发明名称 Monoacylglycerol lipase inhibitors for the treatment of metabolic diseases and related disorders
摘要 Disclosed are compounds, compositions and methods for treating metabolic diseases, including obesity and diabetes. Such compounds are represented by formula (I) as follows:; wherein Y and Z are defined herein.
申请公布号 US9375430(B2) 申请公布日期 2016.06.28
申请号 US201213628452 申请日期 2012.09.27
申请人 Janssen Pharmaceutica NV 发明人 Connelly Margery;Flores Christopher M.;Macielag Mark J.
分类号 A61K31/397;A61K31/00;A61K31/496 主分类号 A61K31/397
代理机构 代理人 Dodd Thomas J.
主权项 1. A method for treating a patient suffering from obesity, said method comprising administering to a subject in need thereof, a therapeutically effective amount of a compound of formula (I) or an enantiomer, diastereomer, solvate, or pharmaceutically acceptable salt thereof;wherein: Y is a heteroaryl selected from the group consisting of thienyl, furanyl, thiazolyl, isothiazolyl, oxazolyl, pyridinyl, isoxazolyl, imidazolyl, furazan-3-yl, pyrazolyl, triazolyl, tetrazolyl, and [1,2,3]thiadiazolyl; wherein Y is optionally independently substituted with one to two substituents selected from the group consisting of fluoro, chloro, bromo, C1-4alkyl, cyano, and trifluoromethyl; Z is a heteroaryl selected from the group consisting of indolyl, indazolyl, benzoxazolyl, benzothiazolyl, benzothienyl, benzofuranyl, imidazo[1,2-a]pyridin-2-yl, pyrrolo[2,3-b]pyridinyl, pyrrolo[3,2-b]pyridinyl, thieno[2,3-b]pyridinyl, quinolinyl, quinazolinyl, and benzimidazolyl; wherein said Z is optionally independently substituted with one to two substituents selected from the group consisting of C1-4alkyl, trifluoromethyl, 2,2,2-trifluoroethoxy-methyl, 2,2,2-trifluoroethoxy, trifluoromethylthio, chloro, fluoro, bromo, and iodo;with the proviso that a compound of formula (I) is other than a compound wherein Y is thiazol-4-yl and Z is 5-fluoro-3H-benzimidazol-2-yl; a compound wherein Y is thiazol-2-yl and Z is 5-fluoro-1H-benzimidazol-2-yl; a compound wherein Y is thiazol-4-yl and Z is 5-chloro-benzofuran-2-yl; a compound wherein Y is isothiazol-5-yl and Z is 6-trifluoromethyl-1H-indol-2-yl; a compound wherein Y is thiazol-4-yl and Z is 5-trifluoromethyl-1H-pyrrolo[3,2-b]pyridin-2-yl; a compound wherein Y is thiazol-2-yl and Z is 8-bromo-6-chloro-imidazo[1,2-a]pyridin-2-yl; or a compound wherein Y is thiazol-2-yl and Z is 6-trifluoromethyl-imidazo[1,2-a]pyridin-2-yl.
地址 Beerse BE