673-20120501-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">wherein</li> <li id="ul0002-0002" num="0000">W is chloro or fluoro;</li> <li id="ul0002-0003" num="0000">Z is a group SO<sub>2</sub>R<sup>1</sup>;</li> <li id="ul0002-0004" num="0000">wherein R<sup>1 </sup>is —C<sub>3</sub>-C<sub>8 </sub>cycloalkyl or heterocyclyl optionally substituted with one or more substituents chosen from halo, —CN, —C<sub>1</sub>-C<sub>6 </sub>alkyl, —SOR<sup>3</sup>, —SO<sub>2</sub>R<sup>3</sup>, —SO<sub>2</sub>N(R<sup>2</sup>)<sub>2</sub>, —N(R<sup>2</sup>)<sub>2</sub>, —NR<sup>2</sup>C(O)R<sup>3</sup>, —CO<sub>2</sub>R<sup>2</sup>, —CONR<sup>2</sup>R<sup>3</sup>, —NO<sub>2</sub>, —OR<sup>2</sup>, —SR<sup>2</sup>, —O(CH<sub>2</sub>)<sub>p</sub>OR<sup>2</sup>, and —O(CH<sub>2</sub>)<sub>p</sub>O(CH<sub>2</sub>)<sub>q</sub>OR<sup>2 </sup>wherein <ul id="ul0003" list-style="none"> <li id="ul0003-0001" num="0000">each R<sup>2 </sup>is independently hydrogen, —C<sub>1</sub>-C<sub>6 </sub>alkyl, —C<sub>3</sub>-C<sub>8 </sub>cycloalkyl, aryl or heteroaryl;</li> <li id="ul0003-0002" num="0000">each R<sup>3 </sup>is independently, —C<sub>1</sub>-C<sub>6 </sub>alkyl, —C<sub>3</sub>-C<sub>8 </sub>cycloalkyl, aryl or heteroaryl;</li> <li id="ul0003-0003" num="0000">p and q are each independently an integer from 1 to 3;</li> </ul> </li> <li id="ul0002-0005" num="0000">and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.</li> </ul> </li> </ul> </p>
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COMPOUNDS HAVING CRTH2 ANTAGONIST ACTIVITY (Fri, 31 Jul 2009)
Compounds of general formula (I): wherein W is chloro or fluoro; Z is a group SO2R1; wherein R1 is -C3-C8 cycloalkyl or heterocyclyl optionally substituted with one or more substituents chosen from halo, -CN, -C1-C6 alkyl, -SOR3, -SO2R3, -SO2N(R2)2, -N(R2)2, -NR2C(O)R3, -CO2R2, -CONR2R3, -NO2, -OR2, -SR2, -O(CH2)POR2, and - O(CH2)pO(CH2)qOR2 wherein each R2 is independently hydrogen, -Ci-C6 alkyl, -C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, -C1-C6 alkyl, -C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
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COMPOUNDS HAVING CRTH2 ANTAGONIST ACTIVITY (Fri, 31 Jul 2009)
Compounds of general formula (I) W is chloro or fluoro; Z is a -SO2YR1 group wherein R1 is C3-C8 heterocyclyl, aryl or heteroaryl any of which may optionally be substituted with one or more substituents selected from halo, -CN, -C1-C6 alkyl, -SOR3, -SO2R3, -SO2N(R2)2, -N(R2)2, -NR2C(O)R3, -CO2R2, -CONR2R3, -NO2, -OR2, -SR2, -O(CH2)POR2, and -O(CH2)pO(CH2)qOR2 wherein each R2 is independently hydrogen, -C1-C6 alkyl, -C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, -C1-C6 alkyl, -C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; Y is a straight or branched C1-C4 alkylene chain; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
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Compounds Having CRTH2 Antagonist Activity (Fri, 24 Jul 2009)
<p id="p-0001-en" num="0000">Compounds of general formula (I)</p> <p id="p-0002-en" num="0000"/> <p id="p-0003-en" num="0000">wherein <ul id="ul0001-en" list-style="none"><li>W is chloro or fluoro;</li><li>R<sup>1 </sup>is phenyl optionally substituted with one or more substituents selected from halo, —CN, —C<sub>1</sub>-C<sub>6 </sub>alkyl, —SOR<sup>3</sup>, —SO<sub>2</sub>R<sup>3</sup>, —SO<sub>2</sub>N(R<sup>2</sup>)<sub>2</sub>, —N(R<sup>2</sup>)<sub>2</sub>, —NR<sup>2</sup>C(O)R<sup>3</sup>, —CO<sub>2</sub>R<sup>2</sup>, —CONR<sup>2</sup>R<sup>3</sup>, —NO<sub>2</sub>, —OR<sup>2</sup>, —SR<sup>2</sup>, —O(CH<sub>2</sub>)<sub>p</sub>OR<sup>2</sup>, and —O(CH<sub>2</sub>)<sub>p</sub>—O—(CH<sub>2</sub>)<sub>q</sub>OR<sup>2 </sup>wherein <ul id="ul0002-en" list-style="none"><li>each R<sup>2 </sup>is independently hydrogen, —C<sub>1</sub>-C<sub>6 </sub>alkyl, —C<sub>3</sub>-C<sub>8 </sub>cycloalkyl, aryl or heteroaryl;</li><li>each R<sup>3 </sup>is independently, —C<sub>1</sub>-C<sub>6 </sub>alkyl, —C<sub>3</sub>-C<sub>8 </sub>cycloalkyl, aryl or heteroaryl;</li><li>p and q are each independently an integer from 1 to 3; <br/> and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis. </li></ul></li></ul></p>
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COMPOUNDS HAVING CRTH2 ANTAGONIST ACTIVITY (Fri, 24 Jul 2009)
Compounds of general formula (I) wherein W is chloro or fluoro; R1 is phenyl optionally substituted with one or more substituents selected from halo, -CN, -C1-C6 alkyl, -SOR3, -SO2R3, -SO2N(R2)2, -N(R2)2, -NR2C(O)R3, -CO2R2, - CONR2R3, -NO2, -OR2, -SR2, -O(CH2)POR2, and -O(CH2)pO(CH2)qOR2 wherein each R2 is independently hydrogen, -C1-C6 alkyl, -C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, -C1-C6 alkyl, -C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
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COMPOUNDS HAVING CRTH2 ANTAGONIST ACTIVITY (Fri, 24 Jul 2009)
<br/><br/><br/>Compounds of general formula (I) wherein W is chloro or fluoro; R1 is phenyl <br/>optionally substituted with one or more <br/>substituents selected from halo, -CN, -C1-C6 alkyl, -SOR3, -SO2R3, -SO2N(R2)2, <br/>-N(R2)2, -NR2C(O)R3, -CO2R2, - CONR2R3, -NO2, <br/>-OR2, -SR2, -O(CH2)p OR2, and -O(CH2)p O(CH2)q OR2 wherein each R2 is <br/>independently hydrogen, -C1-C6 alkyl, -C3-C8 cycloalkyl, <br/>aryl or heteroaryl; each R3 is independently, -C1-C6 alkyl, -C3-C8 cycloalkyl, <br/>aryl or heteroaryl; p and q are each independently an <br/>integer from 1 to 3; and their pharmaceutically acceptable salts, hydrates, <br/>solvates, complexes or prodrugs are useful in orally <br/>administrable compositions for the treatment of allergic diseases such as <br/>asthma, allergic rhinitis and atopic dermatitis.<br/></p>
