ROBERT M. JONES,JUERG LEHMANN,WEICHAO CHEN,ABU J. M. SADEQUE,JEFFREY EDWARDS,GLEN MARQUEZ,MICHAEL E. MORGAN,SUN HEE KIM
申请号:
MX2013003184
公开号:
MX2013003184A
申请日:
2011.09.21
申请国别(地区):
MX
年份:
2013
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,<; i>;N-dimethylbenzamide; -fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-yl)-1,2,4-oxadiaz ol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)-N-methylbenza mide; and 3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-yl)-1,2,4-oxadia zol-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 presente invención se refiere a agonistas del receptor GPR119: 3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-il)-1, 2, 4-oxadiazol-5-iI)piperidin-1-il)pirimidin-4-ilamino)-N, N-dimetilbenzamida; -fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2- iI)-1, 2, 4-oxadiazol-5-il)piperidin-1-il)pirimidin-4-ilamino)-N-m etilbenzamida; y 3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-il )-1, 2, 4-oxadiazol-5-iI)piperidin-1-il)pirimidin-4-ilamino)benzam ida, y sales, solvatos e hidratos farmacéuticamente aceptables de los mismos, que son útiles como un agente farmacéutico individual o en combinación con uno o más agentes farmacéuticos adicionales, tales como, un inhibidor de DPP-IV, una biguanida, un inhibidor de alga-glucosidasa, un análogo de insulina, una sulfonilur