发明公开
- 专利标题： Renin inhibitors
- 专利标题（中）： Renininhibitoren。
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申请号： EP91107400.3申请日： 1991-05-07
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公开(公告)号： EP0456185A2公开(公告)日： 1991-11-13
- 发明人: Rosenberg, Saul H. , Denissen, Jon F.
- 申请人： ABBOTT LABORATORIES
- 申请人地址： One Abbott Park Road Abbott Park, Illinois 60064-3500 US
- 专利权人： ABBOTT LABORATORIES
- 当前专利权人： ABBOTT LABORATORIES
- 当前专利权人地址： One Abbott Park Road Abbott Park, Illinois 60064-3500 US
- 代理机构： Modiano, Guido, Dr.-Ing.
- 优先权： US522349 19900511; US564925 19900809; US683663 19910415
- 主分类号： C07D277/30
- IPC分类号： C07D277/30 ; C07D277/40 ; C07D241/08 ; C07D417/12 ; C07D403/12 ; C07D231/12 ; C07D295/18 ; A61K31/495 ; A61K31/425 ; A61K38/55
摘要：
A renin inhibiting compound of the formula:
wherein R₁ is 4-piperazinyl, 1-methyl-4-piperazinyl, 1-methyl-1-oxo-4-piperazinyl, 2-oxo-4-piperazinyl, 4-morpholinyl, 4-thiomorpholinyl or 1-methyl-4-homopiperazinyl;
R₂ is benzyl, 2-phenylethyl, 1-naphthylmethyl or 2-naphthylmethyl;
R₃ is 4-thiazolyl, 2-amino-4-thiazolyl, 2-thiazolyl, 5-thiazolyl, 1-pyrazolyl, 3-pyrazolyl, 1-imidazolyl, n-propyl, isopropyl, CH₃S- or CH₃SCH₂-;
R₄ is isobutyl or cyclopropyl;
R₅ is hydrogen or loweralkyl; and
X is CH₂ or NH; or a pharmaceutically acceptable salt, ester or prodrug thereof; with the proviso that when X is NH and R₃ is 2-amino-4-thiazolyl, then R₄ is cyclopropyl.
wherein R₁ is 4-piperazinyl, 1-methyl-4-piperazinyl, 1-methyl-1-oxo-4-piperazinyl, 2-oxo-4-piperazinyl, 4-morpholinyl, 4-thiomorpholinyl or 1-methyl-4-homopiperazinyl;
R₂ is benzyl, 2-phenylethyl, 1-naphthylmethyl or 2-naphthylmethyl;
R₃ is 4-thiazolyl, 2-amino-4-thiazolyl, 2-thiazolyl, 5-thiazolyl, 1-pyrazolyl, 3-pyrazolyl, 1-imidazolyl, n-propyl, isopropyl, CH₃S- or CH₃SCH₂-;
R₄ is isobutyl or cyclopropyl;
R₅ is hydrogen or loweralkyl; and
X is CH₂ or NH; or a pharmaceutically acceptable salt, ester or prodrug thereof; with the proviso that when X is NH and R₃ is 2-amino-4-thiazolyl, then R₄ is cyclopropyl.
公开/授权文献
- EP0456185B1 Renin inhibitors 公开/授权日：1995-05-31
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