GLUCAGON ANTAGONISTS
    4.
    发明申请

    公开(公告)号:WO2015191900A1

    公开(公告)日:2015-12-17

    申请号:PCT/US2015/035400

    申请日:2015-06-11

    发明人: ZHI, Lin

    IPC分类号: C07D307/81 C07C309/15

    摘要: Provided herein are compounds, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or co-crystals and prodrugs thereof which have glucagon receptor antagonist or inverse agonist activity. Further, provided herein are pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. Moreover, provided herein are methods of making or manufacturing compounds disclosed herein, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or co-crystals and prodrugs thereof.

    摘要翻译: 本文提供了具有胰高血糖素受体拮抗剂或反向激动剂活性的化合物,包括其对映体纯的形式及其药学上可接受的盐或共晶体和前药。 此外,本文提供了包含其的药物组合物以及治疗,预防,延迟发病时间或降低发生或发展一种或多种胰高血糖素受体拮抗剂的疾病或病症的风险的方法,包括 I型和II型糖尿病,胰岛素抵抗和高血糖。 此外,本文提供了制备或制备本文公开的化合物的方法,包括其对映体纯的形式,及其药学上可接受的盐或共结晶和前药。

    FUSED HETEROCYCLIC COMPOUND
    5.
    发明申请
    FUSED HETEROCYCLIC COMPOUND 审中-公开
    熔融杂环化合物

    公开(公告)号:WO2015122187A1

    公开(公告)日:2015-08-20

    申请号:PCT/JP2015/000639

    申请日:2015-02-12

    CPC分类号: C07D307/81

    摘要: A fused heterocyclic compound having an enteropeptidase inhibitory action and use of the compound as a medicament for treatment or prophylaxis of obesity, diabetes mellitus, etc., are provided. Specifically, a compound represented by the following formula (I): wherein each symbol is as defined herein, or a salt thereof and use of the compound as a medicament for treatment or prophylaxis of obesity, diabetes mellitus, etc., are provided.

    摘要翻译: 提供具有肠肽酶抑制作用的稠合杂环化合物和该化合物作为治疗或预防肥胖症,糖尿病等的药物的用途。 具体地,提供由下式(I)表示的化合物:其中每个符号如本文所定义,或其盐,并且使用该化合物作为治疗或预防肥胖症,糖尿病等的药物。

    PROCESS FOR PREPARATION OF DRONEDARONE BY OXIDATION OF A HYDROXYL GROUP
    7.
    发明申请
    PROCESS FOR PREPARATION OF DRONEDARONE BY OXIDATION OF A HYDROXYL GROUP 审中-公开
    通过氧化羟基来制备二酮的方法

    公开(公告)号:WO2013124745A1

    公开(公告)日:2013-08-29

    申请号:PCT/IB2013/001220

    申请日:2013-02-14

    申请人: SANOFI

    IPC分类号: C07D307/81

    CPC分类号: C07D307/80 C07D307/81

    摘要: The invention relates to a novel process for the preparation of dronedarone (I) and pharmaceutically acceptable salts thereof (formula I), which comprises oxidizing a compound of formula (VI), or a salt thereof and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof. Further aspects of the invention include the novel intermediary compound of formula (VI) and process for the preparation thereof.

    摘要翻译: 本发明涉及制备决奈达隆(I)及其药学上可接受的盐(式I)的新方法,其包括氧化式(VI)化合物或其盐,所得产物如果需要 ,转化为其药学上可接受的盐。 本发明的其它方面包括式(VI)的新型中间体化合物及其制备方法。