申请人:YAMANOUCHI PHARMACEUTICAL CO. LTD.
公开号:EP0454330A1
公开(公告)日:1991-10-30
Benzimidazolinone derivatives of the general formula (I):
wherein R1, R2 and R3, which may be the same or different, each is a hydrogen or halogen atom or a lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, hydroxyl, lower alkoxy, aryloxy, acyl, cyano, carboxyl, a lower alkoxycarbonyl, carbamoyl, nitro or nitrogen-containing 5- or 6-membered heterocyclic group; A is an ethylene group which may optionally have at least one branch ; R4 and R5, which may be the same or different, each is a lower alkyl group or R4 and R5, together with the adjacent nitrogen atom, represent a pyrrolidinyl, piperidino or a morpholino group provided that when
is a piperidino or diethylamino group, at least one of R1, R2 and R3 is other than a hydrogen atom, or pharmaceutically acceptable salts thereof, methods of producing the same and pharmaceutical compositions containing the same are disclosed. Pharmacologically, the above compounds (I) have pulmonary surfactant secretion promoting activity.
通式(I)的苯并咪唑啉酮衍生物:
其中 R1、R2 和 R3 可以相同或不同,各自为氢原子或卤素原子或低级烷基、卤代低级烷基、羟基低级烷基、羟基、低级烷氧基、芳氧基、酰基、氰基、羧基、低级烷氧基羰基、氨基甲酰基、硝基或含氮的 5 或 6 元杂环基团;R4 和 R5(可以相同或不同)各自是低级烷基,或 R4 和 R5 与相邻的氮原子一起代表吡咯烷基、哌啶基或吗啉基,条件是
公开了 R1、R2 和 R3 中至少一个不是氢原子的哌啶或二乙胺基团,或其药学上可接受的盐类,以及生产上述化合物和含有上述化合物的药物组合物的方法。在药理学上,上述化合物(I)具有促进肺表面活性物质分泌的活性。