New amino acid derivatives, processes for the preparation thereof and pharmaceutical composition comprising the same
申请人:FUJISAWA PHARMACEUTICAL CO., LTD.
公开号:EP0300189A2
公开(公告)日:1989-01-25
A compound of the formula :
wherein R1 is lower alkyl optionally substituted with a substituent selected from the group consisting of acyl,hydroxy, lower alkoxy, aryl, lower alkylthio and a group of the formula :
in which R5 is hydrogen or acyl and
R6 is hydrogen or lower alkyl; aryl; or amino optionally substituted with substituent(s) selected from the group consisting of lower alkyl and acyl; and
R2 is hydrogen or lower alkyl; or
R1 and R2 are taken together with the attached nitrogen atom to form a heterocyclic group optionally substituted with substituent(s) selected from the group consisting of lower alkyl, hydroxy(lower)alkyl, lower alkoxy(lower)alkyl, acyl(lower)alkyl, oxo and acyl;
R3 is hydrogen or lower alkyl; and
R4 is lower alkyl;
and its pharmaceutically acceptable salt, processes for the preparation thereof and pharmaceutical composition comprising the same.
一种式如下的化合物
其中 R1 是低级烷基,可任选被选自以下组别的取代基取代:酰基、羟基、低级烷氧基、芳基、低级烷硫基和一个式......的基团:
其中 R5 为氢或酰基,且
R6 是氢或低级烷基;芳基;或被选自低级烷基和酰基的取代基任选取代的氨基;以及
R2 是氢或低级烷基;或
R1 和 R2 与所连接的氮原子一起形成杂环基团,该杂环基团可任选被选自由低级烷基、羟基(低级)烷基、低级烷氧基(低级)烷基、酰基(低级)烷基、氧代和酰基组成的取代基取代;
R3 是氢或低级烷基;和
R4 是低级烷基;
及其药学上可接受的盐、制备工艺和包含这些成分的药物组合物。