Allergic diseases

TRICYCLIC COMPOUND AND JAK INHIBITOR (Thu, 23 Mar 2017)
Novel tricyclic compounds which have JAK inhibitory activities are useful for prevention, treatment or improvement of autoimmune diseases, inflammatory diseases and allergic diseases are provided. Novel tricyclic compound represented by the formula (I), the formula (II) or the formula (III) (wherein : each of A 1 , A 2 and A 3 is a cyclohexane-1,4-diyl group or the like; each of L 1 , L 2 and L 3 is a methylene group or the like; each of X 1 and X 3 is O or NH; each of R 1 and R 3 is a cyano C 1-6 haloalkyl group or the like; and R 2 is an aromatic heterocyclic group), a tautomer or pharmaceutically acceptable salt of the compound or a solvate thereof.
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NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS (Fri, 03 Mar 2017)
<p id="p-0001" num="0000">The present invention discloses compounds according to Formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="34.54mm" wi="69.85mm" file="US20170057928A1-20170302-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein Cy, R<sup>1</sup>, L<sub>1</sub>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, L<sub>a</sub>, and R<sup>a </sup>are as defined herein.</p> <p id="p-0004" num="0000">Novel benzimidazoles according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic diseases, inflammatory diseases, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or hypersecretion of interferons.</p>
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PYRROLO[3,2-D]PYRIMIDINE DERIVATIVES AS INDUCERS OF HUMAN INTERFERON (Fri, 03 Mar 2017)
<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="35.39mm" wi="53.85mm" file="US20170057963A1-20170302-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 hydrogen, methyl or —(CH<sub>2</sub>)<sub>2</sub>OR<sup>3</sup>, R<sup>2 </sup>is methyl or —(CH<sub>2</sub>)<sub>2</sub>OR<sup>4</sup>, or R<sup>1 </sup>and R<sup>2</sup>, together with the nitrogen atom to which they are attached, are linked to form a 5- or 6-membered heterocyclyl wherein the 6-membered heterocyclyl is optionally substituted by two hydroxy substituents; R<sup>3 </sup>and R<sup>4 </sup>are each independently hydrogen or methyl; and n is an integer having a value of 5 or 6, are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment or prevention of various disorders, for example the treatment or prevention 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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TRICYCLIC COMPOUND AND JAK INHIBITOR (Fri, 17 Feb 2017)
<p id="p-0001" num="0000">Novel tricyclic compounds which have JAK inhibitory activities are useful for prevention, treatment or improvement of autoimmune diseases, inflammatory diseases and allergic diseases are provided.</p> <p id="p-0002" num="0000">Novel tricyclic compound represented by the formula (I), the formula (II) or the formula (III) (wherein each of A<sup>1</sup>, A<sup>2 </sup>and A<sup>3 </sup>is a cyclohexane-<b>1,4</b>-diyl group or the like; each of L<sup>1</sup>, L<sup>2 </sup>and L<sup>3 </sup>is a methylene group or the like: each of X<sup>1 </sup>and X<sup>3 </sup>is O or NH; each of R<sup>1 </sup>and R<sup>3 </sup>is a cyano C<sub>1-6 </sub>haloalkyl group or the like; and R<sup>2 </sup>is an aromatic heterocyclic group), a tautomer or pharmaceutically acceptable salt of the compound or a solvate thereof.</p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="111.34mm" wi="69.85mm" file="US20170044161A1-20170216-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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COMPOUND EXHIBITING SELECTIVE EP2 AGONIST ACTIVITY (Thu, 05 Jan 2017)
To provide an excellent selective EP2 agonist in a safe manner. A compound represented by general formula (I): (wherein all symbols are as defined in the specification), a salt or N-oxide of the compound, or a solvate or prodrug of the compound or the salt or N-oxide has a selective EP2 agonist activity and is highly safe, and is therefore useful as a drug, especially as a therapeutic agent for EP2 receptor-related diseases including immune diseases, allergic diseases, neuronal death, dysmenorrhea, premature birth, miscarriage, baldness, ocular diseases, erectile dysfunction, arthritis, lung injury, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, bone diseases, cartilage injury and others.
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A NOVEL COMPOUND (KS 513) ISOLATED FROM PSEUDOLYSIMACHION ROTUNDUM VAR. SUBINTEGRUM, THE COMPOSITION COMPRISING THE SAME AS AN ACTIVE INGREDIENT FOR PREVENTING OR TREATING ALLERGY DISEASE, INFLAMMATORY DISEASE, ASTHMA OR CHRONIC OBSTRUCTIVE PULMONARY DISEASE AND THE USE THEREOF (Fri, 23 Dec 2016)
The present invention relates to a novel (1aS,1bS,2S,4S,5aR,6S,6aS)-1a-(hydroxymethyl)-4-methoxy-2-(((2S,3R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)octahydrooxireno[2',3':4,5]cyclopenta[1,2-c]pyran-6-yl 4-hydroxybenzoate} (KS-513), the isomer thereof, the pharmaceutically acceptable salt or solvates thereof, a composition comprising the same as an active ingredient for preventing or treating allergic disease, inflammatory disease, asthma or chronic obstructive pulmonary disease (COPD) and the use thereof.
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BICYCLIC COMPOUNDS, COMPOSITIONS AND MEDICINAL APPLICATIONS THEREOF (Fri, 19 Aug 2016)
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). (I) These compounds are useful in the treatment, prevention, prophylaxis, management, or adjunct treatment of all medical conditions related to inhibition of of retinoic acid-related orphan receptor gamma (RORƳ) such as inflammatory and/or autoimmune disorder, rheumatoid arthritis, psoriasis, psoriatic arthritis, multiple sclerosis, inflammatory bowel disease, allergic diseases, asthma, COPD, cancer, cell proliferation, type 1 diabetes, myasthenia gravis, hematopoetic disfunction, systemic lupus, erythematosus or other disorders.
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2-(PYRAZIN-2-YLCARBONYLAMINOMETHYL)BENZIMIDAZOLIUM COMPOUNDS AS EPITHELIAL SODIUM CHANNEL INHIBITORS (Fri, 22 Jul 2016)
The present invention relates to compounds of formula (I) or the tautomers or pharmacologically acceptable acid addition salts thereof, characterized by a topological polar surface area value (TPSA) of at least 145, wherein R1, R2, R3, R4, X, and Z- have one of the meanings as defined in the specification, to the use of compounds of formula (I) as medicaments, to pharmaceutical compositions comprising at least one compound of formula (I), as well as to medicament combinations containing one or more compounds of formula (I). The compounds are ENaC inhibitors useful for the treatment of respiratory diseases and allergic diseases of the airways.
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BICYCLIC COMPOUNDS, COMPOSITIONS AND MEDICINAL APPLICATIONS THEREOF (Fri, 15 Jul 2016)
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 retinoic acid-related orphan receptor gamma (RORγ) such as inflammatory and/or autoimmune disorder, rheumatoid arthritis, psoriasis, psoriatic arthritis, multiple sclerosis, inflammatory bowel disease, allergic diseases, asthma, COPD, cancer, cell proliferation, type 1 diabetes, myasthenia gravis, hematopoetic disfunction, systemic lupus, erythematosus or other disorders.
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Substituted hetero-bicyclic compounds, compositions and medicinal applications thereof (Thu, 14 Jul 2016)
The present disclosure provides hetero-bicyclic compounds of formula (I), their tautomers, polymorphs, stereoisomers, 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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ADENINE DERIVATIVES WHICH ARE USEFUL IN THE TREATMENT OF ALLERGIC DISEASES OR OTHER INFLAMMATORY CONDITIONS (Fri, 20 May 2016)
Compounds of formula (I).
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SPHINGOSINE KINASE INHIBITORS (Fri, 08 Apr 2016)
Sphingosine kinases are enzymes that catalyze the biosynthesis of sphingosine-1-phosphate. The invention provides compounds that are effective for inhibition of sphingosine kinase type 1, sphingosine kinase type 2, or both. Certain compounds are selective for sphingosine kinase type 2 relative to sphingosine kinase type 1. Compounds of the invention can be used in treatment of a range of diseases wherein increasing the level of sphingosine-1-phosphate in blood is medically indicated. Diseases that can be treated by administration of an effective dose of a compound of the invention include a neoplastic disease that involves excess vascular growth; macular degeneration or diabetic retinopathy; an allergic disease such as asthma, an inflammatory disease of the eye such as uveitis, scleritis, or vitritis; an inflammatory disease of the kidney; a fibrotic disease; atherosclerosis; or pulmonary arterial hypertension. A compound of the invention can be used to improve the integrity of a vascular barrier in a disease where the vascular barrier is disrupted, such as cancer or Alzheimer's disease.
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PURINE DERIVATIVES FOR USE IN THE TREATMENT OF ALLERGIC, INFLAMMATORY AND INFECTIOUS DISEASES (Thu, 31 Mar 2016)
Compounds of formula (I): wherein R 1 is C 1-6 alkylamino, C 1-6 alkoxy, or C 3-7 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.
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PYRIDAZINONE DERIVATIVES AS PHOSPHOINOSITIDE 3-KINASES INHIBITORS (Fri, 18 Mar 2016)
The invention relates to compounds of formula (I) inhibiting phosphoinositide 3-kinases (PI3K), to pharmaceutical compositions comprising them, and to therapeutic uses thereof in the treatment of disorders associated with PI3K enzymes such as respiratory diseases, allergic diseases, autoimmune diseases or inflammatory disorders.
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A NOVEL COMPOUND ISOLATED FROM PSEUDOLYSIMACHION ROTUNDUM VAR. SUBINTEGRUM CONTAINING ABUNDANT AMOUNT OF ACTIVE INGREDIENT, THE COMPOSITION COMPRISING THE SAME FOR PREVENTING OR TREATING ALLERGY DISEASE, INFLAMMATORY DISEASE, ASTHMA OR CHRONIC OBSTRUCTIVE PULMONARY DISEASE AND THE USE THEREOF (Fri, 29 Jan 2016)
The present invention relates to a novel methanocyclopenta[e][1,3]dioxepin-7-yl 3,4-dihydroxybenzoate derivative (KS534) represented below as the Chemical Formula 1, the pharmaceutically acceptable salt or solvates thereof, a composition comprising the same as an active ingredient for preventing or treating allergic disease, inflammatory disease, asthma or chronic obstructive pulmonary disease (COPD) and the use thereof. Formula (1)
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RAPID CLEARANCE OF ANTIGEN COMPLEXES USING NOVEL ANTIBODIES (Fri, 29 Jan 2016)
The present invention relates to rapid clearance molecules that bind target antigens and FcyRIIb 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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TRICYCLIC PYRROLOPYRIDINE COMPOUND, AND JAK INHIBITOR (Thu, 17 Dec 2015)
To provide a novel tricyclic pyrrolopyridine compound having a JAK inhibitory activity and useful for prevention, treatment and/or improvement of particularly autoimmune diseases, inflammatory diseases and allergic diseases. A novel tricyclic pyrrolopyridine compound represented by the formula (I), a tautomer or pharmaceutically acceptable salt of the compound or a solvate thereof: wherein the respective substituents are defined in detail in the specification, and R 1 is a C 1-6 alkyl group or the like, R 2 is a hydrogen atom or the like, R 3 is a hydrogen atom or the like, the ring A is C 3-11 cycloalkane or the like, L 1 is a C 1-6 alkylene group or the like, and R 4 is NR a R b or the like.
