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Oxygen-containing heterocyclic compound for treating cerebral apoplexy

A compound, stroke technology, applied in the direction of organic chemistry, drug combination, medical preparations containing active ingredients, etc., to achieve good therapeutic activity and broaden the scope of the effect

Active Publication Date: 2021-01-12
THE SECOND PEOPLES HOSPITAL OF SHENZHEN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In summary, although various chemical drugs and natural drugs are in different research stages, there is no drug that splices edaravone and coumarin fragments among the currently marketed stroke drugs

Method used

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  • Oxygen-containing heterocyclic compound for treating cerebral apoplexy
  • Oxygen-containing heterocyclic compound for treating cerebral apoplexy
  • Oxygen-containing heterocyclic compound for treating cerebral apoplexy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Embodiment 1: the synthesis of compound I

[0022] Under ice bath conditions, compound 2 (190mg, 1mmol), dicyclohexylcarbodiimide (413mg, 2mmol), 4-dimethylaminopyridine (244mg, 2mmol) and 10mL of dichloromethane were added to a 150mL three-necked flask , stirred for 20min, added compound 3 (209mg, 1.1mmol) in dichloromethane (15mL) solution, after the addition was completed, the temperature was raised to reflux temperature for 8h reaction, after the reaction was detected by TLC, the reaction solution was cooled to room temperature, and 30mL of water was added. After static liquid separation, the organic phase was concentrated under reduced pressure, and then separated by silica gel column chromatography to obtain the target product I as a white solid with a yield of 41% and a purity of 98.1% by HPLC.

[0023] Molecular formula: C 20 h 14 N 2 o 5 ;ESI-MS: 363.17[M+H] +

[0024] 1 H NMR (400MHz, CDCl 3 )δ2.24(s, 3H), 2.52(s, 2H), 6.07(dd, 1H), 7.22(d, 2H), 7.54(d...

Embodiment 2

[0025] Embodiment 2: The effect of the compound shown in formula I in treating ischemic stroke

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PUM

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Abstract

The present invention relates to a compound for preventing and treating cerebral apoplexy, particularly ischemic cerebral apoplexy, which exhibits good therapeutic activity in a mouse cerebral ischemia reperfusion test, can significantly reduce the proportion of cerebral infarction, and can be used for preventing and treating cerebral apoplexy, particularly ischemic cerebral apoplexy.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a compound for preventing and treating stroke, especially ischemic stroke, and also relates to a preparation method, pharmaceutical composition and use of the compound. Background technique [0002] In recent years, the incidence of stroke in my country has ranked first in the world. The results of the third national cause of death survey confirmed that stroke has become the first cause of death in my country, and the annual growth rate exceeds 8.7%, which has seriously affected the lives and health of Chinese people. Stroke is mainly divided into two types: ischemic stroke (IS) and hemorrhagic stroke (HS). Among them, IS type patients account for three-quarters of the total incidence of patients and are the main cause of stroke. Types of. The key to the treatment of IS is "early diagnosis and early intervention". Various current treatments try to save the ischemic brain tissu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D405/12A61K31/4155A61P9/10
CPCC07D405/12A61P9/10Y02P20/55
Inventor 任力杰谭回胡诗雨冯宏业王洋雷志浩
Owner THE SECOND PEOPLES HOSPITAL OF SHENZHEN
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