发明授权
- 专利标题： Saccharin derivatives useful as proteolytic enzyme inhibitors and compositions and method of use thereof
- 专利标题（中）： 可用作蛋白水解酶抑制剂的糖精衍生物及其使用方法
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申请号： US793033申请日： 1991-11-15
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公开(公告)号： US5236917A公开(公告)日： 1993-08-17
- 发明人: Richard P. Dunlap , Neil W. Boaz , Albert J. Mura , Dennis J. Hlasta , Ranjit C. Desai , Chakrapani Subramanyam , Lee H. Latimer , Eric P. Lodge
- 申请人： Richard P. Dunlap , Neil W. Boaz , Albert J. Mura , Dennis J. Hlasta , Ranjit C. Desai , Chakrapani Subramanyam , Lee H. Latimer , Eric P. Lodge
- 申请人地址： NY New York
- 专利权人： Sterling Winthrop Inc.
- 当前专利权人： Sterling Winthrop Inc.
- 当前专利权人地址： NY New York
- 主分类号： A61K31/425
- IPC分类号： A61K31/425 ; A61K31/415 ; A61K31/428 ; A61K31/47 ; A61P29/00 ; A61P43/00 ; C07D275/04 ; C07D275/06 ; C07D417/06 ; C07D417/12 ; C07D417/14 ; C07D471/04 ; C07D513/04 ; C07F9/6541
摘要：
Novel 2-substituted saccharins which inhibit the enzymatic activity of proteolytic enzymes, are useful in the treatment of degenerative diseases and have the formula ##STR1## wherein: L is --O--, --S--, --SO-- or --SO.sub.2 --;m and n are each independently 0 or 1;R.sub.1 is halo, lower-alkanoyl, 1-oxophenalenyl, phenyl or substituted phenyl, heterocyclyl or substituted heterocyclyl or, when L is --O-- and n is 1, cycloheptatrienon-2-yl or, when L is --S-- and n is 1, cyano or lower-alkoxythiocarbonyl or, when L is --SO.sub.2 -- and n is 1, lower-alkyl or trifluoromethyl;R.sub.2 is hydrogen, lower-alkoxycarbonyl, phenyl or phenylthio; andR.sub.3 and R.sub.4 are each hydrogen or various substituents and processes for preparation and pharmaceutical compositions and method of use thereof are disclosed.
公开/授权文献
- US5716906A Saccharin derivatives 公开/授权日：1998-02-10