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    BILE ACID DERIVATIVES AS FXR/TGR5 AGONISTS AND METHODS OF USE THEREOF
    1.
    发明申请
    BILE ACID DERIVATIVES AS FXR/TGR5 AGONISTS AND METHODS OF USE THEREOF 审中-公开
    双酸衍生物作为FXR / TGR5激动剂及其使用方法

    公开(公告)号：WO2016086218A1

    公开(公告)日：2016-06-02

    申请号：PCT/US2015/062826

    申请日：2015-11-27

    申请人： ENANTA PHARMACEUTICALS, INC.

    发明人： WANG, Guoqiang ,  OR, Yat Sun ,  SHEN, Ruichao ,  LONG, Jiang ,  DAI, Peng ,  XING, Xuechao ,  HE, Jing

    IPC分类号： A61K31/56

    CPC分类号： C07J41/0066 ,  C07J9/005 ,  C07J41/0055 ,  C07J41/0088 ,  C07J41/0094 ,  C07J43/003 ,  C07J43/006 ,  C07J51/00

    摘要： The present invention provides compounds of amino-substituted bile acid derivatives, pharmaceutical compositions comprising these compounds and methods of using these compounds to prevent or treat FXR-mediated or TGR5-mediated diseases or conditions. In one embodiment the present invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound or combination of compounds of the present invention, or a pharmaceutically acceptable salt form, stereoisomer, solvate, hydrate or combination thereof, in combination with a pharmaceutically acceptable carrier or excipient.

    摘要翻译： 本发明提供氨基取代的胆汁酸衍生物的化合物，包含这些化合物的药物组合物和使用这些化合物预防或治疗FXR介导的或TGR5介导的疾病或病症的方法。 在一个实施方案中，本发明提供药物组合物，其包含治疗有效量的本发明化合物或化合物或其药学上可接受的盐形式，立体异构体，溶剂合物，水合物或其组合与药学上可接受的载体 或赋形剂。

    BILE ACID DERIVATIVES AS FXR/TGR5 AGONISTS AND METHODS OF USE THEREOF
    2.
    发明申请
    BILE ACID DERIVATIVES AS FXR/TGR5 AGONISTS AND METHODS OF USE THEREOF 审中-公开
    双酸衍生物作为FXR / TGR5激动剂及其使用方法

    公开(公告)号：WO2016086134A1

    公开(公告)日：2016-06-02

    申请号：PCT/US2015/062679

    申请日：2015-11-25

    申请人： ENANTA PHARMACEUTICALS, INC.

    发明人： WANG, Guoqiang ,  OR, Yat, Sun ,  SHEN, Ruichao ,  LONG, Jiang ,  DAI, Peng ,  XING, Xuechao ,  HE, Jing

    IPC分类号： A61K31/56

    CPC分类号： C07J41/0088 ,  C07J9/005 ,  C07J41/0055 ,  C07J41/0061 ,  C07J41/0094 ,  C07J43/003 ,  C07J51/00

    摘要： The present invention provides compounds of amino-substituted bile acid compounds, pharmaceutical compositions comprising these compounds and methods of using these compounds to prevent or treat FXR-mediated or TGR5-mediated diseases or conditions. In another embodiment, the present invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound or combination of compounds of the present invention, or a pharmaceutically acceptable salt form, stereoisomer, solvate, hydrate or combination thereof, in combination with a pharmaceutically acceptable carrier or excipient.

    摘要翻译： 本发明提供氨基取代的胆汁酸化合物，包含这些化合物的药物组合物和使用这些化合物预防或治疗FXR介导的或TGR5介导的疾病或病症的方法。 在另一个实施方案中，本发明提供药物组合物，其包含治疗有效量的本发明化合物或化合物或其药学上可接受的盐形式，立体异构体，溶剂化物，水合物或其组合的化合物，以及药学上可接受的 载体或赋形剂。

    PROCESS FOR PREPARATION OF SULFONYLUREA BILE ACID DERIVATIVES
    3.
    发明申请
    PROCESS FOR PREPARATION OF SULFONYLUREA BILE ACID DERIVATIVES 审中-公开

    公开(公告)号：WO2018102418A1

    公开(公告)日：2018-06-07

    申请号：PCT/US2017/063720

    申请日：2017-11-29

    申请人： ENANTA PHARMACEUTICALS, INC.

    发明人： WANG, Guoqiang ,  HE, Yong ,  DAI, Peng ,  XU, Guoyou ,  WANG, Bin ,  LONG, Jiang ,  OR, Yat, Sun

    IPC分类号： A61K31/575 ,  C07C305/12

    摘要： The present invention relates to processes for preparing a compound of Formula (I), or a pharmaceutically acceptable salt or solvate thereof. These compounds and pharmaceutical compositions are useful as FXR or TGR5 modulators. Specifically, the present invention relates to bile acid derivatives and methods for their preparation and use. The present invention relates to a process for the preparation of a compound (II) and its salts and derivatives which are useful intermediates in the synthesis of biologically active molecules, especially in the synthesis of FXR and TGR5 modulators. The present invention also relates to a process for the preparation of a compound (III) and its diethylamine salt.