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NOVEL COMPOUNDS (Thu, 01 Oct 2015)
Compounds of formula (I) and salts thereof wherein R<sb>1</sb> is n-C<sb>3-6</sb>alkyl; R<sb>2</sb> is hydrogen or methyl; R<sb>3</sb> is hydrogen or C<sb>1-6</sb>alkyl, 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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GENETIC TEST FOR DETERMINING SUSCEPTIBILITY FOR EOSINOPHILIC ESOPHAGITIS (Fri, 25 Sep 2015)
Methods and compositions disclosed herein generally relate to determination of susceptibility to eosinophilic esophagitis, asthma, and/or allergic diseases, disorders, and/or pulmonary and/or upper gastrointestinal conditions arising therefrom and/or related thereto and the diagnosis, treatment, and/or management of eosinophilic esophagitis, asthma, and/or allergic diseases, disorders, and/or pulmonary and/or upper gastrointestinal conditions arising therefrom and/or related thereto. Embodiments of the invention relate to the association between genes and specific polymorphisms of genes with eosinophilic esophagitis. Embodiments of the invention can be used to determine and manage patient risk factors for development of eosinophilic esophagitis; this determination can then be used to diagnose eosinophilic esophagitis and to treat a patient diagnosed with eosinophilic esophagitis.
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PYRROLO[3,2] PYRIMIDINE DERIVATIVES AS INDUCERS OF HUMAN INTERFERON (Fri, 28 Aug 2015)
Compounds of formula (I) and salts thereof: (I) wherein R1 is hydrogen, methyl or –(CH2 )2 OR3, R2 is methyl or –(CH2)2 OR4, or R1 and R2, together with the nitrogen atom to which they are attached, are linked to form a 5-or 6- membered heterocyclyl wherein the 6-membered heterocyclyl is optionally substituted by two hydroxy substituents; R3 and R4 are each independently hydrogen or methyl; and n is an integer having a value of 5 or 6, are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment or prevention of various disorders, for example the treatment or prevention 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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BENZIMIDAZOLE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS (Fri, 31 Jul 2015)
The present invention discloses compounds according to Formula (I) wherein Cy, R1, L1 R3, R4, R5, La, and Ra are as defined herein. Novel benzimidazoles according to Formula (I), able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic diseases, inflammatory diseases, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or hypersecretion of interferons.
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Compound capable of binding S1P receptor and pharmaceutical use thereof (Thu, 18 Jun 2015)
A compound having an ability to bind to an S1P receptor (particularly EDG-6, preferably EDG-1 and EDG-6), for example, the compound represented by formula (I) of the present invention, 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. 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 1 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 1 is a substituent, and wherein m is 2 or more, R 1 s are the same or different.
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NOVEL AMINO PYRIMIDINE DERIVATIVES (Fri, 05 Jun 2015)
The present invention describes new amino pyrimidine derivatives of formula (I) and pharmaceutically acceptable salts thereof which appear to interact with Bruton's tyrosine kinase (Btk). Accordingly, the novel amino 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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NOVEL AMINO PYRIMIDINE DERIVATIVES (Fri, 05 Jun 2015)
The present invention describes new amino pyrimidine derivatives of formula (I) and pharmaceutically acceptable salts thereof which appear to interact with Bruton's tyrosine kinase (Btk). Accordingly, the novel amino 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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AMINE COMPOUND AND USE THEREOF FOR MEDICAL PURPOSES (Thu, 05 Mar 2015)
The present invention provides a compound represented by the following formula (I): wherein each symbol is as described in the DESCRIPTION, which has a superior peripheral blood lymphocyte decreasing action, and is useful for the treatment or prophylaxis of autoimmune diseases; prophylaxis or suppression of resistance or acute rejection or chronic rejection of transplantation of organ or tissue; treatment or prophylaxis of graft-versus-host (GvH) disease due to bone marrow transplantation; or treatment or prophylaxis of allergic diseases.
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NITROGENATED BICYCLIC AROMATIC HETEROCYCLIC COMPOUND (Thu, 26 Feb 2015)
[Problem] On the basis of a cathepsin S inhibitory effect, an excellent agent for treating or preventing autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like is provided. [Means for Solution] It was found that a nitrogen-containing bicyclic heterocyclic compound has the excellent cathepsin S inhibitory effect, thereby completing the invention. The compound of the present invention has the cathepsin S inhibitory effect, and can be used as an agent for preventing and/or treating autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like.
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SUBSTITUTED HETERO-BICYCLIC COMPOUNDS, COMPOSITIONS AND MEDICINAL APPLICATIONS THEREOF (Thu, 26 Feb 2015)
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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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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NOVEL PIPERIDINO-DIHYDROTHIENOPYRIMIDINE SULFOXIDES AND THEIR USE FOR TREATING COPD AND ASTHMA (Thu, 03 Jul 2014)
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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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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HYPOALLERGENIC VARIANTS OF MAL D 1, THE MAJOR ALLERGEN FROM MALUS DOMESTICA (Thu, 12 Jun 2014)
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.
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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-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 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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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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NOVEL PYRROLO PYRIMIDINE DERIVATIVES (Thu, 15 May 2014)
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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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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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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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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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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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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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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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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PURINE COMPOUNDS AS PRODRUGS OF A2B ADENOSINE RECEPTOR ANTAGONISTS, THEIR PROCESS AND MEDICINAL APPLICATIONS (Thu, 25 Jul 2013)
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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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 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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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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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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PIPERIDINYL COMPOUND AS A MODULATOR OF CHEMOKINE RECEPTOR ACTIVITY (Thu, 25 Apr 2013)
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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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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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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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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PHARMACEUTICAL COMPOSITION FOR INFLAMMATORY DISEASES, ALLERGIC DISEASES AND AUTOIMMUNE DISEASES (Fri, 28 Dec 2012)
The present invention relates to a method and a pharmaceutical composition for suppressing immunity, in each of wherein a fatty acid derivative represented by general formula (I) is utilized. The present invention also relates to a method and a pharmaceutical composition for treating inflammatory diseases, allergic diseases and autoimmune diseases, in each of wherein the fatty acid derivative is utilized.</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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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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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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PRODRUGS OF A PIPERIDINYL DERIVATIVE AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Thu, 16 Aug 2012)
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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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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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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NEW MACROLIDES AND THEIR USE (Thu, 21 Jun 2012)
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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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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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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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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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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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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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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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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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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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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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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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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7-PHENOXYCHROMAN CARBOXYLIC ACID DERIVATIVES (Thu, 27 Oct 2011)
Compounds of Formula I: (I) in which A, A<sp>1</sp>, R<sp>1</sp>, R<sp>7a</sp>, R<sp>7b</sp>, R<sp>8</sp> and R<sp>10</sp> 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<sb>2 </sb>(PGD<sb>2</sb>). 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 (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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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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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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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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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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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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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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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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CHROMENE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Thu, 02 Jun 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 W<sp>1</sp>, W<sp>2</sp>, W<sp>3</sp>, Y, Z, R<sp>2</sp>, R<sp>3</sp>, R<sp>3</sp>' and R<sp>4</sp>, 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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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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PURINE DERIVATIVES FOR USE IN THE TREATMENT OF ALLERGIC, INFLAMMATORY AND INFECTIOUS DISEASES (Thu, 26 May 2011)
Compounds of formula (I): wherein R<sp>1</sp> is C<sb>1-6</sb>alkylamino, C<sb>1-6</sb>alkoxy, or C<sb>3-7</sb>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.
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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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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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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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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)
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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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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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 (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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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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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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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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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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LOW-MOLECULAR POLYSULFATED HYALURONIC ACID DERIVATIVE AND COMPOSITIONS CONTAINING SAME (Fri, 06 Aug 2010)
<br/><br/>An agent for prevention and/or treatment of an allergic disease <br/>selected from pollinosis, allergic rhinitis, allergic <br/>conjunctivitis, atopic dermatitis, and asthma, represented by the <br/>following general formula (IA) or (IB);<br/>(see formula IA)<br/>wherein n represents a number of 0 to 15; R's each independently <br/>represent a hydrogen atom or an SO3H group etc.<br/></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)
<br/><br/>Compounds of Formula I: (I) in which A, A', R1, R7a, R7b, R8 and R10 have the <br/>meanings given in the specification, <br/>are DP2 receptor inhibitors useful in the treatment of useful in the treatment <br/>and prevention of immunologic diseases, allergic diseases <br/>such as asthma, allergic rhinitis and atopic dermatitis, and other <br/>inflammatory diseases mediated by prostaglandin D2 <br/>(PGD2). The compounds of Formula I may also be useful in treating diseases or <br/>medical conditions involving the Th2 T cell via <br/>production of IL-4, IL-5 and/or IL-13.<br/></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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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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Piperidinyl derivatives as modulators of chemokine receptor activity (Thu, 15 Apr 2010)
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<sb>1,</sb> R<sb>3</sb>, R<sb>4</sb>, R<sb>5</sb>, R<sb>5a </sb>and R<sb>5b</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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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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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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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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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, 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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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. </p>
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PURINE DERIVATIVES FOR USE IN THE TREATMENT OF ALLERGIC, INFLAMMATORY AND INFECTIOUS DISEASES (Fri, 19 Feb 2010)
<br/><br/><br/> Compounds of formula (I): wherein R1 is <br/>C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an <br/>integer having a value of 3 to 6; n is an integer having a <br/>value of 0 to 4; and salts thereof are inducers of human <br/> interferon. Compounds which induce human interferon may <br/>be useful in the treatment of various disorders, for example <br/>the treatment of allergic diseases and other inflammatory <br/>conditions for example allergic rhinitis and asthma, the <br/>treatment of infectious diseases and cancer, and may also <br/>be useful as vaccine adjuvants.<br/><br/><br/><br/></p>
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NOVEL ADENINE DERIVATIVES (Fri, 19 Feb 2010)
<br/><br/><br/> Compounds of formula (I) wherein R1 is <br/>C1-6alkylamino, or C1-6alkoxy; R1 is a group having the <br/>structure (II): n is an integer having a value of 1 to 6; Het <br/>is a 6-membered saturated heterocycle containing one nitrogen <br/> atom wherein Het is attached to the -(CH2)n-moiety <br/>at any carbon atom of the heterocycle; R3 is hydrogen, <br/>C1-8alkyl, or C3-7cycloalkylC0-6alkyl; and salts thereof are <br/>inducers of human interferon. Compounds which induce <br/>human interferon may be useful in the treatment of various <br/> disorders, for example the treatment of allergic diseases <br/>and other inflammatory conditions for example allergic <br/>rhinitis and asthma, the treatment of infectious diseases <br/>and cancer, and may also be useful as vaccine adjuvants.<br/><br/><br/><br/><br/></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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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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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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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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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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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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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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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)
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 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.
