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    1,4,5-substituted 1,2,3-triazole analogues as antagonists of the pregnane X receptor
    3.
    发明授权
    1,4,5-substituted 1,2,3-triazole analogues as antagonists of the pregnane X receptor 有权

    公开(公告)号：US10947203B2

    公开(公告)日：2021-03-16

    申请号：US16679007

    申请日：2019-11-08

    Applicant: ST. JUDE CHILDREN'S RESEARCH HOSPITAL

    Inventor： Taosheng Chen ,  Wenwei Lin ,  Yueming Wang

    IPC: A61K31/4192 ,  C07D249/06 ,  A61K9/20 ,  A61K47/02 ,  A61K9/00 ,  A61K47/10 ,  A61K47/36 ,  A61P35/00

    Abstract: In an aspect, the invention relates to 1,4,5-substituted 1,2,3-triazole and 1,2,4,5-substituted imidazoles having a structure represented by a formula: which are modulators the pregnane X receptor (“PXR”); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of modulating an adverse drug reaction in a mammal using the compounds and pharmaceutical compositions; methods of treatment of a disorder of uncontrolled cellular proliferation, such as a cancer, using the compounds and pharmaceutical compositions; methods of modulating pregnane X receptor activity in a mammal using the compounds and pharmaceutical compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

    1,4,5-substituted 1,2,3-triazole analogues as antagonists of the pregnane X receptor
    4.
    发明授权
    1,4,5-substituted 1,2,3-triazole analogues as antagonists of the pregnane X receptor 有权

    公开(公告)号：US10550091B2

    公开(公告)日：2020-02-04

    申请号：US16085972

    申请日：2017-03-10

    Applicant: ST. JUDE CHILDREN'S RESEARCH HOSPITAL

    Inventor： Taosheng Chen ,  Wenwei Lin ,  Yueming Wang

    IPC: C07D249/06 ,  A61K9/20 ,  A61K47/02 ,  A61K9/00 ,  A61K47/10 ,  A61K47/36 ,  A61P35/00

    Abstract: In an aspect, the invention relates to 1,4,5-substituted 1,2,3-triazole and 1,2,4,5-substituted imidazoles, which are modulators the pregnane X receptor (“PXR”); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of modulating an adverse drug reaction in a mammal using the compounds and pharmaceutical compositions; methods of treatment of a disorder of uncontrolled cellular proliferation, such as a cancer, using the compounds and pharmaceutical compositions; methods of modulating pregnane X receptor activity in a mammal using the compounds and pharmaceutical compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

    METHOD AND COMPOSITIONS FOR DETECTING BINDING TO THE PREGNANE X RECEPTOR
    8.
    发明申请
    METHOD AND COMPOSITIONS FOR DETECTING BINDING TO THE PREGNANE X RECEPTOR 审中-公开
    检测与孕激素受体结合的方法和组合物

    公开(公告)号：US20160033531A1

    公开(公告)日：2016-02-04

    申请号：US14773901

    申请日：2014-03-15

    Applicant: ST. JUDE CHILDREN'S RESEARCH HOSPITAL

    Inventor： Taosheng Chen ,  Wenwei Lin

    IPC: G01N33/68 ,  G01N21/64

    CPC classification number: G01N33/6875 ,  G01N21/6428 ,  G01N33/542 ,  G01N33/566 ,  G01N33/582 ,  G01N2021/6439 ,  G01N2333/70567 ,  G01N2500/04 ,  G01N2500/20

    Abstract: In one aspect, the invention relates to compounds useful as fluorescence assay probes, methods of making same, and methods of using same to assay ligand binding interactions with PXR. In various aspects, the invention pertains to compositions comprising a polypeptide comprising a pregnane X receptor polypeptide, or a ligand binding fragment polypeptide thereof; and a molecule comprising a BODIPY residue and a vinca alkaloid residue. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

    Abstract translation: 一方面，本发明涉及可用作荧光测定探针的化合物，其制备方法，以及使用该化合物测定与PXR的配体结合相互作用的方法。 在各个方面，本发明涉及包含含有孕烷X受体多肽或其配体结合片段多肽的多肽的组合物; 和包含BODIPY残基和长春花生物碱残基的分子。 该摘要旨在作为用于在特定技术中进行搜索的扫描工具，而不意在限制本发明。

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