Substituted heteroaryl benzofuran acids

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 405/14 (2006.01) A61K 31/343 (2006.01) A61K 31/4709 (2006.01) A61P 9/00 (2006.01)

Patent

CA 2538711

The present invention relates generally to substituted heteroaryl benzofuran acids and methods of using them (I); or a pharmaceutically acceptable salt or ester form therof wherein: R, R1, R2 and R3 are, independently, hydrogen, alkyl, cycloalkyl, alkanoyl, halo, hydroxy, aryl, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, or perfluoroalkoxy; R4 is hydrogen, alkyl, perfluoroalkyl, alkenyl, alkynyl, arylalkenyl, arylalkynyl, aryl,-C(=O)R5, - C(=S)R5, -CH2R5, OR -CH(OH)R5; R5 is hydrogen, C1-C8 alkyl, C3-C8 cycloalkyl, perfluoroalkyl, aryl, alkenyl, alkynyl, arylalkyl, arylalkenyl, arylalkynyl, alkylaryl, alkenylaryl, or alkynylaryl; R6 is hydrogen, alkyl, aryl, or arylalkyl; x1, x2, x3, x4, x5, x6, x7, and x8 are, independently, carbon or nitrogen, wherein at least one of x1-x8 is a nitrogen atom; n is an integer from 0-6; and A is COOH or an acid mimic or a pharmaceutically acceptable salt thereof.

L'invention concerne en général des acides hétéroaryl benzofurane substitués représentés par la formule (I) ou un sel pharmaceutiquement acceptable ou une forme d'ester de celui-ci et des procédés utilisant lesdits acides. Dans la formule (I), R, R¿1?, R¿2? et R¿3? représentent indépendamment hydrogène, alkyle, cycloalkyle, alcanoyle, halo, hydroxy, aryle, perfluoroalkyle, alkoxy, amino, alkylamino, dialkylamino ou perfluoroalkoxy; R¿4? représente hydrogène, alkyle, perfluoroalkyle, alcènyle, alcynyle, arylalcényle, arylalcynyle, aryle,-C(=O)R¿5?, -C(=S)R¿5?, -CH¿2?R¿5?, ou -CH(OH)R¿5?; R¿5? représente hydrogène, alkyle C¿1?-C¿8?, cycloalkyle C¿3?-C¿8?, perfluoroalkyle, aryle, alcényle, alcynyle, arylalkyle, arylalcényle, arylalcynyle, alkylaryle, alcénylaryle ou alcynylaryle; R¿6? représente hydrogène, alkyle, aryle ou arylalkyle; x¿1?, x¿2?, x¿3?, x¿4?, x¿5?, x¿6?, x¿7?, et x¿8? représentent indépendamment carbone ou azote, où au moins l'un de x¿1?-x¿8? représente un atome d'azote; n est un nombre entier compris entre 0 et 6; et A représente COOH ou un acide mimique ou un sel pharmaceutiquement acceptable de celui-ci.

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