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2-PHENYL-INDOLES AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS (Fri, 10 Jul 2009)
<p id="p-0001-en" num="0000">The present invention is directed to 2-phenyl-indole compounds, their preparation, pharmaceutical compositions containing these compounds, and their pharmaceutical use in treating a patient suffering from a PGD2-mediated disorder including, but not limited to, allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, bronchitis, eczema, urticaria diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which are generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis and the like.</p>
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Chemokine receptor antagonists and use thereof (Fri, 03 Jul 2009)
<p id="p-0001" num="0000">A compound represented by general formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="14.65mm" wi="69.85mm" file="US08168783-20120501-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> a salt thereof, a solvate thereof, or a prodrug thereof wherein all symbols are as defined in the specification has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, systemic erythematosus, retinopathy, macular degeneration, pulmonary fibrosis, transplanted organ rejection, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiac/vascular disease (for example, arteriosclerosis, myocardial infarction, stenocardia, cerebral infarction, chronic arterial occlusive disease, etc.), metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), a preventive and/or therapeutic agent for cancerous diseases or infections, or an agent for regeneration therapy. </p>
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PROCESS FOR PREPARING MATRIX METALLOPROTEINASE INHIBITORS AND CHIRAL AUXILIARY THEREFOR (Thu, 02 Jul 2009)
The present invention relates to β-hydroxy and amino substituted carboxylic acids, which act as matrix metalloprotease inhibitors, particularly diastereomerically pure β-hydroxy carboxylic acids, corresponding processes for the synthesis of and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over- activation of a matrix metalloproteinase using the compounds.
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Antigen Arrays for Treatment of Allergic Eosinophilic Diseases (Fri, 19 Jun 2009)
<p id="p-0001-en" num="0000">The present invention is related to the fields of molecular biology, virology, immunology and medicine. The invention provides a composition comprising an ordered and repetitive antigen or antigenic determinant array, and in particular an array comprising a protein or peptide of IL-5, IL-13 or eotaxin. More specifically, the invention provides a composition comprising a virus-like particle and at least one protein, or peptide of IL-5, IL-13 and/or eotaxin bound thereto. The invention also provides a process for producing the conjugates and the ordered and repetitive arrays, respectively. The compositions of the invention are useful in the production of vaccines for the treatment of allergic diseases with an eosinophilic component and as a pharmaccine to prevent or cure allergic diseases with an eosinophilic component and to efficiently induce immune responses, in particular antibody responses. Furthermore, the compositions of the invention are particularly useful to efficiently induce self-specific immune responses within the indicated context.</p>
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2-PHENYL-INDOLES AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS (Thu, 11 Jun 2009)
The present invention is directed to 2-phenyl-indole compounds (A), their preparation, pharmaceutical compositions containing these compounds, and their pharmaceutical use in treating a patient suffering from a PGD2-mediated disorder including, but not limited to, allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, bronchitis, eczema, urticaria diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which are generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis and the like.
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NOVEL GLUCOCORTICOID RECEPTOR AGONISTS (Fri, 05 Jun 2009)
This invention relates to novel glucocorticoid receptor agonists of formula (I) and to processes and intermediates for their preparation. The present invention also relates to pharmaceutical compositions containing these compounds, to their combination with one or more other therapeutic agents, as well as to their use for the treatment of a number of inflammatory and allergic diseases, disorders and conditions.
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NOVEL GLUCOCORTICOID RECEPTOR AGONISTS (Fri, 05 Jun 2009)
This invention relates to novel glucocorticoid receptor agonists of formula (I) and to processes and intermediates for their preparation. The present invention also relates to pharmaceutical compositions containing these compounds, to their combination with one or more other therapeutic agents, as well as to their use for the treatment of a number of inflammatory and allergic diseases, disorders and conditions. </p>
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CYCLIC MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Thu, 28 May 2009)
The present application describes modulators of MIP-1α or CCR-1 of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n, ring A, T, V, X, R<sb>1</sb>, R<sb>2</sb> and R<sb>8</sb>, are defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.
