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    • 9. 发明授权
    • Therapeutic biaryl derivatives
    • 治疗性联芳衍生物
    • US06251925B1
    • 2001-06-26
    • US09719595
    • 2000-12-13
    • Kelly Horne DonaldsonBarry George ShearerDavid Edward Uehling
    • Kelly Horne DonaldsonBarry George ShearerDavid Edward Uehling
    • C07C22952
    • C07D213/79C07C217/14C07C229/52C07C255/58C07D213/80C07D257/04C07D307/79
    • The present invention relates to therapeutic biaryl derivatives of formula (I), and pharmaceutically acceptable derivatives thereof wherein R1 is a phenyl, naphthyl, pyridyl, thiazolyl, phenoxymethyl, or pyrimidyl group, optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxy, C1-6alkoxy, C1-6alkyl, nitro, cyano, hydroxymethyl, trifluoromethyl, —NR6R6, and —NHSO2R6, where each R6 is independently hydrogen or C1-4alkyl; R2 is hydrogen or C1-6alkyl; X is oxygen, sulfur, —NH, or —NC1-4alkyl; R3 is cyano, tetrazol-5-yl, or —CO2R7 where R7 is hydrogen or C1-6alkyl; R4 and R5 are independently hydrogen, C1-6alkyl, —CO2H, —CO2C1-6alkyl, cyano, tetrazol-5-yl, halogen, trifluoromethyl, or C1-6alkoxy, or, when R4 and R5 are bonded to adjacent carbon atoms, R4 and R5 may, together with the carbon atoms to which they are bonded, form a fused 5 or 6 membered ring optionally containing one or two nitrogen, oxygen, or sulfur atoms; and Y is N or CH, to processes for their preparation and their use in the treatment of diseases susceptible to ameleoration by treatment with a beta-3 adrenoceptor agonist.
    • 本发明涉及式(I)的治疗性联芳基衍生物及其药学上可接受的衍生物,其中R1是苯基,萘基,吡啶基,噻唑基,苯氧基甲基或嘧啶基,任选地被一个或多个选自卤素 ,羟基,C 1-6烷氧基,C 1-6烷基,硝基,氰基,羟甲基,三氟甲基,-NR 6 R 6和-NHSO 2 R 6,其中每个R 6独立地为氢或C 1-4烷基; R2是氢或C1-6烷基; X是氧,硫,-NH或-NC 1-4烷基; R 3是氰基,四唑-5-基或-CO 2 R 7,其中R 7是氢或C 1-6烷基; R 4和R 5独立地是氢,C 1-6烷基,-CO 2 H,-CO 2 C 1-6烷基,氰基,四唑-5-基,卤素,三氟甲基或C 1-6烷氧基,或者当R 4和R 5与相邻碳原子键合时,R 4 并且R 5可以与它们所键合的碳原子一起形成任选地含有一个或两个氮,氧或硫原子的稠合的5或6元环; 并且Y是N或CH,用于其制备及其用于治疗通过用β-3肾上腺素受体激动剂治疗而易于变形的疾病的用途。