ENGINEERED ANTI-TSLP ANTIBODY (Fri, 23 May 2014)
<p id="p-0001" num="0000">The invention relates to binding compounds that specifically bind to human TSLP, as well as uses thereof, e.g., in the treatment of inflammatory disorders.</p>
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ALDOSTERONE SYNTHASE INHIBITORS (Fri, 14 Feb 2014)
<p id="p-0001" num="0000">This invention relates to tricyclic triazole analogues of the formula I or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthetase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthetase.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="33.95mm" wi="61.47mm" file="US20140045819A1-20140213-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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BIOMARKERS FOR PSORIASIS (Fri, 25 Oct 2013)
<p id="p-0001" num="0000">A group of polypeptides that are modulated in a psoriatic sample as compared to a normal sample is provided. These polypeptides can be used as biomarkers for diagnosis and monitoring treatment of psoriasis.</p>
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Compuestos antagonistas del receptor de glucagón, composiciones que contienen dichos compuestos y su uso farmacéutico (Fri, 09 Nov 2012)

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Compuestos antagonistas del receptor de glucagón, composiciones que contienen dichos compuestos y su uso farmacéutico (Fri, 09 Nov 2012)
Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included. (I)
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Method for blocking binding of CX3C chemokines using CX3C chemokine antibodies (Fri, 07 Sep 2012)
<p id="p-0001" num="0000">Nucleic acids encoding a new family of chemokines, the CX3C family, from a mammal, reagents related thereto, including specific antibodies, and purified proteins are described. Methods of using said reagents and related diagnostic kits are also provided.</p>
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5-AMINO-{PYRAZOLO-[4,3-e]-1,2,4-TRIAZOLO[1,5-c]PYRIMIDINE}-2- AND 7-SUBSTITUTED DERIVATIVES AS ADENOSINE A2A RECEPTOR INHIBITORS (Wed, 01 Aug 2012)

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Exo-selective synthesis of himbacine analogs (Fri, 08 Jun 2012)
<p id="p-0001" num="0000">This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists. The chemistry disclosed herein is exemplified in the following synthesis sequence:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="89.32mm" wi="75.78mm" file="US08273790-20120925-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Peptides as NS3-serine protease inhibitors of hepatitis C virus (Wed, 04 Apr 2012)
<p id="p-0001" num="0000">The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.</p>
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NOVEL HETEROCYCLIC COMPOUNDS AS ERK INHIBITORS (Fri, 30 Dec 2011)
The present invention provides a compound of the Formula I:(Formular I should be inserted here) or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2 and R3 are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.
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PENTAFLUOROSULPHOLANE-CONTAINING ANTIDIABETIC COMPOUNDS (Fri, 23 Dec 2011)
<p id="p-0001" num="0000">This invention provides for certain pentafluorosulpholane-containing compounds of the formula or a pharmaceutically acceptable salt, ester, solvate or prodrug thereof, wherein the variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="24.81mm" wi="60.20mm" file="US20110313008A1-20111222-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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BRIDGED AND FUSED HETEROCYCLIC ANTIDIABETIC COMPOUNDS (Fri, 23 Dec 2011)
<p id="p-0001" num="0000">This invention provides for certain bridged and fused heterocyclic compounds of the formula (I) or a pharmaceutically acceptable salt, ester solvate or prodrug thereof wherein: L is: (II) and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="49.02mm" wi="69.85mm" file="US20110312995A1-20111222-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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BRIDGED AND FUSED ANTIDIABETIC COMPOUNDS (Fri, 23 Dec 2011)
<p id="p-0001" num="0000">This invention provides for certain bridged and fused compounds of the formula G-L-A I or a pharmaceutically acceptable salt, ester of solvate thereof wherein: A is: (I) and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="22.10mm" wi="56.47mm" file="US20110312967A1-20111222-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Inhibitors of diacylglycerol acyltransferase (Thu, 15 Dec 2011)
The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase ('DGAT') inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below.
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DEUTERATED COMPOUNDS AS HEPATITIS C VIRUS (HCV) INHIBITORS (Fri, 25 Nov 2011)
<p id="p-0001" num="0000">The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as wet! as methods of using them to treat disorders associated with the HCV protease An illustrative inventsve compound is shown below: Formula (I).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="47.07mm" wi="75.78mm" file="US20110286969A1-20111124-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Exo- and diastereo- selective synthesis of himbacine analogs (Fri, 14 Oct 2011)
<p id="p-0001" num="0000">This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center. The chemistry taught herein can be exemplified by the following:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="76.79mm" wi="75.86mm" file="US08258319-20120904-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Nucleic acids encoding DCRS5 (Fri, 07 Oct 2011)
<p id="p-0001" num="0000">Nucleic acids encoding mammalian, e.g., primate, receptors, purified receptor proteins and fragments thereof. Antibodies, both polyclonal and monoclonal, are also provided. Methods of using the compositions for both diagnostic and therapeutic utilities are described.</p>
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Bicyclic compounds as inhibitors of diacylglycerol acyltransferase (Fri, 16 Sep 2011)
The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase ("DGAT") inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below (I).
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Heterocyclic aspartyl protease inhibitors (Fri, 09 Sep 2011)
<p id="p-0001" num="0000">Disclosed are compounds of the formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.56mm" wi="47.16mm" file="US08242112-20120814-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, <br/> wherein <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">W is a bond, —C(═S)—, —S(O)—, —S(O)<sub>2</sub>—, —C(═O)—, —O—, —C(R<sup>6</sup>)(R<sup>7</sup>)—, —N(R<sup>5</sup>)— or —C(═N(R<sup>5</sup>))—;</li> <li id="ul0002-0002" num="0000">X is —O—, —N(R<sup>5</sup>)— or —C(R<sup>6</sup>)(R<sup>7</sup>)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)<sub>2</sub>—, —C(═O)— or —C(═NR<sup>5</sup>)—;</li> <li id="ul0002-0003" num="0000">U is a bond, —S(O)—, —S(O)<sub>2</sub>—, —C(O)—, —O—, —P(O)(OR<sup>15</sup>)—, —C(═NR<sup>5</sup>)—, —(C(R<sup>6</sup>)(R<sup>7</sup>))<sub>b</sub>— or —N(R<sup>5</sup>)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)<sub>2</sub>—, —O—, or —N(R<sup>5</sup>)—, U is not —S(O)—, —S(O)<sub>2</sub>—, —O—, or —N(R<sup>5</sup>)—; provided that when X is —N(R<sup>5</sup>)— and W is —S(O)—, —S(O)<sub>2</sub>—, —O—, or —N(R<sup>5</sup>)—, then U is not a bond;</li> <li id="ul0002-0004" num="0000">and R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>6</sup>, and R<sup>7 </sup>are as defined in the specification; <br/> and pharmaceutical compositions comprising the compounds of formula I. </li> </ul> </li> </ul> </p> <p id="p-0003" num="0000">Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes.</p> <p id="p-0004" num="0000">Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m<sub>1 </sub>agonist or m<sub>2 </sub>antagonist.</p>
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3,4-Di-Substituted Cyclobutene-1,2-Diones as CXC-Chemokine Receptor Ligands (Fri, 02 Sep 2011)
<p id="p-0001" num="0000">There are disclosed compounds of the formula</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="20.15mm" wi="69.85mm" file="US20110213029A1-20110901-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.</p>
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IL-1-like cytokine antibodies (Fri, 12 Aug 2011)
<p id="p-0001" num="0000">Nucleic acids encoding mammalian, e.g., primate, IL-1ζ, purified IL-1ζ polypeptides and fragments thereof. Binding proteins, e.g., antibodies, both polyclonal and monoclonal, are also provided. Methods of using the compositions for both diagnostic and therapeutic utilities are provided.</p>
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CYCLOPROPYLCHROMENE DERIVATIVES AS MODULATORS OF THE ALPHA-2C RECEPTOR (Fri, 05 Aug 2011)
<p id="p-0001" num="0000">In its many embodiments, the present invention provides a novel class of cyclopropylchromene derivatives as modulators of a2C adrenergic receptor, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the a2C adrenergic receptors using such compounds or pharmaceutical compositions.</p>
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Mouse CX3C chemokine polypeptides (Fri, 05 Aug 2011)
<p id="p-0001" num="0000">Nucleic acids encoding a new family of chemokines, the CX3C family, from a mammal, reagents related thereto, including specific antibodies, and purified proteins are described. Methods of using said reagents and related diagnostic kits are also provided.</p>
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Mammalian Cytokines; Related Reagents and Methods (Fri, 22 Jul 2011)
<p id="p-0001" num="0000">Purified genes encoding cytokine from a mammal, reagents related thereto including purified proteins, specific antibodies, and nucleic acids encoding this molecule are provided. Methods of using said reagents and diagnostic kits are also provided.</p>
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Nucleic acid encoding TNFx protein (Fri, 08 Jul 2011)
<p id="p-0001" num="0000">Nucleic acids encoding mammalian, e.g., primate or rodent, genes, purified proteins and fragments thereof. Antibodies, both polyclonal and monoclonal, are also provided. Methods of using the compositions for both diagnostic and therapeutic utilities are provided.</p>
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Engineered Anti-IL-23R Antibodies (Fri, 01 Jul 2011)
<p id="p-0001" num="0000">Antibodies to human IL-23R are provided, as well as uses thereof, e.g. in treatment of inflammatory, autoimmune, and proliferative disorders.</p>
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Factor IXa crystals, related complexes and methods (Wed, 29 Jun 2011)
<p id="p-0001" num="0000">The present invention relates to factor IXa complexes and crystals thereof as well as methods for identifying inhibitors of factor IXa.</p>
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1,2,4-triazolo[4,3-c]pyrimidin-3-one and pyrazolo[4,3-e]-1,2,4-triazolo[4,3-c]pyrimidin-3-one compounds for use as adenosine A<sub>2a </sub>receptor antagonists (Fri, 24 Jun 2011)
<p id="p-0001" num="0000">Compounds of the Formula I wherein R<sup>1 </sup>and R<sup>2 </sup>together with the carbon atoms to which they are bonded optionally form a further heteroaromatic ring of the formula (II) as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof are adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="51.73mm" wi="55.37mm" file="US08222259-20120717-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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FUSED TRICYCLIC COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS (Fri, 24 Jun 2011)
The present invention relates to certain lactam ring-containing compounds of the Formula (I) and pharmaceutically acceptable salts thereof, wherein D, E, X1, R1, R2, R3, R4, R9, and R10 are as herein described. In addition, the invention relates to pharmaceutically acceptable compositions comprising at least one such compound, and methods of using the compounds for treating or preventing various inflammatory disorders such as rheumatoid arthritis, inflammatory bowel disease, psoriasis, asthma, and chronic obstructive pulmonary disorder.
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PROCESS FOR THE SYNTHESIS OF AZETIDINONES (Fri, 17 Jun 2011)
<p id="p-0001" num="0000">A process is provided for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, comprising reacting a β-(substituted-amino)amide, a β-(substituted-amino)acid ester, or a β-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent selected from the group consisting of alkali metal carboxylates, quaternary ammonium carboxylates, quaternary ammonium hydroxides, quaternary ammonium alkoxides, quaternary ammonium aryloxides and hydrates thereof, or the reaction product of: (i) at least one quaternary ammonium halide and at least one alkali metal carboxylate; or (ii) at least one quaternary ammonium chloride, quaternary ammonium bromide, or quaternary ammonium iodide and at least one alkali metal fluoride, wherein a quaternary ammonium moiety of the cyclizing agent is unsubstituted or substituted by one to four groups independently selected from the group consisting of alkyl, arylalkyl and arylalkyl-alkyl.</p>
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Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents (Wed, 15 Jun 2011)
<p id="p-0001" num="0000">Hydroxy-substituted azetidinone hypocholesterolemic agents of the formula</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="21.42mm" wi="55.20mm" file="USRE042461-20110614-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a pharmaceutically acceptable salt thereof, wherein: <br/> Ar<sup>1 </sup>and Ar<sup>2 </sup>are aryl or R<sup>4</sup>-substituted aryl; <br/> Ar<sup>3 </sup>is aryl or R<sup>5</sup>-substituted aryl; <br/> X, Y and Z are —CH<sub>2</sub>—, —CH(lower alkyl)— or —C(dilower alkyl)—; <br/> R and R<sup>2 </sup>are —OR<sup>6</sup>, —O(CO)R<sup>6</sup>, —O(CO)OR<sup>9 </sup>or —O(CO)NR<sup>6</sup>R<sup>7</sup>; <br/> R<sup>1 </sup>and R<sup>3 </sup>are H or lower alkyl; <br/> q is 0 or 1; r is 0 or 1; m, n and p are 0-4; provided that at least one of q and r is 1, and the sum of m, n, p, q and r is 1-6; and provided that when p is O and r is 1, the sum of m, q and n is 1-5; <br/> R<sup>4 </sup>is selected from lower alkyl, R<sub>5</sub>, —CF<sub>3</sub>, —CN, —NO<sub>2 </sub>and halogen R<sup>5 </sup>is selected from —OR<sup>6</sup>, —O(CO)R<sup>6</sup>, —O(CO)OR<sup>9</sup>, —O(CH<sub>2</sub>)<sub>1-5</sub>OR<sup>6</sup>, —O(CO)NR<sup>6</sup>R<sup>7</sup>, —NR<sub>6</sub>R<sup>7</sup>, —NR<sup>6</sup>(CO)R<sup>7</sup>, —NR<sup>6</sup>(CO)OR<sup>9</sup>, —NR<sup>6</sup>(CO)NR<sup>7</sup>R<sup>8</sup>, —NR<sup>6</sup>SO<sub>2</sub>R<sup>9</sup>, —COOR<sup>6</sup>, —CONR<sup>6</sup>R<sup>7</sup>, —COR<sup>6</sup>, —SO<sub>2</sub>NR<sup>6</sup>R<sup>7</sup>, S(O)<sub>0-2</sub>R<sup>9</sup>, —O(CH<sub>2</sub>)<sub>1-10</sub>—COOR<sup>6</sup>, —O(CH<sub>2</sub>)<sub>1-10</sub>CON<sup>6</sup>R<sup>7</sup>, —(lower alkylene)COOR<sup>6 </sup>and —CH═CH—COOR<sup>6</sup>; <br/> R<sup>6</sup>, R<sup>7 </sup>and R<sup>8 </sup>are H, lower alkyl or aryl-substituted Ic <br/> R<sup>9 </sup>is lower alkyl, aryl or aryl-substituted lower alkyl; <br/> are disclosed, as well as a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor, pharmaceutical compositions containing them; and a process for preparing them. </p>
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IL-D80 polynucleotides (Fri, 10 Jun 2011)
<p id="p-0001" num="0000">Purified genes encoding a cytokine or composite cytokine from a mammal, reagents related thereto including purified proteins, specific antibodies, and nucleic acids encoding these molecules are provided. Methods of using said reagents and diagnostic kits are also provided.</p>
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FUSED TRICYCLIC COMPOUNDS AND DERIVATIVES THEREOF USEFUL FOR THE TREATMENT OF VIRAL DISEASES (Sat, 04 Jun 2011)
The present invention relates to novel fused tricyclic compounds, compositions comprising at least one fused tricyclic compound, and methods of using fused tricyclic compounds for treating or preventing a viral infection or a virus-related disorder in a patient.
