PROCESS FOR PREPARATION OF SULFONYLUREA BILE ACID DERIVATIVES

    公开(公告)号:US20180148469A1

    公开(公告)日:2018-05-31

    申请号:US15826233

    申请日:2017-11-29

    Abstract: 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.

    MACROCYCLIC PROLINE DERIVED HCV SERINE PROTEASE INHIBITORS
    49.
    发明申请
    MACROCYCLIC PROLINE DERIVED HCV SERINE PROTEASE INHIBITORS 审中-公开
    大环丙糖衍生的HCV丝氨酸蛋白酶抑制剂

    公开(公告)号:US20160145298A1

    公开(公告)日:2016-05-26

    申请号:US14946866

    申请日:2015-11-20

    Abstract: The present invention discloses compounds of Formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

    Abstract translation: 本发明公开了式I化合物或其药学上可接受的盐,酯或前药:其抑制丝氨酸蛋白酶活性,特别是丙型肝炎病毒(HCV)NS3-NS4A蛋白酶的活性。 因此,本发明的化合物干扰丙型肝炎病毒的生命周期,也可用作抗病毒剂。 本发明还涉及药物组合物,其包含用于给患有HCV感染的受试者施用的上述化合物。 本发明还涉及通过施用包含本发明化合物的药物组合物来治疗受试者的HCV感染的方法。

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