2-Indolones substituted in 5 by a cyclic hydrazide radical, their preparation and their use in cardio-active medicaments
申请人:LES LABORATOIRES BEECHAM S.A.
公开号:EP0351213A2
公开(公告)日:1990-01-17
A compound of formula (I) or a pharmaceutically acceptable salt thereof,
in which,
R1 is hydrogen or lower alkyl;
R2 is hydrogen or lower alkyl;
R4 and R4 together form a group = N-Ra, or = CRaRb, where
Ra is hydrogen, lower alkyl, aryl, aryloxy, lower alkylcarbonyl, arylcarbonyl, aryloxycarbonyl, lower alkoxy, lower alkoxy carbonyl, lower alkoxy carbonyl alkoxy, lower -thioalkoxy, hydroxy, nitrile, heterocyclyl, or -NRcRd, where Rc is hydrogen, lower alkyl, cycloalkyl, aryl, aralkyl, lower alkylcarbonyl, arylcarbonyl, aminocarbonyl, aminothiocarbonyl, aminoiminocarbonyl, lower alkoxycarbonyl, lower alkoxythiocarbonyl, aryloxycarbonyl, thiocarbonyl, nitrile, carboxyl, heterocyclyl or heterocyclylcarbonyl, and Rd is hydrogen or lower alkyl; Rb is hydrogen, lower alkyl, aryl, lower alkylcarbonyl, lower alkoxycarbonyl, nitrile or nitro;
or R4 is -NH-Ra, in which Ra is as defined above, and R4' is hydrogen or lower alkyl;
each of R3 and R5 is independently hydrogen, lower alkyl, aryl, lower alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, heterocyclylcarbonyl, optionally substituted aminocarbonyl, lower alkoxycarbonyl or aryloxycarbonyl;
R6 is hydrogen, lower alkyl or halogen;
and A is sulphur, oxygen, -NH- or -CH2-,
is useful for the treatment of heart disease.
式 (I) 的化合物或其药学上可接受的盐、
其中
R1 是氢或低级烷基
R2 是氢或低级烷基
R4 和 R4 共同组成一个基团 = N-Ra,或 = CRaRb,其中
Ra是氢、低级烷基、芳基、芳氧基、低级烷基羰基、芳基羰基、芳氧基羰基、低级烷氧基、低级烷氧基羰基、低级烷氧基羰基、低级烷氧基烷氧基、低级硫代烷氧基、羟基、腈基、杂环烷基或-NRcRd,其中 Rc 是氢、低级烷基、环烷基、芳基、芳烷基、芳氧基羰基、低级烷氧基羰基、低级硫代烷氧基、羟基、腈基、杂环烷基、芳基、芳烷基、低级烷基羰基、芳基羰基、氨基羰基、氨基硫代羰基、氨基亚氨基羰基、低级烷氧基羰基、低级烷氧基硫代羰基、芳氧基羰基、硫代羰基、腈、羧基、杂环烷基或杂环烷基羰基,Rd 为氢或低级烷基;Rb 是氢、低级烷基、芳基、低级烷基羰基、低级烷氧基羰基、腈或硝基;
或 R4 是-NH-Ra,其中 Ra 如上定义,R4'是氢或低级烷基;
R3 和 R5 各自独立地为氢、低级烷基、芳基、低级烷基羰基、芳基羰基、芳基羰基、杂环羰基、任选取代的氨基羰基、低级烷氧基羰基或芳氧基羰基;
R6 是氢、低级烷基或卤素;
A是硫、氧、-NH-或-CH2-、
可用于治疗心脏病。