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    Substituted azabenzoxazoles
    9.
    发明授权
    Substituted azabenzoxazoles 有权
    取代的氮杂苯并唑

    公开(公告)号：US08530483B2

    公开(公告)日：2013-09-10

    申请号：US12995314

    申请日：2009-05-28

    申请人： James C. Barrow ,  Scott Harrison ,  James Mulhearn ,  Cyrille Sur ,  David L. Williams ,  Scott Wolkenberg ,  Eric Hostetler

    发明人： James C. Barrow ,  Scott Harrison ,  James Mulhearn ,  Cyrille Sur ,  David L. Williams ,  Scott Wolkenberg ,  Eric Hostetler

    IPC分类号： A01N43/90 ,  A01N43/42 ,  A61K31/519 ,  A61K31/44 ,  C07D239/00 ,  C07D471/00 ,  C07D491/00 ,  C07D513/02 ,  C07D515/02 ,  C07D471/02 ,  C07D491/02 ,  C07D498/02

    CPC分类号： C07D498/04 ,  C07D519/00

    摘要： The present invention relates to novel amyloid binding compounds of formula (I) and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET/) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted azabenzoxazole derivatives, compositions, and therapeutic uses and processes for making such compounds, or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof, wherein: X is O or S; A and Y independently are N, or CH.

    摘要翻译： 本发明涉及式（I）的新型淀粉样蛋白结合化合物和通过测定活体患者淀粉样斑块水平的变化来测定化合物的效果的方法。 更具体地说，本发明涉及使用本发明化合物作为正电子发射断层摄影（PET /）成像中的示踪剂来研究脑中淀粉样蛋白沉积物以允许诊断阿尔茨海默病的方法。 因此，本发明涉及新型淀粉样蛋白结合化合物作为诊断用途。 本发明还涉及测量阿尔茨海默病治疗剂的临床疗效的方法。 具体地，本发明涉及新的芳基或杂芳基取代的氮杂苯并恶唑衍生物，组合物，以及用于制备这些化合物或其药学上可接受的盐，溶剂合物或体内可水解的酯的治疗用途和方法，其中：X是O或S; A和Y独立地为N或CH。

    NOVEL SUBSTITUTED AZABENZOXAZOLES
    10.
    发明申请
    NOVEL SUBSTITUTED AZABENZOXAZOLES 有权
    新型取代的AZABENZOXAZOLES

    公开(公告)号：US20110085985A1

    公开(公告)日：2011-04-14

    申请号：US12995314

    申请日：2009-05-28

    申请人： James C. Barrow ,  Scott Harrison ,  James Mulhearn ,  Cyrille Sur ,  David L. Williams ,  Scott Wolkenberg

    发明人： James C. Barrow ,  Scott Harrison ,  James Mulhearn ,  Cyrille Sur ,  David L. Williams ,  Scott Wolkenberg

    IPC分类号： A61K31/437 ,  C07D498/04 ,  C07D519/00 ,  A61K31/5377 ,  A61K49/00 ,  A61K49/04 ,  A61K49/06 ,  A61P25/28 ,  A61P25/18

    CPC分类号： C07D498/04 ,  C07D519/00

    摘要： The present invention relates to novel amyloid binding compounds of formula (I) and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET/) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted azabenzoxazole derivatives, compositions, and therapeutic uses and processes for making such compounds, or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof, wherein: X is O or S; A and Y independently are N, or CH;

    摘要翻译： 本发明涉及式（I）的新型淀粉样蛋白结合化合物和通过测定活体患者淀粉样斑块水平的变化来测定化合物的效果的方法。 更具体地说，本发明涉及使用本发明化合物作为正电子发射断层摄影（PET /）成像中的示踪剂来研究脑中淀粉样蛋白沉积物以允许诊断阿尔茨海默病的方法。 因此，本发明涉及新型淀粉样蛋白结合化合物作为诊断用途。 本发明还涉及测量阿尔茨海默病治疗剂的临床疗效的方法。 具体地，本发明涉及新的芳基或杂芳基取代的氮杂苯并恶唑衍生物，组合物，以及用于制备这些化合物或其药学上可接受的盐，溶剂合物或体内可水解的酯的治疗用途和方法，其中：X是O或S; A和Y独立地为N或CH;