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SUBSTITUTED BIARYL DERIVATIVES AND METHODS OF USE THEREOF (Sat, 04 Jun 2011)
The present invention relates to Substituted Biaryl Derivatives, compositions comprising a Substituted Biaryl Derivative, and methods of using the Substituted Biaryl Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.
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FUSED TRICYCLIC COMPOUNDS AND DERIVATIVES THEREOF USEFUL FOR THE TREATMENT OF VIRAL DISEASES (Sat, 04 Jun 2011)
The present invention relates to novel fused tricyclic compounds, compositions comprising at least one fused tricyclic compound, and methods of using fused tricyclic compounds for treating or preventing a viral infection or a virus-related disorder in a patient.</p>
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Mammalian receptor protein DCRS5; methods of treatment (Fri, 03 Jun 2011)
<p id="p-0001" num="0000">Nucleic acids encoding mammalian, e.g., primate, receptors, purified receptor proteins and fragments thereof. Antibodies, both polyclonal and monoclonal, are also provided. Methods of using the compositions for both diagnostic and therapeutic utilities are described.</p>
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Process and intermediates for the Synthesis of heterocyclic Substituted Piperazines with CXCR3 Antagonist Activity (Fri, 27 May 2011)
<p id="p-0001" num="0000">The present invention relates to novel processes for the preparation of the compound of the Formula A45:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="42.42mm" wi="75.86mm" file="US20110124867A1-20110526-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or a physiologically acceptable salt, solvate or prodrug thereof, which has utility, for example, as a pharmaceutically active compound with CXCR3 antagonist activity, and to novel intermediates useful in the synthesis thereof.</p>
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FUSED BICYCLIC PYRIMIDINE DERIVATIVES AND METHODS OF USE THEREOF (Fri, 27 May 2011)
The present invention relates to Fused Bicyclic Pyrimidine Derivatives, compositions comprising a Fused Bicyclic Pyrimidine Derivative, and methods of using the Fused Bicyclic Pyrimidine Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) in a patient.
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PYRIMIDINE ETHER DERIVATIVES AND METHODS OF USE THEREOF (Fri, 27 May 2011)
The present invention relates to Pyrimidine Ether Derivatives, compositions comprising a Pyrimidine Ether Derivative, and methods of using the Pyrimidine Ether Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) in a patient.
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Inhibitors of diacylglycerol acyltransferase (Fri, 27 May 2011)
The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase ("DGAT") inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown with this abstract.
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Inhibitors of diacylglycerol acyltransferase (Fri, 27 May 2011)
The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase ("DGAT") inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below.
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Anti-REG4 Antibodies (Fri, 20 May 2011)
<p id="p-0001" num="0000">Antibodies to human REG4 are provided, as well as uses thereof, e.g., in treatment of proliferative disorders. Also provided is a method of screening for an antibody that inhibits REG4 bioactivity.</p>
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NOVEL PEPTIDES AS NS3-SERINE PROTEASE INHIBITORS OF HEPATITIS C VIRUS (Fri, 20 May 2011)
<p id="p-0001" num="0000">The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.</p>
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COMPOUNDS USEFUL AS CHEMOKINE RECEPTOR ANTAGONISTS (Fri, 20 May 2011)
The present invention relates to a compound having the general Formula I: Formula I wherein the variables are as defined in the specification. The present invention further relates to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular for the treatment or prevention of chemokine-mediated disorders such as HIV infection.
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SUBSTITUTED AMINO HETEROCYCLES USEFUL AS HIV ANTAGONISTS (Fri, 20 May 2011)
The present invention relates to compounds of Formula (I): wherein the variables are as defined in the specification. The present invention further relates to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular for the treatment or prevention of chemokine-mediated disorders such as HIV infection.
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CYCLIC UREAS USEFUL AS HIV INHIBITORS (Fri, 20 May 2011)
The present invention relates to a compound having the general Formula (I), wherein the variables are as defined in the specification. The present invention further relates to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular for the treatment or prevention of chemokine-mediated disorders such as HIV infection.
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ALIPHATIC AMINES BASED HETEROCYCLES USEFUL AS HIV ENTRY BLOCKERS (Fri, 20 May 2011)
The present invention relates to a compound of Formula I: Formula I, wherein the variables are as defined in the specification. The present invention further relates to pharmaceutical compositions comprising the compound and to its use in therapy, in particular for the treatment or prevention of chemokine-mediated disorders such as HIV infection.
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BENZENESULFONYL-CHROMANE, THIOCHROMANE, TETRAHYDRONAPHTHALENE AND RELATED GAMMA SECRETASE INHIBITORS (Fri, 13 May 2011)
<p id="p-0001" num="0000">Disclosed are novel gamma secretase inhibitors of the formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, wherein L<sup>1</sup>, n, X, Ar, Y, Z, Q, and Q<sup>1 </sup>are as defined herein. Also disclosed are methods for inhibiting gamma secretase, methods for treating Alzheimer's disease, methods of treating one or more neurodegenerative diseases, and methods of inhibiting the deposition of amyloid protein (e.g., amyloid beta protein) in, on or around neurological tissue (e.g., the brain) using the compounds of formula 1.0.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="42.08mm" wi="76.20mm" file="US20110110948A1-20110512-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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BRIDGED BICYCLIC PIPERIDINE DERIVATIVES AND METHODS OF USE THEREOF (Fri, 06 May 2011)
The present invention relates to Bridged Bicyclic Piperidine Derivatives, compositions comprising a Bridged Bicyclic Piperidine Derivative, and methods of using the Bridged Bicyclic Piperidine Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.
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BRIDGED BICYCLIC PIPERIDINE DERIVATIVES AND METHODS OF USE THEREOF (Fri, 06 May 2011)
The present invention relates to Bridged Bicyclic Piperidine Derivatives, compositions comprising a Bridged Bicyclic Piperidine Derivative, and methods of using the Bridged Bicyclic Piperidine Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.</p>
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Pyrrolidine, piperidine and piperazine derivatives and methods of use thereof (Fri, 29 Apr 2011)
The present invention relates to novel Pyrrolidine, Piperidine and Piperazine Derivatives, pharmaceutical compositions comprising the Pyrrolidine, Piperidine and Piperazine Derivatives and the use of these compounds for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disoder, a metabolic disorder, obesity, an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
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APRIL ANTAGONISTS AND METHODS OF USE (Fri, 22 Apr 2011)
The present invention provides antagonists of APRIL. In particular, the APRIL antagonists block unique receptor binding sited on APRIL, BCMA. TACI, and/or HSPG. Also provided are methods of use.
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SUBSTITUTED PIPERIDINES THAT INCREASE p53 ACTIVITY AND THE USES THEREOF (Fri, 22 Apr 2011)
The present invention provides a compound of Formula (1) as described herein or a pharmaceutically acceptable salt, solvate or ester thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.
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SUBSTITUTED PIPERIDINES THAT INCREASE P53 ACTIVITY AND THE USES THEREOF (Fri, 22 Apr 2011)
<br/> The present invention provides a compound of Formula 1<br/>(see formula 1)<br/>as described herein or a pharmaceutically acceptable salt, solvate or ester <br/>thereof. The representative compounds are useful as inhibitors of the HDM2 <br/>protein. Also disclosed are pharmaceutical compositions comprising the above <br/>compounds and potential methods of treating cancer using the same.<br/></p>
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INHIBITORS OF FATTY ACID BINDING PROTEIN (FABP) (Fri, 15 Apr 2011)
The present invention relates to novel heterocyclic compounds as Fatty Acid Binding Protein (FABP) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the present invention is shown below:
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IMINOTHIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE (Fri, 15 Apr 2011)
In its many embodiments, the present invention provides provides certain iminothiadiazine dioxide compounds, including compounds Formula (a) and include tautomers, solvates, prodrugs, esters, and deuterates thereof, and pharmaceutically acceptable salts of said compounds, tautomers, solvates, prodrugs, esters, and deuterates, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, ring C, m, n, p, q, -L1-, -L2-,L3-, and L4- is selected independently and as defined herein. The compounds of the invention have, surprisingly and advantageously, improved solution stability. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimers Disease, are also disclosed.
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PENTAFLUOROSULFUR IMINO HETEROCYCLIC COMPOUNDS AS BACE-1 INHIBITORS, COMPOSITIONS, AND THEIR USE (Fri, 15 Apr 2011)
In its many embodiments, the present invention provides certain pentafluorosulfur imino heterocyclic compounds, including compounds Formula (a) and pharmaceutically acceptable salts thereof. Compounds of Formula(a) have the general structure: (a) wherein each variable is selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimers Disease, are also disclosed.
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PENTAFLUOROSULFUR IMINO HETEROCYCLIC COMPOUNDS AS BACE-1 INHIBITORS, COMPOSITIONS, AND THEIR USE (Fri, 15 Apr 2011)
In its many embodiments, the present invention provides provides certain pentafluorosulfur imino heterocyclic compounds, including compounds Formula (I): and tautomers thereof, and solvates, prodrugs, esters, and deuterates of said compounds and said tautomers, and pharmaceutically acceptable salts of said compounds, tautomers, solvates, prodrugs, esters, and deuterates, wherein each of R1, R2, R3, R4, R5, R9, R11, ring A, ring B, m, n, p, q, r, -L1-,L2-, and L3- is selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimers Disease, are also disclosed.
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Spiro-imidazolone derivatives as glucagon receptor antagonists (Fri, 15 Apr 2011)
The present invention relates to compounds of the general formula: (I) wherein ring A, ring B, R<sp>1</sp>, R<sp>3</sp>, Z, L<sp>1</sp>, and L<sp>2</sp> are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
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REVERSED BIARYL SPIROAMINOOXAZOLINE ANALOGUES AS ALPHA2C ADRENERGIC RECEPTOR MODULATORS (Fri, 08 Apr 2011)
In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.
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NOVEL COMPOUNDS THAT ARE ERK INHIBITORS (Fri, 08 Apr 2011)
Disclosed are the ERK inhibitors of formula 1.0: (Formula (A1)), and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine ring that can have a bridge or a fused ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula A1.
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NOVEL COMPOUNDS THAT ARE ERK INHIBITORS (Fri, 08 Apr 2011)
Disclosed are the ERK inhibitors of formula 1.0: (Formula (A1)), and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine ring that can have a bridge or a fused ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula A1.</p>
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NOVEL PYRROLIDINES AS GLUCAGON RECEPTOR ANTAGONISTS, COMPOSITIONS, AND METHODS FOR THEIR USE (Fri, 01 Apr 2011)
The present invention relates to compounds of the general formula: (I) wherein ring B, R1, R2, R3, Z, and L1 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
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Heterocyclic substituted piperazines with CXCR3 antagonist activity (Fri, 18 Mar 2011)
<p id="p-0001" num="0000">The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="39.88mm" wi="71.20mm" file="US08207170-20120626-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a pharmaceutically acceptable salt, solvate or ester thereof, wherein the various moieties are defined herein. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1. </p>
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Heterocyclic compounds as factor IXA inhibitors (Fri, 18 Mar 2011)
<p id="p-0001" num="0000">The present invention relates to novel heterocyclic compounds of Formulae I-III; as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="78.32mm" wi="69.85mm" file="US08148363-20120403-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE (Fri, 18 Mar 2011)
The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (DGAT) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below:
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MODULATORS OF CELL CYCLE CHECKPOINTS AND THEIR USE IN COMBINATION WITH CHECKPOINT KINASE INHIBITORS (Fri, 11 Mar 2011)
In its many embodiments, the present invention provides a novel class of pyrimidine analogs as targeted mechanism-based modulators of cell cycle checkpoints. Cancers and/or malignancies can be treated by administration of a cell cycle checkpoint modulator of the invention. Also discussed are suitable combinations of the cell cycle checkpoint modulator with a checkpoint kinase inhibitor to produce synergistic apoptosis in cancer cells. The invention also includes methods of treating cancers by administering the combination of the cell cycle checkpoint modulator and the checkpoint kinase inhibitor, pharmaceutical compositions comprising the cell cycle checkpoint modulator as well as combinations and pharmaceutical kits. An example cell cycle checkpoint modulator is shown below: formula (I).
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ANTI-GITR ANTIBODIES (Fri, 11 Mar 2011)
Antibodies to human GITR are provided, as well as uses thereof, e.g., in treatment of proliferative and immune disorders.
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ANTI-GITR ANTIBODIES (Fri, 11 Mar 2011)
Antibodies to human GITR are provided, as well as uses thereof, e.g., in treatment of proliferative and immune disorders.</p>
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HETEROCYCLIC AMIDE COMPOUNDS AS PROTEIN KINASE INHIBITORS (Fri, 04 Mar 2011)
The present invention relates to heterocyclic amide derivatives of Formula (I): Formula (I) wherein the variables are as defined in the specification. The present invention further relates to compositions comprising said heterocyclic amide derivatives of formula (I) and methods for using said heterocyclic amide derivatives of formula (I) for treating or preventing a disease or disorder related to the activity of a protein kinase, in particular, a proliferative disease, an anti-proliferative disorder, inflammation, arthritis, a neurological or neurodegenerative disease, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease or a fungal infection.
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MORPHOLINONE COMPOUNDS AS FACTOR IXA INHIBITORS (Fri, 04 Mar 2011)
The present invention provides compounds having the formula (I) or a pharmaceutically acceptable salt or a solvate thereof, pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes.
