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Preventive or therapeutic agent for cerebral ischemic injury or cerebral ischemia reperfusion in stroke

A technology for cerebral ischemia-reperfusion and cerebral ischemia, which is applied in the field of prevention or treatment of cerebral ischemia or cerebral ischemia-reperfusion injury in stroke, and can solve the problems of lack of pharmacological effects on blood coagulation system and circulatory system, etc.

Inactive Publication Date: 2009-03-18
SANWAKAGUKU KENKYUSHO CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, Japanese Patent Application No. 4-173791 describes the application of circulatory system diseases, but as reported in the published technical report 2006-500058, fidarestat has no pharmacological effects on the blood coagulation system and circulatory system
That is, there is no report on the use of fidarestat as a preventive or therapeutic agent for cerebral ischemic injury or cerebral ischemia-reperfusion injury

Method used

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  • Preventive or therapeutic agent for cerebral ischemic injury or cerebral ischemia reperfusion in stroke
  • Preventive or therapeutic agent for cerebral ischemic injury or cerebral ischemia reperfusion in stroke
  • Preventive or therapeutic agent for cerebral ischemic injury or cerebral ischemia reperfusion in stroke

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0033] 1. Test method

[0034] As an evaluation system, a mouse model of acute cerebral infarction, that is, a mouse model of middle cerebral artery occlusion was used. The experiment consisted of the following three experiments: Experiment 1 (control group and fidarestat administration group) to evaluate the therapeutic effect of fidarestat, experiment 2 (control group and fidarestat administration group) to evaluate the preventive effect of fidarestat He-administered group) and Experiment 3 (wild-type mouse group and AR gene-deficient mouse group) to evaluate the effect of AR.

[0035] Using mice (C57BL / 6J strain, body weight 22-28 g) under gas anesthesia, the right middle cerebral artery occlusion (MCAO) was performed by suture method for 2 hours. Thereafter the anesthesia was released and the mice were placed in an intensive care system (ThermoCare Inc) for 4-6 hours at 32°C. Neurological symptoms, cerebral infarction size and cerebral infarction volume were used as eval...

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PUM

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Abstract

The present invention provides a preventive or therapeutic agent for cerebral ischemic injury or cerebral ischemic reperfusion injury in stroke such as cerebral infarction and cerebral hemorrhage which exerts its effect through a different mechanism from that of conventional therapeutic agents and can be taken for a long period. The present invention is a preventive or therapeutic agent for cerebral ischemic injury or cerebral ischemic reperfusion injury in stroke which contains 6-fluoro-2',5'-dioxospiro[chroman-4,4'-imidazolidine]-2-carboxamide as an active ingredient. A particularly preferable compound is an optically resolved (2S,4S)-form of fidarestat.

Description

technical field [0001] The present invention relates to a new pharmaceutical application of 6-fluoro-2', 5'-dioxospiro[chroman-4,4'-imidazoline]-2-carboxamide. Background technique [0002] It is estimated that the number of patients in the acute stage of cerebral infarction is about 370,000, and the number of patients will further increase due to the increase of patients with hypertension, arteriosclerosis, and diabetes. In the treatment of strokes such as cerebral infarction and cerebral hemorrhage, it is important to suppress brain damage in the acute stage that is closely related to sequelae. Important factors defining tissue prognosis in the acute phase of cerebral ischemia are residual blood flow and ischemic time. Brain injury is caused by metabolic disturbance caused by interruption of cerebral blood flow. When the ischemia time exceeds a certain limit, changes occur in vascular endothelial cells, and the blood-brain barrier is destroyed, so that plasma components f...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4188A61P7/02A61P9/10C07D491/107
CPCA61K31/4188C07D491/107A61P7/02A61P9/00A61P9/10
Inventor 钟金淑子钟森文日比千寻
Owner SANWAKAGUKU KENKYUSHO CO LTD
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