CARBOCYCLIC- AND HETEROCYCLIC-SUBSTITUTED HEXAHYDROPYRANO[3,4-d][1,3]THIAZIN-2-AMINE COMPOUNDS (Fri, 27 Jun 2014)
The present invention provides compounds of formula (I), wherein the variables R1, R2, R5 and b are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
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ARYL AND HETEROARYL FUSED LACTAMS (Fri, 27 Jun 2014)
This invention relates to compounds of general Formula (I) in which R1, R2, U, V, L, M, R5, m, X, Y and Z are as defined herein, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.
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Chemical Compounds (Fri, 20 Jun 2014)
<p id="p-0001" num="0000">The present invention relates to imidazopyridazine derivatives. More particularly, it relates to 4-(biphenyl-3-yl)-7H-imidazo[4,5-c]pyridazine derivatives of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="28.96mm" wi="69.09mm" file="US20140171435A1-20140619-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">and pharmaceutically acceptable salts thereof, wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4 </sup>and R<sup>5 </sup>are as defined in the description. The imidazopyridazine derivatives of the present invention modulate the activity of the GABA<sub>A </sub>receptor. They are useful in the treatment of a number of conditions, including pain.</p>
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HEXAHYDROPYRANO [3,4-D][1,3]THIAZIN-2-AMINE COMPOUNDS AS INHIBITORS OF BACE1 (Fri, 20 Jun 2014)
The present invention provides compounds of Formula (I), and the tautomers thereof, and the pharmaceutically acceptable salts of the compounds and tautomers, wherein the compounds have the structure (I) wherein the variables R1, R2, R3, R4 and x are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
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IMIDAZOPYRIDAZINE DERIVATIVES AS GABAA RECEPTOR MODULATORS (Fri, 20 Jun 2014)
Chemical Compounds The present invention relates to imidazopyridazine derivatives. More particularly, it relates to 4-(biphenyl-3-yl)-7H-imidazo[4,5- c]pyridazine derivatives of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R 2, R3, R4 and R5 are as defined in the description. The imidazopyridazine derivatives of the present invention modulate the activity of the GABAA receptor. They are useful in the treatment of a number of conditions, including pain.
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NOVEL SELECTIVE ANDROGEN RECEPTOR MODULATORS (Fri, 13 Jun 2014)
The present invention relates to a compound of Formula 1, 2 or 3: wherein A is N or –CR0 --, where R0 is hydrogen, C1 -C6 linear or branched chain alkyl, etc., Z is –CRe --, or, –N--, where Re is hydrogen, C1 -C6 linear or branched chain alkyl,etc.; R1 is hydrogen, C1 -C6 linear or branched chain alkyl, etc.; R2 are independently hydrogen or C1 -C6 linear or branched chain alkyl; R3 and R4 are independently hydrogen, C1 -C6 linear or branched chain alkyl, etc.;. R5 and R6 are independently hydrogen or C1 -C6 linear or branched chain alkyl, etc.; R8 is hydrogen, C1 -C6 linear or branched chain alkyl, etc.; R9 and R10 are independently hydrogen or C1 -C6 linear or branched chain alkyl, etc.; Q is --CO--, --(CH2 )q --, --(CHRS )q --, or –(CRS Rt )q--, where RS and Rt are independently C1 -C6 linear or branched chain alkyl, aryl, alkylaryl, heteroaryl or alkylheteroaryl; where q is 0, 1, 2, or 3; and, where n is 0, 2, 3, 4 or 5; or, a pharmaceutically acceptable salt thereof, to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly, those affected or mediated by the androgen receptor.
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NOVEL SELECTIVE ANDROGEN RECEPTOR MODULATORS (Fri, 06 Jun 2014)
<p id="p-0001" num="0000">The present invention relates to a compound of Formula 1, 2 or 3:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="128.52mm" wi="64.77mm" file="US20140155390A1-20140605-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein A is N or —CR<sub>0</sub>—, where R<sub>0 </sub>is hydrogen, C<sub>1</sub>-C<sub>6 </sub>linear or branched chain alkyl, etc., Z is —CR<sub>e</sub>—, or, —N—, where R<sub>e </sub>is hydrogen, C<sub>1</sub>-C<sub>6 </sub>linear or branched chain alkyl,etc.; R<sub>1 </sub>is hydrogen, C<sub>1</sub>-C<sub>6 </sub>linear or branched chain alkyl, etc.; R<sub>2 </sub>are independently hydrogen or C<sub>1</sub>-C<sub>6 </sub>linear or branched chain alkyl; R<sub>3 </sub>and R<sub>4 </sub>are independently hydrogen, C<sub>1</sub>-C<sub>6 </sub>linear or branched chain alkyl, etc.;. R<sub>5 </sub>and R<sub>6 </sub>are independently hydrogen or C<sub>1</sub>-C<sub>6 </sub>linear or branched chain alkyl, etc.; R<sub>8 </sub>is hydrogen, C<sub>1</sub>-C<sub>6 </sub>linear or branched chain alkyl, etc.; R<sub>9 </sub>and R<sub>10 </sub>are independently hydrogen or C<sub>1</sub>-C<sub>6 </sub>linear or branched chain alkyl, etc.; Q is —CO—, —(CH<sub>2</sub>)<sub>q</sub>—, —(CHR<sub>s</sub>)<sub>q</sub>—, or (CR<sub>s</sub>R<sub>t</sub>)<sub>q</sub>—, where R<sub>s </sub>and R<sub>t </sub>are independently C<sub>1</sub>-C<sub>6 </sub>linear or branched chain alkyl, aryl, alkylaryl, heteroaryl or alkylheteroaryl; where q is 0, 1, 2, or 3; and, where n is 0, 1, 2, 3, 4 or 5; or, a pharmaceutically acceptable salt thereof, to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly, those affected or mediated by the androgen receptor.</p>
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Process for Forming Amorphous Atorvastatin (Fri, 06 Jun 2014)
<p id="p-0001" num="0000">A process for forming amorphous atorvastatin comprising the steps of dissolving atorvastatin in a non-hydroxylic solvent and removing the solvent by freeze-drying, as well as processes of dissolving atorvastatin in a hydroxylic solvent with a solubilizing agent or an alkalizing agent or an antioxidant and removing the solvent by freeze-drying to afford amorphous atorvastatin.</p>
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Tricyclic Compounds, Compositions, And Methods (Fri, 23 May 2014)
<p id="p-0001" num="0000">The present invention is directed to compounds of Formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="42.67mm" wi="67.48mm" file="US20140142316A1-20140522-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or salt thereof, which are modulators of the glucocorticoid receptor. The compounds and salts of the invention are useful in the treatment of conditions mediated by glucocorticoid receptor activity.</p>
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ANTI-NOTCH3 ANTIBODIES AND ANTIBODY-DRUG CONJUGATES (Fri, 16 May 2014)
The present invention provides for anti-Notch3 antibodies, anti-Notch3 antibody- drug conjugates and methods for preparing and using the same.
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PLATELET-DERIVED GROWTH FACTOR B SPECIFIC ANTIBODIES AND COMPOSITIONS AND USES THEREOF (Fri, 16 May 2014)
The present invention provides antibodies, or antigen-binding fragment thereof, which specifically bind to PDGF-B. The invention further provides a method of obtaining such antibodies and nucleic acids encoding the same. The invention further relates to compositions and therapeutic methods for use of these antibodies for the treatment and/or prevention of PDGF-B mediated diseases, disorders or conditions.
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HETEROAROMATIC COMPOUNDS AS DOPAMINE D1 LIGANDS (Fri, 16 May 2014)
The present invention provides, in part, compounds of Formula I and pharmaceutically acceptable salts thereof and N-oxides of the foregoing; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, salts or N-oxides, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, impulsivity, compulsive gambling, overeating, autism spectrum disorder, MCI, age-related cognitive decline, dementia, RLS, Parkinson's disease, Huntington's chorea, anxiety, depression, MDD, TRD, and bipolar disorder.
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ANTI-IL-13 RECEPTOR ALPHA 2 ANTIBODIES AND ANTIBODY-DRUG CONJUGATES (Fri, 16 May 2014)
Disclosed herein are anti-IL-13-Rα2 antibodies and antibody drug conjugates and methods for preparing and using the same.
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HETEROAROMATIC COMPOUNDS AND THEIR USE AS DOPAMINE D1 LIGANDS (Fri, 16 May 2014)
The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides thereof; processes and intermediates for preparation of; and compositions and uses thereof. The present invention further provides D1 agonists with reduced D1R desensitization, D1 agonists with a reduced β- arrestin recruitment activity relative to Dopamine, D1 agonists interacting significantly with the Ser188 but not significantly with the Ser202 of a D1R when binding to the D1R, D1 agonists interacting less strongly with the Asp103 and interacting less strongly with the Ser198 of a D1R when binding to the D1R, and their uses.
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ANTI-NOTCH3 ANTIBODIES AND ANTIBODY-DRUG CONJUGATES (Fri, 09 May 2014)
<p id="p-0001" num="0000">The present invention provides for anti-Notch3 antibodies, anti-Notch3 antibody-drug conjugates and methods for preparing and using the same.</p>
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HETEROAROMATIC COMPOUNDS AND THEIR USE AS DOPAMINE D1 LIGANDS (Fri, 09 May 2014)
<p id="p-0001" num="0000">The present invention provides, in part, compounds of Formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="34.46mm" wi="61.64mm" file="US20140128374A1-20140508-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">and pharmaceutically acceptable salts thereof and N-oxides of the foregoing; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, salts or N-oxides, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, impulsivity, compulsive gambling, overeating, autism spectrum disorder, MCI, age-related cognitive decline, dementia, RLS, Parkinson's disease, Huntington's chorea, anxiety, depression, MDD, TRD, and bipolar disorder.</p>
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N-Link Hydroxamic Acid Derivatives Useful As Antibacterial Agents (Fri, 09 May 2014)
<p id="p-0001" num="0000">The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.</p>
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BRUTON'S TYROSINE KINASE INHIBITORS (Fri, 09 May 2014)
Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (BTK). Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the BTK inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. (Formula I)
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SPLICEOSTATIN ANALOGS (Fri, 09 May 2014)
The present invention is directed to novel cytotoxic spliceostatin analogs (I) and derivatives, to antibody drug conjugates thereof, and to methods for using the same to treat medical conditions including cancer.
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PROCESS FOR THE PREPARATION OF VORICONAZOLE AND ANALOGUES THEREOF (Fri, 25 Apr 2014)
The present invention provides a process for preparing a compound of formula: (Formula XI and XII) (XI) (XII) wherein X, Y, Z, A, B and E are as defined herein, by reacting a compound of formula: (Formula XIII) (XIII) with a compound of formula: (Formula XIV and XV) (XIV) (XV) respectively, in the presence of a transition metal catalyst, a ligand suitable for use with 15 the catalyst and a reducing agent. The invention also provides novel intermediates.
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TROPOMYOSIN-RELATED KINASE INHIBITORS (Fri, 11 Apr 2014)
The present invention relates to compounds of Formula (IA) and (IB) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as Trk antagonists.
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PYRROLO[3,2-C]PYRIDINE TROPOMYOSIN-RELATED KINASE INHIBITORS (Fri, 11 Apr 2014)
The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as Trk antagonists.
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PYRROLO[2,3-D]PYRIMIDINE TROPOMYOSIN-RELATED KINASE INHIBITORS (Fri, 11 Apr 2014)
The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as Trk antagonists.
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BENZAMIDE AND HETEROBENZAMIDE COMPOUNDS (Fri, 04 Apr 2014)
This invention relates to compounds of general formula (I), in which R1, R2, R6, U, V, W, X, Y and Z are as defined herein, and the pharmaceutically acceptable salts thereof, pharmaceutical compositions containing such compounds and salts, and to methods of using such compounds, salts and compositions.
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Amino-Heterocyclic Compounds (Fri, 28 Mar 2014)
<p id="p-0001" num="0000">The invention provides PDE9-inhibiting compounds of Formula (I),</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="35.22mm" wi="54.95mm" file="US20140088081A1-20140327-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">and pharmaceutically acceptable salts thereof, wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, A, and n are as defined herein. Pharmaceutical compositions containing the compounds of Formula I, and uses thereof in treating neurodegenerative and cognitive disorders, such as Alzheimer's disease and schizophrenia, are also provided.</p>
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Novel Bicyclic Pyridinones (Fri, 28 Mar 2014)
<p id="p-0001" num="0000">Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.86mm" wi="62.06mm" file="US20140088111A1-20140327-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.</p>
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NOVEL BICYCLIC PYRIDINONES (Fri, 28 Mar 2014)
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
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ALKYL-SUBSTITUTED HEXAHYDROPYRANO[3,4-d] [1,3]THIAZIN-2-ANIME COMPOUNDS (Fri, 28 Mar 2014)
Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
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2,3-DIHYDRO-1H-INDEN-1-YL-2,7-DIAZASPIRO[3.5]NONANE DERIVATIVES (Fri, 21 Mar 2014)
<p id="p-0001" num="0000">The present invention provides a compound of Formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.52mm" wi="72.98mm" file="US20140080756A1-20140320-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">a pharmaceutically salt thereof wherein R<sup>1</sup>, R<sup>2</sup>, Ra, L, Z, Z<sup>1 </sup>and Z<sup>2 </sup>are as defined herein, that act as Ghrelin antagonists or inverse agonists; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by the antagonism of the Ghrelin receptor.</p>
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Imidazo[5,1-f][1,2,4]Triazines For The Treatment of Neurological Disorders (Fri, 07 Mar 2014)
<p id="p-0001" num="0000">The present invention relates to compounds of the Formula</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.91mm" wi="52.49mm" file="US20140066622A1-20140306-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">and pharmaceutically acceptable salts thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as a method for the treatment of a disease or condition selected from the group consisting of central nervous system disorders, cognitive disorders, schizophrenia, dementia and other disorders in a mammal.</li> </ul> </li> </ul> </p>
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GLYCOCONJUGATION PROCESSES AND COMPOSITIONS (Fri, 21 Feb 2014)
The invention provides eTEC linked glycoconjugates comprising a saccharide covalently conjugated to a carrier protein through a (2-((2-oxoethyl)thio)ethyl)carbamate (eTEC) spacer, immunogenic compositions comprising such glycoconjugates, and methods for the preparation and use of such glycoconjugates and immunogenic compositions.
