Substituted caprylolactam derivatives as antihypertensives, process for preparing and pharmaceutical composition comprising them
申请人:Merck & Co., Inc.
公开号:EP0046292A1
公开(公告)日:1982-02-24
The invention relates to caprylolactam derivatives of the formula:
wherein
R and R3 are hydroxy,
lower alkoxy,
lower alkenoxy,
aryloxy,
arloweralkoxy;
hydrogen,
alkyl of from 1 to 12 carbon atoms which include branched and cyclic and unsaturated alkyl groups,
substituted loweralkyl wherein the substituent(s) can be halo, lower alkoxy, hydroxy, aryloxy, amino, loweralkylamino, aminoloweralkylthio, aminoloweralkoxy, diloweralkylamino, acylamino, arylamino, guanidino, phthalimido, mercapto, loweralkylthio, arylthio, carboxy, carboxamido or carboloweralkoxy,
arloweralkyl, arloweralkenyl, heteroarlower alkyl or heteroarlower alkenyl,
substituted arloweralkyl, or substituted heteroarlower alkyl, or substituted heteroarlower alkenyl, wherein the aryl or heteroaryl substituents are halo, dihalo, lower alkyl, hydroxy, lower alkoxy, amino, aminomethyl, phenyloxy, acylamino, diloweralkylamino, loweralkylamino, carboxyl, haloloweralkyl, acyl or aroyl;
arloweralkyl or heteroarloweralkyl substituted on the alkyl portion by amino, hydroxyl or acylamino;
R2 and R are hydrogen or lower alkyl;
and the pharmaceutically acceptable salts thereof and a process for preparing them. Those compounds are useful as angiotensin converting enzyme inhibitors and as antihypertensives.
本发明涉及式如下的辛酰内
酰胺衍
生物:
式中
R和R3是羟基
低级烷
氧基
低级
烯氧基
芳
氧基
低级烷
氧基
氢、
1 至 12 个
碳原子的烷基,包括支链、环状和不饱和烷基、
取代的低级烷基,其中的取代基可以是卤代、低级烷
氧基、羟基、芳
氧基、
氨基、低级烷基
氨基、
氨醇低级烷
硫基、
氨醇低级烷
氧基、稀释低级烷基
氨基、酰基
氨基、芳基
氨基、
胍基、
酞酰亚胺基、巯基、低级烷
硫基、芳基
硫基、羧基、羧
酰胺基或
碳醇低级烷
氧基、
低级烷基、低级
烯基、杂低级烷基或杂低级
烯基、
取代的芳基或杂芳基,其中芳基或杂芳基取代基为卤代、二卤代、低级烷基、羟基、低级烷
氧基、
氨基、
氨甲基、
苯氧基、酰
氨基、稀低级烷基
氨基、低级烷基
氨基、羧基、卤代低级烷基、酰基或芳基;
烷基部分被
氨基、羟基或酰基
氨基取代的低级烷基或杂芳低级烷基;
R2 和 R 是
氢或低级烷基;
及其药学上可接受的盐类和制备方法。这些化合物可用作
血管紧张素转换酶
抑制剂和降压药。