发明公开
- 专利标题： Histidine derivatives as renin inhibitors
- 专利标题（中）： Histidinderivate ALS Renininhibitoren。
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申请号： EP85307555.4申请日： 1985-10-18
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公开(公告)号： EP0181110A2公开(公告)日： 1986-05-14
- 发明人: Iizuka, Kinji , Kamijo, Tetsuhide , Kubota, Tetsuhiro , Akahane, Kenji , Umeyama, Hideaki , Kiso, Yoshiaki
- 申请人： Kissei Pharmaceutical Co Ltd
- 申请人地址： No. 19-48 Yoshino Matsumoto-shi Nagano JP
- 专利权人： Kissei Pharmaceutical Co Ltd
- 当前专利权人： Kissei Pharmaceutical Co Ltd
- 当前专利权人地址： No. 19-48 Yoshino Matsumoto-shi Nagano JP
- 代理机构： Pearce, Anthony Richmond
- 优先权： JP221853/84 19841022; JP260453/84 19841210; JP271303/84 19841222
- 主分类号： C07K5/06
- IPC分类号： C07K5/06 ; C07D233/64 ; C07D403/02 ; A61K37/02 ; A61K31/415
摘要：
@ Dipeptides are described which are represented by the formula
wherein His represents an L-histidyl group, Ar, represents a phenyl group, a naphthyl group or an indolyl group, Ar 2 represents a phenyl group or a naphthyl group, X represents a chemical bond, -NHCO-, -CONH-, -CO-, -CH 2 -, -NH-, -O- or -(CH=CH) P -wherein p is 1 or 2, Z represents an oxygen atom or
in which R 2 represents a hydrogen atom or combines with R, to form a chemical bond, m and n, which may be the same or different, each represents an integer of from 0 to 3, provided that when X is a chemical bond, the sum of n plus m is from 1 to 6 and when X is not a chemical bond, the sum of n plus m is from 1 to 4, Y represents a chemical bond when X is not a chemical bond, or, when X is a chemical bond, an alkylene group having 1 to 3 carbon atoms, R 1 represents a hydrogen atom or combines with R 2 to form a chemical bond, R 3 represents a formyl group or a hydroxymethyl group, R 4 represents an isobutyl group or a benzyl group, and C represents an L-configurational carbon atom; or the pharmaceutically acceptable salt thereof.
These compounds have a strong inhibitory effect on human renin, and are useful as a therapeutically active agent for the treatment of hypertension, especially renin - associated hypertension.
wherein His represents an L-histidyl group, Ar, represents a phenyl group, a naphthyl group or an indolyl group, Ar 2 represents a phenyl group or a naphthyl group, X represents a chemical bond, -NHCO-, -CONH-, -CO-, -CH 2 -, -NH-, -O- or -(CH=CH) P -wherein p is 1 or 2, Z represents an oxygen atom or
in which R 2 represents a hydrogen atom or combines with R, to form a chemical bond, m and n, which may be the same or different, each represents an integer of from 0 to 3, provided that when X is a chemical bond, the sum of n plus m is from 1 to 6 and when X is not a chemical bond, the sum of n plus m is from 1 to 4, Y represents a chemical bond when X is not a chemical bond, or, when X is a chemical bond, an alkylene group having 1 to 3 carbon atoms, R 1 represents a hydrogen atom or combines with R 2 to form a chemical bond, R 3 represents a formyl group or a hydroxymethyl group, R 4 represents an isobutyl group or a benzyl group, and C represents an L-configurational carbon atom; or the pharmaceutically acceptable salt thereof.
These compounds have a strong inhibitory effect on human renin, and are useful as a therapeutically active agent for the treatment of hypertension, especially renin - associated hypertension.
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