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Novel Bicyclic Pyridinones (Fri, 14 Feb 2014)
<p id="p-0001" num="0000">Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="28.70mm" wi="62.57mm" file="US20140045790A1-20140213-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">as defined herein. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.</p>
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INDAZOLES (Fri, 24 Jan 2014)
<p id="p-0001" num="0000">A method of treating a disease or condition for which a JAK inhibitor is indicated in a subject in need of such treatment, comprising administering to the subject a therapeutically effective amount of a compound of formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="56.64mm" wi="69.85mm" file="US20140024634A1-20140123-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, and particularly, a method for the treatment of various inflammatory diseases, particularly psoriasis, asthma and COPD.</p>
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Isoxazole derivatives useful as antibacterial agents (Fri, 24 Jan 2014)
<p id="p-0001" num="0000">The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.</p>
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SACCHARIDES AND USES THEREOF (Fri, 24 Jan 2014)
The invention relates to novel saccharides and uses thereof. In one aspect, the invention relates to a saccharide having a legionaminic acid moiety, a N- acetylgalactosamine moiety, a galactose moiety, and a glucose moiety. In another aspect, the invention relates to a saccharide having an altruronic acid moiety, a fucose moiety, and a glucose moiety. In yet another aspect, the invention relates to a saccharide having a repeating unit of a glycerol phosphate moiety and a glucose moiety, wherein the saccharide is from Enterococcus faecium. In a further aspect, the invention relates to a saccharide having a repeating unit of -6-β-D-Fruf-2, wherein Fru is a fructose moiety, wherein the saccharide is from Enterococcus faecium. In another aspect, the invention relates to an isolated antibody or fragment thereof that specifically binds to a saccharide described herein and uses thereof.
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NOVEL 4-(SUBSTITUTED-AMINO)-7H-PYRROLO[2,3-d]PYRIMIDINES AS LRRK2 INHIBITORS (Sat, 04 Jan 2014)
The present invention provides novel 4,5-disubstituted-7H-pyrrolo[2,3- c/]pyrimidine derivatives of Formula I, and the pharmaceutically acceptable salts thereof wherein R1, R2, R3, R4 and R5 are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.
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Novel 4-(Substituted Amino)-7H-Pyrrolo[2,3-d] Pyrimidines As LRRK2 Inhibitors (Fri, 03 Jan 2014)
<p id="p-0001" num="0000">The present invention provides novel 4,5-disubstituted-7H-pyrrolo[2,3-d]pyrimidine derivatives of Formula I, and the pharmaceutically acceptable salts thereof</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.74mm" wi="54.53mm" file="US20140005183A1-20140102-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4 </sup>and R<sup>5 </sup>are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.</p>
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Salt forms of [R-(R*,R*)]-2-(4-fluorophenyl)-beta, delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid (Fri, 03 Jan 2014)
<p id="p-0001" num="0000">Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.</p>
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N1-Pyrazolospiroketone acetyl-CoA carboxylase inhibitors (Thu, 26 Dec 2013)
The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R 1 , R 2 , R 3 and R 4 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
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TRICYCLIC COMPOUNDS AS KAT II INHIBITORS (Fri, 20 Dec 2013)
Compounds of Formula (I), wherein R1, R 2, X1, Y1, Z1, and Z2 are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other psychiatric, neurodegenerative and/or neurological disorders in mammals, including humans.
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IMPROVED ANTAGONIST ANTIBODIES AGAINST GDF-8 AND USES THEREFOR (Fri, 20 Dec 2013)
The disclosure provides improved neutralizing anti-GDF-8 antibodies capable of substantially higher levels of expression in host cells compared to previous anti-GDF-8 antibodies. Also provided are methods of using compositions comprising such antibodies to increase muscle mass or strength, and to treat or prevent muscular disorders, neuromuscular disorders, metabolic disorders, adipose tissue disorders or bone disorders.
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USE OF GHRELIN RECEPTOR INVERSE AGONISTS OR ANTAGONISTS FOR TREATING SLEEP DISORDERS (Fri, 13 Dec 2013)
The present invention relates to methods of treating sleep disorders in patients comprising administration of a ghrelin receptor inverse agonist or antagonist. The invention also includes methods of treating sleep disorders comprising the administration of a pharmaceutical composition comprising a ghrelin receptor inverse agonist or antagonist and at least one pharmaceutically acceptable carrier, diluent, or excipient.
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PHARMACEUTICAL COMPOSITIONS AND METHODS OF TREATING DRY EYE DISORDERS (Fri, 15 Nov 2013)
<p id="p-0001" num="0000">Ophthalmic compositions comprising Inhibitors of Janus kinase-3 (“Jak3”) are useful for treating dry eye disorders and other disorders requiring the wetting of the eye.</p>
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Heterocyclic Substituted Hexahydropyrano[3,4-d][1,3]Thiazin-2-Amine Compounds (Fri, 08 Nov 2013)
<p id="p-0001" num="0000">Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="41.83mm" wi="55.88mm" file="US20130296308A1-20131107-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.</p>
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N1-PYRAZOLOSPIROKETONE ACETYL-CoA CARBOXYLASE INHIBITORS (Fri, 08 Nov 2013)
<p id="p-0001" num="0000">The invention provides a compound of Formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.94mm" wi="59.61mm" file="US20130296319A1-20131107-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or a pharmaceutically acceptable salt of the compound, wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3 </sup>and R<sup>4 </sup>are as described herein; pharmaceutical compositions thereof and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.</p>
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GLUCAGON RECEPTOR MODULATORS (Fri, 08 Nov 2013)
<p id="p-0001" num="0000">The present invention provides a compound of Formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="19.90mm" wi="65.45mm" file="US20130296355A1-20131107-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or a pharmaceutically acceptable salt thereof wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, A<sup>1</sup>, A<sup>2</sup>, A<sup>3</sup>, A<sup>4</sup>, L, B<sup>1</sup>, B<sup>2</sup>, B<sup>3 </sup>and B<sup>4 </sup>are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.</p>
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2-Thiopyrimidinones (Fri, 08 Nov 2013)
<p id="p-0001" num="0000">Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.</p>
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HETEROCYCLIC SUBSTITUTED HEXAHYDROPYRANO [3,4-D] [1,3] THIAZIN- 2 -AMINE COMPOUNDS AS INHIBITORS OF APP, BACE1 AND BACE 2. (Fri, 08 Nov 2013)
Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I), wherein the variables R1 and R2 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed. The compounds of formula (I) are useful for the treatment of Alzheimer's disease or diabetes.
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Chemical Compounds (Fri, 18 Oct 2013)
<p id="p-0001" num="0000">The invention relates to benzimidazole and imidazopyridine derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new Na<sub>v</sub>1.8 modulators of formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.77mm" wi="59.61mm" file="US20130274243A1-20131017-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or pharmaceutically acceptable salts thereof, wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>6</sup>, R<sup>7</sup>, X and Y are as defined in the description. Na<sub>v</sub>1.8 modulators are potentially useful in the treatment of a wide range of disorders, particularly pain.</p>
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INDOLE AND INDAZOLE COMPOUNDS THAT ACTIVATE AMPK (Fri, 18 Oct 2013)
The present invention relates to indole and indazole compounds of Formula (I) that activate 5' adenosine monophosphate-activated protein kinase (AMPK). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating or preventing diseases, conditions, or disorders ameliorated by activation of AMPK.
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INDOLE AND INDAZOLE COMPOUNDS THAT ACTIVATE AMPK (Fri, 11 Oct 2013)
<p id="p-0001" num="0000">The present invention relates to indole and indazole compounds of Formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.77mm" wi="62.23mm" file="US20130267493A1-20131010-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">that activate 5′ adenosine monophosphate-activated protein kinase (AMPK). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating or preventing diseases, conditions, or disorders ameliorated by activation of AMPK.</p>
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DIACYLGLYCEROL ACYLTRANSFERASE 2 INHIBITORS (Fri, 11 Oct 2013)
Derivatives of purine, 3H-imidazo[4,5-b]pyrimidine and 1H- imidazo[4,5-d]pyrazine of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.
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Monobactams (Fri, 27 Sep 2013)
<p id="p-0001" num="0000">The present invention is directed to a new class of monobactam derivatives and their use for treating bacterial infections.</p>
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Macrocyclic derivatives for the treatment of diseases (Fri, 27 Sep 2013)
<p id="p-0001" num="0000">The invention relates to compounds of formula (Φ)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="43.18mm" wi="58.17mm" file="US08680111-20140325-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">as further defined herein and to the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to the uses thereof. The compounds and salts of the present invention inhibit anaplastic lymphoma kinase (ALK) and/or EML4-ALK and are useful for treating or ameliorating abnormal cell proliferative disorders, such as cancer.</li> </ul> </li> </ul> </p>
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Benzofuranyl derivatives (Fri, 27 Sep 2013)
<p id="p-0001" num="0000">The present invention provides compounds of Formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="47.07mm" wi="69.85mm" file="US08735396-20140527-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. </p>
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NEISSERIA MENINGITIDIS COMPOSITIONS AND METHODS THEREOF (Fri, 20 Sep 2013)
<p id="p-0001" num="0000">In one aspect, the invention relates to an isolated polypeptide comprising an amino acid sequence that is at least 95% identical to SEQ ID NO: 71. In another aspect, the invention relates to an immunogenic composition including an isolated non-lipidated, non-pyruvylated ORF2086 polypeptide from <i>Neisseria meningitidis </i>serogroup B, and at least one conjugated capsular saccharide from a meningococcal serogroup.</p>
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NEISSERIA MENINGITIDIS COMPOSITIONS AND METHODS THEREOF (Fri, 13 Sep 2013)
In one aspect, the invention relates to an isolated polypeptide comprising an amino acid sequence that is at least 95% identical to SEQ ID NO: 71. In another aspect, the invention relates to an immunogenic composition including an isolated non- lipidated, non-pyruvylated ORF2086 polypeptide from Neisseria meningitidis serogroup B, and at least one conjugated capsular saccharide from a meningococcal serogroup.
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MACROCYCLIC DERIVATIVES FOR THE TREATMENT OF PROLIFERATIVE DISEASES (Fri, 13 Sep 2013)
The invention relates to compounds of formula (Φ) as further defined herein and to the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to the uses thereof. The compounds and salts of the present invention inhibit anaplastic lymphoma kinase (ALK) and/or EML4-ALK and are useful for treating or ameliorating abnormal cell proliferative disorders, such as cancer.
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PYRIDINE-2-DERIVATIVES AS SMOOTHENED RECEPTOR MODULATORS (Fri, 16 Aug 2013)
<p id="p-0001" num="0000">The present application relates to compounds of Formula (I), and Formula (II), or pharmaceutically acceptable salt thereof, wherein A, X, Y, Z, e, f, R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>5b</sup>, R<sup>6</sup>, R<sup>7</sup>, R<sup>8</sup>, R<sup>9</sup>, R<sup>10</sup>, R<sup>11</sup>, R<sup>20</sup>, R<sup>21</sup>, R<sup>22 </sup>and R<sup>23 </sup>are defined herein. These novel pyridine derivatives that are useful in therapy, in particular for treating diseases or conditions mediated by Smo, including the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to methods of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="78.66mm" wi="64.35mm" file="US20130210800A1-20130815-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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BENZIIMIDAZOLE AND IMIDAZOPYRIDINE DERIVATIVES AS SODIUM CHANNEL MODULATORS (Fri, 09 Aug 2013)
The invention relates to benzimidazole and imidazopyridine derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new Nav1.8 modulators of formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7. X and Y are as defined in the description. Nav1.8 modulators are potentially useful in the treatment of a wide range of disorders, particularly pain.