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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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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), 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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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)
<br/><br/><br/>Macrolides of Formula (I) or (I-A): and wherein the residues R1, R2, R3, R4, <br/>R12, R13 and R14 have certain <br/>meanings defined in this application are useful for treating or preventing <br/>inflammatory or allergic diseases or. cancer in animals <br/>and humans.<br/></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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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, 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, 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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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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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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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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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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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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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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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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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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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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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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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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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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PYRAZOLOPYRIMIDINE COMPOUND (Fri, 11 Jul 2008)
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 solvate of any of them.</p>
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PYRAZOLO[3,4-B]PYRIDINE COMPOUNDS, AND THEIR USE AS PDE4 INHIBITORS (Thu, 10 Jul 2008)
The invention provides a compound of formula (I) or a salt thereof: wherein R<sp>2</sp> is H, C<sb>1-3</sb>alkyl, n butyl, C1-2fluoroalkyl, cyclopropyl, cyclobutyl, (cyclopropyl)methyl , CN, or CH<sb>2</sb>OH; R<sp>3</sp> is inter alia optionally substituted C<sb>4-7</sb>cycloalkyl or an optionally substituted heterocyclic group (aa), (bb) or (cc); R<sp>a</sp> is H, methyl or ethyl; R<sp>b</sp> is H or methyl; R<sp>4</sp> is H, methyl, ethyl, n propyl, C(O) Me, or C(O) C1fluoroalkyl; and R<sp>5</sp> is: C(O) (CH2)<sb>n</sb> Ar, C(O) Het, C(O) C<sb>1</sb> 6alkyl, C(O) C1fluoroalkyl, C(O) (CH<sb>2</sb>)<sb>2</sb> C(O) NR<sp>15b</sp>NR<sp>15b</sp>, C(O) CH<sb>2</sb> C(O) NR<sp>15b</sp>NR<sp>15</sp>b, C(O) NR<sp>15b </sp>(CH2)m<sp>1</sp> Ar, C(O) NR<sp>15b</sp> Het, C(O) NR<sp>15b</sp> C<sb>1-6</sb> alkyl, C(O) NR<sp>5a</sp>R<sp>5b</sp>, S(O)<sb>2</sb> (CH<sb>2</sb>)m<sp>2</sp>-<sp>Ar</sp>, S(O)<sb>2</sb> Het, S(O)<sb>2</sb>-C<sb>1</sb>-<sb>6</sb>alkyl, or CH<sb>2</sb> Ar; or R<sp>4</sp> and R<sp>5</sp> taken together are -(CH<sb>2</sb>)<sb>p</sb><sp>1</sp>-, (CH<sb>2</sb>)<sb>2</sb> X<sp>5</sp> (CH<sb>2</sb>)<sb>2</sb> , C(O) (CH<sb>2</sb>)p<sp>2</sp> ,-C(O)-N(R<sp>15</sp>) (CH<sb>2</sb>)p<sp>3</sp> ; or NR<sp>4</sp>R<sp>5</sp> is of sub-formula (y), (y1), (y2) or (y3). 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, rheumatoid arthritis, allergic rhinitis, psoriasis or atopic dermatitis.
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COMPOUND CONTAINING BASIC GROUP AND USE THEREOF (Thu, 10 Jul 2008)
The present invention relates to a compound represented by formula (I): 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.
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SULFONAMIDE DERIVATIVE HAVING PGD2 RECEPTOR ANTAGONISTIC ACTIVITY (Thu, 03 Jul 2008)
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 (II): 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.; a pharmaceutically acceptable salt or a hydrate thereof.
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CONDENSED PYRIDINE DERIVATIVES USEFUL AS A28 ADENOSINE RECEPTOR ANTAGONISTS (Thu, 26 Jun 2008)
</p> <p>re presented by formula (D- Those compounds are useful for treating a subject afflicted with a pathological condition or disease susceptible to amelioration by antagonism of the A<sub>a</sub> adenosine receptor such as asthma, broochoconstrictioo, allergic diseases, hypertension, atherosclerosis, reperfusion injury, myocardial ischemia, retinopathy, inflammation, gastrointestinal tract disorders, cell proliferation disorders, diabetes mcllitus, and/or autoimmune diseases.
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PYRAZOLO[3,4-B]PYRIDINE COMPOUND, AND ITS USE AS A PDE4 INHIBITOR (Thu, 26 Jun 2008)
4- ( I l-(aminocarbonyl)-4-piperidinyl]amino)-N- [(3,4-dimethylphcnyl)methyll-l -ethyl-lH-pyrd- zolo[3,4-b]pyridine-5-carb oxamidc, which is the <br> compound of formula (I), or a salt thereof. The <br> invention also provides the use of said compound or a <br> pharmaceutically acceptable salt thereof as an inhibitor <br> (I) of phosphodiesterase type IV (PDE4), for example in <br> the treatment and/or prophylaxis of an inflammatory <br> and/or allergic disease, cognitive impairment or <br> depression in a mammal. In particular, the invention <br> provides the use of the compound or pharmaceutically <br> acceptable salt in the treatment and/or prophylaxis of atopic dermatitis in a mammal, for example by external topical administration to the mammal such as a human. Pharmaceutical compositions containing said compound or salt, in particular suitable for external topical administration, are also provided.
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INDOLECARBOXYLIC ACID DERIVATIVE HAVING PGD2 RECEPTOR ANTAGONISTIC ACTIVITY (Thu, 19 Jun 2008)
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. A compound of the general formula (I): 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 1 =X 2 -X 3 =X 4 - is a formula of -C(R 1 )=C(R 2 )-C(R 3 )=C(R 4 )- etc.; X 5 is C(R 5 ) or N; R 1 , R 2 , R 3 , R 4 and R 5 is independently a hydrogen atom, a halogen atom etc; R 6 is a formula of -Z-R 10 etc. wherein Z is alkylene etc., and R 10 is carboxy etc.; R 7 is optionally substituted alkyloxy etc.; R 8 is independently a halogen atom etc.; R 9 is independently optionally substituted alkyl etc.; Y is a single bond etc.; n is 0 etc.; q is 0 etc.; a pharmaceutically acceptable salt or a solvate thereof.
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IMIDAZO[1,2-C]PYRIMIDINYLACETIC ACID DERIVATIVES (Thu, 29 May 2008)
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.
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INDOLE DERIVATIVE HAVING PGD2 RECEPTOR ANTAGONIST ACTIVITY (Thu, 01 May 2008)
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. A compound of the generic formula (I) 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 1 , R 2 , R 3 , R 4 and R 5 are independently a hydrogen atom or a halogen atom etc.; R 6 is C2-C4 alkyloxy etc.; R 7 is independently a halogen atom etc.; R 8 is independently C1-C4 alkyl etc.; R 9 is carboxy etc.; Y is a single bond etc.; M is sulfonyl etc.; L 1 , L 2 and L 3 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.
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AZAINDOLE DERIVATIVE HAVING PGD2 RECEPTOR ANTAGONISTIC ACTIVITY (Thu, 17 Apr 2008)
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. A compound of the general formula (I) 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 1 =X 2 -X 3 =X 4 - is a formula of -C(R 1 )=C(R 2 )-C(R 3 )=N- etc.; R 1 , R 2 , R 3 , R 4 and R 5 are independently a hydrogen atom or a halogen atom etc.; R 6 is optionally substituted C1-C6 alkyloxy etc.; R 7 is independently a halogen atom etc.; R 8 is optionally substituted C1-C6 alky etc.; R 9 is carboxy etc.; M is sulfonyl etc.; Y is a single bond etc.; L 1 , L 2 and L 3 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.
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CYCLIC MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Fri, 11 Apr 2008)
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, R1, R2 and R8, 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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CYCLIC DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Fri, 11 Apr 2008)
The present application describes modulators of MIP-1α of formula (I), or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n, A, T, R1, R2 and R8, 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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GLYCOLIPID DERIVATIVE AND THERAPEUTIC AGENT COMPRISING THE SAME AS ACTIVE INGREDIENT (Thu, 03 Apr 2008)
Glycolipid derivatives having the formula (I): wherein R 1 indicates an aldopyranose residue, R 2 indicates a hydrogen atom or hydroxyl group, A indicates -CH 2 -, - CH(OH)-CH 2 - or -CH=CHCH 2 -, Z indicates -O- or -CH 2 -, 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 2 - and x indicates an integer of 4 to 15, y indicates an integer of 26 to 35, and when Z is -CH 2 - 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.
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IRAK MODULATORS FOR TREATING AN INFLAMMATORY CONDITION, CELL PROLIFERATIVE DISORDER, IMMUNE DISORDER (Fri, 14 Mar 2008)
The present invention relates to modulators of IRAK kinase and provides compositions comprising such modulators, as well as methods therewith for treating conditions or diseases mediated by or associated with IRAK kinase, such as rheumatoid arthitis, multiple sclerosis, sepsis, osteoarthrites, inflammatory bowel disease, osteoporosis, myasthenia gravis, stroke, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, psoriasis, cardiac contractile dysfunction, type I diabetes, type II diabetes, familial cold autoinf lammatory syndrome, severe bacterial infections, allergic disease, cancer, psoriasis, asthma, or graft rejection.
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MODULATORS OF INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASE (Fri, 14 Mar 2008)
The present invention relates to modulators of IRAK kinase and provides compositions comprising such modulators, as well as methods therewith for treating conditions or diseases mediated by or associated with IRAK kinase, such as rheumatoid arthitis, multiple sclerosis, sepsis, osteoarthrites, inflammatory bowel disease, osteoporosis, myasthenia gravis, stroke, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, psoriasis, cardiac contractile dysfunction, type I diabetes, type II diabetes, familial cold autoinf lammatory syndrome, severe bacterial infections, allergic disease, cancer, psoriasis, asthma, or graft rejection.</p>
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MATRIX METALLOPROTEINASE INHIBITORS (Fri, 29 Feb 2008)
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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PYRIMDINE COMPOUNDS USEFUL AS KINASE INHIBITORS (Fri, 29 Feb 2008)
A compound of formula (I) or a salt or solvate thereof: Formula (1) compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such mono-anilino pyrimidine derivatives are of potential therapeutic benefit in the treatment of diseases and conditions associated with inappropriate Syk activity, in particular in the treatment of inflammatory and allergic diseases.
