N-Carboxyalkyl dipeptides and derivatives thereof are disclosed which are useful as angiotensin converting enzyme inhibitors and as antihypertensives, and a process for preparing them.
Those compounds are represented by the formula
wherein
R and R5 are individually hydroxy, lower alkoxy, aralkoxy;
R1 is C1-8 alkyl; substituted C1-5 alkyl, substituted aralkyl or substituted heteroaralkyl;
R2 is hydroxy, amino, alkoxy, aralkyloxy;
n is one, two or three;
R3 is aryl, heteroaryl, cycloalkyl, aminoloweralkyl, aralkyl;
R4 is hydrogen or loweralkyl; or
R3 and R4 are joined to form a ring having the following formulae:
R6 is hydrogen or loweralkyl; p is 1, 2, or 3; W is a bond, -CH2-, or C=O; and, Z is a bond, -CH2-, or -CH2CH2-; and, the pharmaceutically acceptable salts thereof.
本发明公开了可用作
血管紧张素转换酶
抑制剂和抗高血压药的 N-羧烷基二肽及其衍
生物,以及制备它们的工艺。
这些化合物用式表示
式中
R 和 R5 分别为羟基、低级烷氧基、烷氧基;
R1 是 C1-8 烷基、取代的 C1-5 烷基、取代的芳基或取代的杂烷基;
R2 是羟基、
氨基、烷氧基、烷氧基;
n 是 1、2 或 3;
R3 是芳基、杂芳基、环烷基、
氨基低级烷基、芳基;
R4 是氢或低级烷基;或
R3 和 R4 连接形成具有下式的环:
R6是氢或低级烷基;p是1、2或3;W是键、-
CH2-或C=O;Z是键、- -或- -;及其药学上可接受的盐。