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Novel estrogen-related receptor alpha agonists and application thereof

An estrogen and agonist technology, applied in the field of diabetes treatment drugs and pharmacology, can solve problems such as hypoglycemia, and achieve the effect of strong agonist activity and novel structure

Active Publication Date: 2019-12-13
EAST CHINA UNIV OF SCI & TECH
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  • Abstract
  • Description
  • Claims
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AI Technical Summary

Problems solved by technology

But so far, the type 2 diabetes treatment drugs that have been on the market have side effects such as hypoglycemia, liver and kidney damage, lactic acidosis, and gastrointestinal reactions; and the number of diabetic patients is increasing, so looking for drugs that can treat type 2 diabetes Targeting and developing therapeutic drugs has been a research hotspot

Method used

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  • Novel estrogen-related receptor alpha agonists and application thereof
  • Novel estrogen-related receptor alpha agonists and application thereof
  • Novel estrogen-related receptor alpha agonists and application thereof

Examples

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Embodiment Construction

[0023] In order to understand the technical content of the present invention more clearly, the following examples are given in detail.

[0024] 1. Combined virtual screening based on ligand three-dimensional structure similarity search and receptor pharmacophore method:

[0025] See figure 1 As shown, the compound molecules in the Enamine database were screened by using the combined virtual screening method based on the similarity search of the three-dimensional structure of the ligand and the receptor pharmacophore, and finally the above-mentioned compound of the present invention was obtained. The specific steps are as follows:

[0026] (1) The first round of screening:

[0027] The Enamine compound database was initially screened by ligand-based three-dimensional structure similarity search and receptor pharmacophore methods, respectively.

[0028] The virtual screening based on small molecule 3D structure similarity search uses DK3 as the query structure, and uses the Sh...

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Abstract

The invention relates to novel estrogen-related receptor alpha (ERRalpha) agonists. The novel ERRalpha agonists are 7,8-dimethyl-4-(1-piperidyl)-2H-1-benzopyran-2-one, 2,4-dichloro-1-naphthyl-1-nipecotic acid, 2-[(hexyloxy-1(2H)-azoheterocyclic)methyl]-8-methyl-4H-pyridino[1,2-a]pyrimidone, 7-chloro-2-[(4-methyl-1-piperidyl)methyl]-4(3H)-quinazolinone, N-[5-[(2-amino-2-oxoethyl)thio]-2-thiazolyl]-3-methyl-1-phenyl-1H-thiophene[2,3-c]pyrazol-5-carboxamide and 4-[(2,4-dichlorophenyl)methoxy]-3-methoxy-2-amino-1-methyl-2-oxoethyl-benzoic acid. The invention further provides a screening method andan application of the novel ERRalpha agonists.

Description

technical field [0001] The invention relates to the technical field of pharmacy, in particular to the technical field of drugs for treating diabetes, and specifically refers to a new estrogen-related receptor alpha (ERRα) agonist and its use. Background technique [0002] With the gradual improvement of people's living standards, diabetes has become the third major disease that endangers human life and health after tumors and cardiovascular diseases. Diabetes mellitus is a systemic disease that is mainly caused by the disorder of glucose metabolism and also includes the disorder of fat and protein metabolism when the human body cannot produce enough insulin or cannot correctly recognize insulin. In addition to elevated blood sugar in the body, diabetic patients also have many clinical manifestations, such as polydipsia, polyphagia, polyuria, weight loss, etc. Medically, it is divided into four categories: type 1 diabetes (absolute insulin deficiency caused by β cell damage)...

Claims

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Application Information

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IPC IPC(8): C07D311/16C07D295/205C07D471/04C07D401/06C07D495/04C07C235/06A61P3/10A61P3/04G16C20/50
CPCA61P3/04A61P3/10C07C235/06C07D295/205C07D311/16C07D401/06C07D471/04C07D495/04G16C20/50
Inventor 刘桂霞王蕊唐赟李冬萍苏琳李伏兴焦茜
Owner EAST CHINA UNIV OF SCI & TECH
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