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.

公开(公告)号：US09908890B2

公开(公告)日：2018-03-06

申请号：US15519109

申请日：2015-10-16

Applicant: ST. JUDE CHILDREN'S RESEARCH HOSPITAL

Inventor： Taosheng Chen ,  Milu Cherian ,  Wenwei Lin

IPC: C07D487/08 ,  C07D403/06 ,  C07D401/06 ,  C07D409/06 ,  C07D403/14 ,  C07D401/14 ,  C07D413/14 ,  C07D405/12 ,  C07D223/28 ,  C07D223/22

CPC classification number: C07D487/08 ,  A61K31/55 ,  C07D223/22 ,  C07D223/28 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D413/12 ,  C07D413/14 ,  A61K2300/00

Abstract: The compounds of the invention are antagonists of CAR, with specificity for CAR over other proteins including PXR. The disclosed compounds are useful in treating or controlling cell proliferative disorders, in particular oncological disorders, such as cancer. 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.

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。