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HETEROCYCLIC DERIVATIVES FOR THE TREATMENT OF DISEASES (Fri, 02 Aug 2013)
<p id="p-0001" num="0000">The invention relates to compounds of Formula (1) and to processes for the preparation of intermediates used in the preparation of compositions containing and the uses of such derivatives. The compounds according to the present invention are useful in numerous diseases in which ALK protein is involved or in which inhibition of ALK activity may induce benefit, especially for the treatment of cancer mediated by a mutated EML4-ALK fusion protein.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="33.95mm" wi="60.28mm" file="US20130196952A1-20130801-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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3-AMINOCYCLOPENTANECARBOXAMIDES AS CHEMOKINE RECEPTOR AGONISTS (Fri, 02 Aug 2013)
<p id="p-0001" num="0000">There is provided a compound of Formula I(a) or I(b):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="76.03mm" wi="71.12mm" file="US20130197008A1-20130801-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or a pharmaceutically acceptable salt thereof, wherein the various substitutents are defined herein.</p>
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N1-PYRAZOLOSPIROKETONE ACETYL-CoA CARBOXYLASE INHIBITORS (Fri, 26 Jul 2013)
<p id="p-0001" num="0000">The invention provides a compound of Formula (I) Z N N O N O A1R2 R1 R3R 3 L A2 (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3,Z, A1, L and A 5 2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.94mm" wi="64.60mm" file="US20130190334A1-20130725-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Pyrimidones for Treatment of Potassium Channel Related Diseases (Fri, 19 Jul 2013)
<p id="p-0001" num="0000">The present invention relates to compounds of Formula I as described herein or a pharmaceutically acceptable salt thereof, pharmaceutical composition comprising a compound of Formula I or a pharmaceutically acceptable salt thereof and methods of treating a disease, disorder, or condition of the central nervous system, including bipolar disorder, depressive disorders, anxiety disorders, cognitive disorders, pain disorders, urogenital disorders, and epilepsy, among the other diseases, disorders or conditions discussed herein as mono-therapy or in combination with another active pharmaceutical ingredient.</p>
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N-AMINOSULFONYL BENZAMIDES (Fri, 12 Jul 2013)
The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I) or a pharmaceutically acceptable salt thereof, wherein Z, R1a, R1b, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
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Substituted Heteroaryls (Fri, 28 Jun 2013)
<p id="p-0001" num="0000">The present invention provides Formula (1A) compounds</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="22.10mm" wi="69.85mm" file="US20130165452A1-20130627-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. X, Y, Z, R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, and R<sup>4 </sup>are as described herein.</p>
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SULFONAMIDE DERIVATIVES AND USE THEREOF AS VGSC INHIBITORS (Fri, 28 Jun 2013)
The invention relates to new sulfonamide Nav1.7 inhibitors and pharmaceutically acceptable salts thereof, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. Nav1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
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IMPROVED PROCESSES FOR PREPARING PEPTIDE CONJUGATES AND LINKERS (Fri, 28 Jun 2013)
The present invention provides a process for preparing a compound of Formula 5b, as well as intermediates thereof, and novel classes of compounds useful in process for preparing these and similar compounds.
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SULFONAMIDE DERIVATIVES (Fri, 21 Jun 2013)
The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav 1.7 inhibitors of Formula (I): or a pharmaceutically acceptable salt thereof, wherein X, Z, R1a, R1b, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
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DIAZEPINE AND DIAZOCANE COMPOUNDS AS MC4 AGONISTS (Thu, 20 Jun 2013)
The present invention relates to compounds of formula (I) wherein R<sp>1</sp>, R<sp>2</sp>, R<sp>3</sp>, R<sp>4</sp>, L and n are as defined in the specification. These compounds are useful as MC4 agonists.
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Novel Sultam Compounds (Fri, 14 Jun 2013)
<p id="p-0001" num="0000">Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.</p>
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Piperidinyl Pyrimidine Amides As KV7 Potassium Channel Openers (Fri, 14 Jun 2013)
<p id="p-0001" num="0000">The present invention relates to compounds of Formula (I) as described herein or a pharmaceutically acceptable salt thereof, pharmaceutical composition comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof and methods of treating, or manufacture of a medicament to treat, a disease, disorder, or condition of the central nervous system, including bipolar disorder, depressive disorders, anxiety disorders, cognitive disorders, pain disorders, urogentital disorder, and epilepsy, among the other diseases, disorders or conditions discussed herein as mono-therapy or in combination with another active pharmaceutical ingredient.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="35.56mm" wi="62.06mm" file="US20130150391A1-20130613-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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CYTOTOXIC PEPTIDES AND ANTIBODY DRUG CONJUGATES THEREOF (Fri, 24 May 2013)
<p id="p-0001" num="0000">The present invention is directed to cytotoxic pentapeptides, to antibody drug conjugates thereof, and to methods for using the same to treat cancer.</p>
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CYTOTOXIC PEPTIDES AND ANTIBODY DRUG CONJUGATES THEREOF (Fri, 24 May 2013)
The present invention is directed to cytotoxic pentapeptides, to antibody drug conjugates thereof, and to methods for using the same to treat cancer.
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2-THIOPYRIMIDINONES (Fri, 17 May 2013)
Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.
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Chemical Compounds (Fri, 10 May 2013)
<p id="p-0001" num="0000">The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula 10 (I):(I) or a pharmaceutically acceptable salt thereof, wherein Z, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.</p>
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(Fri, 03 May 2013)

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(Fri, 03 May 2013)

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(Fri, 03 May 2013)

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(Fri, 03 May 2013)

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Triazine compounds as PI3 kinase and mTOR inhibitors (Fri, 03 May 2013)
<p id="p-0001" num="0000">Compounds of formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="22.18mm" wi="49.61mm" file="US08575159-20131105-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">wherein:</li> <li id="ul0002-0002" 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="24.05mm" wi="54.02mm" file="US08575159-20131105-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> and R<sup>2</sup>, R<sup>4</sup>, and R<sup>6-9 </sup>are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed. </p>
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(4-PHENYLIMIDAZOL-2-YL) ETHYLAMINE DERIVATIVES USEFUL AS SODIUM CHANNEL MODULATORS (Fri, 03 May 2013)
The invention relates to imidazole derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new imidazole Nav1.8 modulators of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4 and R5 are as defined in the description. Nav1.8 modulators are potentially useful in the treatment of a wide range of disorders, particularly pain.
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NEW SALT AND MEDICAL USE (Fri, 26 Apr 2013)
The invention provides 4-[2-(5-amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2- fluoro-N-(1,3-thiazol-4-yl)benzenesulfonamide or a pharmaceutically acceptable salt thereof for the treatment of a disease associated with elevated blood uric acid levels, such as hyperuricemia or gout. In another aspect the invention provides the tosylate salt of 4-[2-(5-amino-1H-pyrazol-4- yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-(1,3-thiazol-4-yl)benzenesulfonamide.
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PHARMACEUTICAL COMPOSITIONS OF N-METHYL-2-[3-((E)-2-PYRIDIN-2-YL-VINYL)-1H-INDAZOL-6-YLSULFANYL]-BENZAMIDE (Fri, 05 Apr 2013)
The present invention relates to pharmaceutical compositions containing axitinib, which is known as N-methyl-2-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-ylsulfanyl]- benzamide or 6-[2-(methylcarbamoyl)phenylsulfanyl]-3-E-[2-(pyridin-2- yl)ethenyl]indazole, or crystalline forms thereof, that protect axitinib from degradation, including photodegradation, as well as the therapeutic use of such compositions. The present invention also relates to novel photodegradants of axitinib.
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PYRROLOPYRIMIDINE AND PURINE DERIVATIVES (Fri, 29 Mar 2013)
The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Q, T, V, W, X, Y, Z, ring A, R1, R2, R3, R4, R5, R5a, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and m are defined herein. There novel pyrrolopyrimidine and purine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.
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Inhibitors of ion channels (Fri, 22 Mar 2013)
<p id="p-0001" num="0000">The invention is directed to compounds of Formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="17.95mm" wi="31.50mm" file="US08741934-20140603-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> in which: <br/> R<sup>5</sup>, R<sup>6</sup>, B and Z are defined supra. </p>
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SOLID FORMS OF A TRANSTHYRETIN DISSOCIATION INHIBITOR (Fri, 22 Mar 2013)
The present invention relates to solid forms of the N-methyl-D-glucamine (meglumine) salt of 6-carboxy-2-(3,5-dichlorophenyl)-benzoxazole and to methods for their preparation. The invention is also directed to pharmaceutical compositions containing at least one solid form and to the therapeutic or prophylactic use of such solid forms and compositions.
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HEXAHYDROPYRANO [3,4-D][1,3] THIAZIN-2-AMINE COMPOUNDS (Fri, 08 Mar 2013)
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I), as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
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NOVEL HETEROCYCLIC COMPOUNDS AS BROMODOMAIN INHIBITORS (Fri, 01 Mar 2013)
Disclosed are compounds of Formula (I): (I) which are useful as bromodomain inhibitors. Pharmaceutical compositions containing compounds of Formula (I) and the use of compounds of Formula (I) to treat diseases or disorders that are bromodomain-dependent are also disclosed. Methods for preparing and using these compounds are further described.
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INTERMEDIATE AND PROCESS FOR THE PREPARATION OF A SULFONAMIDE DERIVATIVE (Fri, 15 Feb 2013)
The invention relates to a crystalline form of 2-chloro-N-{2-[3-(2-{[(4'-hydroxybiphenyl-3- yl)methyl]amino}-2-oxoethyl)phenyl]-1,1-dimethylethyl}acetamide, a process for preparing the same and its use in the preparation of the 2 agonist N-[(4'-hydroxybiphenyl-3- yl)methyl]-2-(3-{2-[((2R)-2-hydroxy-2-{4-hydroxy-3- [(methylsulfonyl)amino]phenyl}ethyl)amino]-2-methylpropyl} phenyl)acetamide which is useful in the treatment of respiratory diseases.
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CRIZOTINIB FOR USE IN THE TREATMENT OF CANCER (Fri, 08 Feb 2013)
The present invention relates to the use of ROS kinase inhibitors for treating abnormal cell growth in mammals. In particular, the invention provides methods of treating mammals suffering from cancer mediated by at least one genetically altered ROS. In particular, the invention provides methods of treating mammals suffering from cancer mediated by at least one genetically altered ROS by administration of crizotinib.
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N1-pyrazolospiroketone acetyl-CoA carboxylase inhibitors (Fri, 01 Feb 2013)
<p id="p-0001" num="0000">The invention provides a compound of Formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.94mm" wi="59.69mm" file="US08507681-20130813-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a pharmaceutically acceptable salt of the compound, wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3 </sup>and R<sup>4 </sup>are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal. </p>
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Indazoles (Fri, 01 Feb 2013)
<p id="p-0001" num="0000">The present invention relates to compounds of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="56.64mm" wi="69.85mm" file="US08575336-20131105-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> to pharmaceutically acceptable salts therefore and to pharmaceutically acceptable solvates of said compounds and salts, wherein the substituents are defined herein; to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly asthma and COPD. </p>
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INDAZOLES (Fri, 01 Feb 2013)
The present invention relates to compounds of formula (I) to pharmaceutically acceptable salts therefore and to pharmaceutically acceptable solvates of said compounds and salts, wherein the substituents are defined herein; to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly asthma and COPD.
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QUINOLINYL GLUCAGON RECEPTOR MODULATORS (Fri, 01 Feb 2013)
The present invention provides a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, A1, A2, A3, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
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GPR 119 MODULATORS (Fri, 25 Jan 2013)
Compounds that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein- coupled receptor GPR119 in animals are described herein.
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ENKEPHALIN ANALOGUES (Fri, 18 Jan 2013)
The present invention relates to dipeptide enkephalin analogues of Formula (I) and their tautomers, ionic forms and pharmaceutically acceptable salts, and their use in medicine, in particular as opioid agonists.
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Benethamine salt forms of atorvastatin (Thu, 03 Jan 2013)
Novel benethamine salt forms of [R-(R*,R*)]-2-(4-fluorophenyl)-beta, delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterised by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for their preparation and pharmaceutical compositions of the same , which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's disease.
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Peptide analogues (Fri, 28 Dec 2012)
<p id="p-0001" num="0000">The present invention relates to compounds of Formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="22.18mm" wi="65.19mm" file="US08598123-20131203-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as opioid agonists. </p>
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Heterocyclic sulfonamides, uses and pharmaceutical compositions thereof (Fri, 21 Dec 2012)
<p id="p-0001" num="0000">The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="43.18mm" wi="72.47mm" file="US08686043-20140401-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> as defined in the specification. The invention is also directed to compositions containing and uses of the compounds of formula I. </p>
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LACTAMS AS BETA SECRETASE INHIBITORS (Fri, 21 Dec 2012)
Compound and pharmaceutically acceptable salts of the compound are disclosed, wherein the compound has the structure (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed. The compound of formula I is useful as beta secretase inhibitor for use in the treatment of Alzheimer's and other neurodegenerative and/or neurological disorders.
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POLYMYXIN DERIVATIVES USEFUL AS ANTIBACTERIAL AGENTS (Fri, 14 Dec 2012)
The present invention provides a new class of polymyxin derivates useful for treating bacterial infections, especially Gram-negative infections, that have reduced renal cytotoxicity.
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PYRAZOLO[3,4-D]PYRIMIDINE COMPOUNDS AND THEIR USE AS PDE2 INHIBITORS AND/OR CYP3A4 INHIBITORS (Fri, 14 Dec 2012)
The present invention provides, inter alia, compounds of Formula (I) and pharmaceutically acceptable salts thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as a method for the treatment of a disease or condition selected from the group consisting of central nervous system disorders, cognitive disorders, schizophrenia, dementia and other disorders in a mammal. The present invention further provides compounds of Formula (Id) and pharmaceutically acceptable salts thereof as CYP3A4 selective inhibitors.
