Novel 3-bromophenyl urea estrogen-related receptor activity regulation compound and medical use thereof

A compound, estrogen technology, used in drug combinations, amide active ingredients, antitumor drugs, etc.

Inactive Publication Date: 2017-03-29
QILU UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

These studies suggest that modulators targeting ERRα have the potential to serve as clinically effective antitumor agents

Method used

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  • Novel 3-bromophenyl urea estrogen-related receptor activity regulation compound and medical use thereof
  • Novel 3-bromophenyl urea estrogen-related receptor activity regulation compound and medical use thereof
  • Novel 3-bromophenyl urea estrogen-related receptor activity regulation compound and medical use thereof

Examples

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Embodiment Construction

[0014] The present invention is described in detail and specifically by specific examples below, to better understand the present invention, but following examples do not limit the scope of the present invention, below will describe in detail the biological activity and pharmacological evaluation of formula I compound of the present invention .

[0015] Embodiment 1 Use reporter gene to test the transcriptional regulation activity of formula I compound to ERR-alpha

[0016]

[0017] This example illustrates that the compound of formula I involved in the present invention can effectively inhibit the expression of the reporter gene regulated by ERR-alpha in human embryonic kidney cells HEK-293, indicating that the compound of formula I involved in the present invention can effectively regulate ERR-alpha alpha function. Reporter gene testing techniques are familiar to those skilled in the art.

[0018] We used the GAL4 fusion receptor activation method to test the transcript...

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Abstract

The invention discloses a novel 3-bromophenyl urea estrogen-related receptor activity regulation compound, its pharmaceutically acceptable salt and application thereof. The compound and its pharmaceutically acceptable salts can be used for preparation of drugs capable of regulating estrogen related receptor ERR-alpha (Estrogen-related receptor alpha, ERR-alpha or ERR alpha) activity, preventing and treating breast cancer, prostate cancer, gastric cancer, colon cancer, ovarian cancer, cervical cancer and other malignant tumors. (formula I).

Description

technical field [0001] The present invention relates to a novel 3-bromophenylurea compound and its pharmaceutically acceptable salt as a modulator and medicine for regulating estrogen-related receptor ERR-alpha (Estrogen-related receptor alpha, ERR-alpha or ERRα) The combination and its use in the preparation of drugs for preventing and / or treating tumors such as breast cancer, prostate cancer, gastric cancer, colon cancer, ovarian cancer, cervical cancer or endometrial cancer. Background technique [0002] ERRα was cloned and identified by Giguere et al. in 1988. As an orphan nuclear receptor (Orphan nuclear receptor), the endogenous ligand of ERRα has not been discovered. ERRα is widely expressed in the body and can be detected from myocardium, digestive tract, brain, skeletal muscle, brown fat, breast cancer, ovarian cancer and other malignant tumors. ERRα has high homology with estrogen receptor α (ERα): DNA binding domain (DNA binding domain, DBD) amino acid similarit...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/18A61P35/00
Inventor 杜永丽李蕊凌浩李群益
Owner QILU UNIV OF TECH
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