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BETA -HYDROXY-AND AMINO-SUBSTITUTED CARBOXYLIC ACIDS AS MATRIX METALLOPROTEINASE INHIBITORS (Fri, 29 Feb 2008)
The present invention relates to .beta.-hydroxy and amino substituted carboxylic acids, which act as matrix metalloprotease inhibitors, particularly diastereomerically pure .beta.-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.</p>
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2,6-SUBSTITUTED-4-MONOSUBSTITUTEDAMINO-PYRIMIDINES AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS (Thu, 28 Feb 2008)
The present invention is directed a compound of Formula (I) as defined herein, a pharmaceutical composition comprising a pharmaceutically effective amount of one or more compounds according to Formula (I) in admixture with 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, discorders 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 a compound according to Formula (I).
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TRICYCLIC SPIRO DERIVATIVES AS CRTH2 MODULATORS (Thu, 28 Feb 2008)
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.
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SPIROPIPERIDINE COMPOUND AND MEDICINAL USE THEREOF (Thu, 21 Feb 2008)
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), a salt thereof, a quaternary ammonium salt thereof, an N-oxide form thereof or a solvate thereof, or a prodrug thereof. 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].
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NOVEL CHALCONE DERIVATIVES WHICH INHIBIT THE IL-5 ACTIVITY (Fri, 15 Feb 2008)
Disclosed herein are novel chalcone derivatives, which are low-molecular nonpeptide substances as interleukin-5 (IL-5) inhibitors having the effect of treating chronic allergic diseases, as well as a preparation method thereof and the use thereof as IL-5 inhibitors. Because the novel chalcone derivatives are low-molecular nonpeptide substances, they have no nonspecific response to proteins, unlike the prior known agents for treating allergic inflammation, and thus will be useful as allergy inhibitors.
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NEW MACROLIDES USEFUL AGAINST INFLAMMATORY AND ALLERGIC DISEASES (Fri, 15 Feb 2008)
Macrolide compounds of formula I: with PDF4 inhibiting activity are described, wherein R1 is a residue -Y-X-Q; Y is S, SO or SO2; 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.ident.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 C1-C4alkylene group; L is -0-, -S-, -SO2-, -NH-, -CO-, -(CO)O-, -O(OC)-, -(CO)NH-, -NH(CO)-, -(SO2)NH-, -HN(SO2)-, -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.</p>
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THIENOTRIAZOLODIAZEPINE COMPOUND AND A MEDICINAL USE THEREOF (Thu, 14 Feb 2008)
[Solving means] A thienotriazolodiazepine compound of the following formula (I) a pharmaceutical agent containing the compound as an active ingredient, and a production intermediate and a production method of the thienotriazolodiazepine compound. [Effect] 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.
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PYRAZOLO[3,4-B]PYRIDINE COMPOUNDS, AND THEIR USE AS PDE4 INHIBITORS (Fri, 08 Feb 2008)
The invention provides a compound of formula (I) or a salt thereof: wherein Ar has the sub-formula (x): and wherein: Q1 is NH or NMe, in which case Q2 is -C(O)-, -S(O)2-, -C(O)NH- or -C(O)NMe-; or Q1 is a bond or -O-, in which case Q2 is a bond; or Q1 is -C(O)-, in which case Q2 is NH or NMe; or Q1 is -S(O)2-, in which case Q2 is NH, NMe or a bond; and L is (CH2)n wherein n is 4 to 13; or L is -(CH2)m1-O-(CH2)m2-. 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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PYRAZOLO[3,4-B]PYRIDINE COMPOUNDS, AND THEIR USE AS PDE4 INHIBITORS (Fri, 08 Feb 2008)
The invention provides a compound of formula (I) or a salt thereof: wherein Ar has the sub-formula (x): and wherein: Q1 is NH or NMe, in which case Q2 is -C(O)-, -S(O)2-, -C(O)NH- or -C(O)NMe-; or Q1 is a bond or -O-, in which case Q2 is a bond; or Q1 is -C(O)-, in which case Q2 is NH or NMe; or Q1 is -S(O)2-, in which case Q2 is NH, NMe or a bond; and L is (CH2)n wherein n is 4 to 13; or L is -(CH2)m 1-O-(CH2)m 2-. 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).</p>
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3-Nitrogen-6, 7-dioxygen steroids and uses related thereto. (Mon, 04 Feb 2008)
A compound of formula (I) and pharmaceutical acceptable salts, solvates, stereoisomers and prodrugs thereof, in isolation or in mixture, wherein, independently at each occurrence: R1 and R2 are selected from hydrogen, oxygen so as to form nitro or oxime, amino, sulfate, and sulfonic acid, and organic groups having 1-30 carbons and optionally containing 1-6 heteroatoms selected from nitrogen, oxygen, phosphorous, silicon, and sulfur, where R1 and R2 may, together with the N to which they are both bonded, form a heterocyclic structure that may be part of an organic group having 1-30 carbons and optionally containing 1-6 heteroatoms selected from nitrogen, oxygen and silicon, and where R1 may be a 2, or 3 atom chain to numeral 2 so that -N-R1 - forms part of a fused bicyclic structure to ring A; R3 and R4 are selected from direct bonds to 6 and 7 respectively so as to form carbonyl groups; hydrogen, or a protecting group such that R3 and/or R4 is part of hydroxyl or carbonyl protecting group; numerals 1 through 17 each represent a carbon having substitution as described. The compounds may be formulated into pharmaceutical compositions, and used in the treatment and/or prevention of various conditions, including inflammation, asthma, an allergic disease, chronic obstructive pulmonary disease, atopic dermatitis, solid tumors, AIDS, ischemia, and cardiac arrhythmias.
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2-PHENYL-INDOLES AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS (Fri, 01 Feb 2008)
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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2-PHENYL-INDOLES AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS (Fri, 01 Feb 2008)
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.</p>
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PYRAZOLO (3, 4-B) PYRIDINE DERIVATIVES AS PDE4 INHIBITORS (Fri, 25 Jan 2008)
The present invention provides a compound of formula (I) or a salt thereof (in particular, a pharmaceutically acceptable salt thereof): The invention also provides the use of the compounds or salts 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, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis, e.g. in a mammal such as a human.
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8-OXOADENINE DERIVATIVES ACTING AS MODULATORS OF TLR7 (Fri, 11 Jan 2008)
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.
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2,3 SUBSTITUTED PYRAZINE SULFONAMIDES AS INHIBITORS OF CRTH2 (Thu, 03 Jan 2008)
The present invention is related to the use of 2,3 substituted pyrazine sulfonamides 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 2,3 substituted pyrazine sulfonamides for the modulation, notably the inhibition, of CRTH2 activity.
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NITROGENOUS HETEROCYCLIC COMPOUND AND MEDICINAL USE THEREOF (Thu, 08 Nov 2007)
A compound represented by formula (I): (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. 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.
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2,6-SUBSTITUTED-4-MONOSUBSTITUTED AMINO-PYRIMIDINE AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS (Fri, 26 Oct 2007)
The present invention is directed to a compound of formula (I) wherein R1 and R2 are as defined herein, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, a pharmaceutically acceptable prodrug thereof, or a pharmaceutically acceptable salt, hydrate or solvate of the prodrug, a pharmaceutical composition comprising a pharmaceutically effective amount of one or more compounds of the invention in admixture with a pharmaceutically acceptable carrier, 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 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 by administering to said patient a pharmaceutically effective amount of a compound of the invention.
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2,6-SUBSTITUTED-4-MONOSUBSTITUTED AMINO-PYRIMIDINE AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS (Fri, 26 Oct 2007)
The present invention is directed to a compound of formula (I) wherein R1 and R2 are as defined herein, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, a pharmaceutically acceptable prodrug thereof, or a pharmaceutically acceptable salt, hydrate or solvate of the prodrug, a pharmaceutical composition comprising a pharmaceutically effective amount of one or more compounds of the invention in admixture with a pharmaceutically acceptable carrier, 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 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 by administering to said patient a pharmaceutically effective amount of a compound of the invention.</p>
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PREVENTATIVE TREATMENT AND REMISSION OF ALLERGIC DISEASES (Fri, 12 Oct 2007)
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 Siphonochilus, Kaempferia, Cienkowskia and Cienkowskiella and the species is optionally selected from Siphonochilus aethiopicus, Siphonochilus natalensis, Kaempferia aethiopica, Kaempferia natalensis, Kaempferia ethelae, Cienkowskia aethiopica and Cienkowskiella aethiopica. The allergic disease is selected from asthma and atopy.
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QUINOLINE DERIVATIVES USEFUL AS PDE4 INHIBITORS (Fri, 28 Sep 2007)
There is provided according to the invention novel compounds of formula (I) or pharmaceutically acceptable salts or solvates thereof. The invention also relates to the use of said compounds, compositions and medicaments, for example as inhibitors of phosphodiesterases and/or for the treatment and/or prophylaxis of diseases or conditions for which a PDE4 inhibitor is indicated, in particular inflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis and allergic rhinitis.
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NITROGENATED HETEROCYCLIC DERIVATIVE, AND PHARMACEUTICAL AGENT COMPRISING THE DERIVATIVE AS ACTIVE INGREDIENT (Fri, 21 Sep 2007)
Disclosed is a compound represented by the general formula (I), a salt or N-oxide of the compound, a solvate of the compound, salt or N-oxide, or a prodrug of the compound, salt, N-oxide or solvate, which can bind specifically to CCR5 and therefore is useful for the prevention and/or treatment of a CCR5-associated disease, such as an inflammatory disease (e.g., asthma, nephritis, nephropathia, hepatitis, arthritis, rheumatoid arthritis, rhinitis, conjunctivitis, ulcerative colitis), an immune-mediated disease (e.g., autoimmune disease, rejection after organ transplantation, immunosuppression, psoriasis, multiple sclerosis), an infectious disease (e.g., infection with human immunodeficiency virus, acquired immunodeficiency syndrome), an allergic disease (e.g., atopic dermatitis, urticaria, allergic bronchopulmonary aspergillosis, allergic eosinophilic gastroenteritis), suppression of ischemia-reperfusion injury, acute respiratory syndrome, shock associated with a bacterial infection, diabetes, cancer metastasis or the like. (I) wherein each symbol is as defined in the description.</p>
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AMINOCARBOXYLIC ACID DERIVATIVE AND MEDICINAL USE THEREOF (Thu, 30 Aug 2007)
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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ACID SALT OF BENZIMIDAZOLE DERIVATIVE AND CRYSTAL THEREOF (Thu, 30 Aug 2007)
The present invention provides acid salts, such as sulfate, hydrochloride, and methanesulfonate, of 4-(1-((4-methylbenzothiophen-3-yl)methyl)benzimidazol-2-ylthio)butanoic acid and the crystals thereof. These benzimidazole derivatives and the crystals thereof have an in vivo chymase inhibitory activity and can be used as a preventive or therapeutic agent for inflammatory diseases, allergic diseases, respiratory diseases, circulatory diseases, or bone/cartilage metabolic diseases.