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4-methylpyridopyrimidinone compounds (Fri, 07 Dec 2012)
<p id="p-0001" num="0000">The present invention is directed to novel 4-methylpyridopyrimidinone compounds of Formula (I),</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.26mm" wi="69.85mm" file="US08633204-20140121-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> and to salts thereof, their synthesis, and their use as inhibitors of phosphoinositide 3-kinase alpha (PI3-Kα). </p>
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KAT II inhibitors (Fri, 30 Nov 2012)
<p id="p-0001" num="0000">Compounds of Formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.01mm" wi="52.49mm" file="US08598200-20131203-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein X, Y, Z, R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4 </sup>are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other psychiatric, neurodegenerative and/or neurological disorders in mammals, including humans. </p>
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Salts and polymorphs of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6h-azepino[5,4,3-cd]indol-6-one (Fri, 30 Nov 2012)
<p id="p-0001" num="0000">The present invention relates to novel polymorphic forms of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer.</p>
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Process for forming amorphous atorvastatin (Fri, 16 Nov 2012)
<p id="p-0001" num="0000">A process for forming amorphous atorvastatin comprising the steps of dissolving atorvastatin in a non-hydroxylic solvent and removing the solvent by freeze-drying, as well as processes of dissolving atorvastatin in a hydroxylic solvent with a solubilizing agent or an alkalizing agent or an antioxidant and removing the solvent by freeze-drying to afford amorphous atorvastatin.</p>
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PYRAZOLOSPIROKETONE DERIVATIVES FOR USE AS ACETYL - COA CARBOXYLASE INHIBITORS (Sat, 27 Oct 2012)
The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof; wherein G is (II) or (III) R1, R2 and R3 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
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PYRROLO[2,3-D]PYRIMIDINE COMPOUNDS (Thu, 25 Oct 2012)
Described herein are pyrrolo[2,3-d]pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing these compounds, and methods for their preparation. (Formula (I))
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Pyrrolopyrazoles, potent kinase inhibitors (Fri, 19 Oct 2012)
<p id="p-0001" num="0000">Pyrrole pyrazole compounds of formula I, compositions including these compounds and methods of their use are provided. Preferred compounds of formula I have activity as protein kinase inhibitors, including as inhibitors of PAK4.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="24.98mm" wi="52.32mm" file="US08530652-20130910-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Salt forms of [R-(R*,R*)]-2-(4-fluorophenyl)-beta, delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid (Fri, 19 Oct 2012)
<p id="p-0001" num="0000">Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.</p>
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Pyrrolo[2,3-d]pyrimidine derivatives: their intermediates and synthesis (Fri, 12 Oct 2012)
<p id="p-0001" num="0000">This invention relates to methods and intermediates useful for the synthesis of pyrrolo[2,3-d]pyrimidine compounds. Specifically novel synthetic methods and intermediates for the synthesis of 3-{(3R,4R)-4-methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino}-piperidin-1-yl)-3-oxo-propionitrile and its corresponding citrate salt are disclosed.</p>
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N-linked hydroxamic acid derivatives useful as antibacterial agents (Fri, 12 Oct 2012)
<p id="p-0001" num="0000">The present invention is directed to a new class of hydroxamic acid derivatives of formula I,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="20.66mm" wi="71.37mm" file="US08664401-20140304-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">wherein the variables G, T, D, L, R<sup>1</sup>, R<sup>2</sup>, R<sup>3 </sup>are as described herein, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections in a patient in need thereof.</li> </ul> </li> </ul> </p>
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PYRROLO [2, 3 -D] PYRIMIDINE DERIVATIVES AS INHIBITORS OF TROPOMYOSIN- RELATED KINASES (Fri, 12 Oct 2012)
The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as Trk antagonists.
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ISOXAZOLE DERIVATIVES USEFUL AS ANTIBACTERIAL AGENTS (Fri, 12 Oct 2012)
The present invention is directed to a new class of hydroxamic acid derivatives of formula (I) or formula (II), their use as Lpx C inhibitors and, more specifically, their use to treat bacterial infections.
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IMIDAZOLE, PYRAZOLE, AND TRIAZOLE DERIVATIVES USEFUL AS ANTIBACTERIAL AGENTS (Fri, 12 Oct 2012)
The present invention is directed to a new class of hydroxamic acid derivatives, their use as Lpx C inhibitors and, more specifically, their use to treat bacterial infections.
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CRYSTALLINE AND NON- CRYSTALLINE FORMS OF TOFACITINIB, AND A PHARMACEUTICAL COMPOSITION COMPRISING TOFACITINIB AND A PENETRATION ENHANCER (Fri, 12 Oct 2012)
The present invention discloses novel crystalline and non-crystalline forms of 3-((3R, 4R)-4-methyl-3-[methyl-(7H-pyrrolo[2, 3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl)-3-oxopropionitrile, pharmaceutical composition containing the same, preparations thereof and the uses thereof.
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Bicyclic pyridinones (Fri, 05 Oct 2012)
<p id="p-0001" num="0000">Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.77mm" wi="62.06mm" file="US08697673-20140415-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> as defined herein. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed. </p>
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NOVEL BICYCLIC PYRIDINONES (Fri, 05 Oct 2012)
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined herein. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
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N1-PYRAZOLOSPIROKETONE ACETYL-COA CARBOXYLASE INHIBITORS (Thu, 20 Sep 2012)
The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R<sp>1</sp>, R<sp>2</sp>, R<sp>3</sp> and R<sp>4</sp> are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl- CoA carboxylase enzyme(s) in an animal.
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Fluoro-pyridinone derivatives useful as antibacterial agents (Fri, 14 Sep 2012)
<p id="p-0001" num="0000">The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.</p>
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ARYL SUBSTITUTED CARBOXAMIDE DERIVATIVES AS TRPM8 MODULATORS (Fri, 14 Sep 2012)
The invention provides a compound of the formula (I): wherein A, R1, R2 and R3 are as defined herein, or a pharmaceutically acceptable salt thereof. Such compounds are small molecule TRPM8 blockers and therefore useful in the propylaxis or treatment of a wide range of diseases, conditions or syndromes, including cold allodynia and Raynaulds syndrome.
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FLUORO-PYRIDINONE DERIVATIVES USEFUL AS ANTIBACTERIAL AGENTS (Fri, 14 Sep 2012)
The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.
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IMIDAZOLE DERIVATIVES AS CASEIN KINASE INHIBITORS (Thu, 06 Sep 2012)
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I), as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
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A METHOD OF TREATING LIVER FIBROSIS (Fri, 31 Aug 2012)
The present invention relates to a method of treating hepatis C and/or liver fibroisis with 3-cycloalkylaminopyrrolidine derivatives of the present invention.
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IMIDAZO[5,1-f][1,2,4]TRIAZINES FOR THE TREATMENT OF NEUROLOGICAL DISORDERS (Fri, 31 Aug 2012)
The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as a method for the treatment of a disease or condition selected from the group consisting of central nervous system disorders, cognitive disorders, schizophrenia, dementia and other disorders in a mammal.
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Imidazo[5,1-f][1,2,4]triazines for the treatment of neurological disorders (Fri, 24 Aug 2012)
<p id="p-0001" num="0000">The present invention relates to compounds of the Formula</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.99mm" wi="52.41mm" file="US08598155-20131203-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">and pharmaceutically acceptable salts thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as a method for the treatment of a disease or condition selected from the group consisting of central nervous system disorders, cognitive disorders, schizophrenia, dementia and other disorders in a mammal.</li> </ul> </li> </ul> </p>
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PYRROLO[2,3-D]PYRIMIDINE COMPOUNDS (Thu, 23 Aug 2012)
Described herein are pyrrolo[2,3-d]pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing these compounds, and methods for their preparation.
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GLUCAGON RECEPTOR MODULATOR (Fri, 17 Aug 2012)
The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
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Glucagon receptor modulators (Fri, 10 Aug 2012)
<p id="p-0001" num="0000">The present invention provides a compound of Formula (I)</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="US08507533-20130813-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a pharmaceutically acceptable salt thereof wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, A<sup>1</sup>, A<sup>2</sup>, A<sup>3</sup>, A<sup>4</sup>, L, B<sup>1</sup>, B<sup>2</sup>, B<sup>3 </sup>and B<sup>4 </sup>are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon. </p>
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Dioxa-bicyclo[3.2.1]octane-2,3,4-triol derivatives (Fri, 20 Jul 2012)
<p id="p-0001" num="0000">Compounds of Formula (A) and (B) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by sodium-glucose transporter inhibitors (in particular, SGLT2 inhibitors).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="63.33mm" wi="69.85mm" file="US08669380-20140311-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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INDAZOLE DERIVATIVES AS SODIUM CHANNEL INHIBITORS (Fri, 20 Jul 2012)
The invention relates to acyl sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new acyl sulfonamide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein U, V, W, X, Y, R° and R1 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
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GLUCAGON RECEPTOR MODULATORS (Fri, 29 Jun 2012)
The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
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NOVEL FUSED PYRIDINE COMPOUNDS AS CASEIN KINASE INHIBITORS (Fri, 29 Jun 2012)
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, A, R4, n, and R7 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
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Benzimidazole derivatives (Fri, 22 Jun 2012)
<p id="p-0001" num="0000">The present invention relates to a compound of the Formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.82mm" wi="64.69mm" file="US08431597-20130430-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a pharmaceutically acceptable salt thereof, wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3A</sup>, R<sup>3B</sup>, R<sup>4</sup>, R<sup>5</sup>, X, m, and n are as defined herein. Such novel benzamidazole derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds. </p>
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Fused pyridine compounds as casein kinase inhibitors (Fri, 22 Jun 2012)
<p id="p-0001" num="0000">Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="28.36mm" wi="40.05mm" file="US08536164-20130917-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> and pharmaceutically acceptable salts thereof, wherein X, Y, A, R<sup>4</sup>, n, and R<sup>7 </sup>are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed. </p>
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Phenanthrenone compounds, compositions and methods (Fri, 22 Jun 2012)
<p id="p-0001" num="0000">The present invention is directed to compounds of Formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="43.10mm" wi="72.81mm" file="US08552035-20131008-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or salt thereof, which are modulators of the glucocorticoid receptor. The compounds and salts of the invention are useful in the treatment of conditions mediated by glucocorticoid receptor activity. </p>
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Sulfonamide derivatives (Fri, 15 Jun 2012)
<p id="p-0001" num="0000">The present invention relates to compounds of the formula</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="20.83mm" wi="62.91mm" file="US08541588-20130924-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain. </p>
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Fused phenyl Amido heterocyclic compounds for the prevention and treatment of glucokinase-mediated diseases (Thu, 14 Jun 2012)
The present invention relates to a compound of formula (VIa): or a pharmaceutically acceptable s alt or solvate thereof, wherein Ring A is pyrazinyl and L 1 , R 1 , R 1a , R 4 , L 2 , R 2 , R 3 , w and n are as defined herein. Such compounds are glucokinase agonists and useful in the treatment of diseases including diabetes and obesity.
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KAT II inhibitors (Fri, 08 Jun 2012)
<p id="p-0001" num="0000">The present invention relates to compounds 3-amino-1-hydroxy-2-oxo-1,2,3, 4-tetrahydroquinoline-7-carbonitrile, 3-amino-1-hydroxy-7-(2-methoxyethoxy)-3,4-dihydroquinolin-2(1H)-one, and 3-amino-1-hydroxy-7-[(1S)-2-methoxy-1-methylethoxy]-3,4-dihydroquinolin-2(1H)-one, including racemic mixtures and resolved enantiomers thereof, to pharmaceutically acceptable salts thereof, and to the treatment of cognitive deficits associated with schizophrenia and other psychiatric, neurodegenerative and/or neurological disorders in mammals, including humans.</p>
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KAT II INHIBITORS (Fri, 08 Jun 2012)
Compounds of Formula I: (I) wherein X, Y, Z, R 1, R 2, R 3, R 4 are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive 5 deficits associated with schizophrenia and other psychiatric, neurodegenerative and/or neurological disorders in mammals, including humans.
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KAT II INHIBITORS (Fri, 08 Jun 2012)
The present invention relates to compounds 3-amino-1-hydroxy-2- oxo-1,2,3,4-tetrahydroquinoline-7-carbonitrile, 3-amino-1-hydroxy-7-(2- methoxyethoxy)-3,4-dihydroquinolin-2(1H)-one, and 3-amino-1-hydroxy-7-[(1S)-2-methoxy-1-methylethoxy]-3,4-dihydroquinolin-2(1H)-one, including racemic mixtures and resolved enantiomers thereof, to pharmaceutically acceptable salts thereof, and to the treatment of cognitive deficits associated with schizophrenia and other psychiatric, neurodegenerative and/or neurological disorders in mammals, including humans.
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MONOBACTAMS (Fri, 08 Jun 2012)
The present invention is directed to a new class of monobactam derivatives and their use for treating bacterial infections.
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4- (5-CYANO-PYRAZOL-1-YL) -PIPERIDINE DERIVATIVES AS GPR 119 MODULATORS (Fri, 01 Jun 2012)
Compounds that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein- coupled receptor GPR119 in animals are described herein.
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N1/N2-LACTAM ACETYL-CoA CARBOXYLASE INHIBITORS (Fri, 04 May 2012)
The invention provides a compound of Formula (I); or a pharmaceutically acceptable salt thereof; wherein G is Formula (II), Formula (III), Formula (IV) and Formula (V) R1, R2 and R3 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
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PYRIDINE- 2- DERIVATIVES AS SMOOTHENED RECEPTOR MODULATORS (Fri, 27 Apr 2012)
The present application relates to compounds of Formula (I), and Formula (II), or pharmaceutically acceptable salt thereof, wherein A, X, Y, Z, e, f, R1, R2, R3, R4, R5, R5b, R6, R7, R8, R9, R10, R11,R20, R21, R22 and R23 are defined herein. These novel pyridine derivatives that are useful in therapy, in particular for treating diseases or conditions mediated by Smo, including the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to methods of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
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Tricyclic compounds, compositions, and methods (Fri, 20 Apr 2012)
<p id="p-0001" num="0000">The present invention is directed to compounds of Formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="42.67mm" wi="67.65mm" file="US08445520-20130521-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or salt thereof, which are modulators of the glucocorticoid receptor. The compounds and salts of the invention are useful in the treatment of conditions mediated by glucocorticoid receptor activity. </p>
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N1-PYRAZOLOSPIROKETONE ACETYL-CoA CARBOXYLASE INHIBITORS (Fri, 06 Apr 2012)
The invention provides a compound of Formula (I) Z N N O N O A1R2 R1 R3R 3 L A 2 (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3,Z, A1, L and A 5 2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
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PYRIMIDONES FOR TREATMENT OF POTASSIUM CHANNEL RELATED DISEASES (Fri, 30 Mar 2012)
The present invention relates to compounds of Formula I as described herein or a pharmaceutically acceptable salt thereof, pharmaceutical composition comprising a compound of Formula I or a pharmaceutically acceptable salt thereof and methods of treating, or manufacture of a medicament to treat, a disease, disorder, or condition of the central nervous system, including bipolar disorder, depressive disorders, anxiety disorders, cognitive disorders, pain disorders, urogenital disorders, and epilepsy, among the other diseases, disorders or conditions discussed herein as mono-therapy or in combination with another active pharmaceutical ingredient.
