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Novel 4-bromophenylurea-type compound with estrogen-related receptor regulation activity and its medical use

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

AI Technical Summary

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 4-bromophenylurea-type compound with estrogen-related receptor regulation activity and its medical use
  • Novel 4-bromophenylurea-type compound with estrogen-related receptor regulation activity and its medical use
  • Novel 4-bromophenylurea-type compound with estrogen-related receptor regulation activity and its medical use

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Experimental program
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Embodiment Construction

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

[0015] Example 1 The transcriptional regulatory activity of the compound of formula I on ERR-alpha was tested 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] We used the GAL4 fusion receptor activation method to test the transcri...

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Abstract

The invention discloses a novel 4-bromophenylurea-type compound with estrogen-related receptor regulation activity and its pharmaceutically acceptable salt and use. The compound is shown in the formula I. The compound and its pharmaceutically acceptable salt are used for preparation of drugs which have estrogen-related receptor alpha (ERR-alpha) regulation activity and are used for preventing and treating cancers such as breast cancer, prostate cancer, gastric cancer, colon cancer, ovarian cancer and cervical cancer.

Description

technical field [0001] The present invention relates to a novel 4-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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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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