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PIPERIDINYL DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Fri, 17 Aug 2007)
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.
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PIPERIDINYL DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Fri, 17 Aug 2007)
The present application describes substituted piperidinyl modulators of MIP-1 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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HETEROCYCLIC JANUS KINASE 3 INHIBITORS (Fri, 13 Jul 2007)
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).
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HETEROCYCLIC JANUS KINASE 3 INHIBITORS (Fri, 13 Jul 2007)
<br/><br/><br/> The present invention provides a compound having an <br/>excellent JAK3 inhibition activity and being useful as an <br/>active ingredient of an agent for treating and/or preventing <br/>various immune diseases including autoimmune diseases, <br/>inflammatory diseases, and allergic diseases.<br/>As a result of studies on a novel condensed heterocyclic <br/>derivative, the inventors have found that a compound having <br/>a cross-linked structure has an excellent JAK3 inhibition <br/>activity, and have completed the present invention.<br/>In other words, it is verified that the compound <br/>according to the present invention has an inhibition activity <br/>against JAK3 and is thus useful as an active ingredient of an <br/>agent for treating or preventing diseases caused by <br/>undesirable cytokine signal transmission (e.g., rejection <br/>during organ/tissue transplantation, autoimmune diseases, <br/>multiple sclerosis, rheumatoid arthritis, psoriasis, asthma, <br/>atopic dermatitis, Alzheimer's disease, and atherosclerotic <br/>disease), or diseases caused by abnormal cytokine signal <br/>transmission (e.g., cancer and leukemia).<br/></p>
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SPIROCYCLIC COMPOUNDS AND THEIR USE AS CXCR4-ANTAGONISTS (Thu, 31 May 2007)
The present invention relates to a compound represented by formula (I-0): 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 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.
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INTERFERON-ALPHA AND C-PHYCOCYANIN FOR THE TREATMENT OF AUTOIMMUNE DISEASES, ALLERGIC DISEASES AND CANCER (Fri, 04 May 2007)
The present invention consists of the combination of Interferon alpha and C- Phycocyanin (IFN-(.alpha./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-.alpha./C-Phyco combination in these diseases. </p>
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DIHYDROGEN PHOSPHATE SALT OF A PROSTAGLANDIN D2 RECEPTOR ANTAGONIST (Fri, 27 Apr 2007)
The present invention is directed to the dihydrogen phosphate salt of 2-(3-{6-[2-(2,4-dichloro-phenyl)-ethylamino]-2-methoxy-pyrimidin-4-yl}-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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DIHYDROGEN PHOSPHATE SALT OF A PROSTAGLANDIN D2 RECEPTOR ANTAGONIST (Fri, 27 Apr 2007)
The present invention is directed to the dihydrogen phosphate salt of 2-(3-{6- [2-(2,4-dichloro-phenyl)-ethylamino]-2-methoxy-pyrimidin-4-yl}-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). </p>
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PYRROLOPYRIMIDINE DERIVATIVES AS SYK INHIBITORS (Fri, 20 Apr 2007)
Pyrrolopyrimidine derivatives of formula (I) are inhibitors of Spleen Tyrosine kinase (Syk) and therefore of potential therapeutic benefit in the treatment of diseases and conditions associated with inappropriate Syk activity, in particular in the treatment of inflammatory and allergic diseases.
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PYRROLOPYRIMIDINE DERIVATIVES AS SYK INHIBITORS (Fri, 20 Apr 2007)
Pyrrolopyrimidine derivatives of formula (I) are inhibitors of Spleen Tyrosine kinase (Syk) and therefore of potential therapeutic benefit in the treatment of diseases and conditions associated with inappropriate Syk activity, in particular in the treatment of inflammatory and allergic diseases.
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PYRROLOPYRIMIDINE DERIVATIVES AS SYK INHIBITORS (Fri, 20 Apr 2007)
Pyrrolopyrimidine derivatives of formula (I) are inhibitors of Spleen Tyrosine kinase (Syk) and therefore of potential therapeutic benefit in the treatment of diseases and conditions associated with inappropriate Syk activity, in particular in the treatment of inflammatory and allergic diseases. </p>
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THIENOPYRAZOLE DERIVATIVE HAVING PDE7 INHIBITORY ACTIVITY (Thu, 19 Apr 2007)
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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PYRAZOLO[3,4-B]PYRIDINE COMPOUND, AND ITS USE AS A PDE4 INHIBITOR (Fri, 06 Apr 2007)
The invention provides N-{[1,6-diethyl-4-(tetrahydro-2H-pyran-4-ylamino)-1H-pyrazolo[3,4-b]pyridin-5-yl]methyl}-3-methyl-5-isoxazolecarboxamide Formula (I): or a salt thereof, such as the compound or a pharmaceutically acceptable salt thereof. The invention also provides the use of the compound or salt as an inhibitor of phosphodiesterase type IV (PDE4) and/or for the treatment and/or prophylaxis of an inflammatory and/or allergic disease, especially an inflammatory and/or allergic skin disease such as atopic dermatitis, in a mammal such as a human. External topical administration, e.g. topical administration to the skin, of the compound or salt is preferred, and external-topical pharmaceutical compositions are provided
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PYRAZOLO[3,4-B]PYRIDINE COMPOUNDS, AND THEIR USE AS PDE4 INHIBITORS (Fri, 06 Apr 2007)
The invention provides a compound of formula (I) or a salt thereof: wherein R2 is H, C1-3alkyl, n butyl, C1-2fluoroalkyl, cyclopropyl, cyclobutyl, (cyclopropyl)methyl , CN, or CH2OH; R3 is inter alia optionally substituted C4-7cycloalkyl or an optionally substituted heterocyclic group (aa), (bb) or (cc); Ra is H, methyl or ethyl; Rb is H or methyl; R4 is H, methyl, ethyl, n propyl, C(O) Me, or C(O) C1fluoroalkyl; and R5 is: C(O) (CH2)n Ar, C(O) Het, C(O) C1 6alkyl, C(O) C1fluoroalkyl, C(O) (CH2)2 C(O) NR15bNR15b, C(O) CH2 C(O) NR15bNR15b, C(O) NR15b (CH2)m1 Ar, C(O) NR15b Het, C(O) NR15b C1-6 alkyl, C(O) NR5aR5b, S(O)2 (CH2)m2-Ar, S(O)2 Het, S(O)2-C1-6alkyl, or CH2 Ar; or R4 and R5 taken together are -(CH2)p1-, (CH2)2 X5 (CH2)2 , C(O) (CH2)p2 ,-C(O)-N(R15) (CH2)p3 ; or NR4R5 is of sub-formula (y), (y1), (y2) or (y3). 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, rheumatoid arthritis, allergic rhinitis, psoriasis or atopic dermatitis.
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SULFONAMIDE DERIVATIVE HAVING PGD2 RECEPTOR ANTAGONISTIC ACTIVITY (Fri, 06 Apr 2007)
<br/><br/> The present invention provides an sulfonamide derivative having DP <br/>receptor antagonistic activity and a pharmaceutical composition comprising the <br/><br/>said compound as an active ingredient, and further a therapeutic agent for <br/>treating allergic diseases. The present invention provides a compound of the <br/>general formula (II):<br/>(see formula II)<br/>wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a <br/>nitrogen-containing non-aromatic heterocyclic ring etc.; the ring C is an <br/>aromatic carbocyclic ring etc.; R1 is carboxy etc.; R2 is independently a <br/>halogen <br/>atom etc.; R3 is optionally substituted alkyloxy etc.; R4 is independently a <br/>halogen atom etc.; R5 is independently optionally substituted alkyl etc.; M is <br/><br/>sulfonyl etc.; Y is a single bond etc.; L1 is a single bond etc.; L2 is a <br/>single bond <br/>etc.; k is 0, 1, 2, 3 or 4; n is 0, 1 or 2; and q is 0, 1, 2 or 3; provided <br/>that a) k is <br/>not 0 when the ring B is a 6-membered nitrogen-containing heterocyclic ring <br/>containing one or two nitrogen atom(s) and the ring C is a benzene ring, etc.; <br/>a <br/>pharmaceutically acceptable salt or a hydrate thereof.<br/></p>
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PURINE DERIVATIVES FOR THE TREATMENT OF VIRAL OR ALLERGIC DISEASES AND CANCERS (Fri, 30 Mar 2007)
The present invention provides compounds of (I) wherein R1, Y1, X1, Z1, X2, Y2, A, Y3, n, R and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
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[1,2,4]TRIAZOLO[1,5-A]PYRIMIDIN-2-YLUREA DERIVATIVE AND USE THEREOF (Thu, 29 Mar 2007)
Novel [1 ,2,4]triazolo[1 ,5-a]pyrimidine derivative of the general formula (1 ): (1 ) its prodrug or a pharmaceutically acceptable salt thereof, which exhibits an antigen presentation inhibiting activity and is useful as a preventive and/or therapeutic agent for immunological rejection and/or graft versus host reaction in organ/bone marrow transplant, autoimmune disease, allergic disease and/or inflammatory disease and also useful as an anticancer drug or as an immunological tolerance inducer for transplanted organ/transplanted bone marrow.</p> <p>Ar <br> X</p> <p> <BR> <BR> <br> R — N <br> H H
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COMPOUND HAVING S1P RECEPTOR BINDING POTENCY AND USE THEREOF (Thu, 08 Mar 2007)
Provided are: a compound represented by formula (I): (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, 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.
