Novel 2-benzyloxy-phenyl formic acid ester compound for regulating activity of estrogen-related receptor as well as medical applications thereof

A compound, estrogen technology, applied in organic chemistry, drug combination, active ingredient of amide, 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 2-benzyloxy-phenyl formic acid ester compound for regulating activity of estrogen-related receptor as well as medical applications thereof
  • Novel 2-benzyloxy-phenyl formic acid ester compound for regulating activity of estrogen-related receptor as well as medical applications thereof
  • Novel 2-benzyloxy-phenyl formic acid ester compound for regulating activity of estrogen-related receptor as well as medical applications thereof

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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 uses reporter gene test formula I compound to the transcription regulation activity of 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 transcriptiona...

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Abstract

The invention discloses a novel 2-benzyloxy-phenyl formic acid ester compound for regulating activity of estrogen-related receptor with a formula I as well as pharmaceutically acceptable salts and applications thereof. The compound and pharmaceutically acceptable salts are used for preparing activity of ERR-alpha (Estrogen-related receptor alpha, ERR-alpha or ERRalpha), and are used for preparing medicaments for preventing and treating breast cancer, prostatic cancer, stomach cancer, colorectal carcinoma, ovarian cancer, cervical carcinoma and other malignant tumors.

Description

technical field [0001] The present invention relates to a novel 2-benzyloxy-benzoic acid ester compound and its pharmaceutically acceptable salts 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%,...

Claims

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Application Information

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