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A novel n-p-tolyl-benzamide compound that regulates the activity of estrogen-related receptors and its medical application

A compound, estrogen technology, applied in organic chemistry, amide active ingredient, drug combination, etc.

Inactive Publication Date: 2018-05-22
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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  • A novel n-p-tolyl-benzamide compound that regulates the activity of estrogen-related receptors and its medical application

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 N-p-tolyl-benzamide compound with formula I for regulating the activity of estrogen-related receptors, 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 present invention relates to a novel N-p-tolyl-benzamide compound and its pharmaceutically acceptable salt as a method for regulating estrogen-related receptor alpha (ERR-alpha or ERRα). Agents and their drug combinations and their use in the preparation of drugs for the prevention and / or treatment of 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 ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C311/08A61K31/18A61P35/00
CPCC07C311/08
Inventor 杜永丽关海星凌浩李群益
Owner QILU UNIV OF TECH
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