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Application of compound SB216763 to preparing cerebrovascular disease preventing and/or treating drugs and pharmaceutical composition of compound SB216763

A technology of SB216763, cerebrovascular disease, applied in the application of compound SB216763 in the preparation of drugs for preventing and/or treating cerebrovascular disease and the field of pharmaceutical compositions, which can solve the problems of reperfusion injury, blood stealing, uncertain curative effect and the like

Inactive Publication Date: 2019-07-05
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the above-mentioned drugs for the treatment of ischemic stroke have the advantages of strong pertinence and clear targets, their curative effect is single, can only provide partial protection, and the clinical curative effect is not good, and it is accompanied by different degrees of toxic and side effects
For example, it is difficult for thrombolytic drugs to enter the damaged brain tissue through the blood-brain barrier and exert their effects, so the curative effect is uncertain, and there are side effects of causing reperfusion injury and bleeding; vasodilators can also dilate blood vessels in normal parts, leading to pathological changes The blood in the area flows to the normal brain tissue, resulting in the so-called "blood stealing" phenomenon

Method used

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  • Application of compound SB216763 to preparing cerebrovascular disease preventing and/or treating drugs and pharmaceutical composition of compound SB216763
  • Application of compound SB216763 to preparing cerebrovascular disease preventing and/or treating drugs and pharmaceutical composition of compound SB216763
  • Application of compound SB216763 to preparing cerebrovascular disease preventing and/or treating drugs and pharmaceutical composition of compound SB216763

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Protective effect of SB216763 on focal ischemic stroke in rats.

[0041]Male SD rats were randomly divided into control group (sham operation group), model group, and SB216763 (Selleck, S1075) administration group (400 pmol), 10 in each group. The rat model of transient middle cerebral artery occlusion (tMCAO) was established by suture method. Before ischemia, 400 pmol SB216763 was injected into the lateral ventricle. The effect of SB216763 on cerebral infarction volume in the acute stage of cerebral ischemia was observed by sectioning after ischemia-reperfusion for 24 hours. Before the rats were sacrificed, the Longa method was used to score the neurological symptoms of the rats after reperfusion (I / R) in the acute stage of cerebral ischemia. The higher the score, the more obvious the neurological deficit. The scoring criteria for neurological symptoms are shown in Table 1.

[0042] Table 1

[0043] score nervous symptoms 0 Normal, no neurological...

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Abstract

The invention provides application of a compound SB216763 to preparing cerebrovascular disease preventing and / or treating drugs and a pharmaceutical composition of the compound SB216763. The compoundSB216763 is 3-(2, 4-dichlorophenyl)-4-(1-methyl-1H-indole-3-yl)-1H-pyrrole-2, 5-diketone with a structural formula shown in the description. Experiments discover that the compound SB216763 can achievesignificant cerebral nerve protecting effects, significantly reduce the volume of acute cerebral infarction of rats with focal cerebral ischemia and improve the nerve symptoms of the rats. The drugsprepared with the compound SB216763 can be applied to preventing or treating diseases such as ischemic brain injury, cerebral thrombosis, cerebral embolism, cerebral infarction, cerebral apoplexy, lacunar infarction, transient cerebral ischemia, cerebral arteriosclerosis and diabetic cerebrovascular complications.

Description

technical field [0001] The present invention relates to the application of compound SB216763 in the preparation of medicines for preventing and / or treating cerebrovascular diseases and its pharmaceutical composition. Background technique [0002] Stroke, also known as cerebral apoplexy or cerebrovascular accident, is a group of diseases whose main clinical manifestations are cerebral tissue ischemia and hemorrhagic injury symptoms. The disease has an acute onset, high disability rate and high mortality rate, and is one of the most important diseases that endanger human health in the world today. Stroke patients are caused by stenosis, occlusion or rupture of intracerebral arteries due to various inducing factors, resulting in acute cerebral blood circulation disorder, clinically manifested as symptoms and signs of transient or permanent brain dysfunction. Stroke is mainly divided into two categories: hemorrhagic stroke (cerebral hemorrhage or subarachnoid hemorrhage) and is...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/404A61P9/10A61P7/02A61P3/10A61P25/00
CPCA61K31/404A61P3/10A61P7/02A61P9/10A61P25/00
Inventor 张慧灵刘金朱永铭
Owner SUZHOU UNIV
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