MELVIN, LAWRENCE S., JR.,ULLRICH, MARTINA,HEGE, HANS-GUENTHER,WEYMANN, JUERGEN
申请号：
CA2695259
公开号：
CA2695259C
申请日:
2008.07.31
申请国别(地区):
CA
年份:
2016
代理人:
摘要：
The invention relates to derivatives andmetabolites of ambrisentan, including compounds ofgeneral Formula (I) or salts, hydrates, solvates, racemates,or optical isomers thereof, wherein R1 is -H or -OCH3； R2 is-H, lower alkyl (e.g. C1-C4 alkyl) or glycosidyl； and R3 andR4 are independently -CH3, -C(O)H or -CH2OR6, whereinR6 is -H or a hydrocarbyl group having 1 to 20 carbonatoms. In some embodiments, compounds of Formula (I)exhibit selective affinity for ETA receptors and serve asendothelin receptor antagonists. In some embodiments,the compounds correspond to metabolites of ambrisentanproduced by the enzymatic action of cytochrome P450 oruridine diphosphate glucuronosyl transferase enzymes, forexample as elucidated in pre-clinical or clinical studies.
