- BENZAMIDES OF PYRAZOLYL-AMINO-PYRIMIDINYL DERIVATIVES, AND COMPOSITIONS AND METHODS THEREOF
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Provided is a novel class of orally and/or topically available, selective and potent JAK inhibitors as safe and effective therapeutics against various diseases and disorders. More particularly, provided are pharmaceutical composition of these compounds and methods of their preparation and use thereof.
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Paragraph 00571; 00653
(2020/07/07)
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- BENZETHERS AND ANILINES OF PYRAZOLYL-AMINO-PYRIMIDINYL DERIVATIVES, AND COMPOSITIONS AND METHODS THEREOF
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Provided is a novel class of orally and/or topically available, selective and potent JAK inhibitors as safe and effective therapeutics against various diseases and disorders. Also provided is pharmaceutical composition of these compounds and methods of th
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Paragraph 00292
(2020/10/21)
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- NOVEL SULFONAMIDE CARBOXAMIDE COMPOUNDS
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The present invention relates to compounds of formula (I) wherein Q is selected from O or S; R1 is a non-aromatic heterocyclic group comprising at least one ring nitrogen atom, wherein R1 is attached to the sulfur atom of the sulfonylurea group by a ring carbon atom, and wherein R1 may optionally be substituted; and R2 is a cyclic group substituted at the α-position, wherein R2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.
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- BENZIMIDAZOLES FOR USE IN THE TREATMENT OF CANCER AND INFLAMMATORY DISEASES
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Provided herein are methods for treating, preventing, or ameliorating one or more symptoms of a condition, disorder, or disease mediated by a lipid kinase or a protein kinase with benzimidazoles, for example, of Formula I or II, and pharmaceutical compositions thereof. Also provided herein are benzimidazoles, and pharmaceutical compositions thereof; and methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease.
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Paragraph 00413; 00414
(2017/04/11)
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- HOMOBISPIPERIDINYL DERIVATIVES AS LIVER X RECEPTOR BETA AGONISTS, COMPOSITIONS, AND THEIR USE
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In its many embodiments, the present invention provides certain substituted bispiperidinyl compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein ring A, ring B, R1, R2, R3, L, R4, X, Z, Li, Q and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver Χ-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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Page/Page column 49
(2017/07/05)
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- BENZIMIDAZOLE DERIVATIVES AS ERBB TYROSINE KINASE INHIBITORS FOR THE TREATMENT OF CANCER
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Provided herein are benzimidazole derivatives, for example, of Formula I, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease.
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Paragraph 00326
(2015/11/10)
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- Discovery of 5-chloro-4-((1-(5-chloropyrimidin-2-yl)piperidin-4-yl)oxy)-1-(2-fluoro-4-(methylsulfonyl)phenyl)pyridin-2(1 H)-one (BMS-903452), an antidiabetic clinical candidate targeting GPR119
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G-protein-coupled receptor 119 (GPR119) is expressed predominantly in pancreatic β-cells and in enteroendocrine cells in the gastrointestinal tract. GPR119 agonists have been shown to stimulate glucose-dependent insulin release by direct action in the pancreas and to promote secretion of the incretin GLP-1 by action in the gastrointestinal tract. This dual mechanism of action has generated significant interest in the discovery of small molecule GPR119 agonists as a potential new treatment for type 2 diabetes. Herein, we describe the discovery and optimization of a new class of pyridone containing GPR119 agonists. The potent and selective BMS-903452 (42) was efficacious in both acute and chronic in vivo rodent models of diabetes. Dosing of 42 in a single ascending dose study in normal healthy humans showed a dose dependent increase in exposure and a trend toward increased total GLP-1 plasma levels.
- Wacker, Dean A.,Wang, Ying,Broekema, Matthias,Rossi, Karen,Oconnor, Steven,Hong, Zhenqiu,Wu, Ginger,Malmstrom, Sarah E.,Hung, Chen-Pin,Lamarre, Linda,Chimalakonda, Anjaneya,Zhang, Lisa,Xin, Li,Cai, Hong,Chu, Cuixia,Boehm, Stephanie,Zalaznick, Jacob,Ponticiello, Randolph,Sereda, Larisa,Han, Song-Ping,Zebo, Rachel,Zinker, Bradley,Luk, Chiuwa Emily,Wong, Richard,Everlof, Gerry,Li, Yi-Xin,Wu, Chunyu K.,Lee, Michelle,Griffen, Steven,Miller, Keith J.,Krupinski, John,Robl, Jeffrey A.
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supporting information
p. 7499 - 7508
(2014/12/11)
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- A library of conformationally restricted saturated heterocyclic sulfonyl chlorides
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An approach to the synthesis of conformationally restricted saturated heterocyclic sulfonyl chlorides is described. Being guided by the principle of diversity-oriented conformational restriction, a mini-library of saturated heterocyclic sulfonyl chlorides
- Zhersh, Sergey,Buryanov, Volodymyr V.,Karpenko, Oleksandr V.,Grygorenko, Oleksandr O.,Tolmachev, Andrey A.
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p. 3669 - 3674
(2011/12/16)
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- 6 SUBSTITUTED 2-HETEROCYCLYLAMINO PYRAZINE COMPOUNDS AS CHK-1 INHIBITORS
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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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Page/Page column 126-127
(2010/04/03)
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- PYRIDONE GPR119 G PROTEIN-COUPLED RECEPTOR AGONISTS
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Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR 119 G protein-coupled receptor modulator therapy. These novel compounds have the structure Formula I or Formula IA.
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Page/Page column 94-96
(2009/02/11)
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- Nitrilase-catalyzed enantioselective synthesis of pyrrolidine- And piperidinecarboxylic acids
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The enantioselective synthesis of the nonproteinogenic amino acids β-proline and nipecotic acids from their readily available nitriles is achieved in high enantiomeric excess by commercially available nitrilases. The presented procedure comprises not more than 4 steps, thus considerably reducing the multiple steps generally required. Amide formation is also observed for specific heterocyclic nitriles.
- Winkler, Margit,Meischler, Dorith,Klempier, Norbert
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p. 1475 - 1480
(2008/09/16)
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- NOVEL ANTIDIABETIC COMPOUNDS HAVING HYPOLIPIDAEMIC, ANTIHYPERTENSIVE PROPERTIES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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New thiazolidin-2,4-dione derivatives of formula (1) in which A, W, Q, B, D, X, Y, Z, R', k and p are defined as in claim 1; their tautomeric forms, their derivatives, their steroisomers, their polymorphs, their pharmaceutical acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. Methods for their preparation and their use as antidiabetic compounds are claimed.
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- Antidiabetic compounds having hypolipidaemic, antihypertensive properties, process for their preparation and pharmaceutical compositions containing them
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Novel antidiabetic compounds, their tautomeric forms, their derivatives, their steroisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutical acceptable compositions containing them: Methods for preparing the antidiabetic compounds and their uses.
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