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Nitrogenated heterocyclic derivative, and pharmaceutical agent comprising the derivative as active ingredient (Fri, 22 May 2009)
<p id="p-0001" num="0000">The compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof specifically binds CCR5, so it is useful for preventing and/or treating CCR5-related diseases, for example, various inflammatory diseases (asthma, nephritis, nephropathy, hepatitis, arthritis, rheumatoid arthritis, rhinitis, conjunctivitis, ulcerative colitis, etc.), immunological diseases (autoimmune diseases, rejection in organ transplantation, immunosuppression, psoriasis, multiple sclerosis, etc.), infectious diseases (infection with human immunodeficiency virus, acquired immunodeficiency syndrome, etc.), allergic diseases (atopic dermatitis, urticaria, allergic bronchopulmonary aspergillosis, allergic eosinophilic gastroenteritis, etc.), ischemic reperfusion injury, acute respiratory distress syndrome, shock accompanying bacterial infection diabetes cancer metastasis and so on</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="11.68mm" wi="69.93mm" file="US08003642-20110823-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">Wherein all symbols in formula are as defined in the specification.</p>
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Thienopyrazole derivative having PDE7 inhibitory activity (Fri, 22 May 2009)
<p id="p-0001" num="0000">To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="23.88mm" wi="52.15mm" file="US07932250-20110426-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> [wherein, especially, R<sup>1 </sup>is a cyclohexyl, a cycloheptyl group or a tetrahydropyranyl group; R<sup>2 </sup>is methyl; R<sup>3 </sup>is a hydrogen atom; and R<sup>4 </sup>is a group: —CONR<sup>5</sup>R<sup>6 </sup>(in which any one of R<sup>5 </sup>and R<sup>6 </sup>is a hydrogen atom)]. </p>
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Pyrazolo[3,4-b]pyridine compounds, and their use as a PDE4 inhibitors (Fri, 22 May 2009)
<p id="p-0001-en" num="0000">The invention provides a compound of formula (I) or a salt thereof:</p> <p id="p-0002-en" num="0000"> <ul id="ul0001-en" list-style="none"> <li> <ul id="ul0002-en" list-style="none"> <li>wherein R<sup>2 </sup>is H, C<sub>1-3</sub>alkyl, n-butyl, C<sub>1-2</sub>fluoroalkyl, cyclopropyl, cyclobutyl, (cyclopropyl)methyl-, —CN, or —CH<sub>2</sub>OH; R<sup>3 </sup>is inter alia optionally substituted C<sub>4-7</sub>cycloalkyl or an optionally substituted heterocyclic group (aa), (bb) or (cc);</li> <li>R<sup>a </sup>is H, methyl or ethyl; R<sup>b </sup>is H or methyl; <br/> R<sup>4 </sup>is H, methyl, ethyl, n-propyl, —C(O)-Me, or —C(O)—C<sub>1</sub>fluoroalkyl; </li> </ul> </li> <li>and R<sup>5 </sup>is: —C(O)—(CH<sub>2</sub>)<sub>n</sub>—Ar, —C(O)-Het, —C(O)—C<sub>1-6</sub>alkyl, —C(O)—C<sub>1 </sub>fluoroalkyl, —C(O)—(CH<sub>2</sub>)<sub>2</sub>—C(O)—NR<sup>15b</sup>NR<sup>15b</sup>, —C(O)—CH<sub>2</sub>—C(O)—NR<sup>15b</sup>NR<sup>15b</sup>, —C(O)—NR<sup>15b</sup>—(CH<sub>2</sub>)m<sup>1</sup>—Ar, —C(O)—NR<sup>15b</sup>—Het, —C(O)—NR<sup>15b</sup>—C<sub>1-6</sub>alkyl, —C(O)—NR<sup>5a</sup>R<sup>5b</sup>, —S(O)<sub>2</sub>—(CH<sub>2</sub>)<sub>m</sub><sup>2</sup>—Ar, —S(O)<sub>2</sub>-Het, —S(O)<sub>2</sub>—C<sub>1-6</sub>alkyl, or —CH<sub>2</sub>—Ar;</li> <li>or R<sup>4 </sup>and R<sup>5 </sup>taken together are —(CH<sub>2</sub>)<sub>p</sub><sup>1</sup>—, —(CH<sub>2</sub>)<sub>2</sub>—X<sup>5</sup>—(CH<sub>2</sub>)<sub>2</sub>—, —C(O)—(CH<sub>2</sub>)<sub>p</sub><sup>2</sup>—, —C(O)—N(R<sup>15</sup>)—(CH<sub>2</sub>)<sub>p</sub><sup>3</sup>—; or NR<sup>4</sup>R<sup>5 </sup>is of sub-formula (y), (y1), (y2) or (y3).</li> </ul> </p> <p id="p-0003-en" num="0000">The invention provides the use of the compounds as inhibitors of phosphodiesterase type IV (PDE4) and/or for the treatment and/or prophylaxis of inflammatory and/or allergic diseases such as COPD and the like.</p>
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Compounds (Fri, 22 May 2009)
<p id="p-0001" num="0000">The present invention includes novel compounds useful in the treatment of various disorders in particular infectious diseases, cancer, and allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, and as vaccine adjuvants.</p>
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Acylaminopiperidine compound (Fri, 22 May 2009)
<p id="p-0001-en" num="0000">To provide a compound which has an excellent activity to modulate the functions of CCR4 or TARC and/or MDC and can be used for the prevention and/or treatment of various inflammatory diseases, allergic diseases, autoimmune diseases and the like.</p> <p id="p-0002-en" num="0000">An acylaminopiperidine compound represented by the formula (I) or a pharmaceutically acceptable salt thereof.</p> <p id="p-0003-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="38.69mm" wi="69.85mm" file="US07790884-20100907-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> [Symbols in the formula represent the following meanings; A: a single bond or C<sub>1</sub>-C<sub>6 </sub>alkylene, R<sup>1</sup>: phenyl which may be substituted, etc., R<sup>2</sup>: —H or C<sub>1</sub>-C<sub>6 </sub>alkyl, R<sup>3</sup>: —H, C<sub>1</sub>-C<sub>6 </sub>alkyl or C<sub>3</sub>-C<sub>8 </sub>cycloalkyl, R<sup>4</sup>: pyrrolidin-2-yl which may be substituted, etc., and D: benzene ring or pyrazole ring]. </p>
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Chemokine receptor antagonists and use thereof (Fri, 08 May 2009)
<p id="p-0001" num="0000">The present invention relates to a compound represented by formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="16.51mm" wi="69.85mm" file="US08293896-20121023-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein all symbols are as defined here, a salt thereof, a solvate thereof, or a prodrug thereof. </p> <p id="p-0003" num="0000">The compound of the present invention has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, rejection of transplanted organ, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy.</p>
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COMPOUND HAVING CYCLIC GROUP BOUND THERETO THROUGH SPIRO BINDING AND USE THEREOF (Thu, 07 May 2009)
A compound represented by general formula (I): a salt thereof, a solvate thereof, or a prodrug thereof wherein all symbols are as defined in the specification has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, retinopathy, macular degeneration, pulmonary fibrosis, transplanted organ rejection, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, cancerous diseases (for example, cancer, cancer metastasis, etc.), a preventive and/or therapeutic agent for cancerous diseases or infections, or an agent for regeneration therapy.
