发明授权
US5118811A Amino acid derivatives possessing prolyl endopeptidase-inhibitory
activities
失效
氨基酸衍生物与PROLYL内含子抑制活性相关
- 专利标题: Amino acid derivatives possessing prolyl endopeptidase-inhibitory activities
- 专利标题(中): 氨基酸衍生物与PROLYL内含子抑制活性相关
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申请号: US613737申请日: 1990-12-12
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公开(公告)号: US5118811A公开(公告)日: 1992-06-02
- 发明人: Itsuo Uchida , Koji Kobayashi , Kazuhiko Nishii , Kunio Iwata , Shin Hara , Koretake Anami
- 申请人: Itsuo Uchida , Koji Kobayashi , Kazuhiko Nishii , Kunio Iwata , Shin Hara , Koretake Anami
- 申请人地址: JPX Tokyo JPX Osaka
- 专利权人: Japan Tobacco Inc.,Yoshitomi Pharmaceutical Industries, Ltd.
- 当前专利权人: Japan Tobacco Inc.,Yoshitomi Pharmaceutical Industries, Ltd.
- 当前专利权人地址: JPX Tokyo JPX Osaka
- 优先权: JPX1-91795 19890413
- 主分类号: C07D207/09
- IPC分类号: C07D207/09 ; C07D207/16 ; C07D207/26 ; C07D207/263 ; C07D207/27 ; C07D277/04 ; C07D277/06 ; C07D417/06 ; C07D417/14
摘要:
Amino acid derivatives of the formula ##STR1## wherein: Q is W--(CH.sub.2).sub.m --(A).sub.n --CO--B-- whereinA is oxygen atom or --NH--;B is ##STR2## or --(CH.sub.2).sub.l -- wherein X is sulfur atom or --CH.sub.2 --, and l is an integer from 1 to 3;W is ##STR3## wherein Hal is halogen atom; n is an integer of 0 or 1; andm is an integer from 0 to 3;Y is sulfur atom or --CH.sub.2 --; andR is hydrogen atom, formyl group, C.sub.1-5 alkoxycarbonyl group, --C.tbd.N or ##STR4## wherein R.sup.1 is hydrogen atom, andR.sup.2 is hydroxyl group, C.sub.1-5 alkylcarboxy group, phenylcarboxy group, C.sub.1-5 alkoxy group or phenyl C.sub.1-5 alkoxy group; with the proviso that when R is hydrogen atom, formyl group or C.sub.1-5 alkoxycarbonyl group, W is ##STR5## The compounds mentioned above specifically inhibit prolyl endopeptidase activity and are useful as agents for the treatment and prevention of dementia and amnesia.
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