发明授权
US6124343A Substituted phenyl compounds with a substituent having a thienyl ring
失效
具有噻吩基环的取代基的取代苯基化合物
- 专利标题： Substituted phenyl compounds with a substituent having a thienyl ring
- 专利标题（中）： 具有噻吩基环的取代基的取代苯基化合物
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申请号： US898547申请日： 1997-07-22
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公开(公告)号： US6124343A公开(公告)日： 2000-09-26
- 发明人: Christopher Smith , Barry Porter , Roger Walsh , Tahir Majid , Clive McCarthy , Neil Harris , Peter Astles , Iain McLay , Andrew Morley , Andrew Bridge , Andrew Van Sickle , Frank Halley , Alan Roach , Martyn Foster
- 申请人： Christopher Smith , Barry Porter , Roger Walsh , Tahir Majid , Clive McCarthy , Neil Harris , Peter Astles , Iain McLay , Andrew Morley , Andrew Bridge , Andrew Van Sickle , Frank Halley , Alan Roach , Martyn Foster
- 申请人地址： GBX West Malling
- 专利权人： Rhone-Poulenc Rorer Limited
- 当前专利权人： Rhone-Poulenc Rorer Limited
- 当前专利权人地址： GBX West Malling
- 优先权： GBX9501635 19190127; GBX9504061 19950301; GBX9509604 19950511; GBX9615752 19960726
- 主分类号： C07C255/54
- IPC分类号： C07C255/54 ; C07D213/30 ; C07D213/61 ; C07D237/08 ; C07D263/56 ; C07D275/02 ; C07D277/24 ; C07D307/12 ; C07D317/54 ; C07D333/16 ; C07D405/12 ; C07D411/12 ; A61K31/381
摘要：
This invention is directed to compounds of formula I ##STR1## wherein R.sup.1 is CN, CH.sub.2 CN, CH.dbd.CHCN, CHO, or CH.dbd.CHCO.sub.2 H;R.sup.2 is aryl lower alkoxy, heteroaryl lower alkoxy, aryl lower alkylthio or heteroaryl lower alkylthio wherein each of the aryl and heteroaryl moieties is optionally substituted;R.sup.3 is halogen;R.sup.4 is optionally substituted aryl or optionally substituted heteroaryl;R.sup.5 is carboxy or an acid isostere;X is oxygen or sulphur; andn is zero or 1; or an N-oxide thereof, prodrug thereof solvate thereof, or pharmaceutically acceptable salt thereof, which compounds have endothelin antagonist activity. The invention is also directed to methods for preparing the compounds of formula I and their pharmaceutical use.
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