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COMPETITIVE INHIBITORS OF INVARIANT CHAIN EXPRESSION AND/OR ECTOPIC CLIP BINDING (Fri, 01 May 2009)
The invention relates to methods for modulating the immune function through targeting of CLIP molecules. The result is wide range of new therapeutic regimens for treating, inhibiting the development of, or otherwise dealing with, a multitude of illnesses and conditions, including autoimmune disease, cancer, Alzheimer's disease, allergic disease, transplant and cell graft rejection, HIV infection and other viral, bacterial, and parasitic infection, and AIDS. Methods are also provided for preparing a peptide having the property of being able to displace CLIP by feeding one or more peptide sequences into software that predicts MHC Class II binding regions in an antigen sequence and related products.
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COMPETITIVE INHIBITORS OF INVARIANT CHAIN EXPRESSION AND/OR ECTOPIC CLIP BINDING (Fri, 01 May 2009)
The invention relates to methods for modulating the immune function through targeting of CLIP molecules. The result is wide range of new therapeutic regimens for treating, inhibiting- the development of, or otherwise dealing with, a multitude of illnesses and conditions, including autoimmutne disease, cancer, Alzheimer's disease, allergic disease, transplant and cell graft rejection, HIV infection and other viral, bacterial, and parasitic infection, and AIDS. Methods are also provided for preparing a peptide having the property of being able to displace CLIP by feeding one or more peptide sequences into software that predicts MHC Class II binding regions in an antigen sequence and related products. </p>
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Indolecarboxylic acid derivative having PGD2 receptor antagonistic activity (Fri, 24 Apr 2009)
<p id="p-0001" num="0000">The present invention provides an indolecarboxylic acid derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases.</p> <p id="p-0002" num="0000">A compound of the general formula (I):</p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="43.60mm" wi="59.18mm" file="US08143285-20120327-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0004" num="0000">wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the formula of -X<sup>1</sup>=X<sup>2</sup>-X<sup>3</sup>=X<sup>4</sup>- is a formula of —C(R<sup>1</sup>)═C(R<sup>2</sup>)—C(R<sup>3</sup>)═C(R<sup>4</sup>)— etc.; X<sup>5 </sup>is C(R<sup>5</sup>) or N; R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4 </sup>and R<sup>5 </sup>is independently a hydrogen atom, a halogen atom etc; R<sup>6 </sup>is a formula of -Z-R<sup>10 </sup>etc. wherein Z is alkylene etc., and R<sup>10 </sup>is carboxy etc.; R<sup>7 </sup>is optionally substituted alkyloxy etc.; R<sup>8 </sup>is independently a halogen atom etc.; R<sup>9 </sup>is independently optionally substituted alkyl etc.; Y is a single bond etc.; n is 0 etc.; q is 0 etc.;</p> <p id="p-0005" num="0000">a pharmaceutically acceptable salt or a solvate thereof.</p>
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QUINOLINE DERIVATIVES USED TO TREAT INFLAMMATORY AND ALLERGIC DISEASES (Fri, 24 Apr 2009)
The present invention relates to compounds of formula (I) and salts thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various diseases, such as allergic rhinitis.
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COMBINATION OF FLUTICASONE FUROATE WITH 4- [ (4-CHL0R0PHENYL)METHYL] -2- ({ (2R)-I- [4-(4-{ [3-(HEXAHYDR0-LH-AZEPIN-L-YL) PROPYL ] OXY} PHENYL) BUTYL] -2-PYRROLIDINYL}METHYL) -1 (2H) - PHTHALAZ INONE (Fri, 24 Apr 2009)
The present invention provides aqueous pharmaceutical compositions which comprise a compound which is 4-[(4-chlorophenyl)methyl]-2-({(2/R)-1-[4-(4-{[3-(hexahydro-1H-azepin- 1-yl)propyl]oxy}phenyl)butyl]-2-pyrrolidinyl}methyl)-1 (2H)-phthalazinone (I) or a pharmaceutically acceptable salt thereof, and to their use in the treatment of various inflammatory and/or allergic diseases such as allergic rhinitis.
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NEW MACROLIDES USEFUL AGAINST INFLAMMATORY AND ALLERGIC DISEASES (Thu, 23 Apr 2009)
Macrolide compounds of formula I: with PDF4 inhibiting activity are described, wherein R1 is a residue -Y-X-Q; Y is S, SO or SO<sb>2</sb>; X is a bond or a linear group consisting of hydrogen atoms and with up to 9 atoms selected from C, N, O and/or S, of which up to 2 atoms can be N and one atom can be O or S, one carbon atom can appear as a CO group and the sulphur atom can appear as an SO2 group and two adjacent C atoms can be present as - CH=CH- or -C≡C- and which group X is unsubstituted or is substituted with - COO-W or -CONH-W; Q is a residue -V-A1-L- A2-W or, if X does not represent a bond, may also be -NR6R7; V is a divalent aromatic or heterocyclic group; W is aryl or heterocyclyl; or in a group -V-A1-L- A2-W, wherein at least one of the groups A1; L or A2 is present, can also be a monovalent substituted or unsubstituted, saturated or unsaturated linear group with up to 5 atoms consisting of C, N, O and/or S of which one carbon can appear as a CO group one sulphur atom can appear as an SO2 group, A1, A2 are independently of each other either absent or a C<sb>1</sb>-C<sb>4</sb>alkylene group; L is -0-, -S-, -SO2-, -NH-, -CO-, -(CO)O-, -O(OC)-, -(CO)NH-, -NH(CO)-, -(SO<sb>2</sb>)NH-, -HN(SO<sb>2</sb>)-, -HN(CO)NH-, -0(CO)NH-, -NH(CO)O-, or can also be absent if Al and/or A2 are present; R2 is hydrogen and R3 is and 0R4 or R2, R3 taken together form a C=O group; R4 is hydrogen or an saturated or unsaturated aliphatic group with 1 to 6 carbon atoms; R6, R7 are independently selected from aryl; aralkyl; heterocyclyl and heterocyclylalkyl; and one of R6 and R7 can also be a group -L-W; and * indicates a chiral centre which is in the (R) or (S) form.
