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MODULATORS OF THE GPR119 RECEPTOR AND THE TREATMENT OF DISORDERS RELATED THERETO
专利权人:
发明人:
申请号:
HK13113753.5
公开号:
HK1187038A
申请日:
2013.12.11
申请国别(地区):
HK
年份:
2014
代理人:
摘要:
The present invention relates to the GPR119 receptor agonists:3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)-N,N-dimethylbenzamide -fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)-N-methylbenzamide and 3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)benzamide, and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single pharmaceutical agent or in combination with one or more additional pharmaceutical agents, such as, a DPP-IV inhibitor, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder a condition ameliorated by increasing secretion of an incretin a condition ameliorated by increasing a blood incretin level a condition characterized by low bone mass a neurological disorder a metabolic-related disorder type 2 diabetes obesity and complications related thereto.La présente invention concerne les agonistes du récepteur GPR119 : 3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl)pipéridin-1-yl)pyrimidin-4-ylamino)-N,N-diméthylbenzamide 3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl)pipéridin-1-yl)pyrimidin-4-ylamino)-N-méthylbenzamide et 3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl)pipéridin-1-yl)pyrimidin-4-ylamino)benzamide, ainsi que leurs sels, solvates et hydrates de qualité pharmaceutique, utiles en tant quagent pharmaceutique seul ou combiné à un ou plusieurs autres agents pharmaceutiques, tels quun inhibiteur de DPP-IV, un biguanide, un inhibiteur dalpha-glucosidase, un analogue dinsuline, une sulfonylurée, un inhibiteur de SGLT2, un méglitinide, une thiazolidi
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