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| Number | Title | Issue Date |
| 8188092 | Substituted pyrazines as DGAT-1 inhibitors DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity | 05/29/2012 |
| 8188093 | Pyrazinecarboxamide derivatives as HDL-cholesterol raising agents The present invention relates to a method of raising HDL cholesterol comprising administering to a patient in need thereof a compound of the formula wherein A, G, R1 to R8 and R17 are as def... | 05/29/2012 |
| 8163758 | Phenyl substituted pyrazinoylguanidine sodium channel blockers possessing beta agonist activity Provided is class of sodium channel blockers. One example of such a compound is shown by the following formula: The compounds are useful for promoting hydration of mucosal surfaces and treating a variety of disease conditio... | 04/24/2012 |
| 8124607 | Poly aromatic pyrazinoylguanidine sodium channel blockers Polyaromatic sodium channel blockers represented by the formula: are provided where the structural variables are defined herein. The invention also includes a variety of compositions, combinations and methods of treatment u... | 02/28/2012 |
| 8114881 | 2-pyrazinone derivatives for the treatment of disease or condition in which inhibition of neutrophil elastase activity is beneficial The invention provides compounds of formula wherein R1, R3, R4, R5, R14, X and W are as defined in the specification and optical isomers, racemates and tautomers thereo... | 02/14/2012 |
| 8110579 | 5,6-bisaryl-2-pyridine-carboxamide derivatives, preparation and application thereof in therapeutics as urotensin II receptor antagonists The present invention relates to derivatives of 5,6-bisaryl-2-pyridine-carboxamide, their preparation and their application in therapeutics as antagonists of urotensin II receptors. ... | 02/07/2012 |
| 8093252 | Crystalline polymorphic form of glucokinase activator A new polymorphic form of 3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-{[(1S)-1-methyl-2-(methyloxy)ethyl]oxy}-N-(5-methylpyrazin-2-yl)benzamide, processes for making it and its use as an activator of glucokinase are described. ... | 01/10/2012 |
| 8084456 | Pyrazine-based tubulin inhibitors A compound of general formula (I) or pharmaceutically acceptable prodrugs, salts, hydrates, solvates, crystal forms or diastereomers thereof is described. A method of treating a hyperproliferation-related disease state or disorder in a subject using a compound of fo... | 12/27/2011 |
| 8071606 | Substituted pyrazinone amides useful for activation of glucokinase 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. The variab... | 12/06/2011 |
| 8067420 | Substituted pyrazinone melanin concentrating hormone receptor-1 antagonists and methods The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1 | 11/29/2011 |
| 8048886 | Substituted pyrazine-3-one-derivatives as IAP inhibitors The present invention relates to novel IAP inhibitor compounds of formula I: ... | 11/01/2011 |
| 8034819 | Glucokinase activator A compound, or a pharmaceutically acceptable salt thereof, represented by the formula (1), (wherein, the carbon atom marked with an * is in the R-configuration, R1 represents a hydrogen atom, a halogen atom, an a... | 10/11/2011 |
| 8012984 | Substituted pyrazinone melanin concentrating hormone receptor-1 antagonists and methods The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1 | 09/06/2011 |
| 8003654 | N-glycinsulfonamide derivatives and uses as orexin receptor antagonists The invention relates to novel sulfonamide compounds of the formula (I) and their use as orexin receptor antagonists. ... | 08/23/2011 |
| 7998965 | Glutamate aggrecanase inhibitors The present invention relates to modulators of metalloproteinase activity. ... | 08/16/2011 |
| 7994179 | Carbamoyl compounds as DGAT1 inhibitors 190 DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity | 08/09/2011 |
| 7994178 | Crystalline rosuvastatin calcium and compositions thereof for treatment of hyperlipidaemia The present invention provides a crystalline form of rosuvastatin calcium characterized by an X-ray powder diffraction pattern having peaks at about 4.7, 19.4 and 22.3° 2θ±0.2° 2θ. The crystalline form of the invention may be further characterized by a DSC ther... | 08/09/2011 |
| 7989456 | Pyrazine kinase inhibitors The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various diseas... | 08/02/2011 |
| 7981898 | Methods of enhancing mucosal hydration and mucosal clearance by treatment with sodium channel blockers and osmolytes The present invention relates to methods and compositions for treating diseases ameliorated by increased mucociliary clearance and mucosal hydration by administering an effective amount of a sodium channel blocker as defined herein and an osmolyte to a subject to a ... | 07/19/2011 |
| 7956059 | Aliphatic amide and ester pyrazinoylguanidine sodium channel blockers The present invention relates to pyrazinoylguanidine compounds represented by formula (I): where the structural variables are defined herein. The compounds are useful as, for example, sodium channel blockers. ... | 06/07/2011 |
| 7932256 | ()-4-(1-cyclopropyl-2-methoxyethyl)-6-(6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino)-5-oxo-4,5-dihydropyrazine-2-carbonitrile: a pyrazinone modulator of corticotropin-releasing factor receptor activity The invention relates to the compound (S)-4-(1-cyclopropyl-2-methoxyethyl)-6-(6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino)-5-oxo-4,5-dihydropyrazine-2-carbonitrile, pharmaceutical compositions of the compound, and methods of using the compound for the treatmen... | 04/26/2011 |
