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    • 4. 发明授权
    • Oxazol/thiazol-derivatives activators of the hPPAR-alpha receptor
    • hPPAR-α受体的恶唑/噻唑衍生物激活剂
    • US07157479B2
    • 2007-01-02
    • US10478936
    • 2002-05-29
    • Francoise Jeanne Gellibert
    • Francoise Jeanne Gellibert
    • A61K31/426C07D277/30
    • C07D277/56
    • A compound of formula (I) and pharmaceutically acceptable salts, solvates and hydrolysable esters thereof 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.
    • 式(I)的化合物及其药学上可接受的盐,溶剂合物和可水解的酯。其中X 1代表O或S; R 1和R 2独立地是H或C 1-3烷基或R 1和R 2, 2个与相同碳原子键合的2个可以与它们所键合的碳原子一起形成3-5元环烷基环; R 3和R 4独立地表示H,卤素,-CH 3 3和-OCH 3 3; R 5表示H或C 1-6烷基,X 2表示NH,NCH 3或O; Y和Z之一是N,另一个是O或S; R 6表示苯基或吡啶基(其中N在位置2或3),并且任选被一个或多个卤素,CF 3,C 1〜 6个直链或支链烷基(任选被卤素取代),条件是当R 6为吡啶基时,N为未取代的。