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PYRAZOLO[3,4-B]PYRIDINE COMPOUNDS, AND THEIR USE AS PDE4 INHIBITORS (Thu, 16 Apr 2009)
The invention provides a compound of formula (I) or a salt thereof: wherein Ar has the sub-formula (x): and wherein: Q<sp>1</sp> is NH or NMe, in which case Q<sp>2</sp> is -C(O)-, -S(O)<sb>2</sb>-, -C(O)NH- or -C(O)NMe-; or Q<sp>1</sp> is a bond or -O-, in which case Q<sp>2</sp> is a bond; or Q<sp>1</sp> is -C(O)-, in which case Q<sp>2</sp> is NH or NMe; or Q<sp>1</sp> is -S(O)<sb>2</sb>-, in which case Q<sp>2</sp> is NH, NMe or a bond; and L is (CH<sb>2</sb>)<sb>n</sb> wherein n is 4 to 13; or L is -(CH<sb>2</sb>)<sb>m</sb><sp>1</sp>-O-(CH<sb>2</sb>)<sb>m</sb><sp>2</sp>-. The invention also provides the use of the compounds as inhibitors of phosphodiesterase type IV (PDE4) and/or for the treatment and/or prophylaxis of inflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, or rhinitis (e.g. allergic and/or non-allergic rhinitis).
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Fused azole-pyrimidine derivatives (Thu, 02 Apr 2009)
The present invention relates to novel fused azolepyrimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-³ inhibition and can be used for the prophylaxis and treatment of diseases associated with PI3K and particularly with PI3K-³ activity. More specifically, the azole derivatives of the present invention are useful for treatment and prophylaxis of diseases as follows: inflammatory and immunoregulatory disorders, such as asthma, atopic dermatitis, rhinitis, allergic diseases, chronic obstructive pulmonary disease (COPD), septic shock, joint diseases, autoimmune pathologies such as rheumatoid arthritis, and Graves' disease, cancer, myocardial contractility disorders, heart failure, thromboembolism, ischemia, and atherosclerosis. The compounds of the present invention are also useful for pulmonary hypertension, renal failure, cardiac hypertrophy, as well as neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease, diabetes and focal ischemia, since the diseases also relate to PI3K activity in a human or animal subject.
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COMPOUND HAVING ACIDIC GROUP WHICH MAY BE PROTECTED, AND USE THEREOF (Thu, 02 Apr 2009)
A compound represented by general formula (I): a salt thereof, a solvate thereof, or a prodrug thereof wherein all symbols are as defined in the specification. The compound of the present invention has antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, systemic erythematosus, retinopathy, macular degeneration, pulmonary fibrosis, transplanted organ rejection, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy.
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PURINE DERIVATIVES FOR THE TREATMENT OF VIRAL OR ALLERGIC DISEASES AND CANCERS (Fri, 27 Mar 2009)
<p id="p-0001-en" num="0000">The present invention provides compounds of formula (I)</p> <p id="p-0002-en" num="0000"/> <p id="p-0003-en" num="0000">wherein R<sup>1</sup>, Y<sup>1</sup>, X<sup>1</sup>, Z<sup>1</sup>, X<sup>2</sup>, Y<sup>2</sup>, A, Y<sup>3</sup>, n, R and R<sup>2 </sup>are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.</p>
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PREVENTATIVE TREATMENT AND REMISSION OF ALLERGIC DISEASES (Fri, 27 Mar 2009)
<p id="p-0001-en" num="0000">The invention provides the use of at least one plant selected from plants of the family Zingiberaceae in the preparation of a medicament for use in the treatment or prophylaxis of allergic diseases. The plant is optionally selected from the genera <i>Siphonochilus, Kaempferia, Cienkowskia </i>and <i>Cienkowskiella </i>and the species is optionally selected from <i>Siphonochilus aethiopicus, Siphonochilus natalensis, Kaempferia aethiopica, Kaempferia natalensis, Kaempferia ethelae, Cienkowskia aethiopica </i>and <i>Cienkowskiella aethiopica</i>. The allergic disease is selected from asthma and atopy.</p>
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Crystals, amorphous substances or salts of methyl N-[3-(6,7-dimethoxy-2-methylaminoquinazolin-4-yl) phenyl] terephthalamic acid (Fri, 06 Mar 2009)
<p id="p-0001" num="0000">Crystals, amorphous substances, salts, and hydrates of a salt of methyl N-[3-(6,7-dimethoxy-2-methylaminoquinazolin-4-yl)phenyl]terephthalamic acid having PDE4 inhibitory action are provided. These compounds are useful for treating allergic diseases such as atopic dermatitis.</p>
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2,3-disubstituted pyrazinesulfonamides as CRTH2 inhibitors (Fri, 27 Feb 2009)
<p id="p-0001" num="0000">The present invention is related to the use of 2,3 substituted pyrazine sulfonamides of formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="29.80mm" wi="56.05mm" file="US08796280-20140805-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> for the treatment and/or prevention of allergic diseases, inflammatory dermatoses and other diseases with an inflammatory component. Specifically, the present invention is related to the use of 2,3 substituted pyrazine sulfonamides for the modulation, notably the inhibition, of CRTH2 activity. </p>
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Indazolinone compositions useful as kinase inhibitors (Fri, 20 Feb 2009)
<p id="p-0001-en" num="0000">The present invention provides compounds of formula I:</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="25.65mm" wi="54.53mm" file="US07842712-20101130-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003-en" num="0000">These compounds, and pharmaceutically acceptable compositions thereof, are useful generally as kinase inhibitors, particularly as inhibitors of PRAK, GSK3, ERK2, CDK2, MK2, SRC, SYK, and Aurora-2. Accordingly, compounds and compositions of the invention are useful for treating or lessening the severity of a variety of disorders, including, but not limited to, heart disease, diabetes, Alzheimer's disease, immunodeficiency disorders, inflammatory diseases, allergic diseases, autoimmune diseases, destructive bone disorders such as osteoporosis, proliferative disorders, infectious diseases and viral diseases.</p>