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MORPHOLINONE COMPOUNDS AS FACTOR IXA INHIBITORS (Fri, 04 Mar 2011)
The present invention provides compounds having the formula (I) or a pharmaceutically acceptable salt or a solvate thereof, pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes.</p>
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2,3-substituted indole derivatives for treating viral infections (Fri, 11 Feb 2011)
<p id="p-0001" num="0000">The present invention relates to 2,3-Substituted Indole Derivatives, compositions comprising at least one 2,3-Substituted Indole Derivative, and methods of using the 2,3-Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.</p>
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PROCESS FOR PREPARING A 2-ALKYNYL SUBSTITUTED 5-AMINO-PYRAZOLO-[4,3-e]-1,2,4-TRIAZOLO[1,5-c]PYRIMIDINE (Fri, 11 Feb 2011)
A process for preparing 7-[2-[4-(6-fluoro -3-methyl -1,2-benzisoxazol-5-yl)-1-piperazinyl]ethyl]-2-(1-propynyl)-7H-pyrazolo-[4,3-e]-[1,2,4]-triazolo[1,5-c]pyrimidin-5-amine, intermediates useful in that process, and processes for preparing said intermediates are disclosed.
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4, 5, 6-TRISUBSTITUTED PYRIMIDINE DERIVATIVES AS FACTOR IXA INHIBITORS (Fri, 11 Feb 2011)
The present invention relates to novel heterocyclic compounds of Formulae (I): (Chemical formula should be inserted here as it appears on abstract in paper form) Formula (I) as disclosed herein, or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder.
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Human Receptor Proteins; Related Reagents and Methods (Fri, 28 Jan 2011)
<p id="p-0001" num="0000">Nucleic acids encoding mammalian, e.g., primate or rodent receptors, purified receptor proteins and fragments thereof. Antibodies, both polyclonal and monoclonal, are also provided. Methods of using the compositions for both diagnostic and therapeutic utilities are provided.</p>
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BENZO-FUSED OXAZEPINE COMPOUNDS AS STEAROYL-COENZYME A DELTA-9 DESATURASE INHIBITORS (Fri, 28 Jan 2011)
The present invention relates to certain 4,5-dihydro-3H-spiro[benzo[b]-[1,4]oxazepine compounds of the Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, m, n, o, and p are as herein described. In addition, the invention relates to compositions comprising at least one such compound, and methods of using the compounds for treating or preventing disorders such as non-insulin dependent (Type 2) diabetes, insulin resistance, hyperglycemia, a lipid disorder, obesity, fatty liver disease, or a skin disorder.
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BENZO-FUSED OXAZEPINE COMPOUNDS AS STEAROYL-COENZYME A DELTA-9 DESATURASE INHIBITORS (Fri, 28 Jan 2011)
The present invention relates to certain 4,5-dihydro-3H-spiro[benzo[b]-[1,4]oxazepine compounds of the Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, m, n, o, and p are as herein described. In addition, the invention relates to compositions comprising at least one such compound, and methods of using the compounds for treating or preventing disorders such as non-insulin dependent (Type 2) diabetes, insulin resistance, hyperglycemia, a lipid disorder, obesity, fatty liver disease, or a skin disorder.</p>
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Bicyclic heterocycle derivatives and their use as GPCR modulators (Fri, 28 Jan 2011)
The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient.
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Bicyclic Heterocycle Derivatives and methods of use thereof (Fri, 21 Jan 2011)
The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient. The compounds are of structure (I).
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Bicyclic Heterocycle Derivatives and use thereof as GPR119 modulators (Fri, 21 Jan 2011)
The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) such as GPR119 in a patient.
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METHODS OF TREATING COPD (Fri, 14 Jan 2011)
<p id="p-0001" num="0000">Disclosed is a method of treating chronic obstructive disease, said method comprising administering an effective amount of a CXCR2 antagonist and administering an effective amount of at least one drug selected from the group consisting of: angiotensin-converting enzyme inhibitors, Angiotensin II receptor antagonists, cardioselective beta blockers, and lipid regulating drugs. Examples of the CXCR2 antagonist include: (formula 1.0A and 1.0B).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="65.53mm" wi="73.66mm" file="US20110009482A1-20110113-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p>
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HYDROGEN CHLORIDE SALT OF A SUBSTITUTED 5-OXAZOL-2-YL-QUINOLINE COMPOUND AND A PROCESS FOR THE PRODUCTION THEREOF (Fri, 07 Jan 2011)
<p id="p-0001" num="0000">The present invention relates to the compound of the Formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="51.39mm" wi="68.92mm" file="US20110003780A1-20110106-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">and to methods of treating upper and lower obstructive airway diseases using said compound, to formulations comprising it, and to a particular crystalline form and processes of synthesis of the crystalline form.</p> <p id="p-0004" num="0000">IM=105109</p>
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Engineered Anti-IL-23 Antibodies (Fri, 07 Jan 2011)
<p id="p-0001" num="0000">Engineered antibodies to human IL-23p19 are provided, as well as uses thereof, e.g. in treatment of inflammatory, autoimmune, and proliferative disorders.</p>
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FUSED TRICYCLIC COMPOUNDS AS NOVEL mTOR INHIBITORS (Fri, 07 Jan 2011)
The present invention provides Fused Tricyclic Compounds of the Formula (I) wherein Q, R1, R2, R3, and R4 are as defined herein, and pharmaceutically acceptable salts of such Fused Tricyclic Compounds. The Fused Tricyclic Compounds are useful in the treatment of cancer and other proliferative disorders.
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METHODS FOR USING PYRROLO-BENZO-1,4-DIAZINES AS SODIUM CHANNEL BLOCKERS (Thu, 30 Dec 2010)
Pyrrolo-benzo-1,4-diazine compounds represented by Formula I or II, or pharmaceutically acceptable salts thereof, are blockers of voltage-gated sodium channels. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, voltage-gated sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy or epilepsy conditions, irritable bowel syndrome, depression, anxiety, bipolar disorder, neurodegenerative disorders, psychiatric disorders, myotonia, arrhythmia, movement disorders, neuroendocrine disorders, ataxia, multiple sclerosis, irritable bowel syndrome, incontinence, neuropathy and tinnitus, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
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PYRROLO-BENZO-1,4-DIAZINES USEFUL AS SODIUM CHANNEL BLOCKERS (Thu, 30 Dec 2010)
Pyrrolo-benzo-1,4-diazine compounds represented by Formula I or II, or pharmaceutically acceptable salts thereof, are blockers of voltage-gated sodium channels. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, voltage-gated sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy or epilepsy conditions, irritable bowel syndrome, depression, anxiety, bipolar disorder, neurodegenerative disorders, psychiatric disorders, myotonia, arrhythmia, movement disorders, neuroendocrine disorders, ataxia, multiple sclerosis, irritable bowel syndrome, incontinence, neuropathy and tinnitus, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
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PROCESS FOR THE PRODUCTION OF SUBSTITUTED 5-QUINOLYL-OXAZOLES AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF (Fri, 24 Dec 2010)
<p id="p-0001-en" num="0000">The present invention relates a process for the preparation of a compound of the formula:</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="43.86mm" wi="35.73mm" file="US20100324295A1-20101223-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003-en" num="0000">wherein R<sub>1</sub>, R<sub>2</sub>, R<sub>6</sub>, R<sub>9 </sub>and R<sub>10 </sub>are as described herein. The compounds are inhibitors of phosphodiesterase 4 (PDE4).</p>
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ANTIVIRAL COMPOUNDS COMPOSED OF THREE LINKED ARYL MOIETIES TO TREAT DISEASES SUCH AS HEPATITIS C (Fri, 03 Dec 2010)
The present invention relates to novel Linked Tricyclic Aryl Compounds, compositions comprising at least one Linked Tricyclic Compound, and methods of using Linked Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient. in one aspect, the present invention provides Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein: Non-limiting examples of the Compounds of Formula (II) include compound 56
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ANTIVIRAL COMPOUNDS COMPOSED OF THREE ALIGNED ARYL MOIETIES TO TREAT DISEASES SUCH AS HEPATITIS C (Fri, 03 Dec 2010)
The present invention relates to novel Tricyclic Compounds, compositions comprising at least one Tricyclic Compound, and methods of using Tricyclic Compounds for treating or preventing a viral infection or a virus-related disorder in a patient. The present invention provides Tricyclic Compounds of Formula (I): Non-limiting examples of the Compounds of Formula (I) include compound 44 The Compounds of Formula (II) can be useful for inhibiting HCV viral replication or replicon activity, and for treating or preventing HCV infection in a patient.
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ANTIVIRAL COMPOUNDS COMPOSED OF THREE LINKED ARYL MOIETIES TO TREAT DISEASES SUCH AS HEPATITIS C (Fri, 03 Dec 2010)
The present invention relates to novel Linked Tricyclic Aryl Compounds, compositions comprising at least one Linked Tricyclic Compound, and methods of using Linked Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient. in one aspect, the present invention provides Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein: Non-limiting examples of the Compounds of Formula (II) include compound 56 </p>
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ANTIVIRAL COMPOUNDS COMPOSED OF THREE ALIGNED ARYL MOIETIES TO TREAT DISEASES SUCH AS HEPATITIS C (Fri, 03 Dec 2010)
The present invention relates to novel Tricyclic Compounds, compositions comprising at least one Tricyclic Compound, and methods of using Tricyclic Compounds for treating or preventing a viral infection or a virus-related disorder in a patient. The present invention provides Tricyclic Compounds of Formula (I): Non-limiting examples of the Compounds of Formula (I) include compound 44 The Compounds of Formula (II) can be useful for inhibiting HCV viral replication or replicon activity, and for treating or preventing HCV infection in a patient. </p>
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Bicyclic heterocycle derivatives and use thereof as GPR119 modulators (Fri, 03 Dec 2010)
The present invention relates to Bicyclic Heterocycle Derivatives of formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR1 19 in a patient.
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GAMMA SECRETASE MODULATORS (Fri, 26 Nov 2010)
<p id="p-0001-en" num="0000">In its many embodiments, the present invention provides a novel class of 5-membered, nitrogen-containing heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.</p>
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NOVEL JNK INHIBITORS (Fri, 26 Nov 2010)
<p id="p-0001-en" num="0000">Disclosed are substituted imidazo[1,2-a]pyridines, imidazo[1,2-a]pyrazines, imidazo[1,2-c]pyrimidines and imidazo[1,2-d]triazines compounds of the formula: (1.0) Also disclosed are methods for treating JNK1 and ERK mediated diseases using the compounds of formula 1.0.</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="27.94mm" wi="54.10mm" file="US20100298314A1-20101125-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p>
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Heterocyclic aspartyl protease inhibitors (Fri, 19 Nov 2010)
<p id="p-0001" num="0000">Disclosed are compounds of the formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.31mm" wi="47.24mm" file="US08183252-20120522-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">W is a bond, —C(═S)—, —S(O)—, —S(O)<sub>2</sub>—, —C(═O)—, —O—, —C(R<sup>6</sup>)(R<sup>7</sup>)—, —N(R<sup>5</sup>)— or —C(═N(R<sup>5</sup>))—;</li> <li id="ul0002-0002" num="0000">X is —O—, —N(R<sup>5</sup>)— or —C(R<sup>6</sup>)(R<sup>7</sup>)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)<sub>2</sub>—, —C(═O)— or —C(═NR<sup>5</sup>)—;</li> <li id="ul0002-0003" num="0000">U is a bond, —S(O)—, —S(O)<sub>2</sub>—, —C(O)—, —O—, —P(O)(OR<sup>15</sup>)—, —C(═NR<sup>5</sup>)—, —(C(R<sup>6</sup>)(R<sup>7</sup>))<sub>b</sub>— or —N(R<sup>5</sup>)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)<sub>2</sub>—, —O—, or —N(R<sup>5</sup>)—, U is not —S(O)—, —S(O)<sub>2</sub>—, —O—, or —N(R<sup>5</sup>)—; provided that when X is —N(R<sup>5</sup>)— and W is —S(O)—, —S(O)<sub>2</sub>—, —O—, or —N(R<sup>5</sup>)—, then U is not a bond;</li> <li id="ul0002-0004" num="0000">and R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>6</sup>, and R<sup>7 </sup>are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.</li> </ul> </li> </ul> </p> <p id="p-0003" num="0000">Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes.</p> <p id="p-0004" num="0000">Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m<sub>1 </sub>agonist or m<sub>2 </sub>antagonist.</p>
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SPIRO 1,3,4-THIADIAZOLINE DERIVATIVES AS KSP INHIBITORS (Fri, 19 Nov 2010)
The present invention relates to compounds of Formula (I), below, (wherein X, R1, R2, R3, p, ring A, and ring B are as defined herein). The present invention also relates to compositions (including pharmaceutically acceptable compositions) comprising these compounds, alone and in combination with one or more additional therapeutic agents, and to methods for their use in inhibiting KSP kinesin activity, and for treating cellular proliferative diseases or disorders associated with KSP kinesin activity.
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FUSED TRICYCLIC ARYL COMPOUNDS USEFUL FOR THE TREATMENT OF VIRAL DISEASES (Fri, 19 Nov 2010)
The present invention relates to novel Fused Tricyclic Aryl Compounds, compositions comprising at least one Fused Tricyclic Aryl Compound, and methods of using the Fused Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient.
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FUSED TRICYCLIC ARYL COMPOUNDS USEFUL FOR THE TREATMENT OF VIRAL DISEASES (Fri, 19 Nov 2010)
The present invention relates to novel Fused Tricyclic Aryl Compounds, compositions comprising at least one Fused Tricyclic Aryl Compound, and methods of using the Fused Tricyclic Aryl Compounds for treating or preventing HCV in-fection in a patient. </p>
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Mammalian receptor proteins DCRS5; method of treatment (Fri, 05 Nov 2010)
<p id="p-0001" num="0000">Nucleic acids encoding mammalian, e.g., primate, receptors, purified receptor proteins and fragments thereof. Antibodies, both polyclonal and monoclonal, are also provided. Methods of using the compositions for both diagnostic and therapeutic utilities are described.</p>
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MAMMALIAN CYTOKINES, RELATED REAGENTS AND METHODS (Mon, 01 Nov 2010)

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SUGAR-SUBSTITUTED 2-AZETIDINONES USEFUL AS HYPOCHOLESTEROLEMIC AGENTS (Mon, 01 Nov 2010)

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HETEROCYCLIC AMIDE COMPOUNDS AS PROTEIN KINASE INHIBITORS (Mon, 01 Nov 2010)

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Engineered anti-IL-23P19 antibodies (Fri, 29 Oct 2010)
<p id="p-0001" num="0000">Engineered antibodies to human IL-23p19 are provided, as well as uses thereof, e.g., in treatment of inflammatory, autoimmune, and proliferative disorders.</p>
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Exo-selective synthesis of himbacine analogs (Fri, 22 Oct 2010)
<p id="p-0001" num="0000">This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists. The chemistry disclosed herein is exemplified in the following synthesis sequence:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="72.14mm" wi="75.86mm" file="US08138180-20120320-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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HUMAN RECEPTOR PROTEINS; RELATED REAGENTS AND METHODS (Fri, 22 Oct 2010)
<p id="p-0001-en" num="0000">Nucleic acids encoding mammalian Toll-like receptors (TLRs) have been identified in human cells. Recombinantly produced TLRs are used in the preparation of antibodies that are capable of binding to the TLRs. The antibodies are advantageously used in the prevention and treatment of septic shock, inflammatory conditions, and viral infections.</p>
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Thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use (Fri, 22 Oct 2010)
In its many embodiments, the present invention provides provides certain thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidone compounds, including compounds (or tautomers or a pharmaceutically acceptable salts thereof) having the structural Formula (III): wherein R<sp>2</sp>, R<sp>3</sp>, R<sp>4</sp>, R<sp>5</sp>, R<sp>6</sp>, R<sp>7</sp>, R<sp>8</sp>, and R<sp>9 </sp>are each selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds, and methods for their preparation and use in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimer's Disease, are also disclosed.
