专利内容由知识产权出版社提供
专利名称：METABOLITES AND DERIVATIVES OF
AMBRISENTAN
发明人：MELVIN, JR., Lawrence S.,ULLRICH,
Martina,HEGE, Hans-guenther,WEYMANN,Jürgen
申请号：EP08794904.6申请日：20080731公开号：EP2183223A2公开日：20100512
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 & Co. KG
地址：7575 West 103rd Avenue, Suite 102 Westminster, CO 80021-5426 US,Max-Planck-Ring 2 65205 Wiesbaden DE
国籍：US,DE
代理机构：Brown, David Leslie
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