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8-azaprostaglandin derivative compound and agent comprising the compound as active ingredient (Fri, 13 Feb 2009)
<p id="p-0001-en" num="0000">An 8-azaprostaglandin represented by formula (I)</p> <p id="p-0002-en" num="0000"> <br/> <br/>(wherein all symbols have the same meanings as described in the specification), a pharmaceutically acceptable salt thereof or a cyclodextrin clathrate thereof. Since the compound represented by formula (I) binds to EP2 subtype among PGE receptor strongly, it is useful for preventive and/or treatment for immune diseases, allergic diseases, neuronal cell death, dysmenorrhea, premature birth, abortion, baldness, retinal neuropathy such as glaucoma, erectile dysfunction, arthritis, pulmonary injury, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, hepatic injury, acute hepatitis, liver cirrhosis, shock, nephritis, renal failure, circulatory diseases, systemic inflammatory response syndrome, sepsis, hemophagocytosis syndrome, macrophage activation syndrome, still disease, Kawasaki Disease, burn, systemic granuloma, ulcerative colitis, Crohn disease, hypercytokinemia at dialysis, multiple organ failure, or bone diseases etc.<br/></p>
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Indole derivative having PGD2 receptor antagonist activity (Fri, 30 Jan 2009)
<p id="p-0001" num="0000">The present invention creates an indole derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases.</p> <p id="p-0002" num="0000">A compound of the generic formula (I)</p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="33.53mm" wi="67.65mm" file="US07956082-20110607-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0004" num="0000">wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a 3- to 8-membered nitrogen-containing non-aromatic heterocyclic ring etc.; R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4 </sup>and R<sup>5 </sup>are independently a hydrogen atom or a halogen atom etc.; R<sup>6 </sup>is C2-C4 alkyloxy etc.; R<sup>7 </sup>is independently a halogen atom etc.; R<sup>8 </sup>is independently C1-C4 alkyl etc.; R<sup>9 </sup>is carboxy etc.; Y is a single bond etc.; M is sulfonyl etc.; L<sup>1</sup>, L<sup>2 </sup>and L<sup>3 </sup>are a single bond or alkylene optionally containing one or two heteroatoms etc.; n is 0 etc.; q is 0 etc.;</p> <p id="p-0005" num="0000">a pharmaceutically acceptable salt or hydrate thereof.</p>
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PIPERIDINE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Fri, 30 Jan 2009)
The present application describes modulators of MIP-1 of formula (I) : or stereoisomers or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as set forth above. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators are disclosed.
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PIPERIDINYL DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Fri, 30 Jan 2009)
The present application describes modulators of MIP-1α of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators of formula (I) are disclosed.
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Imidazo[1,2-C]pyrimidinylacetic acid derivatives (Fri, 09 Jan 2009)
<p id="p-0001-en" num="0000">The present invention relates to an imidazo[1,2-c]pyrimidinylacetic acid derivative and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The imidazo[1,2-c]pyrimidinylacetic acid derivative of the present invention has excellent CRTH2 (G-protein-coupled chemoattractant receptor, expressed on Th2 cells) antagonistic activity and can be used for the prophylaxis and treatment of diseases associated with CRTH2 activity, in particular for the treatment of allergic diseases, such as asthma, allergic rhinitis, atopic dermatitis, and allergic conjunctivitis; eosinophil-related diseases, such as Churg-Strauss syndrome and sinusitis; basophil-related diseases, such as basophilic leukemia, chronic urticaria and basophilic leukocytosis in human and other mammals; and inflammatory diseases characterized by T lymphocytes and profuse leukocyte infiltrates such as psoriasis, eczema, inflammatory bowel disease, ulcerative colitis, Crohn's disease, COPD (chronic obstructive pulmonary disorder) and arthritis.</p>
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3-(4-{ [4-(4-{ [3-(3, 3-dimethyl-1-piperidinyl) propyl] oxy} phenyl)-1-piperidinyl] carbonyl}-1-naphthalenyl) propanoic or propenoic acid as H1 and H3 receptor antagonists for the treatment of inflammatory and/or allergic disorders (Fri, 19 Dec 2008)
<p id="p-0001" num="0000">The present invention relates to a compound of formula (I), or a salt thereof</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="35.48mm" wi="74.42mm" file="US07989629-20110802-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein the naphthalene ring is substituted in the 2, 3, 4, 5, 6, 7 or 8 position by R<sup>1</sup>, and R<sup>1 </sup>represents —CH<sub>2</sub>CH<sub>2</sub>COOH or —CH═C(CH<sub>3</sub>)COOH, and to processes for their preparation, to compositions containing them and to their use in the treatment of various inflammatory and/or allergic diseases, such as diseases such as allergic rhinitis. </p>
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ACYLAMINOPIPERIDINE COMPOUND (Thu, 11 Dec 2008)
[Problem] To provide a compound which has an excellent activity to modulate the functions of CCR4 or TARC and/or MDC and can be used for the prevention and/or treatment of various inflammatory diseases, allergic diseases, autoimmune diseases and the like. [Means for Resolution] An acylaminopiperidine compound represented by the formula (I) or a pharmaceutically acceptable salt thereof. [Symbols in the formula represent the following meanings; A: a single bond or C 1 -C 6 alkylene, R 1 : phenyl which may be substituted, etc., R 2 : -H or C 1 -C 6 alkyl, R 3 : -H, C 1 -C 6 alkyl or C 3 -C 8 cycloalkyl, R 4 : pyrrolidin-2-yl which may be substituted, etc., and D: benzene ring or pyrazole ring].
