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Application of compound Axitinib in preparation of medicine for treating cerebrovascular diseases and pharmaceutical composition thereof

A cerebrovascular disease and composition technology, applied in the field of medicine, can solve problems such as easy bleeding and narrow therapeutic window

Active Publication Date: 2020-04-10
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the narrow therapeutic window of t-PA (it is effective 4.5 hours after stroke) and easy to cause bleeding, only a small number of patients receive thrombolytic therapy

Method used

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  • Application of compound Axitinib in preparation of medicine for treating cerebrovascular diseases and pharmaceutical composition thereof
  • Application of compound Axitinib in preparation of medicine for treating cerebrovascular diseases and pharmaceutical composition thereof
  • Application of compound Axitinib in preparation of medicine for treating cerebrovascular diseases and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Protective effect of axitinib against focal ischemic stroke in mice.

[0040]Male C57 mice were randomly divided into control group (sham operation group), model group, and Axitinib administration group (30pmol / kg, 60nmol / kg, 120nmol / kg), 10 in each group. The mouse model of transient middle cerebral artery occlusion (tMCAO) was established by suture method. After 90 minutes of ischemia and reperfusion, different concentrations of Axitinib were injected intraperitoneally for 12 hours after reperfusion. The brains of the mice were decapitated and sliced ​​to observe the effect of Axitinib on the volume of cerebral infarction in the acute stage of cerebral ischemia. Before the mice were sacrificed, the Longa method was used to score the neurological symptoms of the mice after reperfusion (I / R) in the acute stage of cerebral ischemia. The higher the score, the more obvious the neurological deficit. And measure the grip strength of the mice and observe the use rate of the...

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Abstract

The invention relates to the technical field of medicines, and discloses an application of a compound Axitinib in preparation of a medicine for treating cerebrovascular diseases and a pharmaceutical composition thereof, the compound Axitinib is N-methyl-2-[3-((E)-2-pyridine-2-yl-vinyl)-1H-indole-6-yl sulfonyl]-benzamide, and a structural formula of the compound Axitinib is shown in the specification. According to the technical scheme, the volume of focal cerebral ischemia minor acute stage cerebral infarction is obviously reduced, the neurological symptoms are remarkably improved, the cerebralnerve protection effect is achieved, and especially the good effect on cerebral ischemic diseases is achieved.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the application of a compound Axitinib in the preparation of medicines for treating cerebrovascular diseases and its pharmaceutical composition. Background technique [0002] Cerebral stroke is a group of diseases whose main clinical manifestations are cerebral tissue ischemia and hemorrhagic injury symptoms, also known as stroke or cerebrovascular accident. The disease has an acute onset and high morbidity and mortality rates. It is the second leading cause of death in the world today, and it is becoming more and more serious with the aging of the population. Acute ischemic stroke (acute cerebral infarction) is the most common type of stroke, accounting for 69.6% to 70.8% of strokes in my country, and the mortality rate of hospitalized patients with acute ischemic stroke in my country is about 2.3% within one month after onset ~3.2%, 9%~9.6% fatality rate at 3 months, 34.5%~37....

Claims

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Application Information

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IPC IPC(8): A61K31/4439A61P9/10A61P25/00A61P9/00
CPCA61K31/4439A61P9/10A61P25/00A61P9/00
Inventor 张慧灵郭毅朱永铭林博
Owner SUZHOU UNIV
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