Propionic acid derivatives and their use as hppars activators

C - Chemistry – Metallurgy – 07 – C

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C07C 217/58 (2006.01) A61K 31/18 (2006.01) A61K 31/195 (2006.01) A61K 31/33 (2006.01) C07C 217/80 (2006.01) C07C 233/18 (2006.01) C07C 255/58 (2006.01) C07C 311/08 (2006.01) C07C 311/29 (2006.01) C07C 323/25 (2006.01) C07D 213/74 (2006.01) C07D 213/75 (2006.01) C07D 239/42 (2006.01) C07D 241/20 (2006.01)

Patent

CA 2489359

A compound of formula (I) or a pharmaceutically acceptable salt, solvate, or hydrolysable ester thereof, .Wherein:R1 and R2 are independently hydrogen or C1-3 alkyl;X represents a bond, CH2 or O;R3 and R4 are independently hydrogen, C1-6 alkyl, OCH3, CF3, allyl or halogen;X1 is CH2, SO2, or CO;R5 is -C1-6 alkyl (optionally substituted by C1-6alkoxy or C1-6alkylthio), -C2-6 alkenyl, - C0-6 alkyl phenyl (wherein the phenyl is optionally substituted by one or more CF3, halogen, C1-3 alkyl, C1-3 alkoxy), -COC1-6 alkyl, SO2C1-6 alkyl ;R6 is phenyl or a 6 membered heteroaryl group containing 1,2 or 3 N atoms wherein the phenyl or heteroaryl group is optionally substituted with 1, 2 or 3 moieties selected from the group consisting of C1-6 alkyl, halogen, -OC1-6 alkyl, -SO2C1-3 alkyl, phenyl (optionally substituted by one or more groups selected from halogen, CF3, C1-3 alkyl, OC1-3 alkyl, acetyl, CN).

Cette invention concerne un compos~ repr~sent~ par la formule (I) ou un sel, un solvate ou un ester hydrolisable pharmaceutiquement acceptables de ce compos~. Dans cette formule: R?1´ et R?2´ sont ind~pendamment hydrog­ne ou alkyle en C´1-3?; X repr~sente une liaison, CH´2? ou O; R?3´ et R?4´ sont ind~pendamment hydrog­ne, alkyle en C´1-6?, OCH´3?, CF´3?, allyle ou halog­ne; X?1´ est CH´2?, SO´2?, ou CO; R?5´ est alkyle en -C´1-6? (~ventuellement substitu~ par alkoxy en C´1-6?ou alkylthio en C´1-6?), alc~nyle en-C´2-6?, alkyl ph~nyle en -C´0-6 ? (dans lequel le ph~nyle est ~ventuellement substitu~ par un ou plusieurs CF´3?, halog­ne, alkyle en C´1-3?, alkoxy en C´1-3?),alkyle en -COC´1-6?, alkyle en SO´2?C´1-6 ?alkyle; R?6´ est ph~nyle ou un groupe h~t~roaryle ~ 6 membres renfermant 1,2 or 3 atomes de N, le groupe ph~nyle ou h~t~roaryle ~tant ~ventuellement substitu~ par 1, 2 ou 3 fractions prises dans le groupe compos~ de alkyle en C´1-6?, halog­ne, -OC´1-6 ?alkyle, -SO?2´C´1-3 ?alkyle, ph~nyle (~ventuellement substitu~ par un ou plusieurs groupes pris parmi halog­ne, CF´3?, alkyle en C´1-3?, OC´1-3?alkyle, ac~tyle, CN).

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