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DCRS5 polypeptides (Fri, 15 Oct 2010)
<p id="p-0001" num="0000">Nucleic acids encoding mammalian, e.g., primate, receptors, purified receptor proteins and fragments thereof. Antibodies, both polyclonal and monoclonal, are also provided. Methods of using the compositions for both diagnostic and therapeutic utilities are described.</p>
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Mammalian Genes; Related Reagents and Methods (Fri, 15 Oct 2010)
<p id="p-0001-en" num="0000">Purified genes encoding proteins from a mammal, reagents related thereto including purified proteins, specific antibodies, and nucleic acids encoding these molecules are provided. Methods of using said reagents and diagnostic kits are also provided.</p>
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PYRAZOLO [1, 5-A] PYRIMIDINE DERIVATIVES AS MTOR INHIBITORS (Fri, 15 Oct 2010)
The present invention provides methods for inhibiting mTOR using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with mTOR using such compounds.
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Process for the preparation of 6,6-dimethyl-3-azabicyclo-[3.3.0]-hexane compounds and enantiomeric salts thereof (Fri, 08 Oct 2010)
<p id="p-0001" num="0000">The present invention provides for a process for preparing racemic methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate, its corresponding salt: (1R,2S,5S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate di-p-toluoyl-D-tartaric acid (“D-DTTA”) salt or a (1S,2R,5R)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate di-p-toluoyl-L-tartaric acid salt (“L-DTTA”) in a high enantiomeric excess. This invention also provides for a process for preparing a (1R,2S,5S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate dibenzoyl-D-tartaric acid (“D-DBTA”) salt or a (1S,2R,5R)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate L-tartaric acid (“L-DBTA”) salt in a high enantiomeric excess. Further, this invention provides a process for preparing intermediates II, IIB, III, IV, IV salt, V, VI, and VII.</p>
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BRIDGED BICYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF (Fri, 08 Oct 2010)
The present invention relates to Bridged Bicyclic Heterocycle Derivatives, compositions comprising a Bridged Bicyclic Heterocycle Derivative, and methods of using the Bridged Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a GPCR in a patient.
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BICYCLIC PIPERIDINE AND PIPERAZINE DERIVATIVES AS GPCR MODULATORS FOR THE TREATMENT OF OBESITY, DIABETES AND OTHER METABOLIC DISORDERS (Fri, 08 Oct 2010)
The present invention relates to Bicyclic Piperidine and Piperazine Derivatives, compositions comprising a Bicyclic Piperidine and Piperazine Derivative, and methods of using the Bicyclic Piperidine and Piperazine Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a GPCR in a patient.
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ANTI-MITOTIC AGENT AND AURORA KINASE INHIBITOR COMBINATION AS ANTI-CANCER TREATMENT (Fri, 01 Oct 2010)
<p id="p-0001-en" num="0000">The present invention relates to a method of treating cancer by pretreatment with anti-mitotic agents followed by at least one aurora kinase inhibitor. Extensive illustrations are provided for the antimitotic agents and aurora kinase inhibitors that are useful in the inventive treatment.</p>
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Gamma secretase modulators (Fri, 01 Oct 2010)
<p id="p-0001" num="0000">The present invention provides a novel class of heterocyclic compounds of Formula (I) as modulators of gamma secretase, wherein the definitions of the variables of Formula (I) are defined herein, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="21.34mm" wi="57.49mm" file="US08357682-20130122-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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OXYPIPERIDINE DERIVATIVES AND METHODS OF USE THEREOF (Fri, 01 Oct 2010)
<p id="p-0001-en" num="0000">The present invention relates to novel Oxypiperidine Derivatives, pharmaceutical compositions comprising the Oxypiperidine Derivatives and the use of the Oxypiperidine Derivatives for treating or preventing treating allergy, an allergy-induced airway response, congestion, hypotension, a cardiovascular disease, a gastrointestinal disorder, obesity, a sleep disorder, pain, diabetes, a diabetic complication, impaired glucose tolerance, impaired fasting glucose or a central nervous system (CNS) disorder.</p>
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Gamma secretase modulators (Thu, 30 Sep 2010)
This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).
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BICYCLIC COMPOUNDS AS INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE (Fri, 24 Sep 2010)
The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase ("DGAT") inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below : formula (I).
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BICYCLIC COMPOUNDS AS INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE (Fri, 24 Sep 2010)
The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase ("DGAT") inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below (I).
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BICYCLIC COMPOUNDS AS INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE (Fri, 24 Sep 2010)
The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase ("DGAT") in-hibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or pre-venting a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below (I). </p>
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BICYCLIC COMPOUNDS AS INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE (Fri, 24 Sep 2010)
The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase ("DGAT") in-hibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or pre-venting a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below : formula (I). </p>
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Amino-quinoxaline and amino-quinoline compounds for use as adenosine A2a receptor antagonists (Fri, 24 Sep 2010)
Compounds of the Formula (I), where W represents CH or N; and Q represents -CN, -C(=NOH)NH<sb>2</sb>, -CONHR<sp>1</sp> or various herein described heterocyclic radicals; as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof are adenosine A<sb>2a</sb> receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.
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1,2,4-triazolo[4,3-c]pyrimidin-3-one and pyrazolo [4,3-e] -1,2,4-triazolo [4,3-c] pyrimidin-3-one compounds for use as adenosine A2a receptor antagonists (Fri, 24 Sep 2010)
Compounds of the Formula I wherein R<sp>1</sp> and R<sp>2</sp> together with the carbon atoms to which they are bonded optionally form a further heteroaromatic ring of the formula (II) as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof are adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.
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NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF (Fri, 10 Sep 2010)
<p id="p-0001-en" num="0000">The present invention provides compounds of Formula (I):</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="18.37mm" wi="51.39mm" file="US20100227873A1-20100909-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001-en" list-style="none"> <li>and pharmaceutically acceptable salts, solvates, esters, and tautomers thereof, wherein: <ul id="ul0002-en" list-style="none"><li>Q is selected from the group consisting of:</li></ul></li> </ul> </p> <p id="p-0003-en" num="0000"> <chemistry id="chem-us-00002-en" num="00002"> <img id="emi-c00002-en" he="155.36mm" wi="54.27mm" file="US20100227873A1-20100909-C00002.TIF" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0003-en" list-style="none"> <li>and <ul id="ul0004-en" list-style="none"><li>L is selected from the group consisting of:</li></ul></li> </ul> </p> <p id="p-0004-en" num="0000"> <chemistry id="chem-us-00003-en" num="00003"> <img id="emi-c00003-en" he="93.05mm" wi="51.73mm" file="US20100227873A1-20100909-C00003.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0005-en" num="0000">pharmaceutically compositions comprising one or more compounds of formula (I), and methods of using the compounds of formula (I).</p>
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Process and intermediates for the preparation of (1r,2s,5s)-6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylates or salts thereof (Thu, 09 Sep 2010)
In one embodiment, the present application relates to a process of making a compound of Formula (I); and to certain intermediate compounds that are made within the process of making the compound Formula (I).
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Antibodies that bind DNAX leukocyte associated immunoglobulin-like receptor (Fri, 20 Aug 2010)
<p id="p-0001" num="0000">Nucleic acids encoding various monocyte cell proteins from a primate, reagents related thereto, including specific antibodies, and purified proteins are described. Methods of using reagents and related diagnostic kits are also provided.</p>
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Nucleic acids encoding murine IL-174 (Fri, 20 Aug 2010)
<p id="p-0001" num="0000">CTLA-8 related antigens from mammals, reagents related thereto including purified proteins, specific antibodies, and nucleic acids encoding said antigens. Methods of using said reagents and diagnostic kits are also provided.</p>
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Mammalian cytokines; related reagents and methods (Fri, 13 Aug 2010)
<p id="p-0001" num="0000">Nucleic acids encoding mammalian, e.g., primate, IL-1ζ, purified IL-1ζ polypeptides and fragments thereof. Binding proteins, e.g., antibodies, both polyclonal and monoclonal, are also provided. Methods of using the compositions for both diagnostic and therapeutic utilities are provided.</p>
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PHTHALAZINE-CONTAINING ANTIDIABETIC COMPOUNDS (Fri, 13 Aug 2010)
This invention provides for certain phthalazine-containing compounds of the formula (I) or a pharmaceutically acceptable salt, ester or solvate thereof, wherein G is an optionally substituted N-N containing heteroaryl group and the variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.
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IMIDAZOPYRAZINES AS PROTEIN KINASE INHIBITORS (Fri, 06 Aug 2010)
In its many embodiments, the present invention provides a novel class of imidazopyrazine compounds as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or checkpoint kinases using such compounds or pharmaceutical compositions.
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PENTAFLUOROSULPHOLANE-CONTAINING ANTIDIABETIC COMPOUNDS (Fri, 30 Jul 2010)
This invention provides for certain pentafluorosulpholane-containing compounds of the formula or a pharmaceutically acceptable salt, ester, solvate or prodrug thereof, wherein the variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.
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BRIDGED AND FUSED HETEROCYCLIC ANTIDIABETIC COMPOUNDS (Fri, 30 Jul 2010)
This invention provides for certain bridged and fused heterocyclic compounds of the formula ( I ) or a pharmaceutically acceptable salt, ester solvate or prodrug thereof wherein: L is: ( II ) and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.
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BRIDGED AND FUSED ANTIDIABETIC COMPOUNDS (Fri, 30 Jul 2010)
ABSTRACT This invention provides for certain bridged and fused compounds of the formula G-L-A I or a pharmaceutically acceptable salt, ester of solvate thereof wherein: A is: (I) and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.
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PENTAFLUOROSULPHOLANE-CONTAINING ANTIDIABETIC COMPOUNDS (Fri, 30 Jul 2010)
This invention provides for certain pentafluorosulpholane-containing compounds of the formula or a pharmaceutically acceptable salt, ester, solvate or prodrug thereof, wherein the variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders. </p>
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BRIDGED AND FUSED ANTIDIABETIC COMPOUNDS (Fri, 30 Jul 2010)
This invention provides for certain bridged and fused compounds of the formula G-L-A I or a pharmaceutically acceptable salt, ester of solvate thereof wherein: A is: (I) and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders. </p>
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BRIDGED AND FUSED HETEROCYCLIC ANTIDIABETIC COMPOUNDS (Fri, 30 Jul 2010)
This invention provides for certain bridged and fused heterocyclic compounds of the formula (I) or a pharmaceutically acceptable salt, ester solvate or prodrug thereof wherein: L is: (II) and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders. </p>
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Gamma secretase modulators (Fri, 30 Jul 2010)
This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I) wherein R<sp>2</sp> is a fused bicyclic ring of the formula (II). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I).
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NOVEL JNK INHIBITORS (Fri, 16 Jul 2010)
<p id="p-0001-en" num="0000">Disclosed are compounds of the formula (I) wherein X is N or CH, and Y is N or CR<sup>5</sup>. Also disclosed are methods of treating JNK and ERK mediated diseases using the compounds of formula 1.0.</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="21.76mm" wi="69.85mm" file="US20100179141A1-20100715-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p>
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Macrocyclic beta-secretase inhibitors (Fri, 16 Jul 2010)
<p id="p-0001" num="0000">Disclosed are novel compounds of the formula</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.23mm" wi="56.64mm" file="US08012953-20110906-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a pharmaceutically acceptable salt or solvate thereof, wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, n and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of β-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies. </p>
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Heterocyclic compounds and use thereof as ERK inhibitors (Thu, 08 Jul 2010)
Disclosed are the ERK inhibitors of formula 1.0, and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.
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COMPOUNDS FOR INHIBITING KSP KINESIN ACTIVITY (Sat, 03 Jul 2010)
The present invention relates to compounds of Formula (I), below, (wherein X, R COPYRIGHT KIPO WIPO 2010
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BICYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF (Sat, 03 Jul 2010)
The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient. COPYRIGHT KIPO WIPO 2010
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Engineered anti-IL-23R antibodies (Fri, 02 Jul 2010)
<p id="p-0001" num="0000">Antibodies to human IL-23R are provided, as well as uses thereof, e.g. in treatment of inflammatory, autoimmune, and proliferative disorders.</p>
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Heterocyclic substituted pyridine compounds with CXCR3 antagonist activity (Fri, 02 Jul 2010)
<p id="p-0001" num="0000">The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="36.07mm" wi="71.04mm" file="US08017616-20110913-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a pharmaceutically acceptable salt, solvate or ester thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1. </p>
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BICYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF (Fri, 02 Jul 2010)
The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a GPCR in a patient.
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BICYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF (Fri, 02 Jul 2010)
The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a GPCR in a patient.
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GAMMA SECRETASE MODULATORS (Fri, 02 Jul 2010)
This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (Chemical formula should be inserted here as it appears on abstract in paper form). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).
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GAMMA SECRETASE MODULATORS (Fri, 02 Jul 2010)
This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (Chemical formula should be inserted here as it appears on abstract in paper form). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).
