Carbostyril compounds, compositions containing same and processes for preparing same
申请人:OTSUKA PHARMACEUTICAL CO., LTD.
公开号:EP0052016A1
公开(公告)日:1982-05-19
A carbostyril compound of the formula (I)
wherein R1 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, or a phenyl-lower alkyl group;
R2 represents a hydrogen atom, a lower alkyi group, a lower alkoxy group, a halogen atom, or a hydroxy group;
R3 represents a hydrogen atom, a lower alkyl group, a halogen atom, a nitroso group, an amino group which may be substituted with a lower alkyl group, a lower alkanoylamino group, a N.N-di-lower alkylaminomethyl group, a carbamoylmethyl group, a cyanomethyl group, or a carboxymethyl group;
R4 and R5, which may be the same or different, each represents a hydrogen atom, a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group, or a nitro group;
the bonding between the 3- and 4-positions of the carbostyril nucleus is a single bond or a double bond; and the position at which the imidazopyridyl group of the formula
is attached to the carbostyril nucleus is the 5- or 6-position;
with the proviso that when the imidazopyridyl group is attached to the 5-position of the carbostyril nucleus, R2 should not be a hydrogen atom, a lower alkyl group, or a halogen atom; or its pharmaceutically acceptable salt, and a composition containing the compound of the formula (I) or its pharmaceutically acceptable salt as an active ingredient, and process for preparing same. The Compound of the formula (I) and its pharmaceutically acceptable salts have cardiotonic effects.
式(I)的碳十四化合物
其中 R1 代表氢原子、低级烷基、低级烯基、低级炔基或苯基-低级烷基;
R2 代表氢原子、低级烷基、低级烷氧基、卤素原子或羟基;
R3 代表氢原子、低级烷基、卤素原子、亚硝基、可被低级烷基取代的氨基、低级烷酰基氨基、N.N-二低级烷基氨基甲基、氨基甲酰基甲基、氰基甲基或羧基甲基;
R4和R5可以相同或不同,各自代表氢原子、卤素原子、低级烷基、羟基、低级烷氧基或硝基;
碳二吡啶核的 3 位和 4 位之间的键是单键或双键;以及式中的咪唑吡啶基连接到碳二吡啶核的位置
式中的咪唑吡啶基连接到氨基苯乙烯核的位置是 5-位或 6-位;
或其药学上可接受的盐,以及含有式(I)化合物或其药学上可接受的盐作为活性成分的组合物和制备方法。式(I)化合物及其药学上可接受的盐具有强心作用。