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NITROGENATED HETEROCYCLIC DERIVATIVE, AND PHARMACEUTICAL AGENT COMPRISING THE DERIVATIVE AS ACTIVE INGREDIENT (Thu, 27 Nov 2008)
The compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof specifically binds CCR5, so it is useful for preventing and/or treating CCR5-related diseases, for example, various inflammatory diseases (asthma, nephritis, nephropathy, hepatitis, arthritis, rheumatoid arthritis, rhinitis, conjunctivitis, ulcerative colitis, etc.), immunological diseases (autoimmune diseases, rejection in organ transplantation, immunosuppression, psoriasis, multiple sclerosis, etc.), infectious diseases (infection with human immunodeficiency virus, acquired immunodeficiency syndrome, etc.), allergic diseases (atopic dermatitis, urticaria, allergic bronchoplumonary aspergillosis, allergic eosinophilic gastroenteritis, etc.), ischemic reperfusion injury, acute respiratory distress syndrome, shock accompanying bacterial infection, diabetes, cancer metastasis and so on. Wherein all symbols in formula are as defined in the specification
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NOVEL CRYSTALLINE BEPOTASTINE METAL SALT HYDRATE, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME (Fri, 17 Oct 2008)
The present invention discloses a non-hygroscopic crystalline bepotastine metal salt hydrate, a method for preparing same, and a pharmaceutical composition comprising same for treating or preventing a histamine-mediated disease or an allergic disease.
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NOVEL CRYSTALLINE BEPOTASTINE METAL SALT HYDRATE, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME (Fri, 17 Oct 2008)
The present invention discloses a non-hygroscopic crystalline bepotastine metal salt hydrate, a method for preparing same, and a pharmaceutical composition comprising same for treating or preventing a histamine-mediated disease or an allergic disease. </p>
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Composition Comprising Isoorientin for Suppressing Histamine (Fri, 05 Sep 2008)
<p id="p-0001-en" num="0000">The present invention relates to a pharmaceutical composition for the prevention or treatment of diseases mediated by excessive histamine comprising naturally-derived isoorientin, a use of isoorientin for the manufacture of a medicament for the prevention or treatment of diseases mediated by excessive histamine, and a method for preventing or treating diseases mediated by excessive histamine comprising administering a therapeutically effective amount of isoorientin to a subject. The composition, use and method of the present invention show excellent histamine suppression effects, and so can be used for the prevention or treatment of various kinds of allergic disease, atopic disease, inflammatory disease, skin disease, hyperacidity and nervous system disorder.</p>
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Compound having S1P receptor binding potency and use thereof (Fri, 29 Aug 2008)
<p id="p-0001" num="0000">Provided are: a compound represented by formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="11.85mm" wi="61.04mm" file="US08039674-20111018-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> (wherein ring A and ring D each represent a cyclic group which may have a substituent(s); E and G each represent a bond or a spacer having 1 to 8 atoms in its main chain; L represents a hydrogen atom or a substituent; X represents amino which may have a substituent(s), or a heterocyclic group which contains at least one nitrogen atom and which may have a substituent(s); n represents 0 to 3, in which when n is 2 or more, a plurality of ring A's may be the same or different from one another); a salt thereof; an N-oxide form thereof; a solvate thereof, a prodrug thereof; and a medicament which includes those. The compound represented by formula (I) is capable of binding S1P receptors (in particular, EDG-1 and/or EDG-6), and useful for preventing and/or treating rejection in transplantation, autoimmune diseases, allergic diseases, etc. </p>
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PURINE DERIVATIVES AS IMMUNOMODULATORS (Fri, 29 Aug 2008)
Compounds of formula (I) wherein R1 is C1-8alkylamino, C1-8alkoxy, C3-7cycloalkylC1-6alkylamino, C3-7cycloalkylC1-6alkoxy, C1-3alkoxyC2-3alkoxy, or Hetb-C1-3alkoxy; Hetb is a 5- or 6-membered saturated aliphatic heterocyle containing one oxygen atom; R2 is -(CH2)n-Het; n is an integer having a value of 1 to 4; Het is a 5- or 6-membered saturated aliphatic heterocycle containing one oxygen heteroatom, which heterocycle may be substituted by one or two C1-4alkyl groups, and salts and solvates thereof, are inducers of human interferon and may be useful in the treatment of various disorders in particular infectious diseases, cancer, and allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, and as vaccine adjuvants.
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BASIC GROUP-CONTAINING COMPOUND AND USE THEREOF (Thu, 28 Aug 2008)
A compound represented by general formula (I): a salt thereof, a solvate thereof, or a prodrug thereof wherein all symbols are as defined in the specification has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, systemic erythematosus, retinopathy, macular degeneration, pulmonary fibrosis, transplanted organ rejection, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiac /vascular disease(for example, arteriosclerosis, myocardial infarction, stenocardia, cerebral infarction, chronic arterial occlusive disease, etc.), metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), a preventive and/or therapeutic agent for cancerous diseases or infections, or an agent for regeneration therapy.