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PYRIMIDINE DERIVATIVES AS GPCR MODTTLATORS FOR USE IN THE TREATMENT OF OBESITY AND DIABETES (Fri, 02 Jul 2010)
The present invention relates to Pyriraidine Derivatives of formula (I), compositions comprising a Pyrimidine Derivative, and methods of using the Pyrimidine Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein -coupled receptor (GPCR) in a patient.
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GAMMA SECRETASE MODULATORS (Fri, 02 Jul 2010)
This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (Chemical formula should be inserted here as it appears on abstract in paper form). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I). </p>
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BICYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF (Fri, 02 Jul 2010)
The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a GPCR in a patient. </p>
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PYRIMIDINE DERIVATIVES AND METHODS OF USE THEREOF (Fri, 02 Jul 2010)
The present invention relates to Pyriraidine Derivatives of formula (I), compositions comprising a Pyrimidine Derivative, and methods of using the Pyrimidine Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein -coupled receptor (GPCR) in a patient. </p>
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GAMMA SECRETASE MODULATORS (Fri, 02 Jul 2010)
This invention provides novel compounds that are modulators of gamma secretase. The compounds have the for-mula (Chemical formula should be inserted here as it appears on abstract in paper form). Also disclosed are methods of modulat-ing gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I). </p>
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SPIRO-CONDENSED 1, 3, 4-THIADIAZOLE DERIVATIVES FOR INHIBITING KSP KINESIN ACTIVITY (Thu, 01 Jul 2010)
The present invention relates to compounds of Formula, below, (wherein X, R1, R2, R3, p, E, ring A, and ring B are as defined herein). The present invention also relates to compositions (including pharmaceutically acceptable compositions) comprising these compounds, alone and in combination with one or more additional therapeutic agents, and to methods for their use in inhibiting KSP kinesin activity, and for treating cellular proliferative diseases or disorders associated with KSP kinesin activity. COPYRIGHT KIPO WIPO 2010
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SUBSTITUTED INDOLE DERIVATIVES AND METHODS OF USE THEREOF (Tue, 22 Jun 2010)
The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient. COPYRIGHT KIPO WIPO 2010
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Anti-MDL-1 antibodies (Fri, 18 Jun 2010)
<p id="p-0001" num="0000">Antibodies to human MDL-1 are provided, as well as uses thereof, e.g., in treatment of immune disorders, in particular, infectious diseases and sepsis.</p>
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DEUTERATED COMPOUNDS AS HEPATITIS C VIRUS (HCV) INHIBITORS (Fri, 18 Jun 2010)
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as wet! as methods of using them to treat disorders associated with the HCV protease An illustrative inventsve compound is shown below: Formula (I). </p>
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2,3-SUBSTITUTED AZAINDOLE DERIVATIVES FOR TREATING VIRAL INFECTIONS (Wed, 16 Jun 2010)
The present invention relates to 2,3-Substituted Azaindole Derivatives, compositions comprising at least one 2,3-Substituted Azaindole Derivatives, and methods of using the 2,3-Substituted Azaindole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient. COPYRIGHT KIPO WIPO 2010
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Functionally selective ALPHA2C adrenoreceptor agonists (Fri, 11 Jun 2010)
<p id="p-0001" num="0000">In its many embodiments, the present invention provides a novel class of naphthene- and indane-type as inhibitors of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.</p>
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Compounds for the treatment of inflammatory disorders (Fri, 11 Jun 2010)
<p id="p-0001" num="0000">This invention relates to compounds of the Formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="28.70mm" wi="60.20mm" file="US08039467-20111018-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF-α or combinations thereof. </p>
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Process for the preparation of 6,6-dimethyl-3-azabicyclo-[3.1.0]-hexane compounds utilizing bisulfite intermediate (Fri, 11 Jun 2010)
<p id="p-0001" num="0000">The present invention provides for a process for preparing 6,6-Dimethyl-3-aza-bicyclo[3.1.0]hexane-2-sulfonate, an intermediate useful in the efficient preparation of (1R,2S,5S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylic acid and esters and salts thereof, processes for preparing (1R,2S,5S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylic acid and esters and salts thereof from the sulfonate intermediate and processes for preparing 6,6-Dimethyl-3-aza-bicyclo[3.1.0]hexane-2-sulfonate.</p>
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Process for preparing (1R,2S,5S)-N-[(1S)-3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[(2S)-2-[[[(1,1-dimethylethyl)amino]-carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide (Fri, 11 Jun 2010)
<p id="p-0001" num="0000">The present invention relates also to a process for the preparation of intermediate compounds useful in preparing the compounds of Formula (I) using the process of Scheme (II).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="39.20mm" wi="72.81mm" file="US08163937-20120424-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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MORPHOLINONE COMPOUNDS AS FACTOR IXA INHIBITORS (Fri, 11 Jun 2010)
The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt or a solvate thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
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MORPHOLINONE COMPOUNDS AS FACTOR IXA INHIBITORS (Fri, 11 Jun 2010)
The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt or a solvate thereof. The present invention also provides pharmaceutical compositions comprising one or more said com-pounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes. </p>
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TETRACYCLIC INDOLE DERIVATIVES AND METHODS OF USE THEREOF (Thu, 10 Jun 2010)
The present invention relates to Tetracyclic Indole Derivatives, compositions comprising at least one Tetracyclic Indole Derivative, and methods of using the Tetracyclic Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient. COPYRIGHT KIPO WIPO 2010
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NOVEL 4-CYANO, 4-AMINO, AND 4-AMINOMETHYL DERIVATIVES OF PYRAZOLO[1,5-a]PYRIDINES, PYRAZOLO[1,5-c]PYRIMIDINES AND 2H-INDAZOLE COMPOUNDS AND 5-CYANO, 5-AMINO, AND 5-AMINOMETHYL DERIVATIVES OF IMIDAZO[1,2-a]PYRIDINES, AND IMIDAZO[1,5-a]PYRAZINES AS CYCLIN DEPENDENT KINASE INHIBITORS (Fri, 04 Jun 2010)
<p id="p-0001-en" num="0000">In its many embodiments, the present invention provides a novel class of 4-cyano, 4-amino, and 4-aminomethyl derivatives of pyrazolo[1,5-a]pyridine, pyrazolo[1,5-c]pyrimidine, and 2H-Indazole compounds and 5-cyano, 5-amino, and 5-aminomethyl derivatives of imidazo[1,2-a]pyridine and imidazo[1,5-a]pyrazine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.</p>
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MAMMALIAN CYTOKINE RECEPTOR SUBUNIT PROTEINS, RELATED REAGENTS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME (Tue, 01 Jun 2010)

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Mammalian Cell Membrane Proteins; Related Reagents (Fri, 28 May 2010)
<p id="p-0001-en" num="0000">The purification and isolation of various genes which encode mammalian cell surface polypeptides. Nucleic acids, proteins, antibodies, and other reagents useful in modulating development of cells, e.g., lymphoid and myeloid, are provided, along with methods for their use.</p>
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IL-B50 polypeptide (Fri, 28 May 2010)
<p id="p-0001" num="0000">Purified genes encoding cytokines from a mammal, reagents related thereto including purified proteins, specific antibodies, and nucleic acids encoding this molecule are provided. Methods of using said reagents and diagnostic kits are also provided.</p>
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INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE (Fri, 28 May 2010)
The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase ("DGAT") inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown with this abstract.
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INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE (Fri, 28 May 2010)
The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase ("DGAT") inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below.
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INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE (Fri, 28 May 2010)
The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase ("DGAT") inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below: formula (I).
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INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE (Fri, 28 May 2010)
The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase ("DGAT") inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown with this abstract. <img he="0" wi="0" file="" alt="" img-content="undefined" img-format="jpg" inline="yes" orientation="portrait"/> </p>
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INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE (Fri, 28 May 2010)
The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase ("DGAT") inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below. </p>
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INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE (Fri, 28 May 2010)
The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase ("DGAT") inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below: formula (I). </p>
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Methods for inhibiting protein kinases (Fri, 21 May 2010)
<p id="p-0001" num="0000">The present invention provides methods for inhibiting protein kinases selected from the group consisting of AKT, Checkpoint kinase, Aurora kinase, Pim kinases, and tyrosine kinase using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with protein kinases using such compounds.</p>
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GAMMA SECRETASE MODULATORS (Fri, 21 May 2010)
In its many embodiments, the present invention provides a novel class of heterocyclic compounds of Group A or Group, as defined herein, as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
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COMPOUNDS USEFUL AS HIV BLOCKERS (Fri, 21 May 2010)
The present invention relates to a compound having the general Formula (I): wherein the variables are as defined in the specification. The present invention further relates to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular for the treatment or prevention of chemokine-mediated disorders such as HIV infection.
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INHIBITORS OF FATTY ACID BINDING PROTEIN (FABP) (Fri, 21 May 2010)
The present invention relates to novel heterocyclic compounds as Fatty Acid Binding Protein ("FABP") inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the present invention is shown below: (I)
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GAMMA SECRETASE MODULATORS (Fri, 21 May 2010)
In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
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GAMMA SECRETASE MODULATORS (Fri, 21 May 2010)
In its many embodiments, the present invention provides a novel class of heterocyclic compounds of Group A or Group, as defined herein, as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions. </p>
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INHIBITORS OF FATTY ACID BINDING PROTEIN (FABP) (Fri, 21 May 2010)
The present invention relates to novel heterocyclic compounds as Fatty Acid Binding Protein ("FABP") inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the present invention is shown below: (I) </p>
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ENGINEERED ANTI-IL-23P19 ANTIBODIES (Tue, 18 May 2010)

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GAMMA SECRETASE MODULATORS (Sat, 15 May 2010)
In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
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GAMMA SECRETASE MODULATORS (Sat, 15 May 2010)
In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
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GAMMA SECRETASE MODULATORS (Sat, 15 May 2010)
In its many embodiments, the present invention provides novel heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
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COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS (Sat, 15 May 2010)
This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.
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COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS (Sat, 15 May 2010)
This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.
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GAMMA SECRETASE MODULATORS (Sat, 15 May 2010)
In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions. </p>
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GAMMA SECRETASE MODULATORS (Sat, 15 May 2010)
In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions. </p>
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GAMMA SECRETASE MODULATORS (Sat, 15 May 2010)
In its many embodiments, the present invention provides novel heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions. </p>
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Compounds for the treatment of inflammatory disorders (Fri, 14 May 2010)
<p id="p-0001" num="0000">This invention relates to compounds of the Formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.18mm" wi="63.42mm" file="US08178553-20120515-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-α or combinations thereof.</li> </ul> </li> </ul> </p>
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Compounds for inhibiting KSP kinesin activity (Fri, 14 May 2010)
The present invention relates to compounds of Formula (I), below, (wherein X, R<sp>1</sp>, R<sp>2</sp>, R<sp>3</sp>, R<sp>27</sp>, R<sp>28</sp>, p, E, ring A, and ring B are as defined herein). The present invention also relates to compositions (including pharmaceutically acceptable compositions) comprising these compounds, alone and in combination with one or more additional therapeutic agents, and to methods for their use in inhibiting KSP kinesin activity, and for treating cellular proliferative diseases or disorders associated with KSP kinesin activity.
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PYRIDAZINONE DERIVATIVES USEFUL AS GLUCAN SYNTHASE INHIBITORS (Thu, 13 May 2010)
In its many embodiments, the present invention provides-substituted pyridazinone compounds as glucan synthase inhibitors, methods of preparing such compounds, pharmaceutical including one or more of such compounds, methods of preparing pharmaceutical formulations including one or more such compounds or one or more such compounds along with other antifungal agents, and methods of treatment, prevention, inhibition, or amelioration of one or more fungal infections associated with glucan synthase using such compounds or pharmaceutical compositions. COPYRIGHT KIPO WIPO 2010
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2, 3-SUBSTITUTED INDOLE DERIVATIVES FOR TREATING VIRAL INFECTIONS (Thu, 13 May 2010)
The present invention relates to 2,3-Substituted Indole Derivatives, compositions comprising at least one 2,3-Substituted Indole Derivative, and methods of using the 2,3-Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient. COPYRIGHT KIPO WIPO 2010
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ENGINEERED ANTI-IL-23P19 ANTIBODIES (Fri, 07 May 2010)
<p id="p-0001-en" num="0000">Engineered antibodies to human IL-23p19 are provided, as well as uses thereof, e.g. in treatment of inflammatory, autoimmune, and proliferative disorders.</p>
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PREPARATION OF 3-AMINO-3-(CYCLOBUTYLMETHYL)-2-(HYDROXY)-PROPIONAMIDE HYDROCHLORIDE (Fri, 07 May 2010)
<p id="p-0001-en" num="0000">Disclosed is a process for preparing 3-(amino)-3-cyclobutylmethyl-2-hydroxy-propionamide hydrochloride, an intermediate useful in the preparation of the HCV protease inhibitor (1R,5S)—N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide.</p>
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HETEROCYCLIC AMIDE COMPOUNDS AS PROTEIN KINASE INHIBITORS (Tue, 04 May 2010)
The present invention relates to novel heterocyclic amide compounds of Formula I: as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are compositions comprising said compounds, and methods for using said compoundsfor treating or preventing a proliferative disease, an anti-proliferative disorder, inflammation, arthritis, a neurological or neurodegenerative disease, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease or a fungal disease. COPYRIGHT KIPO WIPO 2010
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BENZENESULFONYL-CHROMANE, THIOCHROMANE, TETRAHYDRONAPHTHALENE AND RELATED GAMMA SECRETASE INHIBITORS (Sat, 01 May 2010)
Disclosed are novel gamma secretase inhibitors of the formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, wherein L COPYRIGHT KIPO WIPO 2010
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Mammalian genes; related reagents and methods (Fri, 30 Apr 2010)
<p id="p-0001" num="0000">Nucleic acids encoding mammalian, e.g., primate or rodent, genes, purified proteins and fragments thereof. Antibodies, both polyclonal and monoclonal, are also provided. Methods of using the compositions for both diagnostic and therapeutic utilities are provided.</p>
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TETRAHYDROPYRANOCHROMENE GAMMA SECRETASE INHIBITORS (Fri, 30 Apr 2010)
Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)-O-C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)-O-C(O)-heteroaryl and a basic tertiary amine. COPYRIGHT KIPO WIPO 2010
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ANTI-MITOTIC AGENT AND AURORA KINASE INHIBITOR COMBINATION AS ANTI-CANCER TREATMENT (Sat, 24 Apr 2010)
The present invention relates to a method of treating cancer by pretreatment with anti-mitotic agents followed by at least one aurora kinase inhibitor. Extensive illustrations are provided for the antimitotic agents and aurora kinase inhibitors that are useful in the inventive treatment. COPYRIGHT KIPO WIPO 2010
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PYRROLIDINE, PIPERIDINE AND PIPERAZINE DERIVATIVES AND METHODS OF USE THEREOF (Fri, 23 Apr 2010)
The present invention relates to novel Pyrrolidine, Piperidine and Piperazine Derivatives, pharmaceutical compositions comprising the Pyrrolidine, Piperidine and Piperazine Derivatives and the use of these compounds for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disoder, a metabolic disorder, obesity, an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
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PYRROLIDINE, PIPERIDINE AND PIPERAZINE DERIVATIVES AND METHODS OF USE THEREOF (Fri, 23 Apr 2010)
The present invention relates to novel Pyrrolidine, Piperidine and Piperazine Derivatives, pharmaceutical compositions comprising the Pyrrolidine, Piperidine and Piperazine Derivatives and the use of these compounds for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disoder, a metabolic disorder, obesity, an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. </p>
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Substituted N-arylsulfonylheterocyclic amines as gamma-secretase inhibitors (Fri, 16 Apr 2010)
<p id="p-0001" num="0000">Disclosed are novel gamma secretase inhibitors of the formula:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.69mm" wi="54.10mm" file="US07998958-20110816-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">Also disclosed are methods for inhibiting gamma secretase, for treating one or more neurodegenerative diseases, for inhibiting the deposition of beta amyloid protein, and for treating Alzheimer's disease using the compounds of formula (I).</p>
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Nucleic acids encoding CCL27 (Fri, 16 Apr 2010)
<p id="p-0001" num="0000">Novel CC chemokines from human, reagents related thereto including purified proteins, specific antibodies and nucleic acids encoding these chemokines are provided. Also provided are methods of making and using said reagents and diagnostic kits.</p>
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PIPERIDINYL-PIPERIDINE AND PIPERAZINYL-PIPERIDINE FOR USE IN THE TREATMENT OF DIABETES OR PAIN (Fri, 16 Apr 2010)
<p id="p-0001-en" num="0000">The present invention relates to Compounds of Formula (I), compositions comprising the compounds, and methods of using the compounds to treat or prevent pain, diabetes, a diabetic complication, impaired glucose tolerance (IGT) or impaired fasting glucose (IFG) in a patient.</p> <p id="p-0002-en" num="0000"/>
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BENZODIOXAN ANALOGUES AS ALPHA2C ADRENERGIC RECEPTOR MODULATORS (Fri, 16 Apr 2010)
In its many embodiments, the present invention provides a novel class of benzodioxan analogues as modulators of the α2C adrenergic receptor, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.
