申请人:SMITH KLINE & FRENCH LABORATORIES
LIMITED
公开号:EP0096517A2
公开(公告)日:1983-12-21
Pyrazinone derivatives of the formula (I):
or a pharmaceutically acceptable salt thereof, wherein R', R2 and R3 are independently hydrogen or C1-4 alkyl, and R4 is hydrogen, a C1-6 alkoxycarbonyl group optionally substituted by amino, hydroxy, C1-4 alkoxy or carboxy (wherein the substituent is not on the carbon atom adjacent to the -CO-O moiety); or R4 is a group -CO-(NR5)n-R6 wherein n is zero or one, R6 is hydrogen, optionally substituted C1-6 alkyl, optionally substituted phenyl, or optionally substituted pyridyl, and R5 is hydrogen, C1-6 alkyl or RS and R6 form together with the nitrogen atom to which they are attached to piperidine, morpholino, piperazine or N-/C1-6)- alkylpiperazine ring; are described.
Processes for their preparation are described, involving inter alia novel phenyl pyrazinone intermediates. Their use in pharmaceutical compositions is described, as is their use as inotropic agents.
式 (I) 的吡嗪酮衍生物:
或其药学上可接受的盐,其中 R'、R2 和 R3 独立地为氢或 C1-4 烷基,R4 为氢、任选被氨基、羟基、C1-4 烷氧基或羧基取代的 C1-6 烷氧基羰基(其中取代基不在与 -CO-O 分子相邻的碳原子上);或 R4 是基团 -CO-(NR5)n-R6,其中 n 为 0 或 1,R6 为氢、任选取代的 C1-6 烷基、任选取代的苯基或任选取代的吡啶基,R5 为氢、C1-6 烷基或 RS 和 R6 与它们所连接的氮原子一起形成哌啶、吗啉、哌嗪或 N-/C1-6)-烷基哌嗪环。
描述了它们的制备过程,其中包括新型苯基吡嗪酮中间体。介绍了它们在药物组合物中的用途,以及它们作为肌张力剂的用途。