Substituted caprolactam derivatives, a process for preparing and a pharmaceutical composition containing the same, and intermediates
申请人:Merck & Co., Inc.
公开号:EP0049505A2
公开(公告)日:1982-04-14
Substituted caprolactam derivatives are disclosed which are useful as converting enzyme inhibitors and as antihypertensives, and a process for preparing them. Those compounds are represented by the formula
wherein
R1 is hydrogen, loweralkyl, cyclic loweralkyl, amino loweralkyl, alkylamino loweralkyl, hydroxyalkyl, acylamino loweralkyl, dialkylamino loweralkyl including cyclic polyethyleneamino loweralkyl, arloweralkyl, aryl, substituted aryl wherein the substituent is halo, alkyl, aminoalkyl, or alkoxy; heteroaryl, heteroarloweralkyl;
R2 is hydrogen or loweralkyl;
R3 is hydroxyl, loweralkoxy, or aralkyloxy;
R4 is hydrogen or loweralkanoyl.
本发明公开了可用作转化酶抑制剂和降压药的取代己内酰胺衍生物及其制备方法。这些化合物用式表示
式中
R1 是氢、低级烷基、环状低级烷基、氨基低级烷基、烷基氨基低级烷基、羟基烷基、酰氨基低级烷基、二烷基氨基低级烷基(包括环状聚乙烯氨基低级烷基)、芳基、取代芳基,其中取代基是卤、烷基、氨基烷基或烷氧基;杂芳基、杂芳基低级烷基;
R2 是氢或低级烷基
R3 是羟基、低级烷氧基或芳氧基;
R4 是氢或低级烷酰基。