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SPIROAMINOOXAZOLINE ANALOGUES AS ALPHA2C ADRENERGIC RECEPTOR MODULATORS (Fri, 16 Apr 2010)
In its many embodiments, the present invention provides a novel class of spiroaminooxazoline analogues as modulators of α2C adrenergic receptor, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.
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BIARYL SPIROAMINOOXAZOLINE ANALOGUES AS ALPHA2C ADRENERGIC RECEPTOR MODULATORS (Fri, 16 Apr 2010)
In its many embodiments, the present invention provides a novel class of biaryi spiroaminooxazoline analogues as modulators of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.
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SPIRO-IMIDAZOLONE DERIVATIVES AS GLUCAGON RECEPTOR ANTAGONISTS (Fri, 09 Apr 2010)
The present invention relates to compounds of the general formula: (I) wherein ring A, ring B, R1, R3, Z, L1, and L2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto. </p>
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GAMMA SECRETASE MODULATORS (Fri, 09 Apr 2010)
In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions. COPYRIGHT KIPO WIPO 2010
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PIPERAZINA-PIPERIDINAS SUBSTITUÍDAS POR PIRAZINILA COM ATIVIDADE DE ANTAGONISTA CXCR3 (Wed, 07 Apr 2010)
PIPERAZINA-PIPERIDINAS SUBSTITUÍDAS POR PIRAZINILA COM ATIVIDADE DE ANTAGONISTA CXCR3. O presente pedido descreve um composto, ou enantiômeros, estereoisômeros, rotâmeros, tautômeros, racematos ou profármaco do referido composto, ou sais farmaceuticamente aceitáveis, solvatos ou ésteres do referido composto, ou do referido profármaco, o referido composto tendo a estrutura geral mostrada na Fórmula 1: e os sais farmaceuticamente aceitáveis, solvatos e ésteres deste. Também descrito é um método de tratar doenças mediadas por quimiocina, tais como, terapia paliativa, terapia curativa, terapia profilática de certas doenças e condições tais como doenças inflamatórias (exemplos não limitantes incluem psoríase), doenças autoimunes (exemplos não limitantes incluem, artrite reumatóide, esclerose múltipla), rejeição a enxerto (exemplos não limitantes incluem, rejeição a aloenxerto, rejeição a xenoenxerto), doenças infecciosas (por exemplo, lepra tuberculóide), erupções de fármaco fixo, respostas de hipersensibilidade tipo retardo cutâneo, inflamação oftálmica, diabetes tipo I, meningite viral e tumores empregando-se um composto da Fórmula 1.
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COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS (Fri, 02 Apr 2010)
This invention relates to compounds of the Formula (I)-(IX):, as defined herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- α combinations thereof.
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Cannabinoid receptor ligands (Thu, 01 Apr 2010)
There are disclosed compounds of the formula (I), or a pharmaceutically acceptable salt of the compound, which exhibit anti-inflammatory and immunomodulatory activity. Also disclosed are pharmaceutical compositions containing said compounds.
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P1-NONEPIMERIZABLE KETOAMIDE INHIBITORS OF HCV NS3 PROTEASE (Fri, 26 Mar 2010)
<p id="p-0001-en" num="0000">The present invention discloses novel compounds, which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.</p>
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FUNCTIONALLY SELECTIVE AZANITRILE ALPHA2C ADRENORECEPTOR AGONISTS (Fri, 26 Mar 2010)
In its many embodiments, the present invention provides a novel class of azanitrile compounds as inhibitors of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.
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Aspartyl protease inhibitors (Fri, 19 Mar 2010)
<p id="p-0001" num="0000">Disclosed are compounds of formula I (Chemical formula should be inserted here as it appears on abstract in paper form) Formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>14</sup>, V, W, X, Y, Z, p, and ring A are as described in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m<sub>1 </sub>agonist or m<sub>2 </sub>antagonist.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="34.12mm" wi="56.22mm" file="US08093254-20120110-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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PYRROLO [3, 2-A] PYRIDINE DERIVATIVES FOR INHIBITING KSP KINESIN ACTIVITY (Fri, 19 Mar 2010)
<p id="p-0001-en" num="0000">The present invention provides compounds of Formula I (wherein R, R<sup>1</sup>, R<sup>3</sup>, R<sup>4</sup>, X, and ring Y are as defined herein). The present invention also provides compositions comprising these compounds that are useful for treating cellular proliferative diseases or disorders associated with KSP kinesin activity and for inhibiting KSP kinesin activity.</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="25.57mm" wi="55.96mm" file="us20100068181a1-20100318-c00001.tif" img-content="chem" img-format="tif"/> </chemistry> </p>
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MAMMALIAN CHEMOKINES; RECEPTORS; REAGENTS; USES (Fri, 19 Mar 2010)
<p id="p-0001-en" num="0000">Novel chemokines and 7 transmembrane receptors from mammals, reagents related thereto, including purified proteins, specific antibodies, and nucleic acids encoding the chemokines and receptors are disclosed. Methods of using the chemokines, receptors, reagents and diagnostic kits are also provided.</p>
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PROCESS FOR PREPARING CCR-5 RECEPTOR ANTAGONISTS UTILIZING 4-SUBSTITUTED 1-CYCLOPROPANE-SULFONYL-PIPERIDINYL COMPOUNDS (Fri, 12 Mar 2010)
<p id="p-0001-en" num="0000">The present invention discloses a novel process to prepare 4-substituted 1-Cyclopropane-sulfonyl-Piperidinyl compounds, which are useful intermediates for the preparation of antagonists of CCR5 receptor and therefore useful for the treatment of HIV virus infected mammals. It specifically discloses a novel process to synthesize 4-[4-[(R)-[1-[cyclopropylsulfonyl)-4-piperidinyl](3-fluorophenyl)methyl]-3(S)-methyl-1-piperazinyl]-1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]-4-methylpiperidine] compounds.</p>
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ENGINEERED ANTI-IL-23R ANTIBODIES (Fri, 12 Mar 2010)
Antibodies to human IL-23R are provided, as well as uses thereof, e.g. in treatment of inflammatory, autoimmune, and proliferative disorders.
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POLYCYCLIC INDAZOLE DERIVATIVES AND THEIR USE AS ERK INHIBITORS FOR THE TREATMENT OF CANCER (Wed, 10 Mar 2010)
Disclosed are the ERK inhibitors of formula 1.0: (Chemical formula should be inserted here as it appears on abstract in paper form) and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0. COPYRIGHT KIPO WIPO 2010
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2-aminothiazole-4-carboxylic amides as protein kinase inhibitors (Fri, 05 Mar 2010)
<p id="p-0001" num="0000">The present invention relates to novel Anilinopiperazine Derivatives of formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="35.81mm" wi="62.57mm" file="US08227605-20120724-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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POLYCYCLIC GUANINE DERIVATIVES AND METHODS OF USE THEREOF (Thu, 04 Mar 2010)
The present invention relates to Polycyclic Guanine Derivatives, compositions comprising the Polycyclic Guanine Derivatives and methods of using the Polycyclic Guanine Derivatives to treat pain or an inflammatory disease. COPYRIGHT KIPO WIPO 2010
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SUBSTITUTED PYRIDINE AND PYRIMIDINE DERIVATIVES AND THEIR USE IN TREATING VIRAL INFECTIONS (Fri, 26 Feb 2010)
The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19 and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders.
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ETHYNYL-SUBSTITUTED PYRIDINE AND PYRIMIDINE DERIVATIVES AND THEIR USE IN TREATING VIRAL INFECTIONS (Fri, 26 Feb 2010)
The present invention provides compounds of Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19 and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing dieases or disorders such as viral infections and virus-related disorders.
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ETHENYL-SUBSTITUTED PYRIDINE AND PYRIMIDINE DERIVATIVES AND THEIR USE IN TREATING VIRAL INFECTIONS (Fri, 26 Feb 2010)
The present invention provides compounds of Formula (A): (Chemical formula should be inserted here as it appears on abstract in paper form) (A) and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19, R22, R23, and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing dieases or disorders such as viral infections and virus-related disorders.
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AZO-SUBSTITUTED PYRIDINE AND PYRIMIDINE DERIVATIVES AND THEIR USE IN TREATING VIRAL INFECTIONS (Fri, 26 Feb 2010)
The present invention provides compounds of Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19, and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing dieases or disorders such as viral infections and virus-related disorders.
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AZO-SUBSTITUTED PYRIDINE AND PYRIMIDINE DERIVATIVES AND THEIR USE IN TREATING VIRAL INFECTIONS (Fri, 26 Feb 2010)
The present invention provides compounds of Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19, and n is selected independently and as defmed herein. Compositions comprising such compounds are also pro- vided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing dieases or disorders such as viral infections and virus-related disorders. </p>
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ETHYNYL-SUBSTITUTED PYRIDINE AND PYRIMIDINE DERIVATIVES AND THEIR USE IN TREATING VIRAL INFECTIONS (Fri, 26 Feb 2010)
The present invention provides com-pounds of Formula (I): (Chemical formula should be in-serted here as it appears on abstract in paper form) (I) and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and pro-drugs of said compounds, wherein wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19 and n is selected independently and as defined herein. Compo-sitions comprising such compounds are also provided. The compounds of the invention are effective as in-hibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing dieas-es or disorders such as viral infections and virus-related disorders. </p>
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SUBSTITUTED PYRIDINE AND PYRIMIDINE DERIVATIVES AND THEIR USE IN TREATING VIRAL INFECTIONS (Fri, 26 Feb 2010)
The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and pro-drugs of said compounds, wherein wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19 and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders. </p>
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GAMMA SECRETASE MODULATORS (Fri, 26 Feb 2010)
In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions. COPYRIGHT KIPO WIPO 2010
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ETHENYL-SUBSTITUTED PYRIDINE AND PYRIMIDINE DERIVATIVES AND THEIR USE IN TREATING VIRAL INFECTIONS (Fri, 26 Feb 2010)
<br/>The present invention provides compounds of Formula (A):<br/>(See Formula A)<br/>and tautomers, isomers, and esters of said compounds, and pharmaceutically <br/>acceptable <br/>salts, solvates, and prodrugs of said compounds, wherein each of R, R1, X, Y, <br/>Z, R2, R3,<br/>R4, R5, R6, R7, R8, R9, R18, R19 and n is selected independently and as <br/>defined herein.<br/>Compositions comprising such compounds are also provided. The compounds of the <br/><br/>invention are effective as inhibitors of HCV, and are useful, alone and <br/>together with other <br/>therapeutic agents, in treating or preventing diseases or disorders such as <br/>viral infections <br/>and virus-related disorders.<br/></p>
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Anti-mitotic agent and aurora kinase inhibitor combination as anti-cancer treatment (Fri, 26 Feb 2010)
The present invention relates to a method of treating cancer by pretreatment with anti-mitotic agents followed by at least one aurora kinase inhibitor. Extensive illustrations are provided for the antimitotic agents and aurora kinase inhibitors that are useful in the inventive treatment.
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IL-B30 antibodies (Fri, 19 Feb 2010)
<p id="p-0001" num="0000">Purified genes encoding cytokine referred to as interleukin-B30 (IL-B30) from a mammal, reagents related thereto including purified proteins, specific antibodies, and nucleic acids encoding this molecule are provided. Methods of using said reagents and diagnostic kits are also provided.</p>
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GAMMA SECRETASE MODULATORS (Wed, 17 Feb 2010)
In its many embodiments, the present invention provides a novel class of heterocycliccompounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions. COPYRIGHT KIPO WIPO 2010
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SYNTHESIS OF CCR5 RECEPTOR ANTAGONISTS (Fri, 12 Feb 2010)
<p id="p-0001-en" num="0000">The present invention is directed to the synthesis of 4-[4-[(R)-[1-[cyclopropylsulfonyl)-4-piperidinyl](3-fluorophenyl)methyl]-3(S)-methyl-<b>1</b>-piperazinyl]-1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]-4-methylpiperidine], and intermediates therefor from readily available starting materials by a novel route.</p>
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UREA DERIVATIVES AS ANTIBACTERIAL AGENTS (Fri, 12 Feb 2010)
This invention relates to compounds of the Formula (I):or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which is useful for the treatment of diseases or conditions mediated by LpxC.
