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Antagon of endostadin receptor pyrazole carboxylic acids

A technology for endothelin receptors and antagonists, applied in the field of novel pyrazole carboxylic acid endothelin receptor antagonists, which can solve the problems of lack of therapeutic drugs

Inactive Publication Date: 2004-03-10
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
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Problems solved by technology

There is currently no effective treatment for these diseases

Method used

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  • Antagon of endostadin receptor pyrazole carboxylic acids
  • Antagon of endostadin receptor pyrazole carboxylic acids
  • Antagon of endostadin receptor pyrazole carboxylic acids

Examples

Experimental program
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Effect test

Embodiment 4

[0059] Embodiment 4-benzyloxy-2-hydroxyacetophenone

[0060] Dissolve 5g (0.033mol) of 2,4-dihydroxyacetophenone in 150ml of acetone, add 6.5g (0.05mol) of K 2 CO 3 , 3g KI, 0.1g TBAB, slowly drop 4.9g (0.039mol) benzyl chloride under stirring, react at room temperature for 0.5hr, then reflux for 2hr, cool to room temperature, filter, the filtrate is evaporated to dryness, and the residue is washed with anhydrous Recrystallization from ethanol gave 5.6 g of white needle crystals, with a yield of 70%. 4-(p-chlorobenzyloxy)-2-hydroxyacetophenone

[0061] Dissolve 7.6g (0.05mol) of 2,4-dihydroxyacetophenone in 150ml of acetone, add 7g (0.05mol) of K 2 CO 3 , 3g KI, 0.1g TBAB was slowly dripped into 7.7g (0.05mol) p-chlorobenzyl chloride under stirring, reacted at room temperature for 0.5hr, then refluxed for 3hr, cooled to room temperature, filtered, the filtrate was evaporated to dryness, and the residue was used Recrystallization from absolute ethan...

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Abstract

A pyrazole-carboxylic acid kind of endothelin receptor antagon for treating cardiovascular and cerebrovascular diseases, tumor, diabetes, nephretis and asthma is disclosed.

Description

technical field [0001] The present invention relates to novel pyrazole carboxylic acid endothelin receptor antagonists and their application in treating cardiovascular and cerebrovascular diseases, tumors, diabetes, nephropathy and asthma. Background technique [0002] The mortality rate of cardiovascular and cerebrovascular diseases ranks first among various diseases, and the final cause of death is overwhelmingly cardiac hypertrophy, heart failure (heart failure), stroke and fatal arrhythmia. Especially in recent years, the fatality rate of severe heart failure has remained high, which has become a difficult problem in the international medical community. These diseases currently lack effective therapeutic drugs. [0003] Endothelin (ET) is one of the strongest known vasoconstrictor factors discovered in 1988, and ETs include ET-1, ET-2 and ET-3. There are two main types of ET receptors in mammals: ET A and ET B . ET-1-selective ET mainly expressed in vessel walls and...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/415A61P3/10A61P5/16A61P9/10A61P11/06A61P13/12A61P35/00C07D231/14
Inventor 吉民戴德哉华维一戴茵刘立刚黄敏
Owner CHINA PHARM UNIV
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