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    3-ARYL-ISOXAZOLE-4-CARBONYL-BENZOFURAN DERIVATIVES
    6.
    发明申请
    3-ARYL-ISOXAZOLE-4-CARBONYL-BENZOFURAN DERIVATIVES 审中-公开
    3-芳基 - 异恶唑-4-羰基苯并呋喃衍生物

    公开(公告)号：WO2007054444A2

    公开(公告)日：2007-05-18

    申请号：PCT/EP2006067879

    申请日：2006-10-27

    Applicant: HOFFMANN LA ROCHE ,  BUETTELMANN BERND ,  HAN BO ,  KNUST HENNER ,  NETTEKOVEN MATTHIAS ,  THOMAS ANDREW

    Inventor： BUETTELMANN BERND ,  HAN BO ,  KNUST HENNER ,  NETTEKOVEN MATTHIAS ,  THOMAS ANDREW

    IPC: C07D413/06 ,  A61K31/42 ,  A61P25/28 ,  C07D413/14

    CPC classification number: C07D413/06 ,  C07D413/14

    Abstract: The present invention is concerned with 3-aryl-isoxazole-4-carbonyl-benzofuran derivatives of formula (I) wherein R1 is hydrogen or halogen; R2 is hydrogen, halogen, hydroxy, lower alkoxy, OCF3, -OCH2-R, R3 is hydrogen or lower alkoxy; or R2 and R3 form together with the carbon atom to which they are attached a ring with -CH=CH-CH=-CH-; R is aryl or heteroaryl, optionally substituted by halogen or lower alkyl, or is C(O)NH-lower alkyl, or is -C(O)-heteroaryl, wherein the heteroaryl group is optionally substituted by lower alkyl or phenyl, and with their pharmaceutically acceptable acid addition salts. It has been found that this class of compounds show high affinity and selectivity for GABA A cc5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.

    Abstract translation: 本发明涉及其中R 1为氢或卤素的式（I）的3-芳基 - 异恶唑-4-羰基 - 苯并呋喃衍生物; R2是氢，卤素，羟基，低级烷氧基，OCF3，-OCH2-R，R3是氢或低级烷氧基; 或者R2和R3与它们所连接的碳原子一起形成具有-CH = CH-CH = -CH-的环; R 2为芳基或杂芳基，任选被卤素或低级烷基取代，或为C（O）NH-低级烷基，或为-C（O） - 杂芳基，其中杂芳基任选被低级烷基或苯基取代， 其药学上可接受的酸加成盐。 已经发现，这类化合物对GABA A cc5受体结合位点显示出高亲和力和选择性，并可用作认知增强剂或用于治疗认知障碍如阿尔茨海默氏病。

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