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专利名称：METABOLITES AND DERIVATIVES OF
AMBRISENTAN
发明人：MELVIN, JR., LAWRENCE S.,ULLRICH,
MARTINA,HEGE, HANS-GUENTHER,WEYMANN, JUERGEN
申请号：US2008009236申请日：20080731
公开号：WO2009017777A3公开日：20090409
摘要：The invention relates to derivatives and metabolites of ambrisentan, includingcompounds of general Formula (I) or salts, hydrates, solvates, racemates, or opticalisomers thereof, wherein R1 is -H or -OCH3; R2 is-H, lower alkyl (e.g. C1-C4 alkyl) orglycosidyl; and R3 and R4 are independently -CH3, -C(O)H or -CH2OR6, wherein R6 is -Hor a hydrocarbyl group having 1 to 20 carbon atoms. In some embodiments, compoundsof Formula (I) exhibit selective affinity for ETA receptors and serve as endothelin receptorantagonists. In some embodiments, the compounds correspond to metabolites ofambrisentan produced by the enzymatic action of cytochrome P450 or uridine
diphosphate glucuronosyl transferase enzymes, for example as elucidated in pre-clinicalor clinical studies.
申请人：GILEAD COLORADO, INC.,ABBOTT GMBH & KG CO.,MELVIN, JR., LAWRENCES.,ULLRICH, MARTINA,HEGE, HANS-GUENTHER,WEYMANN, JUERGEN
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