发明授权
US5536737A Compound having prolyl endopeptidase inhibitory activity and
pharmaceutical use thereof
失效
具有脯氨酰内肽酶抑制活性的化合物及其药物用途
- 专利标题： Compound having prolyl endopeptidase inhibitory activity and pharmaceutical use thereof
- 专利标题（中）： 具有脯氨酰内肽酶抑制活性的化合物及其药物用途
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申请号： US446592申请日： 1995-05-24
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公开(公告)号： US5536737A公开(公告)日： 1996-07-16
- 发明人: Koji Kobayashi , Minoru Akamatsu , Shinji Yata , Hiroyuki Abe , Katsuo Toide , Motohiro Kogayu , Itsuo Uchida
- 申请人： Koji Kobayashi , Minoru Akamatsu , Shinji Yata , Hiroyuki Abe , Katsuo Toide , Motohiro Kogayu , Itsuo Uchida
- 申请人地址： JPX Tokyo
- 专利权人： Japan Tobacco Inc.
- 当前专利权人： Japan Tobacco Inc.
- 当前专利权人地址： JPX Tokyo
- 优先权： JPX4-333899 19921120; JPX5-089775 19930416
- 主分类号： C07D207/16
- IPC分类号： C07D207/16 ; C07D277/06 ; C07D417/06 ; C07D403/06 ; A61K31/40 ; A61K31/425
摘要：
Compounds of the formula ##STR1## wherein R is a hydrogen atom or an acyl; U is --O--, --CHR.sup.1 -- or --NR.sup.2 -- wherein R.sup.1 is a hydrogen atom or a hetero ring, and R.sup.2 is a hydrogen atom or a lower alkoxycarbonyl lower alkyl; V is --O--, --S--, --CHR.sup.3 -- or --NR.sup.4 -- wherein R.sup.3 is a hydrogen atom or a lower alkoxycarbonyl, and R.sup.4 is a hydrogen atom, a lower alkyl or an acyl; W is methyl, a hetero ring or optionally substituted phenyl; X and Y are the same or different and each is --CH.sub.2 -- or --S--; m is an integer of 0 to 6; and n is an integer of 1 to 4, and pharmaceutically acceptable salts thereof.The compounds of the present invention have specifically strong inhibitory activity against prolyl endopeptidase, and suppress decomposition and inactivation of TRH, substance P, neurotensin, vasopressin and the like. Accordingly, the compounds can be used for the prophylaxis and/or treatment of dementia and amnesia including Alzheimer's disease.
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