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PROCESS FOR THE PREPARATION OF ( S ) - 3 - CYANO - 5 - METHYLHEXANOIC ACID DERIVATIVES ADN OF PREGABALIN (Fri, 02 Mar 2012)
The invention provides a process for the manufacture of a compound of formula (I) using an enzyme catalysed reduction of a compound of formula (lla) or llb). Compounds of formula (I) are useful for preparing pregabalin.
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Substituted imidazoles and their use as pesticides (Thu, 01 Mar 2012)
This invention relates to a range of alpha substituted 2-benzyl substituted imidazole compounds and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes for their synthesis and their use as parasiticides.
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6 SUBSTITUTED 2-HETEROCYCLYLAMINO PYRAZINE COMPOUNDS AS CHK-1 INHIBITORS (Thu, 26 Jan 2012)
The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, their synthesis, and their use as CHK-1 inhibitors.
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Preparation of pregabalin and related compounds (Fri, 20 Jan 2012)
<p id="p-0001" num="0000">Materials and methods for preparing (S)-(+)-3-aminomethyl-5-methyl-hexanoic acid and structurally related compounds via enzymatic kinetic resolution are disclosed.</p>
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SULFONAMIDE DERIVATIVES AS NAV1.7 INHIBITORS FOR THE TREATMENT OF PAIN (Fri, 20 Jan 2012)
The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I):or a pharmaceutically acceptable salt thereof, wherein Ar1, X, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
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N-SULFONYLBENZAMIDE DERIVATIVES USEFUL AS VOLTAGE GATED SODIUM CHANNEL INHIBITORS (Fri, 20 Jan 2012)
The invention relates to sulfonamide derivatives, to their use i n medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein Het1, X, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
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N- SULFONYLBENZAMIDES AS INHIBITORS OF VOLTAGE - GATED SODIUM CHANNELS (Fri, 20 Jan 2012)
PC71695A Abstract Chemical Compounds The invention relates to sulfonamide derivatives, to their use in medicine, to 5 compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I):10 X NH O S O O R1 R2 R5 R4 R3 Het1 (I) or a pharmaceutically acceptable salt thereof, wherein X, Het1, R1, R2, R3, R4 and R5 are as defined in the description. 15 Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
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N- SULFONYLBENZAMIDES AS INHIBITORS OF VOLTAGE - GATED SODIUM CHANNELS (Fri, 20 Jan 2012)
The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein X, Ar1, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
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N- SULFONYLBENZAMIDES AS INHIBITORS OF VOLTAGE - GATED SODIUM CHANNELS (Fri, 20 Jan 2012)
The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula 10 (I): (I) or a pharmaceutically acceptable salt thereof, wherein Z, R 1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
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CHEMICAL COMPOUNDS (Fri, 20 Jan 2012)
PC71695A Abstract Chemical Compounds The invention relates to sulfonamide derivatives, to their use in medicine, to 5 compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I):10 X NH O S O O R1 R2 R5 R4 R3 Het1 (I) or a pharmaceutically acceptable salt thereof, wherein X, Het1, R1, R2, R3, R4 and R5 are as defined in the description. 15 Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.</p>
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N-SULFONYLBENZAMIDE DERIVATIVES USEFUL AS VOLTAGE GATED SODIUM CHANNEL INHIBITORS (Fri, 20 Jan 2012)
The invention relates to sulfonamide derivatives, to their use i n medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein Het1, X, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.</p>
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CHEMICAL COMPOUNDS (Fri, 20 Jan 2012)
The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula 10 (I): (I) or a pharmaceutically acceptable salt thereof, wherein Z, R 1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.</p>
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CHEMICAL COMPOUNDS (Fri, 20 Jan 2012)
The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein X, Ar1, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.</p>
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SULFONAMIDE DERIVATIVES AS NAV1.7 INHIBITORS FOR THE TREATMENT OF PAIN (Fri, 20 Jan 2012)
The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I):or a pharmaceutically acceptable salt thereof, wherein Ar1, X, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.</p>
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BENZOFURANYL DERIVATIVES USED AS GLUCOKINASE INHIBITORS (Thu, 19 Jan 2012)
The present invention provides compounds of Formula (I) that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase.
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Sulfonamide derivatives as Nav 1.7 inhibitors (Fri, 13 Jan 2012)
<p id="p-0001" num="0000">This invention relates to sulfonamide derivative of formula (I), to their use in medicine, to compositions containing them, to processes for their preparation, and to intermediates used in such processes.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.77mm" wi="61.55mm" file="US08592629-20131126-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">These compounds are inhibitors of Nav1.7.</p>
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Chemical compounds (Fri, 13 Jan 2012)
<p id="p-0001" num="0000">The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes.</p> <p id="p-0002" num="0000">More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I):</p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.69mm" wi="61.04mm" file="US08685977-20140401-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a pharmaceutically acceptable salt thereof, wherein Ar<sup>1</sup>, X, R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4 </sup>and R<sup>5 </sup>are as defined in the description. </p> <p id="p-0004" num="0000">Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.</p>
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CHEMICAL COMPOUNDS (Fri, 13 Jan 2012)
The invention relates to new sulfonamide Nav1.7 inhibitors and pharmaceutically acceptable salts thereof, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
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BENZENESULFONAMIDES USEFUL AS SODIUM CHANNEL INHIBITORS (Fri, 13 Jan 2012)
The invention relates to sulfonamide derivatives, to their use i n medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide Nav1.7 inhibitors of formula (I): or pharmaceutically acceptable salts thereof, wherein Z1, Ra, Rb, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
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BENZENE SULFONAMIDES AS INHIBITORS OF VOLTAGE-GATED SODIUM CHANNELS (Fri, 13 Jan 2012)
The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide Nav1.7 inhibitors of formula (I) or pharmaceutically acceptable salts thereof, wherein X, Y1, Y2, Z, R1, R2 and R3 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
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PIPERIDINYL PYRIMIDINE AMIDES AS KV7 POTASSIUM CHANNEL OPENERS (Fri, 13 Jan 2012)
The present invention relates to compounds of Formula (I) as described herein or a pharmaceutically acceptable salt thereof, pharmaceutical composition comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof and methods of treating, or manufacture of a medicament to treat, a disease, disorder, or condition of the central nervous system, including bipolar disorder, depressive disorders, anxiety disorders, cognitive disorders, pain disorders, urogentital disorder, and epilepsy, among the other diseases, disorders or conditions discussed herein as mono-therapy or in combination with another active pharmaceutical ingredient.
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CHEMICAL COMPOUNDS (Fri, 13 Jan 2012)
The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide Nav1.7 inhibitors of formula (I) or pharmaceutically acceptable salts thereof, wherein X, Y1, Y2, Z, R1, R2 and R3 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.</p>
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PIPERIDINYL PYRIMIDINE AMIDES AS KV7 POTASSIUM CHANNEL OPENERS (Fri, 13 Jan 2012)
The present invention relates to compounds of Formula (I) as described herein or a pharmaceutically acceptable salt thereof, pharmaceutical composition comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof and methods of treating, or manufacture of a medicament to treat, a disease, disorder, or condition of the central nervous system, including bipolar disorder, depressive disorders, anxiety disorders, cognitive disorders, pain disorders, urogentital disorder, and epilepsy, among the other diseases, disorders or conditions discussed herein as mono-therapy or in combination with another active pharmaceutical ingredient.</p>
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BIPHENYLOXYBENZENSULPHONAMIDE DERIVATIVES (Fri, 13 Jan 2012)
The invention relates to sulfonamide derivatives, to their use i n medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide Nav1.7 inhibitors of formula (I): or pharmaceutically acceptable salts thereof, wherein Z1, Ra, Rb, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.</p>
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SULFONAMODE NAV1.7 INIHIBITORS (Fri, 13 Jan 2012)
The invention relates to new sulfonamide Nav1.7 inhibitors and pharmaceutically acceptable salts thereof, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.</p>
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2-(3,5-DISUBSTITUTEDPHENYL)PYRIMIDIN-4(3H)-ONE DERIVATIVES (Fri, 23 Dec 2011)
O N NH R3 R2 O R1 168 ABSTRACT The present invention provides a 2-(3,5-disubstitutedphenyl)pyrimidin- 4(3H)-one compound of Formula (I) 5 (I) or a pharmaceutically acceptable salt thereof wherein R 1, R2 and R3 are as defined herein. The compounds of Formula (I) have been found to act as glucokinase activators. Consequently, the compounds of Formula (I) and 10 the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucokinase.
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HEPATITIS C VIRUS INHIBITORS (Fri, 16 Dec 2011)
The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts thereof; to compositions containing such compounds; and to the of such compounds as inhibitors of HCV replication.
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CONJUGATES FOR THE PREVENTION OR TREATMENT OF NICOTINE ADDICTION (Fri, 09 Dec 2011)
<p id="p-0001" num="0000">The present invention relates in part to nicotine-derived hapten-carrier conjugates of the formula (III):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.77mm" wi="76.03mm" file="US20110300174A1-20111208-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein m, n, W, -(spacer)-, X* and Y are as defined in the description. In certain embodiments, said nicotine-derived hapten-carrier conjugates can be used to prepare vaccines for the treatment and/or prevention of nicotine addiction.</p>
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CONJUGATES FOR THE PREVENTION OR TREATMENT OF NICOTINE ADDICTION (Fri, 09 Dec 2011)
The present invention relates in part to nicotine-derived hapten-carrier conjugates of the formula (III): wherein m, n, W, -(spacer)-, X* and Y are as defined in the description. In certain embodiments, said nicotine-derived hapten-carrier conjugates can be used to prepare vaccines for the treatment and/or prevention of nicotine addiction.
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CONJUGATES FOR THE PREVENTION OR TREATMENT OF NICOTINE ADDICTION (Fri, 09 Dec 2011)
The present invention relates in part to nicotine-derived hapten-carrier conjugates of the formula (III): wherein m, n, W, -(spacer)-, X* and Y are as defined in the description. In certain embodiments, said nicotine-derived hapten-carrier conjugates can be used to prepare vaccines for the treatment and/or prevention of nicotine addiction.</p>
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Pyrrolo[2,3-D]pyrimidine compounds (Fri, 02 Dec 2011)
<p id="p-0001" num="0000">Described herein are pyrrolo[2,3-d]pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing these compounds, and methods for their preparation.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="38.61mm" wi="64.94mm" file="US08372854-20130212-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Amino-heterocyclic compounds used as pde9 inhibitors (Thu, 01 Dec 2011)
The invention provides PDE9-inhibiting compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein R<sp>1</sp>, R<sp>2</sp>, R<sp>3</sp>, A1 and n are as defined herein. Pharmaceutical compositions containing the compounds of Formula I, and uses thereof in treating neurodegenerative and cognitive disorders, such as Alzheimer's disease and schizophrenia, are also provided.
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Pyrrolo[2,3-d]pyrimidine derivatives; their intermediates and synthesis (Fri, 25 Nov 2011)
<p id="p-0001" num="0000">This invention relates to methods and intermediates useful for the synthesis of pyrrolo[2,3-d]pyrimidine compounds. Specifically novel synthetic methods and intermediates for the synthesis of 3-{(3R,4R)-4-methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino}-piperidin-1-yl)-3-oxo-propionitrile and its corresponding citrate salt are disclosed.</p>
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2-PHENYL BENZOYLAMIDES (Fri, 25 Nov 2011)
Compounds of Formula I that inhibit microsomal triglyceride transfer protein (MTP) and/or apolipoprotein B (Apo B) secretion and their uses in the treatment of diseases linked thereto in animals are described herein.
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2-PHENYL BENZOYLAMIDES (Fri, 25 Nov 2011)
Compounds of Formula I that inhibit microsomal triglyceride transfer protein (MTP) and/or apolipoprotein B (Apo B) secretion and their uses in the treatment of diseases linked thereto in animals are described herein.</p>
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MORPHOLINE COMPOUNDS AS MINERALOCORTICOID RECEPTOR ANTAGONISTS (Fri, 18 Nov 2011)
Mineralocorticoid receptor antagonists (MRa), pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetic nephropathy and hypertension in mammals, including humans.
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MORPHOLINE COMPOUNDS AS MINERALOCORTICOID RECEPTOR ANTAGONISTS (Fri, 18 Nov 2011)
Mineralocorticoid receptor antagonists (MRa), pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetic nephropathy and hypertension in mammals, including humans.</p>
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HETEROCYCLIC DERIVATIVES AS ALK INHIBITORS (Fri, 11 Nov 2011)
The invention relates to compounds of Formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases in which ALK protein is involved or in which inhibition of ALK activity may induce benefit, especially for the treatment of cancer mediated by a mutated EML4-ALK fusion protein.
