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    Compounds and methods for treating diabetes
    1.
    发明授权
    Compounds and methods for treating diabetes 有权
    用于治疗糖尿病的化合物和方法

    公开(公告)号：US09550782B2

    公开(公告)日：2017-01-24

    申请号：US13789376

    申请日：2013-03-07

    申请人： Medivation Technologies, Inc.

    发明人： Andrew Asher Protter ,  Sarvajit Chakravarty ,  Rajendra Parasmal Jain ,  Michael John Green

    IPC分类号： A61K31/55 ,  A61K31/444 ,  C07D487/04 ,  A61K45/06 ,  C07D471/04 ,  C07D471/14 ,  C07D471/18 ,  C07D471/22 ,  C07D451/00 ,  C07D455/03

    CPC分类号： C07D487/04 ,  A61K31/444 ,  A61K31/55 ,  A61K45/06 ,  C07D451/00 ,  C07D455/03 ,  C07D471/04 ,  C07D471/14 ,  C07D471/18 ,  C07D471/22

    摘要： Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor α2A. The compounds may also bind to and are an antagonist of the adrenergic receptor α2B; or the compounds are not antagonists of the adrenergic receptor α2B and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.

    摘要翻译： 描述了氢化吡啶并[4,3-b]吲哚，吡啶并[3,4-b]吲哚和氮杂环[4,5-b]吲哚。 该化合物可以结合肾上腺素能受体α2A并且是拮抗剂。 该化合物还可以结合并且是肾上腺素能受体α2B的拮抗剂; 或者化合物不是肾上腺素能受体α2B的拮抗剂，并且化合物与减少或预期降低个体血压的第二药剂一起施用。 该化合物可用于治疗，例如调节血糖水平，增加胰岛素分泌并治疗对胰岛素产生增加或预期是响应的疾病或病症。 特别描述了化合物治疗2型糖尿病的用途。

    Fused pyrimidine compounds and use thereof
    4.
    发明授权
    Fused pyrimidine compounds and use thereof 有权
    熔融嘧啶化合物及其用途

    公开(公告)号：US09422267B2

    公开(公告)日：2016-08-23

    申请号：US14141003

    申请日：2013-12-26

    申请人： Medivation Technologies, Inc.

    发明人： Sarvajit Chakravarty ,  Roopa Rai ,  Michael John Green

    IPC分类号： C07D401/14 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14 ,  C07D491/107 ,  A61K31/502 ,  C07D405/14 ,  C07F9/6558

    CPC分类号： C07D401/14 ,  A61K31/517 ,  C07D239/84 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D491/107 ,  C07F9/65583

    摘要： The present invention provides fused pyrimidine compounds of the general Formula (I): or a salt thereof, wherein the variables are as defined in the specification. Fused pyrimidine compounds of the general Formula (I) are provided as kinase inhibitors, such as multi-kinase inhibitors. In one aspect, fused pyrimidine compounds of the general Formula (I) are provided as IGF-IR inhibitors. The compounds may be used in a method of treating cancer. Pharmaceutical compositions containing a fused pyrimidine compounds of the general Formula (I) and a pharmaceutically acceptable carrier are also provided, as are kits containing a fused pyrimidine compound of the general Formula (I) or salt thereof and instructions for use, e.g., in a method of treating cancer.

    摘要翻译： 本发明提供通式（I）的稠合嘧啶化合物或其盐，其中变量如说明书中所定义。 提供通式（I）的稠合嘧啶化合物作为激酶抑制剂，如多激酶抑制剂。 一方面，通式（I）的稠合嘧啶化合物作为IGF-1R抑制剂提供。 该化合物可用于治疗癌症的方法。 还提供含有通式（I）的稠合嘧啶化合物和药学上可接受的载体的药物组合物，以及含有通式（I）的稠合嘧啶化合物或其盐的试剂盒和使用说明书，例如在 治疗癌症的方法