申请人:Yamanouchi Pharmaceutical Co., Ltd.
公开号:US05162318A1
公开(公告)日:1992-11-10
Benzimidazolinone derivatives of the general formula (I): ##STR1## wherein R.sup.1, R.sup.2 and R.sup.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.sup.4 and R.sup.5, which may be the same or different, each is a lower alkyl group or R.sup.4 and R.sup.5, together with the adjacent nitrogen atom, represent a pyrrolidinyl, piperidino or a morpholino group provided that when ##STR2## is a piperidino or diethylamino group, at least one of R.sup.1, R.sup.2 and R.sup.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.
通式(I)的苯并咪唑啉衍生物:##STR1## 其中R.sup.1,R.sup.2和R.sup.3,可以相同或不同,分别是氢原子或卤素原子或较低的烷基,卤代较低的烷基,羟基较低的烷基,羟基,较低的烷氧基,芳氧基,酰基,氰基,羧基,较低的烷氧羰基,氨基甲酰基,硝基或含氮的5或6元杂环基;A是乙烯基,可以选择性地具有至少一个支链;R.sup.4和R.sup.5,可以相同或不同,分别是较低的烷基或R.sup.4和R.sup.5与相邻的氮原子一起表示吡咯啉基,哌啶基或吗啉基,但当##STR2##为哌啶基或二乙基氨基基团时,R.sup.1,R.sup.2和R.sup.3中至少有一个不是氢原子,或其药学上可接受的盐,公开了制备上述化合物(I)的方法和包含它们的制药组合物。从药理学角度来看,上述化合物(I)具有促进肺表面活性物质分泌的活性。