申请人:FISONS plc
公开号:EP0137746A2
公开(公告)日:1985-04-17
There are described compounds of formula I,
in which
Z is R2CH (COOH) NH- or R1SCH2-,
R1is hydrogen or R8CO-,
R8 is alkyl C1 to 10 or phenyl,
R is hydrogen, alkyl C1 to 6, or alkyl C1 to 6 substituted by phenyl, -NH2, -COOH or by alkyl C1 to 6 thio,
R2 is hydrogen, alkyl C1 to 10, cycloalkyl C3 to 10, phenyl, phenylalkyl C7 to 12, alkoxy C1 to 6 - alkyl C1 to 6, alkyl C1 to 6 - thioalkyl C1 to 6, phenyloxyalkyl C7 to 12 or phenylthioalkyl C7 to 12,
R. and R5, which may be the same or different, are each hydrogen, alkyl C1 to 10, cycloalkyl C3 to 10, phenylalkyl C7 to 12, or phenyl; the phenyl and phenylalkyl each optionally being substituted by one or more alkyl C1 to 6, alkoxy C1 to 6 or halogen groups, or
R. and R5 together form a - (CH2),,- or - (CW2)5- chain, and
R6 is hydrogen, alkyl C1 to 6 or phenylalkyl C7 to 12, and pharmaceutically acceptable salts and esters thereof.
There are also described processes for making the compounds and their formulation and use as pharmaceuticals, eg. angiotensin converting enzyme inhibitors.
所述化合物为式 I、
其中
Z 是 R2CH (COOH) NH- 或 R1SCH2-、
R1 是氢或 R8CO-、
R8 是 C1-10 烷基或苯基、
R 是氢、C1-6 烷基或被苯基、-NH2、-COOH 或 C1-6 硫代烷基取代的 C1-6 烷基、
R2 是氢、C1 至 10 的烷基、C3 至 10 的环烷基、苯基、C7 至 12 的苯基烷基、C1 至 6 的烷氧基、C1 至 6 的烷基、C1 至 6 的硫代烷基、C7 至 12 的苯氧基烷基或 C7 至 12 的苯硫基烷基、
R.和 R5(可以相同或不同)各自为氢、C1-10 烷基、C3-10 环烷基、C7-12 苯烷基或苯基;苯基和苯烷基各自可选择被一个或多个 C1-6 烷基、C1-6 烷氧基或卤素基团取代,或
R.和 R5 一起形成-(CH2),-或-(CW2)5-链,和
R6 是氢、C1-6 烷基或 C7-12 苯烷基,以及它们的药学上可接受的盐和酯。
此外,还介绍了这些化合物的制造工艺及其作为药物(如血管紧张素转换酶抑制剂)的配制和使用。