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HETEROCYCLIC DERIVATIVES AS ALK INHIBITORS (Fri, 11 Nov 2011)
The invention relates to compounds of Formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases in which ALK protein is involved or in which inhibition of ALK activity may induce benefit, especially for the treatment of cancer mediated by a mutated EML4-ALK fusion protein.</p>
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SUBSTITUTED ISOXAZOLINE DERIVATIVES (Fri, 14 Oct 2011)
<p id="p-0001" num="0000">This invention recites substituted isoxazoline derivatives of Formula (1)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="50.29mm" wi="65.36mm" file="US20110251247A1-20111013-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or a veterinarily acceptable salt thereof, with parasiticidal activity, compositions thereof, and their use as a parasiticide in animals or birds where R<sup>1a</sup>, R<sup>1b</sup>, R<sup>1c</sup>, R<sup>2</sup>, R<sup>3</sup>, and n are as described herein.</p>
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SULTAM COMPOUNDS (Fri, 14 Oct 2011)
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
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SUBSTITUTED 3,5- DI PHENYL - ISOXAZOLINE DERIVATIVES AS INSECTICIDES AND ACARICIDES (Fri, 14 Oct 2011)
This invention recites substituted isoxazoline derivatives of Formula (I) or a veterinarily acceptable salt thereof, with parasiticidal activity, compositions thereof, and their use as a parasiticide in animals or birds where R1a, R1b, R1c, R2, R3, and n are as described herein.
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SUBSTITUTED 3,5-DIPHENYL-ISOXAZOLINE DERIVATIVES AS INSECTICIDES AND ACARICIDES (Fri, 14 Oct 2011)
This invention recites substituted isoxazoline derivatives of Formula (I) or a veterinarily acceptable salt thereof, with parasiticidal activity, compositions thereof, and their use as a parasiticide in animals or birds where R1a, R1b, R1c, R2, R3, and n are as described herein.</p>
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NOVEL SULTAM COMPOUNDS (Fri, 14 Oct 2011)
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.</p>
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3-Aminocyclopentanecarboxamides as chemokine receptor modulators (Thu, 06 Oct 2011)
There is provided a compound of Formula I(a) or I(b) or a pharmaceutically acceptable salt thereof, wherein the various substitutents are defined herein.
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Process for forming amorphous atorvastatin (Fri, 30 Sep 2011)
<p id="p-0001" num="0000">A process for forming amorphous atorvastatin comprising the steps of dissolving atorvastatin in a non-hydroxylic solvent and removing the solvent by freeze-drying, as well as processes of dissolving atorvastatin in a hydroxylic solvent with a solubilizing agent or an alkalizing agent or an antioxidant and removing the solvent by freeze-drying to afford amorphous atorvastatin.</p>
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Substituted imidazoles useful for treating type II diabetes (Fri, 23 Sep 2011)
<p id="p-0001" num="0000">The present invention provides Formula (1A) compounds</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="22.18mm" wi="69.85mm" file="US08329920-20121211-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. X, Y, Z, R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, and R<sup>4 </sup>are as described herein. </p>
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2,3-dihydro-1H-inden-1-yl-2,7-diazaspiro[3.5] nonane derivatives (Fri, 23 Sep 2011)
<p id="p-0001" num="0000">The present invention provides a compound of Formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.35mm" wi="70.87mm" file="US08609680-20131217-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a pharmaceutically salt thereof wherein R<sup>1</sup>, R<sup>2</sup>, Ra, L, Z, Z<sup>1 </sup>and Z<sup>2 </sup>are as defined herein, that act as Ghrelin antagonists or inverse agonists; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by the antagonism of the Ghrelin receptor. </p>
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2,3 DIHYDRO- 1H - INDEN- 1 - YL -2,7 -DIAZASPIRO [ 3.5 ] NONANE DERIVATIVES AND THEIR USE AS ANTAGONISTS OR INVERSE AGONISTS OF THE GHRELIN RECEPTOR (Fri, 23 Sep 2011)
The present invention provides a compound of Formula (I) or a pharmaceutically salt thereof wherein R1, R2, Ra, L, Z, Z1 and Z2 are as defined herein, that act as Ghrelin antagonists or inverse agonists; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by the antagonism of the Ghrelin receptor.
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2,3 DIHYDRO-1H-INDEN-1-YL-2,7-DIAZASPIRO [3.5] NONANE DERIVATIVES AND THEIR USE AS ANTAGONISTS OR INVERSE AGONISTS OF THE GHRELIN RECEPTOR (Fri, 23 Sep 2011)
The present invention provides a compound of Formula (I) or a pharmaceutically salt thereof wherein R1, R2, Ra, L, Z, Z1 and Z2 are as defined herein, that act as Ghrelin antagonists or inverse agonists; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by the antagonism of the Ghrelin receptor.</p>
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Novel Lactams as Beta Secretase Inhibitors (Fri, 16 Sep 2011)
<p id="p-0001" num="0000">Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment methods of synthesis, and intermediates are also disclosed.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="38.52mm" wi="47.58mm" file="US20110224231A1-20110915-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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PEPTIDE ANALOGUES (Fri, 02 Sep 2011)
The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as opioid agonists.
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PEPTIDE ANALOGUES (Fri, 02 Sep 2011)
The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as opioid agonists.</p>
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(R)-4-((4-((4-(TETRAHYDROFURAN-3-YLOXY)BENZO[D]ISOXAZOL-3-YLOXY)METHYL)PIPERIDIN-1-YL)METHYL)TETRAHYDRO-2H-PYRAN-4-OL, A PARTIAL AGONIST OF 5-HT4 RECEPTORS (Fri, 26 Aug 2011)
(R)-4-((4-((4-(tetrahydrofuran-3-yloxy)benzo[d]isoxazol-3- yloxy)methyl)piperidin-1-yl)methyl)tetrahydro-2H-pyran-4-ol and its use in treating neurodegenerative disorders, is described herein.
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(R)-4-((4-((4-(TETRAHYDROFURAN-3-YLOXY)BENZO[D]ISOXAZOL-3-YLOXY)METHYL)PIPERIDIN-1-YL)METHYL)TETRAHYDRO-2H-PYRAN-4-OL, A PARTIAL AGONIST OF 5-HT4 RECEPTORS (Fri, 26 Aug 2011)
(R)-4-((4-((4-(tetrahydrofuran-3-yloxy)benzo[d]isoxazol-3- yloxy)methyl)piperidin-1-yl)methyl)tetrahydro-2H-pyran-4-ol and its use in treating neurodegenerative disorders, is described herein.</p>
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SALTS AND POLYMORPHS OF 8-FLUORO-2-{4-[(METHYLAMINO}METHYL]PHENYL}-1,3,4,5-TETRAHYDRO-6H-AZEPINO[5,4,3-CD]INDOL-6-ONE (Fri, 19 Aug 2011)
The present invention relates to novel polymorphic forms of 8-fluoro-2-{4- [(methylamino)methyl]phenyf}-1,3,4,5-tetrahydro-6H-azepino(5,4,3-cd]indol-6-one;(I), and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer.
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SALTS AND POLYMORPHS OF 8-FLUORO-2-{4-[(METHYLAMINO}METHYL]PHENYL}-1,3,4,5-TETRAHYDRO-6H-AZEPINO[5,4,3-CD]INDOL-6-ONE (Fri, 19 Aug 2011)
The present invention relates to novel polymorphic forms of 8-fluoro-2-{4- [(methylamino)methyl]phenyf}-1,3,4,5-tetrahydro-6H-azepino(5,4,3-cd]indol-6-one;(I), and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer.</p>
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PYRROLO [ 2, 3 - D] PYRIMIDINE UREA COMPOUNDS AS JAK INHIBITORS (Fri, 12 Aug 2011)
The present invention provides pyrrolo{2,3-d}pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing this compounds, and methods for the preparation of these compounds.
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PYRROLO [ 2, 3 - D] PYRIMIDINE UREA COMPOUNDS AS JAK INHIBITORS (Fri, 12 Aug 2011)
The present invention provides pyrrolo{2,3-d}pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing this compounds, and methods for the preparation of these compounds.</p>
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AMINOCYCLOHEXANES AND AMINOTETRAHYDROPYRANS AND RELATED COMPOUNDS AS GAMMA-SECRETASE MODULATORS (Fri, 05 Aug 2011)
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
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AMINOCYCLOHEXANES AND AMINOTETRAHYDROPYRANS AND RELATED COMPOUNDS AS GAMMA-SECRETASE MODULATORS (Fri, 05 Aug 2011)
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.</p>
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Hydroxamic acid derivatives useful as antibacterial agents (Fri, 22 Jul 2011)
<p id="p-0001" num="0000">The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II); and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B. L<sup>1</sup>-L<sup>4 </sup>A, B, R<sup>1</sup>-R<sup>4 </sup>and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.</p>
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Salt forms of [R-(R*,R*)]-2-(4-fluorophenyl)-beta, alpha-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid (Fri, 15 Jul 2011)
<p id="p-0001" num="0000">Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.</p>
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HYDROCHLORIDE SALT OF BIPHENYL-2-YL-CARBAMIC ACID 1-{9-[(3-FLUORO-4-HYDROXY-BENZOYL)-METHYL-AMINO]-NONYL}-PIPERIDIN-4-YL ESTER (Fri, 15 Jul 2011)
This invention relates to the hydrochloride salt of biphenyl-2-yl-carbamic acid -{9-[(3-fluoro-4-hydroxy-benzoyl)-methyl-amino]-nonyl}-piperidin-4-yl ester and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, said compound. The invention also relates to the hydrates, solvates and polymorphs of the hydrochloride salt of Biphenyl-2-yl-carbamic acid 1-{9-[(3-fluoro-4-hydroxy-benzoyl)-methyl- amino]-nonyl}-piperidin-4-yl ester.
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Sulfonyl amide derivatives for the treatment of abnormal cell growth (Fri, 08 Jul 2011)
<p id="p-0001" num="0000">The present invention relates to a compound of the formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="36.75mm" wi="63.16mm" file="US08247411-20120821-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R<sup>1 </sup>to R<sup>6</sup>, A, B, n and m are as defined herein. Such novel sulfonyl amide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds. </p>
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COMBINATION THERAPY FOR TUBERCULOSIS (Thu, 07 Jul 2011)
The present invention relates to methods of treating tuberculosis, including multi-drug resistant varieties and latent tuberculosis. More particularly, the present invention relates to a method of treating tuberculosis in a mammal comprising administering to said mammal in need thereof an effective amount of a compound of formula (I), (S)—N-[[3-[3-fluoro-4-(4-thiomorpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide, or a pharmaceutically acceptable salt thereof in combination with at least two agents useful in the treatment of tuberculosis. The present invention also relates to a pharmaceutical composition comprising a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, (ii) a therapeutically effective amount of at least one agent useful in the treatment of tuberculosis and (iii) one or more pharmaceutically acceptable carriers or vehicles.
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PIPERIDINECARBOXAMIDES AS MPGES - 1 INHIBITORS (Fri, 01 Jul 2011)
The invention relates to piperidinecarboxamides of formula (I), to their use in medicine as mPGES-1 inhibitors for the treatment of pain, to compositions containing them, to processes for their preparation and to intermediates used in such processes.
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PROLINE DERIVATIVES HAVING AFFINITY FOR THE CALCIUM CHANNEL ALPHA-2-DELTA SUBUNIT, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME AND COMBINATIONS COMPRISING SAID DERIVATIVES WITH ANOTHER ACTIVE AGENT (Fri, 01 Jul 2011)

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PROLINE DERIVATIVES HAVING AFFINITY FOR THE CALCIUM CHANNEL ALPHA-2-DELTA SUBUNIT, PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME AND COMBINATIONS COMPRISING SAID DERIVATIVES WITH ANOTHER ACTIVE AGENT (Fri, 01 Jul 2011)

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N-LINKED HYDROXAMIC ACID DERIVATIVES USEFUL AS ANTIBACTERIAL AGENTS (Fri, 24 Jun 2011)
The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections. Formula (I).
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PYRROLO[2,3-D]PYRIMIDINE COMPOUNDS (Fri, 24 Jun 2011)
Described herein are pyrrolo[2,3-d]pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing these compounds, and methods for their preparation. (Formula (I))
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N-LINKED HYDROXAMIC ACID DERIVATIVES USEFUL AS ANTIBACTERIAL AGENTS (Fri, 24 Jun 2011)
The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections. Formula (I).</p>
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PYRROLO[2,3-D]PYRIMIDINE COMPOUNDS (Fri, 24 Jun 2011)
Described herein are pyrrolo[2,3-d]pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing these compounds, and methods for their preparation. (Formula (I))</p>
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DIOXA-BICYCLO[3.2.1.]OCTANE-2,3,4-TRIOL DERIVATIVES (Thu, 23 Jun 2011)
Compounds of Formula (I) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by sodium-glucose transporter inhibitors (in particular, SGLT2 inhibitors).The compounds disclosed herein are useful for the prevention and treatment of obesity and its associated co-morbidities, inn particular type Il (type 2) diabetes.
