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Medicine for preventing and treating cerebral arterial thrombosis and application thereof

A pharmacy and compound technology, applied in the field of medicine, can solve the problems of complex pathogenesis of ischemic cerebrovascular disease, lack of effective drugs in clinical treatment, etc., to prevent and treat ischemic stroke, reduce the percentage of the whole brain, reduce The effect of the degree of edema

Inactive Publication Date: 2017-06-13
MUDANJIANG MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, due to the complex pathogenesis of ischemic cerebrovascular disease and the lack of effective drugs for clinical treatment, it has become the focus of medical research in the world today, so active research and development of therapeutic drugs has important clinical significance

Method used

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  • Medicine for preventing and treating cerebral arterial thrombosis and application thereof
  • Medicine for preventing and treating cerebral arterial thrombosis and application thereof
  • Medicine for preventing and treating cerebral arterial thrombosis and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Embodiment 1: N-{3-[5,7-dihydroxyl-2-(4-methoxyphenyl)-4-oxochroman-3-yl]propyl}propane-1-sulfonamide ( Compound 1)

[0041]

[0042] Dissolve N-(3-bromopropyl)propane-1-sulfonamide (2.9g, 12mmol) in 100mL of anhydrous tetrahydrofuran, and add new shaved magnesium chips (0.30g, 12.5mmol) dropwise under stirring, 1 grain of iodine Into the flask, first drop a small amount, and then slowly drop in after the Grignard reaction is triggered. After about 20 minutes, the dripping is completed, then stir and reflux until the magnesium chips are basically completely dissolved, stop heating, wait for the Grignard reagent to cool to 30-40°C, and add the catalyst Zirconocene dichloride (0.15g, 0.5mmol) and 5,7-dihydroxy-2-(4-methoxyphenyl)-4H-chromen-4-one (2.8g, 10.0mmol), and reflux Reacted for 2h, after the reaction was completed, the reaction solution was cooled to room temperature, and then saturated NH 4 Cl aqueous solution (100mL), extracted with petroleum ether (100mL×...

Embodiment 2

[0046] Example 2: N-[(5,7-dimethoxy-4-oxo-2-phenylchroman-3-yl)methyl]-2-(pyrroline-1-yl)ethanesulfonamide (compound 2)

[0047]

[0048] According to the method of Example 1, replace N-(3-bromopropyl) propane-1-sulfonamide with N-(bromomethyl)-2-(pyrroline-1-yl)ethanesulfonamide, and use 5, 7-dimethoxy-2-phenyl-4H-chromen-4-one in place of 5,7-dihydroxy-2-(4-methoxyphenyl)-4H-chromen-4-one gives Light yellow solid N-[(5,7-dimethoxy-4-oxo-2-phenylchroman-3-yl)methyl]-2-(pyrrolin-1-yl)ethanesulfonamide, Yield 72%.

[0049] ESI-MS: 475.18[M+H] +

[0050] Elemental analysis: theoretical value / measured value, C (60.74 / 60.89), H (6.37 / 6.27), N (5.90 / 5.81), O (20.23 / 20.33), S (6.76 / 6.80).

Embodiment 3

[0051] Example 3: N-(2-{1-[5,7-bis(2-ethoxyethoxy)-4-oxo-2-phenylchroman-3-yl]cyclopropyl}ethyl ) methanesulfonamide (compound 3)

[0052]

[0053] According to the method of Example 1, N-[2-(1-bromocyclopropyl)ethyl]methanesulfonamide is used to replace N-(3-bromopropyl)propane-1-sulfonamide, and 5,7-bis (2-Ethoxyethoxy)-2-phenyl-4H-chromene-4-one instead of 5,7-dihydroxy-2-(4-methoxyphenyl)-4H-chromene-4 -ketone, giving N-(2-{1-[5,7-bis(2-ethoxyethoxy)-4-oxo-2-phenylchroman-3-yl]cyclopropyl} as a white solid Ethyl)methanesulfonamide, 52% yield.

[0054] ESI-MS: 562.24[M+H] +

[0055] Elemental analysis: theoretical value / measured value, C (62.01 / 62.12), H (7.00 / 6.87), N (2.49 / 2.58), O (22.79 / 22.73), S (5.71 / 5.60).

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Abstract

The invention relates to a medicine for preventing and treating ischemic stroke. In the mouse cerebral ischemia-reperfusion model, the compound of the present invention can significantly reduce the behavioral score, can significantly reduce the percentage of cerebral infarction / whole brain, and can significantly reduce the water content of ischemia-reperfusion damaged brain tissue, and relieve ischemia. The degree of lateral cerebral hemisphere edema can be used to prevent and treat ischemic stroke.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a medicine for preventing and treating ischemic stroke. Background technique [0002] Cerebrovascular disease (stroke) is a disease caused by blockage or rupture of cerebral blood vessels that blocks blood flow in the brain. It is divided into ischemic stroke and hemorrhagic stroke. According to reports, the results of sample surveys of urban and rural populations in my country show that the annual incidence rates are 219 / 100,000 and 185 / 100,000, respectively, and the mortality rates are 116 / 100,000 and 141.8 / 100,000, and they tend to be younger. There are about 1.5 to 2 million new stroke patients in my country every year, and ischemic stroke accounts for about 60 to 80% of the stroke cases. In 1992, among the causes of death of urban and rural population in my country, stroke ranked second, accounting for 21.13% and 16.18% of the total number of deaths. [0003] Ischemic str...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D311/60A61K31/352A61P9/10
CPCC07D311/60
Inventor 安宁张宇战海艳姚冬杰梁爽崔江河
Owner MUDANJIANG MEDICAL UNIV
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