[EN] ISOXAZOLOPYRIDINE DERIVATIVES FOR USE IN THE TREATMENT OF HIF-MEDIATED CONDITIONS<br/>[FR] DÉRIVÉS D'ISOXAZOLOPYRIDINE DESTINÉS À ÊTRE UTILISÉS DANS LE TRAITEMENT D'ÉTATS À MÉDIATION PAR HIF
申请人:FIBROGEN INC
公开号:WO2009073669A1
公开(公告)日:2009-06-11
The present invention relates to novel compounds of formula (I) capable of modulating the stability and/or activity of hypoxia inducible factor (HIF) by inhibiting the activity of at least one HIF hydroxylase enzyme.
facile and practical method for the preparation of (E)-β-arylenamides [(E)-N-(1-arylprop-1-en-2-yl]acetamides] has been developed by reductive acetylation of the corresponding oximes with iron(II) acetate as the reducing reagent. Employment of hexamethylphosphoramide as the solvent was found to be critical for the high E/Z selectivity. The methodology has been applied in efficient syntheses of a key