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NOVEL BLT2-MEDIATED DISEASE, AND BLT2 BINDING AGENT AND COMPOUND (Thu, 25 Jan 2007)
[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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BENZOIMIDAZOLE COMPOUND CAPABLE OF INHIBITING PROSTAGLANDIN D SYNTHETASE (Fri, 19 Jan 2007)
A benzoimidazole compound represented by the general formula (I) or a salt thereof: (I) wherein X1 represents an oxygen atom or a carbonyl group; and R1 represents a furan ring having 1 to 3 substituents or a pyrrole ring which may have 1 to 3 substituents, provided that a compound represented by the general formula (I) wherein the substituent is a phosphoric acid group or a phosphate ester group is excluded. The benzoimidazole compound or salt thereof has an excellent prostaglandin D synthetase inhibitory activity, and is useful as a prophylactic and/or therapeutic agent for a disease associated with prostaglandin D2 or a metabolite thereof, such as an allergic disease or an inflammatory disease or as an inhibitor for the exacerbation of Alzheimer disease or cerebral damage. </p>
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FURANOPYRIDINE DERIVATIVES AS ACK1 AND LCK MODULATORS (Fri, 08 Dec 2006)
The present invention relates to furanopyridine compounds having the general Formula (I) and stereoisomers, tautomers, solvates, pharmaceutically acceptable salts and derivatives, and prodrugs thereof. The invention also includes pharmaceutical compositions comprising a compound of Formula I, methods of modulating Lck and ACK-1 enzymes and of treating various related diseases and conditions, including inflammation, inhibition of T cell activation, proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma, thymoma, just to name a few, in a mammal, comprising administering to the mammal a therapeutically effective amount a compound of Formula I, as described above, and methods of manufacturing medicaments comprising the compound of Formula (I).
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FURANOPYRIDINE DERIVATIVES AND METHODS OF USE (Fri, 08 Dec 2006)
The present invention relates to furanopyridine compounds having the general Formula I (I) and stereoisomers, tautomers, solvates, pharmaceutically acceptable salts and derivatives, and prodrugs thereof. The invention also includes pharmaceutical compositions comprising a compound of Formula I, methods of modulating Lck and ACK-1 enzymes and of treating various related diseases and conditions, including inflammation, inhibition of T cell activation, proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma, thymoma, just to name a few, in a mammal, comprising administering to the mammal a therapeutically effective amount a compound of Formula I, as described above, and methods of manufacturing medicaments comprising the compound of Formula I. </p>
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8-OXOADENINE COMPOUND (Thu, 07 Dec 2006)
An 8-oxoadenine compound useful as an immuno-modulator having specific activity against Th1/Th2, specifically a prophylactic and therapeutic agent for a topical application for allergic diseases, viral siseases and cancers, which is represented by the following formula (1): , wherein A is a group of a formula represented by the formula (2): , wherein R 2 is a substituted or unsubstituted alkyl group and so on, R 3 is hydrogen atom or an alkyl group, R is a halogen atom and so on, n is 0-2, X 1 is oxygen atom, Z is straight or branched chain alkylene, and R 1 is an alkyl group which is optionally substituted by hydroxy group, an alkoxy group, alkoxycarbonyl group and so on, or its pharmaceutically acceptable salt.
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TRICYCLIC SPIRO DERIVATIVES AS CRTH2 MODULATORS (Fri, 01 Dec 2006)
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.
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TRICYCLIC SPIRO DERIVATIVES AS CRTH2 MODULATORS (Fri, 01 Dec 2006)
<br/><br/><br/>The present invention is related to the use of spiro derivatives of Formula <br/>(I) for the treatment and/or prevention of allergic diseases, inflammatory <br/>dermatoses and other diseases with an inflammatory component. Specifically, <br/>the present invention is related to the use of spiro derivatives for the <br/>modulation of CRTH2 activity.<br/></p>
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IMIDAZO 1,2-C PYRIMIDINYLACETIC ACID DERIVATIVES (Thu, 09 Nov 2006)
The present invention relates to an imidazo&lsqb;1,2-c&rsqb;pyrimidinylacetic acid derivative and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The imidazo&lsqb;1,2-c&rsqb;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.
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2,3 SUBSTITUTED PYRAZINE SULFONAMIDES AS INHIBITORS OF CRTH2 (Fri, 27 Oct 2006)
The present invention is related to the use of 2,3 substituted pyrazine sulfonamides 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 2,3 substituted pyrazine sulfonamides for the modulation, notably the inhibition, of CRTH2 activity.
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2,3 SUBSTITUTED PYRAZINE SULFONAMIDES (Fri, 27 Oct 2006)
<br/><br/>The present invention is related to the use of 2,3 substituted pyrazine <br/>sulfonamides of <br/>Formula (I)<br/>(see formula I)<br/>or stereoisomers, tautomers and pharmaceutically acceptable salts thereof, <br/>wherein: <br/>A is:<br/>(see formula A1) (see formula A2) (see formula A3) (see formula A4) <br/>(see formula A5) or (see formula A8)<br/>where n is 0, 1, 2, 3 or 4; m is either 1 or 2; B is phenyl or piperazinyl; R1 <br/>is hydrogen; R2 is <br/>aryl, wherein R2 is optionally substituted with one or more substituents <br/>selected from the <br/>group consisting of halogen, cyano, C1-C6-alkyl, C1-C6-alkoxy, thioalkoxy and <br/>thioalkyl; R3 is <br/>C1-C6-alkyl, aryl, heteroaryl, C1-C6-alkylaryl, C1-C6-alkylheteroaryl, C3-C8-<br/>cycloalkyl or <br/>C3-C8-heterocycloalkyl wherein each of said C1-C6-alkyl, aryl, heteroaryl,<br/>C1-C6-alkylheteroaryl, C3-C8-cycloalkyl and C3-C8-heterocycloalkyl is <br/>optionally substituted <br/>with one or more substituents selected from the group consisting of halogen, <br/>cyano, <br/>C1-C6-alkyl, C1-C6-alkoxy, heteroaryl, aryl, thioalkoxy and thioalkyl, or <br/>wherein said aryl,<br/>heteroaryl, C1-C6-alkylaryl, C -C6-alkylheteroaryl, C3-<br/>C8-cycloalkyl or<br/>C3-C8-heterocycloalkyl may be fused to one or more aryl, heteroaryl, C3-C8-<br/>cycloalkyl or <br/>C3-C8-heterocycloalkyl groups and may be substituted with one or more <br/>substituents selected<br/><br/><br/>of the group consisting of C1-C6-alkyl, alkoxy, aryl, heteroaryl, carboxyl, <br/>cyano, halogen, <br/>hydroxy, amino, aminocarbonyl, nitro, sulfoxy, sulfonyl, sulfonamide and <br/>trihaloalkyl; R7 is <br/>hydrogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, heteroaryl, C3-C8-<br/>cycloalkyl, <br/>C3-C8-heterocycloalkyl, carboxy, cyano, amino or hydroxy; the aryl is phenyl <br/>or napthyl; and <br/>the heteroaryl is pyridyl, indolyl, 3H-indolyl, benzimidazolyl or <br/>quinolinzinyl for the <br/>treatment and/or prevention of allergic diseases, inflammatory dermatoses and <br/>other diseases <br/>with an inflammatory component. Specifically, the present invention is related <br/>to the use of <br/>2,3 substituted pyrazine sulfonamides for the modulation, notably the <br/>inhibition, of CRTH2 <br/>activity.<br/></p>
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PYRAZOLO[3,4-b]PYRIDINE COMPOUNDS AND THEIR USE AS PHOSPHODIESTERASE INHIBITORS (Thu, 28 Sep 2006)
roalkyl or -(CI-M^OH; R<sup>2</sup> is a hydrogen atom (H), methyl or Cifluoroalkyl; R<sup>3a</sup> is a hydrogen atom (H) or C<sub>h</sub>alky]; R<sup>3</sup> is optionally substituted bratnehed C^alkyl, optionally substituted C<sub>3</sub>.gcycloalkyl, optionally substituted mono-unsaturated-Cs^cycloalt-ccnyl, opo tionally substituted phenyl, or an optionally substituted heterocyclic group? of sub-formula (aa), or (bb) or (cc) in which n<sup>1</sup> and n<sup>2</sup> © independently sare 1 or 2; and Y is O, S, S0<sub>2</sub>, or NR<sup>4</sup>; and wherein Het is o S sub-formula (i), or (ii), or (iii), or (iv) or (v). The compounds are phosphodiesterase (PDE) inhibitors, in particular PDE4 inhibit ors. Also provided is the use of a compound o f formula</p> <p>O (Γ), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the treatment and/or prophyla is of an inflammatory and/or allergic disease in a mammal such as a human, for example chronic obstructive pulmonary disease (COPD), asthma, or allesrgic rhinitis.
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COMPOSITION COMPRISING ISOORIENTIN FOR SUPPRESSING HISTAMINE (Fri, 22 Sep 2006)
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.
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COMPOSITION COMPRISING ISOORIENTIN FOR SUPPRESSING HISTAMINE (Fri, 22 Sep 2006)
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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SUBSTITUTED PYRAZOLES AS MODULATORS OF CHEMOKINE RECEPTORS (Fri, 25 Aug 2006)
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.
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SUBSTITUTED PYRAZOLES AS MODULATORS OF CHEMOKINE RECEPTORS (Fri, 25 Aug 2006)
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>
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2-PHENYL-INDOLES AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS (Fri, 04 Aug 2006)
The present invention is directed to a compound of Formula (XVI) wherein R, R2, R3, R4, R5, R6, R7 and n are as defined herein, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, a pharmaceutically acceptable prodrug thereof, or a pharmaceutically acceptable salt, hydrate or solvate of the prodrug, a pharmaceutical composition comprising a pharmaceutically effective amount of one or more compounds according to Formula (XVI) in admixture with a pharmaceutically acceptable carrier, 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 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 by administering to said patient a pharmaceutically effective amount of a compound according to Formula (XVI).
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2-PHENYL-INDOLES AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS (Fri, 04 Aug 2006)
The present invention is directed to a compound of Formula (XVI) wherein R, R2, R3, R4, R5, R6, R7 and n are as defined herein, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, a pharmaceutically acceptable prodrug thereof, or a pharmaceutically acceptable salt, hydrate or solvate of the prodrug, a pharmaceutical composition comprising a pharmaceutically effective amount of one or more compounds according to Formula (XVI) in admixture with a pharmaceutically acceptable carrier, 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 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 by administering to said patient a pharmaceutically effective amount of a compound according to Formula (XVI). </p>
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FUSED AZOLE-PYRIMIDINE DERIVATIVES (Thu, 27 Jul 2006)
( maceutic.-!] preparations containing them . 'Ilic fused azolcpyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinosilol-.Vkinusc (P I 3 K~) inhibition, especially for Ρ13Κ-γ inhibition and can be used for the prophylaxis and treatment of diseases associated with 13K jul particularly vvilh I 3Κ-γ activity. More specifically, the azole derivatives of the present</p> <p>© i nvention are useful for treatment and pr-ophylaxis of diseases as follows: inflammatory and immunoregulalory disorders, such as © asthma, atopic dermatitis, rhinitis, allergic diseases, chmnic obstructive pulmonary disease (COPD). septic shock, joint diseases, auloixnmunc pathologies such as rheumatoid arthritis, and Graves' disease, cancer, myocardial contractility disorders, heart failure, t hromboembolism, 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 discuses also relate to P I 3K activity in a human or animal subject.
