发明公开
EP0049842A2 Substituted enantholactam derivatives, a process for the preparation and a pharmaceutical composition useful in the treatment of hypertension comprising the same, and intermediates
失效
庚取代的衍生物，它们的制备方法和药物组合物的方法含有它们，用于对抗高血压和中间体的用途。
- 专利标题： Substituted enantholactam derivatives, a process for the preparation and a pharmaceutical composition useful in the treatment of hypertension comprising the same, and intermediates
- 专利标题（中）： 庚取代的衍生物，它们的制备方法和药物组合物的方法含有它们，用于对抗高血压和中间体的用途。
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申请号： EP81107932.6申请日： 1981-10-05
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公开(公告)号： EP0049842A2公开(公告)日： 1982-04-21
- 发明人: Harris, Elbert E. , Taub, David , Thorsett, Eugene D.
- 申请人： Merck & Co., Inc.
- 申请人地址： 126, East Lincoln Avenue P.O. Box 2000 Rahway New Jersey 07065-0900 US
- 专利权人： Merck & Co., Inc.
- 当前专利权人： Merck & Co., Inc.
- 当前专利权人地址： 126, East Lincoln Avenue P.O. Box 2000 Rahway New Jersey 07065-0900 US
- 代理机构： Abitz, Walter, Dr.-Ing.
- 优先权： US194691 19801006; US299051 19810904
- 主分类号： C07D225/02
- IPC分类号： C07D225/02 ; A61K31/395
摘要：
Substituted enantholactam dipeptides and derivatives thereof and a process for preparing them are disclosed. Those comnounds have the formula
in which
R' ishydrogen, lower alkyl, cycloalkyl, aminoalkyl, hydroxyalkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, heterocycloalkyl, or substituted aryl wherein the substituent is halo, alkyl, aminoalkyl, or alkoxy;
R 2 ishydrogen, lower alkyl, aminolower alkyl, indolyl lower alkyl or phenyl lower alkyl;
R 3 ishydroxy, lower alkoxy or aralkoxy;
R 4 ishydrogen or lower alkanoyl;
R 5 is hydrogen or lower alkyl.
The compounds are useful as derivating enzyme inhibitors and as antihypertensives.
in which
R' ishydrogen, lower alkyl, cycloalkyl, aminoalkyl, hydroxyalkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, heterocycloalkyl, or substituted aryl wherein the substituent is halo, alkyl, aminoalkyl, or alkoxy;
R 2 ishydrogen, lower alkyl, aminolower alkyl, indolyl lower alkyl or phenyl lower alkyl;
R 3 ishydroxy, lower alkoxy or aralkoxy;
R 4 ishydrogen or lower alkanoyl;
R 5 is hydrogen or lower alkyl.
The compounds are useful as derivating enzyme inhibitors and as antihypertensives.
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