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Nitrogen-containing heterocyclic compound for treating cerebral apoplexy

A compound, stroke technology, applied in the field of medicinal chemistry, achieves good therapeutic activity and broadens the range of effects

Pending Publication Date: 2021-02-12
THE SECOND PEOPLES HOSPITAL OF SHENZHEN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] To sum up, although various chemical and natural medicines are in different research stages, there is no drug that splices edaravone and danshensu fragments among the currently marketed stroke drugs

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1: the synthesis of compound I

[0023] Compound 2 (283mg, 1.5mmol), HOAt (273mg, 2mmol), PyAOP (1044mg, 2mmol), DIPEA (347μL, 2mmol) and 10mL DMSO were added to a 150mL three-necked flask, stirred for 15min, and compound 3 (198mg, 1mmol) of DMSO (10mL) solution, after adding, stir and react at room temperature for 18h. After the reaction is detected by TLC, add 20mL water and 30mL dichloromethane, stand for liquid separation after extraction, and separate the organic phase through silica gel column chromatography to obtain yellow The target product I was a brown solid, with a yield of 49% and a purity of 97.6% by HPLC.

[0024] Molecular formula: C 19 h 19 N 3 o 5 ;ESI-MS: 370.72[M+H] +

[0025] 1 H NMR (400MHz, CDCl 3 )δ1.90(s, 3H), 2.19(s, 3H), 2.83(s, 1H), 3.12(m, 2H), 4.59(m, 1H), 5.43(d, 2H), 6.63-6.81(m , 3H), 7.60 (m, 2H), 7.85 (m, 2H).

Embodiment 2

[0026] Embodiment 2: The effect of the compound shown in formula I in treating ischemic stroke

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Abstract

The present invention relates to a compound for preventing and treating cerebral apoplexy, particularly ischemic cerebral apoplexy, wherein the compound 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] 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 tissue by recanalizing the blood flow of the early infarcted brain tissue, but its short "t...

Claims

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Application Information

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IPC IPC(8): C07D231/26A61K31/4152A61P9/10
CPCC07D231/26A61P9/10
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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