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4-AMINOQUINOLINE-3-CARBOXAMIDE DERIVATIVES AS PDE4 INHIBITORS (Thu, 29 Jun 2006)
Compounds of formula (I) or pharmaceutically acceptable salts thereof: (I) are inhibitors of phosphodiesterase type IV (PDE4) and are of use in the treatment of inflammatory and/or allergic diseases.
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NITROGEN-CONTAINING HETEROCYCLIC DERIVATIVES AND DRUGS CONTAINING THE SAME AS THE ACTIVE INGREDIENT (Thu, 29 Jun 2006)
</p> <p>by !he following general formula (7). its <br> salt, solvates thereof or prodrugs thereof: <br> (I) (wherein each symbol is as defined in © the description. ) The compounds repre <BR> <br> 30 sented by the general formula (Γ) are useful in preventing and/or treating various inflammatory diseases (asthma, nephritis, nephropathy, hepatitis, arthritis, rheumatoid arthritis, rhinitis, conjunctivitis, ulcerative colitis, etc. ). i munoiocical diseases (autoimmune diseases, rejection in organ transplantation, immunosuppression, psoriasis, mul o tiple sclerosis, etc. ). infection with h uman immunodeficiency virus (acquired immunodeficiency syndrome, etc.), allergic diseases (atopic dermatitis, urticaria, allergic bronchoplumonary aspergil losi s, 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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AMINOCARBOXYLIC ACID DERIVATIVE AND MEDICINAL USE THEREOF (Fri, 23 Jun 2006)
<br/>The present invention relates to a compound represented by the formula (I), a <br/>salt thereof, an <br/>N-oxide form thereof, a solvate thereof, or a prodrug thereof, and a <br/>medicament containing the <br/>same. The compound represented by the formula (I) has an ability to bind to an <br/>S1P receptor <br/>(particularly, EDG-1, EDG-6, and/or EDG-8) and is useful for preventing and/or <br/>treating for <br/>rejection to transplantation, graft-versus-host disease, autoimmune diseases, <br/>allergic diseases, <br/>neurodegenerating diseases, and the like.<br/>(see formula I)<br/>wherein all symbols are described in the specification.<br/></p>
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1,3-DISUBSTITUTED AZETIDINE DERIVATIVES FOR USE AS CCR-3 RECEPTOR ANTAGONISTS IN THE TREATMENT OF INFLAMMATORY AND ALLERGIC DISEASES (Thu, 08 Jun 2006)
Compounds of formula Ia or Ib in free or salt form, wherein Ar, X<sp>1</sp>, X<sp>2</sp>, m, R<sp>1</sp>, Q, Y, R<sp>2</sp> and R<sp>3</sp> have the meanings as indicated in the specification, are useful for treating conditions that are mediated by CCR-3, for example an inflammatory or allergic condition, particularly an inflammatory or obstructive airways disease. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
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CARBOXYLIC ACID COMPOUNDS AND MEDICINAL COMPOSITIONS CONTAINING THE SAME AS THE ACTIVE INGREDIENT (Thu, 08 Jun 2006)
A compound represented by formula (I) 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.
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CHEMOKINE RECEPTOR ANTAGONIST AND MEDICAL USE THEREOF (Thu, 01 Jun 2006)
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). 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.
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COMPOUND CAPABLE OF BINDING S1P RECEPTOR AND PHARMACEUTICAL USE THEREOF (Thu, 01 Jun 2006)
A compound having an ability to bind to an S1P receptor (particularly EDG-6, preferably EDG-1 and EDG-6), for example, the compound represented by formula (I) of the present invention, 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. 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 1 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 1 is a substituent, and wherein m is 2 or more, R 1 s are the same or different.
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2, 6-SUBSTITUTED-4-MONOSUBSTITUTEDAMINO-PYRIMIDINE AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS (Fri, 28 Apr 2006)
The present invention is directed a compound of Formula (I) as defined herein, a pharmaceutical composition comprising a pharmaceutically effective amount of one or more compounds according to Formula (I) in admixture with 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, discorders 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 a compound according to Formula (I).
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2,6-SUBSTITUTED-4-MONOSUBSTITUTED AMINO-PYRIMIDINE AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS (Fri, 28 Apr 2006)
<br/><br/><br/>The present invention is directed a compound of Formula (I) as defined herein, <br/>a pharmaceutical composition comprising a pharmaceutically effective amount of <br/>one or more compounds according to Formula (I) in admixture with a <br/>pharmaceutically acceptable carrier, and a method of treating a patient <br/>suffering from a PGD2-mediated disorder including, but not limited to, <br/>allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic <br/>dermatitis, bronchial asthma and food allergy), systemic mastocytosis, <br/>discorders accompanied by systemic mast cell activation, anaphylaxis shock, <br/>bronchoconstriction, bronchitis, urticaria, eczema, diseases accompanied by <br/>itch (such as atopic dermatitis and urticaria), diseases (such as cataract, <br/>retinal detachment, inflammation, infection and sleeping disorders) which is <br/>generated secondarily as a result of behavior accompanied by itch (such as <br/>scratching and beating), inflammation, chronic obstructive pulmonary diseases, <br/>ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid <br/>arthritis, pleurisy, ulcerative colitis and the like by administering to said <br/>patient a pharmaceutically effective amount of a compound according to Formula <br/>(I).<br/></p>
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NITROGENOUS HETEROCYCLIC DERIVATIVE AND MEDICINE CONTAINING THE SAME AS AN ACTIVE INGREDIENT (Fri, 24 Mar 2006)
A compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof: (see formula I) (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 bronchoplumonary aspergillo sis, 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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PYRIDINYLPYRAZOLOPYRIMIDINONE DERIVATIVES AS PDE 7 INHIBITORS (Thu, 23 Mar 2006)
To provide the compounds inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic disease, inflammatory disease or immunologic disease. The compound is pyridinylpyrazolopyrimidinone compound represented by the following formula (IA) or (IB): especially, R<sp>1</sp> is cyclohexyl or cycloheptyl group, R<sp>2</sp> is methyl; R<sp>3</sp> is a group: -NR<sp>5</sp>R<sp>6</sp> or -S(O)<sb>0-2</sb>R<sp>8</sp>; hydrogen atom; nitro group; cyano group; a halogen atom; heteroaryl group; and R<sp>4</sp> is methoxy or ethoxy group.
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PYRIMIDINE DERIVATIVES USEFUL FOR THE TREATMENT OF DISEASES MEDIATED BY CRTH2 (Thu, 16 Mar 2006)
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.
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[1,2,4]TRIAZOLO[1,5-a]PYRIMIDIN-2-YLUREA DERIVATIVE AND USE THEREOF (Thu, 02 Mar 2006)
Novel [1,2,4]triazolo[1,5-a]pyrimidine derivative of the general formula (1): (1) its prodrug or a pharmaceutically acceptable salt thereof, which exhibits an antigen presentation inhibiting activity and is useful as a preventive and/or therapeutic agent for immunological rejection and/or graft versus host reaction in organ/bone marrow transplant, autoimmune disease, allergic disease and/or inflammatory disease and also useful as an anticancer drug or as an immunological tolerance inducer for transplanted organ/transplanted bone marrow.
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BENZOFURAN COMPOUND AND MEDICINAL COMPOSITION CONTAINING THE SAME (Thu, 23 Feb 2006)
The present invention relates to a benzofuran compound of the formula (I) wherein each symbol is as defined in the description, a pharmaceutically acceptable salt thereof and the like. The compound of the present invention has superior leukotriene inhibitory action, BLT2 competitive inhibitory action, BLT2 blocking action, action for the prophylaxis or treatment of allergy, action for the prophylaxis or treatment of asthma and action for the prophylaxis or treatment of inflammation, and is useful as an agent for the prophylaxis or treatment of diseases such as allergic disease, asthma, inflammation and the like, and other diseases.
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NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS AND USE THEREOF (Thu, 02 Feb 2006)
A pharmaceutical composition comprising, as an active ingredient, the compounds represented by formula (1) (wherein all of the symbols have the same meanings as defined in specification.), salts thereof, solvates thereof, or prodrugs thereof. The compounds represented by formula (I) are used for prevention and/or treatment of various inflammatory diseases (asthma, nephritis, nephropathy, hepatitis, arthritis, chronic rheumatoid arthritis, rhinitis, conjunctivitis, ulcerative colitis and the like), immunologic diseases (treatment of autoimmune diseases, transplant rejection, immunosuppression, psoriasis, multiple sclerosis and the like), human immunodeficiency virus infection (acquired immunodeficiency syndrome and the like), allergic diseases (atopic dermatitis, nettle rash, allergic bronchopulmonary aspergillosis, allergic eosinophilic gastroenteritis and the like), suppression of ischemia-reperfusion injury, acute respiratory distress syndrome, shock accompanied by bacterial infection, diabetes mellitus, or metastasis and the like.
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SPIROPIPERIDINE COMPOUND AND MEDICINAL USE THEREOF (Thu, 26 Jan 2006)
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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Triazaspiro¬5.5|undecane derivatives and pharmaceutical composition comprising the same as active ingredient (Thu, 26 Jan 2006)
Triazaspiro[5.5]undecane derivatives of the formula (I), quaternary ammonium salts thereof, N-oxides thereof, non-toxic salts thereof, or pharmaceutical compositions comprising them, as active ingredients (wherein R 1 is formula (II) or formula (III); R 2 is alkyl or alkynyl etc.; R 3 , R 4 is H, (substituted) alkyl etc., or R 3 and R 4 together to form formula (IV); R 5 is H or alkyl). Therefore the compounds of the formula (I) regulate the effect of chemokine/chemokine receptor, they are used for prevention and treatment of various inflammatory diseases, asthma, atopic dermatitis, urticaria, allergic diseases, nephritis, nephropathy, hepatitis, arthritis or rheumatoid arthritis etc.
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BENZOXAZINYL-AMIDOCYCLOPENTYL-HETEROCYCLIC MODULATORS OF CHEMOKINE RECEPTORS (Thu, 19 Jan 2006)
Cyclopentyl compounds linked to a benzoxazinyl group through an amido moiety utilizing the ring nitrogen of the benzoxazine, and further substituted with a heterocyclic moiety, 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.