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CYCLOPROPYLCHROMENE DERIVATIVES AS MODULATORS OF THE ALPHA-2C RECEPTOR (Fri, 12 Feb 2010)
In its many embodiments, the present invention provides a novel class of cyclopropylchromene derivatives as modulators of a2C adrenergic receptor, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the a2C adrenergic receptors using such compounds or pharmaceutical compositions.
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UREA DERIVATIVES AS ANTIBACTERIAL AGENTS (Fri, 12 Feb 2010)
This invention relates to compounds of the Formula (1):or a pharmaceutically acceptable salt, solvate, ester or iso-mer thereof, which is useful for the treatment of diseases or conditions mediated by LpxC. </p>
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ENGINEERED ANTI-IL-23R ANTIBODIES (Thu, 11 Feb 2010)
Antibodies to human IL-23R are provided, as well as uses thereof, e.g. in treatment of inflammatory, autoimmune, and proliferative disorders. COPYRIGHT KIPO WIPO 2010
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PREPARATION OF KETONE AMIDES (Fri, 05 Feb 2010)
<p id="p-0001-en" num="0000">The present invention discloses a novel process to prepare ketone amides, which are useful intermediates for the preparation of antagonists of CCR5 receptor and therefore useful for the treatment of HIV virus infected mammals. It specifically discloses a novel process to synthesize 1-(2,4-dimethylpyrimidine-5-carbonyl)-4-piperidone, 1-[(2,4-dimethyl-3-pyridinyl)carbonyl]-4-piperidone and related compounds. A salient feature of the invention is the use of a three-phase reaction medium with an organic phase and a buffer salt slurry.</p>
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Extended release oral dosage composition (Fri, 29 Jan 2010)
<p id="p-0001" num="0000">A bilayer solid composition comprising (a) an immediate release first layer comprising an anti-allergic effective amount of desloratadine and at least one pharmaceutically acceptable excipient and (b) a sustained release second layer comprising an effective amount of a nasal decongestant, e.g. pseudoephedrine sulfate and a pharmaceutically acceptable sustained release agent wherein the composition contains less than about 2% of desloratadine decomposition products is disclosed. A solid composition comprising an anti-allergic effective amount of desloratadine and at least one, and preferably two pharmaceutically acceptable antioxidants is also disclosed.</p>
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3,4-DI-SUBSTITUTED CYCLOBUTENE-1,2-DIONES AS CXC-CHEMOKINE RECEPTOR LIGANDS (Wed, 27 Jan 2010)
There are disclosed compounds of Formula (I) or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acuteand chronic inflammatory disorders and cancer. COPYRIGHT KIPO WIPO 2010
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BICYCLIC HETEROCYCLE DERIVATIVES AND USE THEREOF AS GPR119 MODULATORS (Fri, 22 Jan 2010)
The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) such as GPR119 in a patient.
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NIACIN DERIVATIVES USEFUL TO TREAT METABOLIC SYNDROMES (Fri, 22 Jan 2010)
The present invention provides compounds of the Formula I: (I) wherein R' represents a recoverable residue of a non-steroidal anti-inflammatory drug (NSAID); and G represents a hydrolysable or metabolizable linker group; and salts, solvates, esters and prodrugs thereof, as well as pharmaceutical compositions containing them, and methods of using them to treat metabolic syndrome, dyslipidemia, cardiovascular diseases, disorders of the peripheral and central nervous system, hematological diseases, cancer, inflammation, respiratory diseases, gastroenterological diseases, diabetes, and non-alcoholic fatty liver diseases.
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NICOTINIC ACID RECEPTOR AGONIST COMPOUNDS USEFUL TO TREAT METABOLIC SYNDROMES (Fri, 22 Jan 2010)
The present invention provides compounds of the Formula (I) wherein R' represents a recoverable residue of a non-steroidal anti-inflammatory drug (NSAID); G represents a hydrolysable or metabolizable linker group; and R represents a recoverable residue of a nicotinic acid receptor agonist; and salts, solvates, esters and prodrugs thereof, as well as pharmaceutical compositions containing them, and methods of using them to treat metabolic syndrome, dyslipidemia, cardiovascular diseases, disorders of the peripheral and central nervous system, hematological diseases, cancer, inflammation, respiratory diseases, gastroenterological diseases, diabetes, and non-alcoholic fatty liver diseases.
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BICYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF (Fri, 22 Jan 2010)
The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient. The compounds are of structure (I).
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BICYCLIC HETEROCYCLE DERIVATIVES AND THEIR USE AS GPCR MODULATORS (Fri, 22 Jan 2010)
The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient.
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ACETYLSALICYCLIC ACID DERIVATIVES USEFUL TO TREAT METABOLIC SYNDROMES (Fri, 22 Jan 2010)
The present invention provides compounds of the Formula I: (I) wherein G represents a hydrolysable or metabolizable linker group; and R represents a recoverable residue of a nicotinic acid receptor agonist; and salts, solvates, esters and prodrugs thereof, as well as pharmaceutical compositions containing them, and methods of using them to treat metabolic syndrome, dyslipidemia, cardiovascular diseases, disorders of the peripheral and central nervous system, hematological diseases, cancer, inflammation, respiratory diseases, gastroenterological diseases, diabetes, and non-alcoholic fatty liver diseases.
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BICYCLIC HETEROCYCLE DERIVATIVES AND USE THEREOF AS GPR119 MODULATORS (Fri, 22 Jan 2010)
The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bi-cyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, dia-betes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) such as GPR119 in a patient. </p>
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BICYCLIC HETEROCYCLE DERIVATIVES AND THEIR USE AS GPCR MODULATORS (Fri, 22 Jan 2010)
The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient. </p>
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BICYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF (Fri, 22 Jan 2010)
The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a. G protein-coupled receptor (GPCR) in a patient. The compounds are of structure (I) </p>
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Polycyclic Guanine Derivatives and use thereof (Fri, 22 Jan 2010)
The present invention relates to Polycyclic Guanine Derivatives, compositions comprising the Polycyclic Guanine Derivatives and methods of using the Polycyclic Guanine Derivatives to treat pain or an inflammatory disease.
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PROCESS FOR PREPARING SUBSTITUTED 5-AMINO-PYRAZOLO-[4,3-e]-1,2,4-TRIAZOLO[1,5-c]PYRIMIDINES (Fri, 01 Jan 2010)
<p id="p-0001-en" num="0000">A process for preparing substituted 5-amino-pyrazolo[4,3-e]-1,2,4-triazolo-[1,5-c]pyrimidine compounds having an aminoalkyl substituent at the 7-position is disclosed, wherein the pyrimidine ring is cyclized using a cyanating agent.</p>
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OX2 RECEPTOR HOMOLOGS (Fri, 01 Jan 2010)
Nucleic acids encoding mammalian, e.g., primate, receptors of OX2, purified proteins and fragments thereof. Antibodies, both polyclonal and monoclonal, are also provided. Method of using the compositions for both diagnostic and therapeutic utilities are described. COPYRIGHT KIPO WIPO2010
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NOVEL PSYMBERIN DERIVATIVES, COMPOSITIONS, AND THEIR USE AS ANTINEOPLASTIC AGENTS (Thu, 31 Dec 2009)
The present invention provides compounds according to Formula (I): or pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, and isomers thereof, wherein: ring A, n, q, R1, R2, R3, R4, R5, R6, each R7, each R7A, and R8 are each selected independently of each other and as defined herein. The invention also provides pharmaceutical compositions comprising such compounds (optionally in combination with one or more additional active ingredients), and methods for their use in treating or preventing a wide range of cancers.
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SYNTHESIS AND USE OF HETEROCYCLIC ANTIBACTERIAL AGENTS (Thu, 31 Dec 2009)
This invention relates to compounds of the following Formula (I); or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which is useful for the treatment of diseases or conditions mediated by LpxC.
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SYNTHESIS AND USE OF HETEROCYCLIC ANTIBACTERIAL AGENTS (Thu, 31 Dec 2009)
This invention relates to compounds of the following Formula (I); or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which is useful for the treatment of diseases or conditions mediated by LpxC. </p>
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Mammalian CX<sub>3</sub>C chemokine antibodies (Fri, 25 Dec 2009)
<p id="p-0001-en" num="0000">Nucleic acids encoding a new family of chemokines, the CX3C family, from a mammal, reagents related thereto, including specific antibodies, and purified proteins are described. Methods of using said reagents and related diagnostic kits are also provided.</p>
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Gamma secretase modulators (Fri, 25 Dec 2009)
In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
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PROCESS AND INTERMEDIATES FOR THE PREPARATION OF 3-(AMINO)-3-CYCLOBUTYLMETHYL-2-HYDROXY-PROPIONAMIDE OR SALTS THEREOF (Fri, 18 Dec 2009)
<p id="p-0001-en" num="0000">In one embodiment, the present application relates to a process of making a compound of formula I:</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="25.99mm" wi="53.68mm" file="us20090312576a1-20091217-c00001.tif" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003-en" num="0000">and to certain intermediate compounds that are made within the process of making the compound of formula I.</p>
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Cyclic amine bace-1 inhibitors having a heterocyclic substituent (Fri, 18 Dec 2009)
<p id="p-0001" num="0000">Disclosed are novel compounds of the formula</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="28.79mm" wi="58.84mm" file="US07910590-20110322-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a pharmaceutically acceptable salt or solvate thereof, wherein <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">R<sup>1 </sup>is</li> </ul> </li> </ul> </p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="105.24mm" wi="68.75mm" file="US07910590-20110322-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0003" list-style="none"> <li id="ul0003-0001" num="0000"> <ul id="ul0004" list-style="none"> <li id="ul0004-0001" num="0000">X is —O—, —C(R <sup>14</sup>)<sub>2</sub>— or —N(R)—;</li> <li id="ul0004-0002" num="0000">Z is —C(R<sup>14</sup>)<sub>2</sub>— or —N(R)—;</li> <li id="ul0004-0003" num="0000">t is 0, 1, 2 or 3;</li> <li id="ul0004-0004" num="0000">each R and R<sup>2 </sup>is independently H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, alkenyl or alkynyl;</li> <li id="ul0004-0005" num="0000">each R<sup>14 </sup>is H, alkyl, alkenyl, alkynyl, halo, —CN, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, —OR<sup>35</sup>, —N(R<sup>24</sup>)(R<sup>25</sup>) or —SR<sup>35</sup>;</li> <li id="ul0004-0006" num="0000">R<sup>41 </sup>is alkyl, cycloalkyl, —SO<sub>2</sub>(alkyl), —C(O)-alkyl, —C(O)-cycloalkyl or -alkyl-NH—C(O)CH<sub>3</sub>; <br/> and the remaining variables are as defined in the specification. </li> </ul> </li> </ul> </p> <p id="p-0004" num="0000">Also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating cognitive or neurodegenerative diseases with compounds of formula I.</p> <p id="p-0005" num="0000">Also disclosed are pharmaceutical compositions and methods of treatment comprising compounds of formula I in combination with other agents useful in treating cognitive or neurodegenerative diseases.</p>
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TRICYCLIC INDOLE DERIVATIVES AND METHODS OF USE THEREOF (Fri, 18 Dec 2009)
The present invention relates to Tricyclic Indole Derivatives, compositions comprising at least one Tricyclic Indole Derivatives, and methods of using the Tricyclic Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient
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TRICYCLIC INDOLE DERIVATIVES AND METHODS OF USE THEREOF (Fri, 18 Dec 2009)
The present invention relates to Tricyclic Indole Derivatives, compositions comprising at least one Tricyclic Indole Derivatives, and methods of using the Tricyclic Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient </p>
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3,4-di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands (Fri, 11 Dec 2009)
<p id="p-0001" num="0000">There are disclosed compounds of the formula</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="19.90mm" wi="69.85mm" file="US07947720-20110524-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer. </p>
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Heterocyclic aspartyl protease inhibitors (Fri, 11 Dec 2009)
<p id="p-0001" num="0000">Disclosed are compounds of the formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.23mm" wi="47.16mm" file="US08178513-20120515-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W, U, X, R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, and R<sup>4 </sup>are as defined herein, and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of using such compounds to inhibit aspartyl protease and to treat a variety of disease or disorders, including cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic antagonist </p>
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HETEROCYCLIC COMPOUNDS AS FACTOR IXA INHIBITORS (Fri, 27 Nov 2009)
The present invention relates to novel heterocyclic compounds of Formulae I-III; as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder.
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BICYCLIC HETEROCYCLE DERIVATIVES AND USE THEREOF AS GPR119 MODULATORS (Fri, 27 Nov 2009)
The present invention relates to Bicyclic Heterocycle Derivatives of formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR1 19 in a patient.
