公开(公告)号：EP0454330A1

公开(公告)日：1991-10-30

申请号：EP91303264.5

申请日：1991-04-12

申请人： YAMANOUCHI PHARMACEUTICAL CO. LTD.

发明人： Hara, Hiromu ,  Maruyama, Tatsuya ,  Saito, Munetoshi ,  Takeuchi, Makoto ,  Mase, Toshiyasu

IPC分类号： C07D235/26 ,  A61K31/415 ,  C07D403/04

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D235/26 ,  C07D249/08

摘要： Benzimidazolinone derivatives of the general formula (I):
wherein R 1 , R 2 and R 3 , 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 ; R 4 and R 5 , which may be the same or different, each is a lower alkyl group or R 4 and R 5 , 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 R 1 , R 2 and R 3 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.

摘要翻译： 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，各自是氢或卤原子或低级烷基，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，低级烷氧羰基，氨基甲酰基，硝基或含氮的5-或6-元杂环基团; A是任选具有至少一个分支的亚乙基; R4和R5可以相同或不同，各自为低级烷基或R4和R5与相邻的氮原子一起代表吡咯烷基，哌啶子基或吗啉代基，条件是当为哌啶子基或二乙基氨基时，在 公开了R 1，R 2和R 3中的至少一个不是氢原子，或其药学上可接受的盐，其制备方法和包含其的药物组合物。 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。