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    Therapeutic biaryl derivatives
    9.
    发明授权
    Therapeutic biaryl derivatives 有权
    治疗性联芳衍生物

    公开(公告)号：US06251925B1

    公开(公告)日：2001-06-26

    申请号：US09719595

    申请日：2000-12-13

    申请人： Kelly Horne Donaldson ,  Barry George Shearer ,  David Edward Uehling

    发明人： Kelly Horne Donaldson ,  Barry George Shearer ,  David Edward Uehling

    IPC分类号： C07C22952

    CPC分类号： C07D213/79 ,  C07C217/14 ,  C07C229/52 ,  C07C255/58 ,  C07D213/80 ,  C07D257/04 ,  C07D307/79

    摘要： 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.

    摘要翻译： 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。