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A kind of 4-bromophenylurea compound that regulates the activity of estrogen-related receptors and its medical application

A compound and estrogen technology, applied in the direction of drug combination, antineoplastic drugs, amide active ingredients, etc.

Inactive Publication Date: 2019-08-20
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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  • A kind of 4-bromophenylurea compound that regulates the activity of estrogen-related receptors and its medical application
  • A kind of 4-bromophenylurea compound that regulates the activity of estrogen-related receptors and its medical application

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Embodiment Construction

[0012] In the following, the present invention will be described in detail and specifically through specific examples to better understand the present invention, but the following examples do not limit the scope of the present invention.

[0013] The biological activity and pharmacological evaluation of the compound of formula I of the present invention will be described in detail below.

[0014] Implementation column 1:

[0015] Testing the transcriptional regulatory activity of compounds of Formula I on ERR-alpha using a reporter gene

[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]...

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Abstract

The invention discloses a novel 4-bromophenylurea compound with formula I for regulating estrogen-related receptor activity, a pharmaceutically acceptable salt thereof and applications thereof. The compound and its pharmaceutically acceptable salts can be used to prepare estrogen-related receptor ERR-alpha (Estrogen-related receptor alpha, ERR-alpha or ERRα) activity for the prevention and treatment of breast cancer, prostate cancer, gastric cancer, colon cancer Cancer, ovarian cancer, cervical cancer and other malignant tumors.

Description

technical field [0001] The invention relates to a 4-bromophenylurea compound and a pharmaceutically acceptable salt thereof as a modulator for regulating estrogen-related receptor alpha (ERR-alpha, ERR-alpha or ERRα) and a pharmaceutical combination thereof 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 similarity is 68%, and ligand bindi...

Claims

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Application Information

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Patent Type & Authority Patents(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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