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Novel N-phenyl-benzamide-based estrogen-related receptor activity regulating compound and medical uses thereof

A compound, estrogen technology, applied in organic chemistry, amide active ingredient, drug combination, 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 N-phenyl-benzamide-based estrogen-related receptor activity regulating compound and medical uses thereof
  • Novel N-phenyl-benzamide-based estrogen-related receptor activity regulating compound and medical uses 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 present invention discloses a novel N-phenyl-benzamide-based estrogen-related receptor activity regulating compound having a structure represented by a formula I, a pharmaceutically acceptable salt and applications thereof, wherein the compound and the pharmaceutically acceptable salt thereof can be used for preparation of drugs for regulating the activity of estrogen-related receptors ERR-alpha (Estrogen-related receptor alpha, ERR-alpha or ERRalpha) and preventing and treating breast cancer, prostate cancer, gastric cancer, colon cancer, ovarian cancer, cervical cancer and other malignant tumors. The formula I is defined in the specification.

Description

technical field [0001] The present invention relates to a novel N-phenyl-benzamide compound and a pharmaceutically acceptable salt thereof as a regulator of estrogen-related receptor alpha (ERR-alpha, ERR-alpha or ERRα) and The drug combination thereof and its application 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 ligan...

Claims

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Application Information

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IPC IPC(8): C07C311/08A61K31/18A61P35/00
CPCC07C311/08
Inventor 杜永丽李蕊凌浩李群益
Owner QILU UNIV OF TECH
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