摘要 |
This invention is directed to compounds of formula I wherein R1 is CN, CH2CN, CH=CHCN, CHO, or CH=CHCO2H; R2 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; R3 is halogen; R4 is optionally substituted aryl or optionally substituted heteroaryl; R5 is carboxy or an acid isostere; X is oxygen or sulphur; and n 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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申请人 |
RHONE-POULENC RORER LIMITED |
发明人 |
SMITH, CHRISTOPHER;PORTER, BARRY;WALSH, ROGER;MAJID, TAHIR;MCCARTHY, CLIVE;HARRIS, NEIL;ASTLES, PETER;MCLAY, IAIN;MORLEY, ANDREW;BRIDGE, ANDREW;VAN SICKLE, ANDREW;HALLEY, FRANK;ROACH, ALAN;FOSTER, MARTYN |