| 7919497 | Analogs of dehydrophenylahistins and their therapeutic use Compounds represented by the following structure (II) are disclosed: as are methods for making such compounds. Compositions and methods for treating various disease conditions including cancer and non-cancer diseases associ... | 04/05/2011 |
| 7884108 | Certain substituted pyrazinones Compounds of Formula I that inhibit Btk are described herein. Pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicl... | 02/08/2011 |
| 7875619 | Hetero substituted sodium channel blockers The present invention relates to group of butylphenyl-pyrazinoylguanidine compounds useful as sodium channel blockers. The compounds may be used to promote promoting hydration of mucosal surfaces. ... | 01/25/2011 |
| 7868010 | Capped pyrazinoylguanidine sodium channel blockers The invention relates to substituted pyrazinoylguanidine compounds. These compounds are useful as sodium channel blockers, and may be effective in treating a variety of conditions including chronic bronchitis and cystic fibrosis. ... | 01/11/2011 |
| 7851476 | Crystalline forms of 1-benzoyl-4-[2-[4-methoxy-7-(3-methyl-1-1,2,4-triazol-1-YL)-1-[(phosphonooxy)methyl]-1-pyrrolo[2,3-]pyridin-3-YL]-1,2-dioxoethyl]-piperazine Crystalline forms of 1-benzoyl-4-[2-[4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-yl)-1-[(phosphonooxy)methyl]-1H-pyrrolo[2,3-c]pyridin-3-yl]-1,2-dioxoethyl]-piperazine its salts and solvates thereof are herein set forth, as ar... | 12/14/2010 |
| 7842697 | Soluble amide and ester pyrazinoylguanidine sodium channel blockers The present invention relates to pyrazinoylguanidine compounds represented by the formula: where the structural variables are defined herein. The compounds are useful as sodium channel blockers. ... | 11/30/2010 |
| 7820678 | Sodium channel blockers Provided are methods of increasing hydration of mucosal surfaces by topically administering sodium channel blocking pyrazinoylguanidine compounds. ... | 10/26/2010 |
| 7812028 | 3-pyridinecarboxamide derivatives as HDL-cholesterol raising agents The present invention relates to a method of raising HDL cholesterol comprising administering to a patient in need thereof a compound of the formula wherein A, G, R1 to R8 and R17 are as def... | 10/12/2010 |
| 7803804 | Substituted pyrazines for use in the treatment of inflammatory or allergic conditions Disclosed herein are substituted pyrazine compounds and tautomers, stereoisomers, solvates, or pharmaceutically acceptable salts thereof for the treatment of conditions mediated by the blockade of an epithelial sodium channel, particularly an inflammatory or allergi... | 09/28/2010 |
| 7737151 | Pyrazine kinase inhibitors The present invention relates to compounds useful as inhibitors of protein kinases of the following formula: or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutically acceptable composition... | 06/15/2010 |
| 7737152 | 6-carboaryl-oxy-pyrazin-2-yl-carboaryl-amines and compositions comprising said compounds The present invention pertains to certain 6-carboaryloxy-pyrazin-2-yl-carboaryl-amines of the following formula, and pharmaceutically acceptable salts thereof, which, inter alia, inhibit RAF (e.g., B-RAF) activity, inhibit cell proliferation, treat cancer, etc., whe... | 06/15/2010 |
| 7727991 | Substituted melanocortin receptor-specific single acyl piperazine compounds Melanocortin receptor-specific compounds of the general formula and pharmaceutically acceptable salts thereof, where J is a substituted or unsubstituted monocyclic or bicyclic ring structure, W is a heteroatom unit with at ... | 06/01/2010 |
| 7662825 | N-pyrazinyl-phenylsulphonamides and their use in the treatment of chemokine mediated diseases The invention provides N-pyrazinyl-phenyl-sulphonamides of formula (I) for use in the treatment of chemokine mediated diseases. Particularly inflammatory diseases, such as asthma. ... | 02/16/2010 |
| 7572797 | Amino substituted pyrazine derivatives for the treatment of pain The present invention relates to compounds of the formula and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containin... | 08/11/2009 |
| 7473693 | Stable dispersion of solid particles comprising a water-insoluble pyrazine compound A process for the preparation of a stable dispersion of solid particles, in an aqueous medium comprising combining (a) a first solution comprising a substantially water-insoluble substance which is a pyrazine compound of Formula I, a water-miscible organic solvent a... | 01/06/2009 |
| 7399766 | Soluble amide & ester pyrazinoylguanidine sodium channel blockers The present invention provides a pyrazinoylguanidine compound represented by formula (I): where the structural variables are as defined herein. The compounds are useful for promoting hydration of mucosal surfaces. ... | 07/15/2008 |
| 7388013 | Capped pyrazinoylguanidine sodium channel blockers The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers. ... | 06/17/2008 |
| 7375107 | Alaphatic pyrazinoylguanidine sodium channel blockers The present invention provides compound represented by formula (I): where the structural variables are defined herein. The compounds function as sodium channel blockers and may be used to treat a variety of respiratory cond... | 05/20/2008 |
| 7368450 | Sodium channel blockers The present invention relates to compounds represented by formula (I): in which at least one of R3 and R4 is a group represented by formula (A): where the st... | 05/06/2008 |