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3-aminocyclopentanecarboxamides as chemokine receptor agonists (Fri, 17 Jun 2011)
<p id="p-0001" num="0000">There is provided a compound of Formula I(a) or I(b)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="71.63mm" wi="71.37mm" file="US08293903-20121023-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a pharmaceutically acceptable salt thereof, wherein the various substituents are defined herein. </p>
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6 substituted 2-heterocyclylamino pyrazine compounds as CHK-1 inhibitors (Fri, 17 Jun 2011)
<p id="p-0001" num="0000">The present invention is directed to compounds of formula (I),</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.82mm" wi="54.53mm" file="US08518952-20130827-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> and pharmaceutically acceptable salts thereof, their synthesis, and their use as CHK-1 inhibitors. </p>
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Pyrrolo[2,3-b]pyridine derivatives active as kinase inhibitors (Fri, 10 Jun 2011)
<p id="p-0001" num="0000">Compounds which are pyrrolo[2,3-b]pyridine derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases and neurodegenerative disorders; also disclosed is a process under SPS conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.</p>
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Diazepine and diazocane compounds as MC4 agonists (Fri, 10 Jun 2011)
<p id="p-0001" num="0000">The present invention relates to compounds of formula (I) wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, L and n are as defined in the specification. These compounds are useful as MC4 agonists.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="33.36mm" wi="69.85mm" file="US08592403-20131126-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Pyrrolo[2,3-D]pyrimidine compounds (Fri, 10 Jun 2011)
<p id="p-0001" num="0000">Described herein are pyrrolo[2,3-d]pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing these compounds, and methods for their preparation.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="37.51mm" wi="67.82mm" file="US08633206-20140121-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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IMIDAZO-PYRAZOLES AS GPR119 INHIBITORS (Fri, 27 May 2011)
Compounds of formula (I) wherein: X is (A) or (B); Y is O or a bond; R1 is -C(O)-O-R3 or R2 is hydrogen, cyano, C1-C6 alkyl, or C3-C6 cycloalkyl; R5 is hydrogen, cyano, nitro, C1-C6 fluoroalkyl, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 fluoroalkoxy, or C3-C6 cycloalkyl; R6 is hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, -C(O)-NH2, or C1-C6 alkyl substituted with hydroxy or C1- C6 alkoxy; m is 1 or 2, wherein when m is 1 then R8 is hydrogen, C1-C6 alkyl, -CH2-(C1- C5)haloalkyl, C3-C6 cycloalkyl, or C1-C6 alkyl substituted with hydroxy; and when m is 2 then each R8 is independently C1-C3 alkyl or -CH2-(C1-C2)haloalkyl; modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G- protein-coupled receptor GPR119 in animals are described herein.
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IMIDAZO-PYRAZOLES AS GPR119 INHIBITORS (Fri, 27 May 2011)
Compounds of formula (I) wherein: X is (A) or (B); Y is O or a bond; R1 is -C(O)-O-R3 or R2 is hydrogen, cyano, C1-C6 alkyl, or C3-C6 cycloalkyl; R5 is hydrogen, cyano, nitro, C1-C6 fluoroalkyl, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 fluoroalkoxy, or C3-C6 cycloalkyl; R6 is hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, -C(O)-NH2, or C1-C6 alkyl substituted with hydroxy or C1- C6 alkoxy; m is 1 or 2, wherein when m is 1 then R8 is hydrogen, C1-C6 alkyl, -CH2-(C1- C5)haloalkyl, C3-C6 cycloalkyl, or C1-C6 alkyl substituted with hydroxy; and when m is 2 then each R8 is independently C1-C3 alkyl or -CH2-(C1-C2)haloalkyl; modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G- protein-coupled receptor GPR119 in animals are described herein.</p>
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Process for preparing chiral compounds (Fri, 20 May 2011)
<p id="p-0001" num="0000">The present invention is directed to a 2-deoxyribose-5-phosphate aldolase (DERA) chemoenzymatic process for making chiral compounds.</p>
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SUBSTITUTED TRIAZOLOPYRIMIDINES AS PDE8 INHIBITORS (Fri, 20 May 2011)
Compounds of Formula (I): wherein R1 , R2, R3, R4, and R5 are as defined herein, are disclosed.
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N1-PYRAZOLOSPIROKETONE ACETYL-COA CARBOXYLASE INHIBITORS (Fri, 20 May 2011)
The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl- CoA carboxylase enzyme(s) in an animal.
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N2-PYRAZOLOSPIROKETONE ACETYL-COA CARBOXYLASE INHIBITORS (Fri, 20 May 2011)
The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of said compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl- CoA carboxylase enzyme(s) in an animal.
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N-2 PYRAZOLOSPIROKETONE ACETYL-COA CARBOXYLASE INHIBITORS (Fri, 20 May 2011)
The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of said compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl- CoA carboxylase enzyme(s) in an animal.</p>
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N1-PYRAZOLOSPIROKETONE ACETYL-COA CARBOXYLASE INHIBITORS (Fri, 20 May 2011)
The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl- CoA carboxylase enzyme(s) in an animal.</p>
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N1-pyrazolospiroketone acetyl-CoA carboxylase inhibitors (Fri, 13 May 2011)
<p id="p-0001" num="0000">The invention provides a compound of Formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="33.27mm" wi="60.03mm" file="US08288405-20121016-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a pharmaceutically acceptable salt of the compound, wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3 </sup>and R<sup>4 </sup>are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal. </p>
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IMIDAZOLE DERIVATIVES AS CASEIN KINASE INHIBITORS (Fri, 06 May 2011)
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I), as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
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DIOXA-BICYCLO[3.2.1]OCTANE-2,3,4-TRIOL DERIVATIVES (Fri, 06 May 2011)
Compounds of Formula (A) and (B) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by sodium-glucose transporter inhibitors (in particular, SGLT2 inhibitors).
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DIOXA-BICYCLO[3.2.1]OCTANE-2,3,4-TRIOL DERIVATIVES (Fri, 06 May 2011)
Compounds of Formula (A) and (B) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by sodium-glucose transporter inhibitors (in particular, SGLT2 inhibitors).</p>
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IMIDAZOLE DERIVATIVES AS CASEIN KINASE INHIBITORS (Fri, 06 May 2011)
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I), as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.</p>
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Compounds as casein kinase inhibitors (Fri, 29 Apr 2011)
<p id="p-0001" num="0000">Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="43.69mm" wi="61.47mm" file="US08518944-20130827-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed. </p>
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NOVEL HETEROARYL IMIDAZOLES AND HETEROARYL TRIAZOLES AS GAMMA-SECRETASE MODULATORS (Fri, 29 Apr 2011)
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I; (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
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NOVEL HETEROARYL IMIDAZOLES AND HETEROARYL TRIAZOLES AS GAMMA-SECRETASE MODULATORS (Fri, 29 Apr 2011)
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I; (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.</p>
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C-LINKED HYDROXAMIC ACID DERIVATIVES USEFUL AS ANTIBACTERIAL AGENTS (Fri, 22 Apr 2011)
The present invention is directed to a new class of alpha - alkylsulfonyl hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.
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PYRROLO[2,3-D] PYRIMIDINE COMPOUNDS (Fri, 22 Apr 2011)
Described herein are pyrrolo[2,3-d]pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing these compounds, and methods for their preparation.
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C-LINKED HYDROXAMIC ACID DERIVATIVES USEFUL AS ANTIBACTERIAL AGENTS (Fri, 22 Apr 2011)
The present invention is directed to a new class of alpha - alkylsulfonyl hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.</p>
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PYRROLO[2,3-D]PYRIMIDINE COMPOUNDS (Fri, 22 Apr 2011)
Described herein are pyrrolo[2,3-d]pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing these compounds, and methods for their preparation.</p>
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NOVEL FORMS OF (2,8-DIMETHYL-5-[2-(6-METHYLPYRIDIN-3-YL)ETHYL]-3,4-DIHYDRO-1H-PYRIDO[4,3-B] INDOLE) (Fri, 08 Apr 2011)
The present invention relates to novel solid forms of latrepirdine, also known as Dimebon) designated Form A, Form B, and a noncrystalline form, and relates to methods for the preparation of each form. The present invention also relates to a novel MVP oxalate salt and hydrate thereof, and its preparation and use in the preparation of latrepirdine.
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POLYMORPHIC FORM OF A [1, 2, 4] TRIAZOLO [4, 3-A]PYRIDINE DERIVATIVE FOR TREATING INFLAMMATORY DISEASES (Thu, 07 Apr 2011)
The present invention relates to a polymorphic form B of Λ/-[3-tert-butyl-1-(3- chloro-4-hydroxyphenyl)-1 H-pyrazol-5-yl]-<i>N</i>-{2-[(3-{2-[(2-hydroxyethyl)sulfanyl] phenyl}[1,2.4]triazolo[4,3-a]pyridin-6-yl)sulfanyl]benzyl}urea (I) as defined herein. This polymorph is useful in the treatment of various conditions, particularly in the treatment of inflammatory conditions such as chronic obstructive pulmonary disease.
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GPR 119 MODULATORS (Fri, 01 Apr 2011)
Compounds of formula (I) that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.
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USE OF PROLINE DERIVATIVES HAVING AFFINITY FOR THE CALCIUM CHANNEL ALPHA-2-DELTA SUBUNIT IN THE MANUFACTURE OF MEDICAMENTS FOR TREATMENT OF PAIN (Fri, 01 Apr 2011)

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GPR 119 MODULATORS (Fri, 01 Apr 2011)
Compounds of formula (I) that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.</p>
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NOVEL CLASS OF SPIRO PIPERIDINES FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES (Thu, 31 Mar 2011)
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
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TRIAZOLE DERIVATIVES USEFUL FOR THE TREATMENT OF DISEASES (Thu, 31 Mar 2011)
The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
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Preparation of pregabalin and related compounds (Fri, 18 Mar 2011)
<p id="p-0001" num="0000">Materials and methods for preparing (S)-(+)-3-aminomethyl-5-methyl-hexanoic acid and structurally related compounds via enzymatic kinetic resolution are disclosed.</p>
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BENZIMIDAZOLE DERIVATIVES (Fri, 11 Mar 2011)
The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1A, R1B, R1C, R2, R3, R4, R5, RA, RB, RC and X are as defined herein. These novel benzimidazole derivatives are useful in therapy, in particular for treating diseases or conditions mediated by SMO, including the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
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BENZIMIDAZOLE DERIVATIVES (Fri, 11 Mar 2011)
The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1A, R1B, R1C, R2, R3, R4, R5, RA, RB, RC and X are as defined herein. These novel benzimidazole derivatives are useful in therapy, in particular for treating diseases or conditions mediated by SMO, including the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.</p>
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4-[3-(ARYLOXY)BENZYLIDENE]-3-METHYL PIPERIDINE ARYL CARBOXAMIDE COMPOUNDS USEFUL AS FAAH INHIBITORS (Fri, 04 Mar 2011)
<p id="p-0001" num="0000">The present invention relates to compounds of Formula (I), wherein Ar is optionally substituted phenyl or heteroaryl and X, Y and Z are independently N or CH; or a pharmaceutically acceptable salt thereof; processes for the preparation of the compounds; intermediates used in the preparation of the compounds; compositions containing the compounds; and uses of the compounds in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="29.63mm" wi="76.03mm" file="US20110053949A1-20110303-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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ETHER BENZYLIDENE PIPERIDINE 5-MEMBERED ARYL CARBOXAMIDE COMPOUNDS USEFUL AS FAAH INHIBITORS (Fri, 04 Mar 2011)
<p id="p-0001" num="0000">The present invention relates to compounds of the Formula (I), and pharmaceutically acceptable salts thereof, and their use in the treatment of FAAH-mediated diseases or condition.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.99mm" wi="72.64mm" file="US20110053982A1-20110303-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Process for the synthesis C-2, C-3 substituted N-alkylated indoles useful as cPLA<sub>2 </sub>inhibitors (Fri, 04 Mar 2011)
<p id="p-0001" num="0000">The present invention provides a compound of formula 1:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="64.52mm" wi="69.26mm" file="US08034960-20111011-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R<sup>1 </sup>is CF<sub>3</sub>, R<sup>2 </sup>is H′ R<sup>3 </sup>is H. </p>
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Polymorphs Of Prostaglandin Agonists And Methods For Making The Same (Fri, 25 Feb 2011)
<p id="p-0001" num="0000">The present invention relates to polymorphic crystalline forms or a non-crystalline form or amorphous of the compound (3-(((4-tert-butyl-benzyl)-(pyridine-3-sulfonyl)-amino)-methyl)-phenoxy)-acetic acid sodium salt or a hydrate thereof together with processes for preparing, methods for using, and pharmaceutical compositions containing the same. The invention also relates to substantially pure polymorphic crystalline forms or a non-crystalline form or amorphous form of (3-(((4-tert-butyl-benzyl)-(pyridine-3-sulfonyl)-amino)-methyl)-phenoxy)-acetic acid sodium salt or a hydrate thereof.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.43mm" wi="70.70mm" file="US20110046385A1-20110224-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Fused phenyl amido heterocyclic compounds (Fri, 18 Feb 2011)
<p id="p-0001" num="0000">The present invention relates to a compound of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="16.00mm" wi="69.85mm" file="US08119624-20120221-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, wherein:</p> <p id="p-0004" num="0000">Ring A is (4-12)-membered heterocyclyl;</p> <p id="p-0005" num="0000">Ring B is a fused benzene ring selected from the group consisting of:</p> <p id="p-0006" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="68.24mm" wi="69.85mm" file="US08119624-20120221-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0007" num="0000">Ring A, ring B, ring C, R<sup>1</sup>, R<sup>1a</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, L<sup>2</sup>, n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).</p>
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Imidazopyridinones (Fri, 18 Feb 2011)
<p id="p-0001" num="0000">The invention relates to imidazopyridinones, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes.</p> <p id="p-0002" num="0000">By activating TLRs, it should be possible to induce or stimulate immune cells to mount an immune response. In particular, the TLR7 has been implicated in viral infections (such as HCV or HBV), cancers and tumours, and T2 Helper cell (TH2) mediated diseases, and hence TLR7 agonists are potentially useful in the treatment of such diseases.</p> <p id="p-0003" num="0000">We have now found a series of imidazopyridinones which are agonists of TLR7. According, there is provided a compound of formula (I)</p> <p id="p-0004" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="28.96mm" wi="59.86mm" file="US20110039884A1-20110217-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0005" num="0000">or a pharmaceutically acceptable salt or solvate thereof, wherein <br/> R<sup>1 </sup>is 3- to 8-membered saturated heterocyclic group wherein one ring member is —O—; and R<sup>2 </sup>is phenyl or pyridinyl, each optionally substituted by C<sub>1</sub>-C<sub>6</sub>alkyl. </p>
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Pyrazolospiroketone acetyl-CoA carboxylase inhibitors (Fri, 04 Feb 2011)
<p id="p-0001" num="0000">The invention provides compounds of Formula (1) or a pharmaceutically acceptable salt of said compound, wherein R<sup>1</sup>, R<sup>2</sup>, and R<sup>3 </sup>are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of acetyl-CoA carboxylase enzyme(s) in an animal.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.94mm" wi="62.74mm" file="US08318762-20121127-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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PROCESSES FOR THE PREPARATION OF 1-[(BENZOIMIDAZOLE-1-YL) QUINOLIN- 8-YL] PIPERIDIN-4-YLAMINE DERIVATIVES (Tue, 01 Feb 2011)

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Pharmaceutical compositions comprising adsorbates of an amorphous drug (Thu, 20 Jan 2011)
Pharmaceutical compositions comprise a low-solubility drug adsorbed onto a high surface area substrate to form an adsorbate. The compositions in some embodiments include a concentration-enhancing polymer.
