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Compound used as a regulator of estrogen-related receptor and applications thereof

A compound, halogen technology, applied in digestive system, organic chemistry, drug combination, etc.

Active Publication Date: 2009-09-16
东莞市恩联干细胞生物科技研究院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As for ERRα, which can improve insulin sensitivity by enhancing the function of PGC1, there are no reports of related small molecule agonists.

Method used

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  • Compound used as a regulator of estrogen-related receptor and applications thereof
  • Compound used as a regulator of estrogen-related receptor and applications thereof
  • Compound used as a regulator of estrogen-related receptor and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0276] 7-methoxy-3-methyl-2-phenylquinazolin-4(3H)-one

[0277] (7-methoxy-3-methyl-2-phenylquinazolin-4(3H)-one)

[0278]

[0279] Step 1. 7-Methoxy 2-phenyl-4H-benzo[d][1,3]oxazoline-4-one (7-methoxy-2-phenyl-4H-benzo[d][1,3] oxazin-4-one)

[0280] Dissolve 2-amino-4-methoxybenzoic acid (2-amino-4-methoxybenzoic acid, 1.67 g, 10 mmol) in 10 mL of pyridine at room temperature, slowly add benzoyl chloride (1.7 g, 6 mmol, dissolved in 5 mL pyridine). After stirring at room temperature for 6 hours, the reaction mixture was poured into 50 g of ice water. Extracted with ethyl acetate and purified by column chromatography (petroleum ether: ethyl acetate = 5:1) to obtain 1.96 g of product (white solid, 77.5%).

[0281] Step 2. 7-methoxy-3-methyl-2-phenylquinazolin-4(3H)-one (7-methoxy-3-methyl-2-phenylquinazolin-4(3H)-one)

[0282] Mix 0.253 g (1.0 mmol) of the compound obtained above with 0.675 g methylamine hydrochloride (10 mmol) in 10 mL DMF, and heat to reflux for 5 hou...

Embodiment 2

[0286] 7-methoxy-3-methyl-2-(4-chlorophenyl)quinazolin-4(3H)-one

[0287] (2-(4-chlorophenyl)-7-methoxy-3-methylquinazolin-4(3H)-one)

[0288] The synthesis method is as in Example 1.

[0289] 1 HNMR (400MHz, CDCl 3 ), δ 8.21(d, J=8.4Hz, 1H), 7.53~7.10(m, 4H); 7.11~7.06(m, 2H), 3.91(s, 3H), 3.48(s, 3H);

[0290] MS (ESI), m / z: 300 (M + ).

Embodiment 3

[0292] 7-methoxy-3-methyl-2-(4-fluorophenyl)quinazolin-4(3H)-one

[0293] (2-(4-fluorophenyl)-7-methoxy-3-methylquinazolin-4(3H)-one)

[0294] The synthesis method is as in Example 1.

[0295] 1HNMR (400MHz, CDCl 3 ), δ 8.19(d, J=8.8Hz, 1H), 7.59~7.56(m, 2H); 7.26~7.19(m, 2H), 710(d, J=2.0Hz, 1H), 7.06(dd, J =2.0, 8.8Hz, 1H), 3.89(s, 3H), 3.46(s, 3H);

[0296] MS(ESI), m / z: 285(M+H) + .

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Abstract

The invention discloses a compound with a formula I, pharmaceutically acceptable acid or alkali salt and applications thereof. The compound and the pharmaceutically acceptable acid or alkali salt thereof can be used for preparing medicaments that can regulate the estrogen-related receptor (ERR) and cure metabolic diseases such as hyperlipemia, fatty liver, hyperglycemia, diabetes mellitus, obesity, etc. The definitions of all genes in the formula are detailed in the specification.

Description

technical field [0001] The present invention relates to a class of compounds used as estrogen-related receptor modulators and applications thereof. Background technique [0002] In recent years, the incidence of metabolic diseases such as obesity, diabetes, hypertension, and atherosclerosis has continued to increase. These metabolic diseases can further induce the occurrence and deterioration of heart disease, seriously affecting the healthy life of people in all countries. Metabolic diseases have become one of the heaviest burdens on the healthcare system in both developing and developed countries. Therefore, it is of great social and economic value to discover new drug targets and develop new therapeutic drugs for such diseases. [0003] Diabetes can be divided into two types: type I diabetes (insulin dependent) and type II diabetes (non-insulin dependent). But they all have the property of continuously increasing blood sugar concentration in the state of fasting or eati...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/36A61K31/505A61P3/00A61P9/10
CPCC07D239/91C07D471/04C07D239/90C07D487/04C07D239/86A61P1/16A61P3/00A61P3/04A61P3/06A61P43/00A61P9/00A61P9/10A61P3/10
Inventor 丁克黄志伟康战方彭丽洁周曦
Owner 东莞市恩联干细胞生物科技研究院
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