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NITROGENOUS HETEROCYCLIC COMPOUND AND USE THEREOF (Thu, 19 Jan 2006)
The present invention relates to a medicament comprising the compound of formula (I) wherein all symbols have the same meanings as defined in the specification, a salt thereof or a prodrug thereof The compound of the present invention is useful for the prevention and/or treatment of immune diseases such as various types of inflammation, autoimmune disease, allergic diseases, etc.; infection concerning inflammation or HIV infections (e.g. asthma, nephritis, nephropathy, hepatitis, arthritis, rheumatoid arthritis, rhinitis, conjunctivitis, ulcerative colitis, etc .), organ transplantation rejection, immunosuppression, psoriasis, multiple sclerosis, optic neuritis, polymyalgia rheumatica syndrome, uveitis, vasculitis, human immunodeficiency virus infection (acquired immunodeficiency syndrome etc.), atopic dermatitis, urticaria, allergic bronchopulmonary aspergillosis, allergic eosinophilic gastroenteritis, osteoarthritis, ischemic reperfusion injury, acute respiratory distress syndrome, shock accompanying bacteria infection, diabetes, cancer metastasis, atherosclerosis, etc .).
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FURANOPYRIMIDINES (Fri, 13 Jan 2006)
The present invention relates to furanopyrimidine compounds having the general Formula (I) and stereoisomers, tautomers, solvates, pharmaceutically acceptable salts and derivatives, and prodrugs thereof. The invention also includes pharmaceutical compositions comprising a compound of Formula (I), methods of treating various diseases and conditions in a mammal, including inflammation, inhibition of T cell activation, proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma and thymoma, comprising administering to the mammal a therapeutically effective amount of a compound of Formula (I). The invention also relates to methods of manufacturing medicaments, which comprise one or more compounds of Formula (I).
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TOPICAL FORMULATIONS FOR TREATING ALLERGIC DISEASES (Fri, 13 Jan 2006)
Methods for topically treating allergic diseases of the eye, ear or nose using tricyclic compounds are disclosed.
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THIENOPYRAZOLE DERIVATIVE HAVING PDE 7 INHIBITORY ACTIVITY (Fri, 13 Jan 2006)
Toprovide 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): (see formula I) [wherein, especially, R1 is a cyclohexyl, a cycloheptyl group or a tetrahydropyranyl group; R2 is methyl; R3 is a hydrogen atom; and R4 is a group: -CONR5R6 (in which any one of R5 and R6 is a hydrogen atom)]. </p>
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FURANOPYRIMIDINES (Fri, 13 Jan 2006)
The present invention relates to furanopyrimidine compounds having the general Formula (I) and stereoisomers, tautomers, solvates, pharmaceutically acceptable salts and derivatives, and prodrugs thereof. The invention also includes pharmaceutical compositions comprising a compound of Formula (I), methods of treating various diseases and conditions in a mammal, including inflammation, inhibition of T cell activation, proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma and thymoma, comprising administering to the mammal a therapeutically effective amount of a compound of Formula (I). The invention also relates to methods of manufacturing medicaments, which comprise one or more compounds of Formula (I). </p>
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TOPICAL FORMULATIONS FOR TREATING ALLERGIC DISEASES (Fri, 13 Jan 2006)
Methods for topically treating allergic diseases of the eye, ear or nose using tricyclic compounds are disclosed. </p>
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AMINO CYCLOPENTYL HETEROCYCLIC AND CARBOCYCLIC MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Fri, 06 Jan 2006)
Compounds of the formulae (I) and (II): (wherein Q, X, E, G1, G2, R2, R3, R4, R5, R6 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.
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AMINO CYCLOPENTYL HETEROCYCLIC AND CARBOCYCLIC MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Fri, 06 Jan 2006)
Compounds of the formulae (I) and (II): (wherein Q, X, E, G1, G2, R2, R3, R4, R5, R6 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>
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TETRAHYDROPYRANYL CYCLOPENTYL TETRAHY-DROPYRIDOPYRIDINE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Fri, 23 Dec 2005)
Compounds of Formula I (wherein n, R1, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, Y 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.
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TETRAHYDROPYRANYL CYCLOPENTYL TETRAHY-DROPYRIDOPYRIDINE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Fri, 23 Dec 2005)
Compounds of Formula I (wherein n, R1, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, Y 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>
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NITROGEN-CONTAINING HETEROCYCLIC DERIVATIVES AND DRUGS CONTAINING THE SAME AS THE ACTIVE INGREDIENT (Thu, 15 Dec 2005)
A compound represented by the following general formula (I), its salt, solvates thereof or prodrugs thereof: (I) (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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Triazaspiro[5.5]undecane derivatives and drugs comprising the same as the active ingredient (Fri, 02 Dec 2005)
<p id="p-0001-en" num="0000"> Compounds represented by formula (I) <chemistry id="chem-us-00001-en" num="1"><img id="emi-c00001" he="24.38mm" wi="69.85mm" file="US20050267114A1-20051201-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/></chemistry> (wherein all of the symbols have the same meanings as defined in specification.), quaternary ammonium salts thereof, N-oxides thereof or salts thereof. The compounds represented by formula (I) are used for prevention and/or treatment of various inflammatory diseases (asthma, nephritis, nephropathy, hepatitis, arthritis, chronic rheumatoid arthritis, rhinitis, conjunctivitis, ulcerative colitis and the like), immunologic diseases (autoimmune diseases, transplant rejection, immunosuppression, psoriasis, multiple sclerosis and the like), human immunodeficiency virus (acquired immunodeficiency syndrome and the like), allergic diseases (atopic dermatitis, nettle rash, allergic bronchopulmonary aspergillosis, allergic eosinophilic gastroenteritis and the like), ischemia-reperfusion injury, acute respiratory distress syndrome, shock accompanied by bacterial infection, diabetes mellitus, or metastasis and the like. </p>
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INDOLE DERIVATIVE COMPOUNDS AND DRUGS CONTAINING THE COMPOUNDS AS THE ACTIVE INGREDIENT (Thu, 01 Dec 2005)
An indole derivative compound represented by formula (I) <CHEM> (wherein the symbols in the formula are as mentioned in the specification) and a salt thereof Since the compounds represented by formula (I) binds to PGD2 receptors and shows antagonistic activity, they are believed to be useful for prevention and/or treatment of diseases such as allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, systemic mast cell activating disorder, anaphylaxis shock, airway contraction, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis, urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleep disorder) 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, autoimmune disease, chronic articular rheumatism, pleuritis, ulcerative colitis and irritable bowel syndrome.
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Piperizinones as modulators of chemokine receptor activity (Fri, 25 Nov 2005)
<p id="p-0001-en" num="0000">The present application describes modulators of CCR3 of formula (I):</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="21.00mm" wi="60.96mm" file="US07514430-20090407-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases. </p>
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TETRAHYDROPYRANYL CYCLOPENTYL 1-SUBSTITUTED AND 1,1-DISUBSTITUTED TETRAHYDROISOQUINOLINE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Fri, 25 Nov 2005)
Compounds of Formula I: I (wherein n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, Y 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.
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TETRAHYDROPYRANYL CYCLOPENTYL 1-SUBSTITUTED AND 1,1-DISUBSTITUTED TETRAHYDROISOQUINOLINE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Fri, 25 Nov 2005)
Compounds of Formula I: I (wherein n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, Y 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>
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PYRIMIDINE DERIVATIVES (Thu, 17 Nov 2005)
The present invention provides a pyrimidine derivative represented by Formula (I) <CHEM> Äwherein Ar represents substituted or unsubstituted aryl, etc., R<1> represents -NR<2>R<3> (wherein R<2> represents a hydrogen atom or substituted or unsubstituted lower alkyl and R<3> represents substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl, etc.), etc. A represents a single bond, Formula (III) <CHEM> (wherein m<1> represents an integer of 0 to 2, n<1> represents an integer of 0 to 4, a<1> represents a number ranging from 0 to a substitutable number, R<5> represents substituted or unsubstituted lower alkyl, etc. and each R<5> may be the same or different when a<1> is 2 or more), etc. and Q represents -NR<6>R<7> (wherein R<6> and R<7> may be the same or different and each represents a hydrogen atom, a substituted or unsubstituted heteroalicyclic group, etc.), a substituted or unsubstituted heteroalicyclic group, substituted or unsubstituted piperidin-4-ylamino, etc.Ü, or quaternary ammonium salts thereof, or pharmaceutically acceptable salts thereof which have anti-inflammatory activities, modulating activities on TARC and/or MDC functions and the like, and are useful for treating and/or preventing diseases which is related to T cells such as allergic diseases, autoimmune diseases, transplant rejection, etc.
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3,3-DISUBSTITUTED TETRAHYDROPYRANYL CYCLOPENTYL AMIDE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Fri, 11 Nov 2005)
Compounds of Formula I (wherein n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, Y 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.
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3,3-DISUBSTITUTED TETRAHYDROPYRANYL CYCLOPENTYL AMIDE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY (Fri, 11 Nov 2005)
Compounds of Formula I (wherein n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, Y 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>
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Use of compounds having ccr antagonism (Fri, 04 Nov 2005)
<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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THERAPEUTIC HEPARINS AND THEIR BINDING TO INTERLEUKINS 4 AND 5, AND PECAM-1 (Fri, 28 Oct 2005)
The present invention relates generally to chemical agents 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. More particularly, the chemical agents contemplated by the present invention are selected from glycosaminoglycan (GAG) molecules derived from a larger GAG, GAG-like molecules which resemble GAGs in some of their characteristics but may be derived from a larger non-GAG polysaccharide and molecules having a GAG-like composite structure as well as agents which bind to the same sites as GAGs, GAG-like molecules or GAG-like composite molecules. The present invention also provides assays to identify GAG and GAG-like therapeutic agents including GAG-like composite structures as well as analogs, homologs and orthologs thereof.
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CONDENSED PYRIDINE DERIVATIVES USEFUL AS A28 ADENOSINE RECEPTOR ANTAGONISTS (Fri, 28 Oct 2005)
The present invention relates to new antagonists of the A2B adenosine receptor represented by formula (I). Those compounds are useful for treating a subject afflicted with a pathological condition or disease susceptible to amelioration by antagonism of the A2B adenosine receptor such as asthma, bronchoconstriction, allergic diseases, hypertension, atherosclerosis, reperfusion injury, myocardial ischemia, retinopathy, inflammation, gastrointestinal tract disorders, cell proliferation disorders, diabetes mellitus, and/or autoimmune diseases.
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THERAPEUTIC HEPARINS AND THEIR BINDING TO INTERLEUKINS 4 AND 5, AND PECAM-1 (Fri, 28 Oct 2005)
The present invention relates generally to chemical agents 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. More particularly, the chemical agents contemplated by the present invention are selected from glycosaminoglycan (GAG) molecules derived from a larger GAG, GAG-like molecules which resemble GAGs in some of their characteristics but may be derived from a larger non-GAG polysaccharide and molecules having a GAG-like composite structure as well as agents which bind to the same sites as GAGs, GAG-like molecules or GAG-like composite molecules. The present invention also provides assays to identify GAG and GAG- like therapeutic agents including GAG-like composite structures as well as analogs, homologs and orthologs thereof. </p>
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