FXR receptor modulator, and preparation method and application thereof

A receptor modulator and solvate technology, applied in the field of FXR receptor modulator and its preparation, can solve the problem of not activating human or mouse receptors
CN106946867AActive Publication Date: 2017-07-14GUANGZHOU HENOVCOM BIOSCI CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
GUANGZHOU HENOVCOM BIOSCI CO LTD
Publication Date
2017-07-14

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Abstract

The invention discloses an FXR receptor modulator, and a preparation method and an application thereof, belonging to the field of medicinal chemistry. The FXR receptor modulator with a structure characteristic as shown in a formula I in the specification or pharmaceutically-acceptable salts or stereoisomers or solvates or prodrugs thereof can bind with an FXR (i.e., NR1H4) receptor and is used as an agonist or a partial agonist of the FXR receptor, thereby being able to be applied to prevention and treatment of FXR mediated diseases, such as chronic intrahepatic or extrahepatic cholestasis, hepatic fibrosis caused by chronic cholestasis or acute intrahepatic cholestasis, or chronic hepatitis B, or gallstone, or liver cancer, or colon cancer, or inflammatory bowel diseases, etc., wherein a part of compounds specifically can reach an FXR-excited EC<50> of 100 nM or below, show good FXR agonist activity, have excellent application prospects, and provide a new medicine choice for clinical treatment of the FXR mediated diseases.
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Description

technical field

[0001] The invention relates to the technical field of medicinal chemistry, in particular to a FXR receptor modulator and its preparation method and application. Background technique

[0002] Multicellular organisms rely on advanced information transmission mechanisms between cells and body compartments. The information transmitted can be highly complex and can lead to changes involving genetic programs of cell differentiation, proliferation, or regeneration. The signals (or hormones) used for transmission are usually low-molecular-weight molecules, such as peptides, fatty acids, or cholesterol derivatives.

[0003] Many of these signals exert their effects by ultimately altering the transcription of specific genes. A well-studied group of proteins that regulate cellular responses to various signals is the family of transcription factors known as nuclear receptors, often referred to hereinafter as "NR". Members of this "NR" group include: steroid hormones, ...

Claims

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