Oxazol/thiazol-derivatives activators of the hppar-alpha...

C - Chemistry – Metallurgy – 07 – D

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C07D 277/56 (2006.01) A61K 31/42 (2006.01) A61K 31/425 (2006.01)

Patent

CA 2448205

A compound of formula (I) and pharmaceutically acceptable salts,solvates and hydrolysable esters thereof Formula I:(I); wherein X1 represents O or S; R1 and R2 are independently H or C1-3 alkyl or R1 and R2 which are bonded to the same carbon atom may together with the carbon atom to which they are bonded form a 3-5 membered cycloalkyl ring; R3 and R4 independently represent H, Halogen, -CH3 and OCH3_; R5 represents H or C1-6 alkyl X2 represents NH, NCH3 or O; One of Y and Z is N, and the other is O or S; R6 represents phenyl or pyridyl (wherein the N is in position 2 or 3) and is optionally substituted by one or more halogen, CF3, C1-6 straight or branched alkyl (optionally substituted by halogen), with the provision that when R6 is pyridyl, the N is unsubstituted.

L'invention concerne un composé de formule (I), ainsi que des sels, des solvates et des esters hydrolysables pharmaceutiquement acceptables de celui-ci, dans laquelle X¿1? représente O ou S; R?1¿ et R?2¿ représentent indépendamment H ou C¿1-3? alkyle ou R?1¿ et R?2¿, qui sont liés au même atome de carbone, peuvent former avec cet atome de carbone un anneau cycloalkyle à 3-5 chaînons; R?3¿ et R?4¿ représentent indépendamment H, halogène, -CH¿3? et OCH¿3?; R?5¿ représente H ou C¿1-6? alkyle; X¿2? représente NH, NCH¿3? ou O; si l'un des deux éléments Y et Z représente N, l'autre représente O ou S; R?6¿, qui représente phényle ou pyridyle (N étant en position 2 ou 3), est éventuellement substitué par au moins un halogène, CF¿3?, alkyle linéaire ou ramifié (éventuellement substitué par halogène), pour autant que, lorsque R?6¿ représente pyridyle, N soit non substitué.

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