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HETERO BICYCLIC CARBOXAMIDE DERIVATIVES AND THEIR PHARMACEUTICAL USE AND COMPOSITIONS (Fri, 14 Jan 2011)
<p id="p-0001" num="0000">The present invention relates to compounds of Formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="33.19mm" wi="68.66mm" file="US20110009435A1-20110113-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">and pharmaceutically acceptable salts thereof, processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as anti-inflammatory agents.</p>
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HEPATITIS C VIRUS INHIBITORS (Fri, 14 Jan 2011)
The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts thereof, to compositions containing such compounds and to the use of such compounds as inhibitors of HCV replication.
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Polymorphic form of a [1,2,4]triazole[4,3-A] pyridine derivative inflammatory diseases (Fri, 07 Jan 2011)
<p id="p-0001" num="0000">The present invention relates to a polymorphic form B of Λ/-[3-tert-butyl-1-(3-chloro-4-hydroxyphenyl)-1H-pyrazol-5-yl]-N-{2-[(3-{2-[(2-hydroxyethyl)sulfanyl]phenyl}[1,2,4]triazolo[4,3-a]pyridin-6-yl)sulfanyl]benzyl}urea (I) as de-fined herein. This polymorph is useful in the treatment of various conditions, particularly in the treatment of inflammatory conditions such as chronic obstructive pulmonary disease.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="38.78mm" wi="75.52mm" file="US08222273-20120717-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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HETEROCYCLIC SULFONAMIDES, USES AND PHARMACEUTICAL COMPOSITIONS THEREOF (Thu, 30 Dec 2010)
The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula (I) as defined in the specification. The invention is also directed to compositions containing and uses of the compounds of formula I.
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Substituted pyrrolo-pyrazole derivatives as kinase inhibitors (Thu, 30 Dec 2010)
Compounds represented by formula (Ia) or (Ib) and wherein R and R 1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.
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HETEROCYCLIC SULFONAMIDES, USES AND PHARMACEUTICAL COMPOSITIONS THEREOF (Thu, 30 Dec 2010)
The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula (I) as defined in the specification. The invention is also directed to compositions containing and uses of the compounds of formula I.</p>
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Bicyclic [3.1.0] heteroaryl amides as type 1 glycine transport inhibitors (Fri, 24 Dec 2010)
<p id="p-0001" num="0000">The present invention relates to a series of substituted bicyclic[3.1.0]heteroaryl amides of the Formula I, wherein A, Q, X, Y, Z and R<sub>1</sub>-R<sub>5 </sub>groups are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.</p>
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Bicyclic and tricyclic compounds as KAT II inhibitors (Fri, 24 Dec 2010)
<p id="p-0001" num="0000">Compounds of Formula X:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.67mm" wi="53.59mm" file="US08183238-20120522-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein A, X, Y, Z, R<sup>5</sup>, R<sup>6a</sup>, and R<sup>6b </sup>are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other neurodegenerative and/or neurological disorders in mammals, including humans. </p>
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BICYCLIC AND TRICYCLIC COMPOUNDS AS KAT II INHIBITORS (Fri, 24 Dec 2010)
Compounds of Formula X: wherein A, X, Y, Z, R5, R6a, and R6b are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other neurodegenerative and/or neurological disorders in mammals, including humans.
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BICYCLIC AND TRICYCLIC COMPOUNDS AS KAT II INHIBITORS (Fri, 24 Dec 2010)
Compounds of Formula X: wherein A, X, Y, Z, R5, R6a, and R6b are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other neurodegenerative and/or neurological disorders in mammals, including humans. </p>
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Compounds useful in therapy (Fri, 17 Dec 2010)
<p id="p-0001" num="0000">The present invention provides compounds of formula (I),</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="31.58mm" wi="62.91mm" file="US08093400-20120110-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or pharmaceutically acceptable derivatives thereof wherein the variables Z, Q, Ring A, V, X, Y and Y′ are as defined herein, and pharmaceutical compositions comprising these compounds. The compounds of formula (I) and pharmaceutical compositions comprising them are useful for treating a disorder for which a V1a antagonist is indicated, in particular, dysmenorrhoea. </p>
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L- ( PIPERIDIN-4-YL) -PYRAZOLE DERIVATIVES AS GPR 119 MODULATORS (Fri, 10 Dec 2010)
Compounds of Formula I that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.
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GPR 119 MODULATORS (Fri, 10 Dec 2010)
<br/><br/><br/>Compounds of Formula I that modulate the activity of the G-protein-coupled <br/>receptor GPR119 and their uses in <br/>the treatment of diseases linked to the modulation of the G-protein-coupled <br/>receptor GPR119 in animals are described herein.<br/></p>
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Cycloalkylamino acid derivatives and pharmaceutical compositions thereof (Thu, 09 Dec 2010)
The invention relates to compounds of formula (I) and to pharmaceutically acceptable salts, prodrugs, solvates or hydrates thereof; wherein B, D, E, R 1 , R 2 , R 3 , R 4 , R 5 , R 8 , m, n, p, q, r, s, t and u are as defined herein. This invention also relates to a method of using such compounds in the treatment of hyperproliferative diseases and autoimmune diseases in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
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NOVEL GLUCOCORTICOID RECEPTOR AGONISTS (Fri, 03 Dec 2010)
This invention relates to novel glucocorticoid receptor agonists of formula (I) and to processes and intermediates for their preparation. The present invention also relates to pharmaceutical compositions containing these compounds, to their combination with one or more other therapeutic agents, as well as to their use for the treatment of a number of inflammatory and allergic diseases, disorders and conditions.
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NOVEL GLUCOCORTICOID RECEPTOR AGONISTS (Fri, 03 Dec 2010)
This invention relates to novel glucocorticoid receptor agonists of formula (I) and to processes and intermediates for their preparation. The present invention also relates to pharmaceutical compositions containing these compounds, to their combination with one or more other therapeutic agents, as well as to their use for the treatment of a number of inflammatory and allergic diseases, disorders and conditions. </p>
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CYCLOBUTENEDIONE DERIVATIVES (Fri, 19 Nov 2010)
The present invention relates to compounds of the formula (I): to pharmaceutically acceptable salts therefore and to pharmaceutically acceptable solvates of said compounds and salts, wherein the substituents are defined herein; to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly inflammatory conditions.
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CYCLOBUTENEDIONE DERIVATIVES (Fri, 19 Nov 2010)
The present invention relates to compounds of the formula (I): to pharmaceutically acceptable salts therefore and to pharmaceutically acceptable solvates of said compounds and salts, wherein the substituents are defined herein; to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly inflammatory conditions.
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CYCLOBUTENEDIONE DERIVATIVES (Fri, 19 Nov 2010)
The present invention relates to compounds of the formula (I): to pharmaceutically acceptable salts therefore and to pharmaceutically acceptable solvates of said compounds and salts, wherein the substituents are defined herein; to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly inflammatory conditions.
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Tricyclic compounds, compositions and methods (Fri, 12 Nov 2010)
<p id="p-0001" num="0000">The present invention is directed to compounds of Formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="42.33mm" wi="67.48mm" file="US08158660-20120417-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or salt thereof, which are modulators of the glucocorticoid receptor. The compounds and salts of the invention are useful in the treatment of conditions mediated by glucocorticoid receptor activity. </p>
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GPR 119 MODULATORS (Fri, 12 Nov 2010)
<p id="p-0001-en" num="0000">Compounds of Formula (I) that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.</p>
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GPR 119 MODULATORS (Fri, 12 Nov 2010)
Compounds of Formula (I) that modulate the activity of the G -protein-coupled receptor GPFM 19 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.
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GPR 119 MODULATORS (Fri, 12 Nov 2010)
Compounds of Formula (I) that modulate the activity of the G-protein-coupled receptor GPR1 19 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.
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GPR 119 MODULATORS (Fri, 12 Nov 2010)
Compounds of Formula (I) that modulate the activity of the G -protein-coupled receptor GPFM 19 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein. </p>
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GPR 119 MODULATORS (Thu, 11 Nov 2010)
Compounds of Formula (I) that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein. </p>
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PYRAZOLINE COMPOUNDS (Fri, 05 Nov 2010)
<p id="p-0001-en" num="0000">Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I:</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="30.90mm" wi="58.17mm" file="US20100280016A1-20101104-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003-en" num="0000">wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3A</sup>, R<sup>3B</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>6</sup>, R<sup>7</sup>, R<sup>8</sup>, and X are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, and intermediates are also disclosed.</p>
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Sulfonamide derivatives for the treatment of diseases (Fri, 29 Oct 2010)
<p id="p-0001" num="0000">The invention relates to compounds of formula (1)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="29.38mm" wi="75.44mm" file="US08013019-20110906-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions. </p>
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Benzimidazolone Compounds Having 5-HT4 Receptor Agonistic Activity (Fri, 29 Oct 2010)
<p id="p-0001-en" num="0000">This invention provides a compound of the formula (I):</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="34.54mm" wi="69.85mm" file="US20100273794A1-20101028-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003-en" num="0000">or a pharmaceutically acceptable salt thereof, and compositions containing such compounds and the use of such compounds for the manufacture of medicament for gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes and apnea syndrome.</p> <p id="p-0004-en" num="0000">These compounds have 5-HT<sub>4 </sub>receptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans.</p>
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COMPOSITIONS OF SULOPENEM AND USE FOR TREATING TUBERCULOSIS (Fri, 29 Oct 2010)
The present invention relates to methods of treating tuberculosis, including multi-drug resistant varieties and latent tuberculosis. More particularly, the present invention relates to a method of treating tuberculosis in a mammal comprising administering to said mammal in need thereof an effective amount of (5R,6S)-6-[(1R)-1-hydroxyethyl]-7-oxo-3-[[(1R,3S)-tetrahydro-1-oxido-3-thienyl]thio]-4-thia-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid ("sulopenem") or a pharmaceutically acceptable salt or prodrug thereof. The present invention also relates to a method of treating tuberculosis in a mammal comprising administering to said mammal in need thereof an effective amount of sulopenem or a pharmaceutically acceptable salt or prodrug thereof in combination with an agent useful in the treatment of tuberculosis. The present invention also relates to a pharmaceutical composition comprising (i) a therapeutically effective amount of sulopenem or a pharmaceutically acceptable salt or prodrug thereof (ii) a therapeutically effective amount of at least one other agent useful in the treatment of tuberculosis and (iii) one or more pharmaceutically acceptable carriers or vehicles.
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Substituted bicyclocarboxyamide compounds (Fri, 22 Oct 2010)
<p id="p-0001" num="0000">This invention provides a compound of the formula</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.06mm" wi="69.77mm" file="US07964732-20110621-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">These compounds are useful for the treatment of disease conditions caused by overactivation of the VR1 receptor such as pain, or the like in mammal. This invention also provides a pharmaceutical composition comprising the above compound.</p>
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Pharmaceutical compositions and methods of treating dry eye disorders (Fri, 22 Oct 2010)
<p id="p-0001" num="0000">Inhibitors of Janus kinase-3 (“Jak3”) are useful for treating dry eye disorders and other disorders requiring the wetting of the eye. Jak3 inhibitors useful for treating eye disorders include the compound 3-{(3R,4R)-4-Methyl-3-[methyl-(7H-pyrrolo [2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl}-3-oxo-propionitrile.</p>
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EP2/4 AGONISTS (Fri, 15 Oct 2010)
EP2/4 compounds having improved dual pharmacological activity are described. The uniqueness of using EP2/4 dual agonists resides in their ability to modify both uveoscleral outflow via the ciliary muscle and conventional outflow via trabecular meshwork and Schlemm's canal all in the same treatment paradigm. The compounds can be employed for the treatment of glaucoma and ocular hypertension. Formula (I).
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4, 5-DIHYDRO-1H-PYRAZOLE COMPOUNDS AND THEIR PHARMACEUTICAL USES (Fri, 15 Oct 2010)
Mineralocorticoid receptor antagonists (MRa), pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetic nephropathy and hypertension in mammals, including humans.
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