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BICYCLIC HETEROCYCLE DERIVATIVES AND USE THEREOF AS GPR119 MODULATORS (Fri, 27 Nov 2009)
The present invention relates to Bicyclic Heterocycle Derivatives of formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR1 19 in a patient. </p>
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HETEROCYCLIC COMPOUNDS AS FACTOR IXA INHIBITORS (Fri, 27 Nov 2009)
The present invention relates to novel heterocyclic compounds of Formulae I-III; as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder. <img he="0" wi="0" file="" alt="" img-content="undefined" img-format="jpg" inline="yes" orientation="portrait"/> </p>
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Exo- and diastereo-selective syntheses of himbacine analogs (Fri, 13 Nov 2009)
<p id="p-0001" num="0000">This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center. The chemistry taught herein can be exemplified by the following:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="77.64mm" wi="75.86mm" file="US07989653-20110802-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Monoclonal antibodies to human CTLA-8 (IL-17A) (Fri, 06 Nov 2009)
<p id="p-0001" num="0000">Human CTLA-8 protein, antibodies that specifically bind to human CTLA-8, and nucleic acids encoding human CTLA-8. Methods of using these molecules and diagnostic kits are also provided.</p>
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ENGINEERED ANTI-IL-23P19 ANTIBODIES (Wed, 04 Nov 2009)
Engineered antibodies to human IL-23p19 are provided, as well as uses thereof, e.g., in treatment of inflammatory, autoimmune, and proliferative disorders. COPYRIGHT KIPO&WIPO 2010
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HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS (Wed, 04 Nov 2009)
Disclosed are compounds of the formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond,-C(=S)-,-S(O)-,-S(O)2-,-C(=O)-,-O-,-C(R6)(R7)-,-N(R5)-or-C(=N(R5))-; X is-O-,-N(R5)-or-C(R6)(R7)-; provided that when X is-O-, U is not-O-,-S(O)-,-S(O)2-,-C(=O)-or-C(=NR5)-; U is a bond,-S(O)-,-S(O)2-,-C(O)-,-O-,-P(O)(OR15)-,-C(=NR5)-,-(C(R6)(R7))b-or-N(R5)-; wherein b is 1 or 2; provided that when W is-S(O)-,-S(O)2-,-O-, or-N(R5)-, U is not-S(O)-,-S(O)2-,-O-, or-N(R5)-; provided that when X is-N(R5)-and W is-S(O)-,-S(O)2-,-O-, or-N(R5)-, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula (I). Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist. COPYRIGHT KIPO&WIPO 2010
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THIOPHENYL-SUBSTITUTED 2-IMINO-3-METHYL PYRROLO PYRIMIDINONE COMPOUNDS AS BACE-1 INHIBITORS, COMPOSITIONS, AND THEIR USE (Fri, 30 Oct 2009)
In its many embodiments, the present invention provides provides certain thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidone compounds, including compounds (or tautomers or a pharmaceutically acceptable salts thereof) having the structural Formula (III): wherein R2, R3, R4, R5, R6, R7, R8, and R9 are each selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds, and methods for their preparation and use in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimer's Disease, are also disclosed.
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PHENYL-SUBSTITUTED 2-IMINO-3-METHYL PYRROLO PYRIMIDINONE COMPOUNDS AS BACE-1 INHIBITORS, COMPOSITIONS, AND THEIR USE (Fri, 30 Oct 2009)
In its many embodiments, the present invention provides provides certain 2-imino-3-methyl pyrrolo pyrimidone compounds, including compounds Formula (II): and include tautomers, steroisomers, or pharmaceutically acceptable salts or solvates of said compounds, stereoisomers, or said tautomers, wherein R2, R3, R4, R5, R6, R7, R8, and R9 are each selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds, and methods for their preparation and use in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimer's Disease, are also disclosed.
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THIOPHENYL-SUBSTITUTED 2-IMINO-3-METHYL PYRROLO PYRIMIDINONE COMPOUNDS AS BACE-1 INHIBITORS, COMPOSITIONS, AND THEIR USE (Fri, 30 Oct 2009)
In its many embodiments, the present invention provides provides certain thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidone compounds, including compounds (or tautomers or a pharmaceutically acceptable salts thereof) having the structural Formula (III): wherein R2, R3, R4, R5, R6, R7, R8, and R9 are each selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds, and methods for their preparation and use in treating pathologies associated with amyloid beta (A.BETA.) protein, including Alzheimer's Disease, are also disclosed. </p>
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FUNCTIONALLY SELECTIVE ALPHA2C ADRENORECEPTOR AGONISTS (Fri, 30 Oct 2009)
2C adrenergic receptors using such compounds or pharmaceutical compositions. COPYRIGHT KIPO&WIPO 2010
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PHENYL-SUBSTITUTED 2-IMINO-3-METHYL PYRROLO PYRIMIDINONE COMPOUNDS AS BACE-1 INHIBITORS, COMPOSITIONS, AND THEIR USE (Fri, 30 Oct 2009)
In its many embodiments, the present invention provides provides certain 2- imino-3-methyl pyrrolo pyrimidone compounds, including compounds Formula (II): and include tautomers, steroisomers, or pharmaceutically acceptable salts or solvates of said compounds, stereoisomers, or said tautomers, wherein R2, R3, R4, R5, R6, R7, R8, and R9 are each selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds, and methods for their preparation and use in treating pathologies associated with amyloid beta (A.beta.) protein, including Alzheimer's Disease, are also disclosed. </p>
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3,4-DIHYDR0-L,4-BENZ0XAZINE, 3, 4-DIHYDR0-1, 4-BENZOTHIAZINE AND 1,2,3,4-TETRAHYDRO-QUINOXALINE DERIVATIVES AS ALPHA2C ADRENORECEPTOR AGONISTS (Tue, 27 Oct 2009)
The present invention relates to a novel class of phenylmorpholine and phenyl thiomorpholine compoundsuseful as alpha2C adrenergic receptor agonists, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition,-or amelioration of one or more diseases associated with the alpha2C adrenergic receptor agonists, such as allergic rhinitis, congestion, pain, diarrhea, glaucoma, congestive heart failure, cardiac ischemia, manic disorders, depression, anxiety and schizophrenia. COPYRIGHT KIPO&WIPO 2010
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FUNCTIONALLY SELECTIVE ALPHA2C ADRENORECEPTOR AGONISTS (Sat, 24 Oct 2009)
In its many embodiments, the present invention provides a novel class of indolines as inhibitors of E2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the E2C adrenergic receptors using such compounds or pharmaceutical compositions. COPYRIGHT KIPO&WIPO 2010
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MAMMALIAN CELL MEMBRANE PROTEINS; RELATED REAGENTS (Fri, 23 Oct 2009)
<p id="p-0001-en" num="0000">The purification and isolation of various genes which encode mammalian cell surface polypeptides. Nucleic acids, proteins, antibodies, and other reagents useful in modulating development of cells, e.g., lymphoid and myeloid, are provided, along with methods for their use.</p>
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Heterocyclic aspartyl protease inhibitors (Fri, 16 Oct 2009)
<p id="p-0001" num="0000">Disclosed are compounds of the formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.31mm" wi="47.24mm" file="US07973067-20110705-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">W is a bond, —C(═S)—, —S(O)—, —S(O)<sub>2</sub>—, —C(═O)—, —O—, —C(R<sup>6</sup>)(R<sup>7</sup>)—, —N(R<sup>5</sup>)— or —C(═N(R<sup>5</sup>))—;</li> <li id="ul0002-0002" num="0000">X is —O—, —N(R<sup>5</sup>)— or —C(R<sup>6</sup>)(R<sup>7</sup>)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)<sub>2</sub>—, —C(═O)— or —C(═NR<sup>5</sup>)—;</li> <li id="ul0002-0003" num="0000">U is a bond, —S(O)—, —S(O)<sub>2</sub>—, —C(O)—, —O—, —P(O)(OR<sup>15</sup>)—, —C(═NR<sup>5</sup>)—, —(C(R<sup>6</sup>)(R<sup>7</sup>))<sub>b</sub>— or —N(R<sup>5</sup>)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)<sub>2</sub>—, —O—, or —N(R<sup>5</sup>)—, U is not —S(O)—, —S(O)<sub>2</sub>—, —O—, or —N(R<sup>5</sup>)—; provided that when X is —N(R<sup>5</sup>)— and W is —S(O)—, —S(O)<sub>2</sub>—, —O—, or —N(R<sup>5</sup>)—, then U is not a bond;</li> <li id="ul0002-0004" num="0000">and R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>6</sup>, and R<sup>7 </sup>are as defined in the specification; <br/> and pharmaceutical compositions comprising the compounds of formula I. </li> </ul> </li> </ul> </p> <p id="p-0003" num="0000">Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes.</p> <p id="p-0004" num="0000">Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m<sub>1 </sub>agonist or m<sub>2 </sub>antagonist.</p>
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4, 5-RING ANNULATED INDOLE DERIVATIVES FOR TREATING OR PREVENTING OF HCV AND RELATED VIRAL INFECTIONS (Sat, 10 Oct 2009)
The present invention relates to 4, 5-ring annulated indole derivatives of formula (I), compositions comprising at leas t one 4, 5-ring annulated indole derivatives, and methods of using the 4, 5-ring annulated ^ndole derivatives for treating or preventing a viral inf ection or a virus-related disorder in a patient, (I) wherein ring Z of formula (I), is cyclohexyl, cyclohexenyl, 6-membered heterocycloalkyl, 6-membered heterocycloalkenyl, 6-membered aryl or 6-membered heteroaryl, wherein R1, R2, R3, R6. R7 and R10 are as described herein. COPYRIGHT KIPO&WIPO 2010
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Process and intermediates for the preparation of (1<i>R</i>,2<i>S</i>,5<i>S</i>)-6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylates or salts thereof (Fri, 02 Oct 2009)
<p id="p-0001-en" num="0000">In one embodiment, the present application relates to a process of making a compound of formula I.</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="26.75mm" wi="58.84mm" file="US07728165-20100601-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> and to certain intermediate compounds that are made within the process of making the compound of formula I. </p>
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SPIRO SUBSTITUTED CYCLOPROPANE COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS (Fri, 25 Sep 2009)
<p id="p-0001-en" num="0000">A compound of the Formula I:</p> <p id="p-0002-en" num="0000"/> <p id="p-0003-en" num="0000">or a pharmaceutically acceptable salt, solvate or isomer thereof, can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-α or combinations thereof.</p>
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Process for the preparation of 6,6-dimethyl-3-azabicyclo-[3.1.0]-hexane compounds and enantiomeric salts thereof (Fri, 25 Sep 2009)
<p id="p-0001-en" num="0000">The present invention provides for a process for preparing racemic methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate, its corresponding salt: (2S, 3R, 4S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate di-p-toluoyl-D-tartaric acid (“D-DTTA”) salt or a (2R, 3S, 4R)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate di-p-toluoyl-L-tartaric acid salt (“L-DTTA”) in a high enantiomeric excess. This invention also provides for a process for preparing a (2S, 3R, 4S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate dibenzoyl-D-tartaric acid (“D-DBTA”) salt or a (2R, 3S, 4R)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate L-tartaric acid (“L-DBTA”) salt in a high enantiomeric excess. Further, this invention provides a process for preparing intermediates II, IIB, III, IV, IV salt, V, VI, and VII.</p>
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AMINO-QUINOXALINE AND AMINO-QUINOLINE COMPOUNDS FOR USE AS ADENOSINE A2A RECEPTOR ANTAGONISTS (Sat, 12 Sep 2009)
Compounds of the Formula (I), where W represents CH or N; and Q represents -CN, -C(=NOH)NH2, -CONHR1 or various herein described heterocyclic radicals; as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof are adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.
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1,2,4-TRIAZOLO[4,3-C]PYRIMIDIN-3-ONE AND PYRAZOLO [4,3-E] -1,2,4-TRIAZOLO [4,3-C] PYRIMIDIN-3-ONE COMPOUNDS FOR USE AS ADENOSINE A2A RECEPTOR ANTAGONISTS (Sat, 12 Sep 2009)
Compounds of the Formula I wherein R1 and R2 together with the carbon atoms to which they are bonded optionally form a further heteroaromatic ring of the formula (II) as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof are adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.
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1,2,4-TRIAZOLO[4,3-C]PYRIMIDIN-3-ONE AND PYRAZOLO [4,3-E] -1,2,4-TRIAZOLO [4,3-C] PYRIMIDIN-3-ONE COMPOUNDS FOR USE AS ADENOSINE A2A RECEPTOR ANTAGONISTS (Sat, 12 Sep 2009)
Compounds of the Formula I wherein R1 and R2 together with the carbon atoms to which they are bonded optionally form a further heteroaromatic ring of the formula (II) as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof are adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease. </p>
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AMINO-QUINOXALINE AND AMINO-QUINOLINE COMPOUNDS FOR USE AS ADENOSINE A2A RECEPTOR ANTAGONISTS (Sat, 12 Sep 2009)
Compounds of the Formula (I), where W represents CH or N; and Q represents - CN, -C(=NOH)NH2, -CONHR1 or various herein described heterocyclic radicals; as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof are adenosine A2. receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease. </p>
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Functionally selective alpha2C adrenoreceptor agonists (Fri, 11 Sep 2009)
In its many embodiments, the present invention provides a novel class of indolines as inhibitors of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.
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Modified tumor necrosis factor-alpha converting enzyme and methods of use thereof (Fri, 04 Sep 2009)
<p id="p-0001-en" num="0000">The present invention discloses a modified tumor necrosis factor-alpha converting enzyme (TACE) catalytic domain, that unlike the native TACE catalytic domain, is stable at high protein concentrations. The present invention further discloses methods for generating crystals of the modified TACE protein in protein-ligand complexes with a number of inhibitors. In addition, the present invention discloses methods of using the proteins, crystals and/or three-dimensional structures obtained to identify compounds that can modulate the enzymatic activity of TACE.</p>
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GAMMA SECRETASE MODULATORS FOR THE TREATMENT OF ALZHEIMER ' S DISEASE (Fri, 04 Sep 2009)
This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula: Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I).
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GAMMA SECRETASE MODULATORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE (Fri, 04 Sep 2009)
This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula: Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I). </p>
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4,5-RING ANNULATED INDOLE DERIVATIVES FOR TREATING OR PREVENTING OF HCV AND RELATED VIRAL INFECTIONS (Fri, 04 Sep 2009)
The present invention relates to 4,5-ring annulated indole derivatives, compositions comprising at least one 4,5-ring annulated indole derivatives, and methods of using the 4,5-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder ina patient. Wherein ring Z, of formula (I), is a cyclopentyl, cyclopentenyl, 5-membered heterocycloalkyl, 5-membered heterocycloalkenyl or 5-membered heteroaryl ring. COPYRIGHT KIPO&WIPO 2010
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Functionally selective alpha2C adrenoreceptor agonists (Fri, 04 Sep 2009)
In its many embodiments, the present invention provides a novel class of biaryl compounds as inhibitors of ÿ2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ÿ2C adrenergic receptors using such compounds or pharmaceutical compositions.
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3,4-dihydr0-l,4-benz0xazine, 3, 4-dihydr0-1, 4-benzothiazine and 1,2,3,4-tetrahydro-quinoxaline derivatives as alpha2C adrenoreceptor agonists (Fri, 04 Sep 2009)
The present invention relates to a novel class of phenylmorpholine and phenyl thiomorpholine compounds useful as alpha2C adrenergic receptor agonists, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition,- or amelioration of one or more diseases associated with the alpha2C adrenergic receptor agonists, such as allergic rhinitis, congestion, pain, diarrhea, glaucoma, congestive heart failure, cardiac ischemia, manic disorders, depression, anxiety and schizophrenia.
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