Melvin Jr., Lawrence S.,Hege, Hans-guenther,Ullrich, Martina,Weymann, Jurgen
申请号：
AU2008282773
公开号：
AU2008282773B2
申请日:
2008.07.31
申请国别(地区):
AU
年份:
2012
代理人:
摘要：
The invention relates to derivatives and metabolites of ambrisentan, includingcompounds of general Formula (I) or salts, hydrates, solvates, racemates, oroptical isomers thereof, wherein R is -H or -OCH； Ris-H, lower alkyl (e.g. C-C alkyl) orglycosidyl； and Rand R are independently -CH3,-C(O)H or -CHOR, wherein R is -H or a hydrocarbylgroup having 1 to 20 carbon atoms. In some embodiments, compounds of Formula (I)exhibit selective affinity for ET receptors and serve as endothelinreceptor antagonists. In some embodiments, the compounds correspond to metabolitesof ambrisentan produced by the enzymatic action of cytochrome P450 or uridinediphosphate glucuronosyl transferase enzymes, for example as elucidated inpre-clinical or clinical studies.