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CRYSTAL, AMORPHOUS FORM AND SALT OF METHYL N-[3-(6,7-DIMETHOXY-2-METHYLAMINOQUINAZOLIN-4-YL)PHENYL]TEREPHTHALAMIC ACID (Fri, 22 Aug 2008)
Disclosed is a crystal, an amorphous form, a salt or a hydrate of the salt of methyl N-[3-(6,7-dimethoxy-2- methylaminoquinazolin-4-yl)phenyl]terephthalamic acid, which has a PDE4-inhibiting activity and therefore is useful for the treatment of an allergic disease such as atopic dermatitis.</p>
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Dihydrogen phosphate salt of a prostaglandin D2 receptor antagonist (Fri, 15 Aug 2008)
<p id="p-0001-en" num="0000">The present invention is directed to dihydrogen phosphate salt 2-(3-{6-[2-(2,4-dichloro-phenyl)-ethylamino]-2-methoxy-pyrimidin-4-yl}-phenyl)-2-methyl-propionic acid of Formula (III),</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="40.39mm" wi="76.20mm" file="US07642249-20100105-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of Formula (III), and a pharmaceutically acceptable carrier; and a method of treating a patient suffering from a PGD2-mediated disorder including, but not limited to, allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, bronchitis, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis and the like, by administering to said patient a pharmaceutically effective amount of the compound of Formula (III). </p>
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INTERFERON-ALPHA AND C-PHYCOCYANIN FOR THE TREATMENT OF AUTOIMMUNE DISEASES, ALLERGIC DISEASES AND CANCER (Thu, 14 Aug 2008)
The present invention consists of the combination of Interferon alpha and C-Phycocyanin (IFN-±/C-Phyco) for obtaining a pharmaceutical preparation for autoimmune disease, allergy and cancer treatments. The anti-inflammatory, immunomodulator, antioxidant, anti-viral, anti-proliferative and anti-tumoral effects, associated to the regulatory T cell inducer effect demonstrated in this invention is the rationale for the use of the IFN-±/C-Phyco combination in these diseases.
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DIHYDROGEN PHOSPHATE SALT OF A PROSTAGLANDIN D2 RECEPTOR ANTAGONIST (Thu, 31 Jul 2008)
The present invention is directed to the dihydrogen phosphate salt of 2-(3-&lcub;6-&lsqb;2-(2,4-dichloro-phenyl)-ethylamino&rsqb;-2-methoxy-pyrimidin-4-yl&rcub;-phenyl)-2-methyl-propionic acid of Formula (III), a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of Formula (III), and a pharmaceutically acceptable carrier; and a method of treating a patient suffering from a PGD2-mediated disorder including, but not limited to, allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, bronchitis, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis and the like, by administering to said patient a pharmaceutically effective amount of the compound of Formula (III).
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Pyrazolo[3,4-b]Pyridine Compounds, and their Use as Phosphodiesterase Inhibitors (Fri, 25 Jul 2008)
<p id="p-0001-en" num="0000">The invention relates to a compound of formula (I) or a salt thereof:</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="29.29mm" wi="54.44mm" file="US20080175914A1-20080724-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003-en" num="0000">wherein: <ul id="ul0001-en" list-style="none"><li>R<sup>1 </sup>is C<sub>1-4</sub>alkyl, C<sub>1-3</sub>fluoroalkyl, —CH<sub>2</sub>CH<sub>2</sub>OH or —CH<sub>2</sub>CH<sub>2</sub>CO<sub>2</sub>C<sub>1-2</sub>alkyl;</li><li>R<sup>2 </sup>is a hydrogen atom (H), methyl or C<sub>1</sub>fluoroalkyl;</li><li>R<sup>3 </sup>is optionally substituted C<sub>3-8</sub>cycloalkyl or optionally substituted mono-unsaturated-C<sub>5-7</sub>cycloalkenyl or an optionally substituted heterocyclic group of sub-formula (aa), (bb) or (cc);</li></ul></p> <p id="p-0004-en" num="0000"> <chemistry id="chem-us-00002-en" num="00002"> <img id="emi-c00002-en" he="72.98mm" wi="55.63mm" file="US20080175914A1-20080724-C00002.TIF" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0002-en" list-style="none"> <li>in which n<sup>1 </sup>and n<sup>2 </sup>independently are 1 or 2; and in which Y is O, S, SO<sub>2</sub>, or NR<sup>10</sup>;</li> <li>or R<sup>3 </sup>is a bicyclic group (dd) or (ee):</li> <li>and wherein X is NR<sup>4</sup>R<sup>5 </sup>or OR<sup>5a</sup>.</li> </ul> </p> <p id="p-0005-en" num="0000"> <chemistry id="chem-us-00003-en" num="00003"> <img id="emi-c00003-en" he="45.38mm" wi="52.24mm" file="US20080175914A1-20080724-C00003.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0006-en" num="0000">The compounds are phosphodiesterase (PDE) inhibitors, in particular PDE<b>4</b> inhibitors. Also provided is the use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the treatment and/or prophylaxis of an inflammatory and/or allergic disease in a mammal such as a human, for example chronic obstructive pulmonary disease (COPD), asthma, or allergic rhinitis.</p>
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CONDENSED PYRIDINE COMPOUND (Fri, 18 Jul 2008)
[PROBLEMS] To provide a compound having an excellent JAK3-inhibiting activity and useful as an active ingredient for a therapeutic or prophylactic agent for various immune diseases including autoimmune diseases, inflammatory diseases and allergic diseases. [MEANS FOR SOLVING PROBLEMS] A study is made on a novel condensed heterocyclic derivative, and it is confirmed that the condensed pyridine compound of the invention has an excellent JAK3-inhibiting activity. It is confirmed that the compound is useful as an active ingredient for a therapeutic or prophylactic agent for a disease induced by undesirable cytokine signaling such as rejection upon living donor transplantation, an autoimmune disease, asthma, atopic dermatitis, rheumatism, psoriasis and atherosclerosis or a disease induced by abnormal cytokine signaling such as cancer and leukemia because of its inhibitory activity on JAK3.</p>
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Substituted Pyrazoles as Modulators of Chemokine Receptors (Fri, 11 Jul 2008)
<p id="p-0001-en" num="0000">Substituted pyrazole compounds such compounds represented by formula I: which are used to modulate the CCR-2 chemokine receptor to prevent or treat inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis; and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions.</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="24.05mm" wi="69.93mm" file="US20080167322A1-20080710-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p>
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