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Carboxylic acid derivatives compound and preparation method and application thereof

A compound and alkyl technology, applied in the field of carboxylic acid derivatives and their preparation and application, can solve the side effects of rhabdomyolysis syndrome and other problems

Active Publication Date: 2013-04-17
SHANGHAI SHYNDEC PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Attempts to combine the two types of drugs have resulted in severe side effects of rhabdomyolysis syndrome in some patients

Method used

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  • Carboxylic acid derivatives compound and preparation method and application thereof
  • Carboxylic acid derivatives compound and preparation method and application thereof
  • Carboxylic acid derivatives compound and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0087] Embodiment 1: the preparation of compound a1

[0088] Gemfibrozil 1g, dicyclohexylcarbodiimide 1.07g, 2,4‐dihydroxyacetophenone 0.608g, dichloromethane 60ml in a 100ml one-mouth bottle, react at room temperature for 5 hours, evaporate to dryness, ethanol Recrystallization gave 1.19 g of compound a1. MS (ESI) 385 (M+H).

Embodiment 2

[0089] Embodiment 2: the preparation of compound a2

[0090]Gemfibrozil 1g, dicyclohexylcarbodiimide 1.07g, 2,5-dihydroxypropiophenone 0.608g, dichloromethane 60ml in a 100ml one-mouth bottle, react at room temperature for 5 hours, evaporate the solvent to dryness, and ethanol weight Crystallization gave 1.21 g of compound a2. MS (ESI): 385 (M+H + ).

Embodiment 3

[0091] Embodiment 3: the preparation of compound a3

[0092] Gemfibrozil 1g, dicyclohexylcarbodiimide 1.07g, 3,5-dihydroxyacetophenone 0.608g, dichloromethane 60ml were placed in a 100ml one-mouth bottle, reacted at room temperature for 5 hours, evaporated to dryness, Recrystallization from ethanol gave 1.18 g of compound a3. MS (ESI): 385 (M+H + ).

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Abstract

The invention discloses a substituted arone derivate, an aryloxy-phenoxy, and a carboxylic acids compound formed by the derivates of the aryloxy-phenoxy. The compound shows a good effect in pharmacological research, can reduce cholesterol, low-density lipoprotein and triglyceride in the blood at the same time, and has obvious advantages on efficacy. The conventional p-hydroxyacetophenone or aryloxy-phenoxy compound has no capacity of reducing the three components at the same time and nearly plays no effect to the p-hydroxyacetophenone and triglyceride; and the aryloxy-phenoxy compound does not work well with respect to the cholesterol and the low-density lipoprotein. The compound with a dosage of 80mg / kg has the capacity of reducing the cholesterol and the low-density lipoprotein similar to the capacity of the p-hydroxyacetophenone with the dosage of 150mg / kg.

Description

technical field [0001] The present invention relates to a novel carboxylic acid derivative compound and its preparation method and application, in particular to a carboxylic acid derivative compound composed of substituted aryl ketone derivatives, phenoxyaromatic acid and its derivatives and its preparation method and apply. Background technique [0002] Cardiovascular and cerebrovascular diseases are currently the most serious disease that endangers human life and health, and are common and frequently-occurring diseases among middle-aged and elderly people. It ranks first in morbidity and mortality in many countries. Atherosclerosis is the basis of many cardiovascular and cerebrovascular diseases. A large number of experimental and clinical data prove that atherosclerosis is closely related to abnormal blood lipid metabolism. Therefore, lipid-regulating drugs have become an important field of current drug research. [0003] Through prospective, random and controlled clin...

Claims

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Application Information

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IPC IPC(8): C07C69/712C07C67/08C07C67/14C07C233/73C07C235/24C07C231/12C07C231/02A61K31/222A61K31/167A61P3/06A61P1/16
Inventor 于振鹏魏宝康王国平刘石侯建
Owner SHANGHAI SHYNDEC PHARMA CO LTD
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