Novel thiolester compounds are disclosed which are orally effective angiotensin converting enzyme inhibitors useful in the treatment of mammalian hypertension. They have the formula, R.sub.1 -A.sub.1 -S-Z, wherein Z denotes -B-A.sub.2, R.sub.1 is H or an acyl group, A.sub.1 is a carboxylic acid containing at least one amino or imino -N-, A.sub.2 is a carboxylic acid containing at least one amino or imino -N- or a lower alkyl ester or amide thereof, B is a 2-4 carbon backbone chain in mercapto linkage to S which includes a carbonyl or sulfonyl group joined in carboxamido or sulfonamido linkage, respectively, to A.sub.2. Preferably A.sub.2 includes a 4-6 membered C-N ring or a 5 membered ring of one N, one S and 3 C atoms.
披露了新型硫醇酯化合物,它们是口服有效的血管紧张素转化酶抑制剂,用于治疗哺乳动物的 hypertension。它们具有以下公式,R.sub.1 -A.sub.1 -S-Z,其中 Z 表示 -B-A.sub.2,R.sub.1 是 H 或一个酰基团,A.sub.1 是至少含有一个氨基或亚氨基 -N- 的羧酸,A.sub.2 是至少含有一个氨基或亚氨基 -N- 的羧酸或其低级烷基酯或酰胺,B 是一个 2-4 碳骨架链,通过巯基连接到 S,并包括一个碳酰基或磺酰基团,分别通过羧酰胺或磺酰胺连接到 A.sub.2。优选的是 A.sub.2 包含一个 4-6 成员的 C-N 环或一个由一个 N、一个 S 和 3 个 C 原子组成的 5 成员环。
Mercaptoacyl derivatives of substituted prolines
申请人:E. R. Squibb & Sons, Inc.
公开号:US04316906A1
公开(公告)日:1982-02-23
New mercaptoacyl derivatives of substituted prolines which have the general formula ##STR1## are useful as hypotensive agents.
新的取代脯氨酸巯基酰衍生物具有一般公式##STR1##,可用作降压剂。
Derivatives of mercaptoacyl prolines and pipecolic acids
申请人:E. R. Squibb & Sons, Inc.
公开号:US04311697A1
公开(公告)日:1982-01-19
This invention is directed to compounds of the formula ##STR1## and various intermediates therefore. The final products possess useful hypotensive activity.
这项发明涉及公式##STR1##的化合物及其各种中间体。最终产品具有有用的降压活性。
Mercaptoacyl derivatives of 4-disubstituted prolines and 4-substituted
申请人:E. R. Squibb & Sons, Inc.
公开号:US04291040A1
公开(公告)日:1981-09-22
This invention is directed to compounds of the formulas ##STR1## and various intermediates therefore. The final products possess useful hypotensive activity.
这项发明涉及公式为##STR1##的化合物以及各种中间体。最终产物具有有用的降压活性。
Anti-hypertensive agents
申请人:University of Miami
公开号:US04690936A1
公开(公告)日:1987-09-01
Novel inhibitors of angiotensin converting enzyme having the general formula R--A--S--Z are disclosed as potent inhibitors of angiotensin converting enzyme and are useful anti-hypertensive agents.