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Use of 4,7-dihydrotetrazyl[1,5-alpha]pyrimidine compound and its derivatives in preparation of drug for prevention or treatment on cerebral hemorrhage

A technology of dihydrotetrazole and compound, applied in the field of compound, can solve problems such as limited

Inactive Publication Date: 2013-07-10
深圳瀜新生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, although several ROCK inhibitors have entered phase I or II clinical research (such as BA-210), there is only one ROCK inhibitor that has been successfully marketed, that is, Fasudil, which is mainly used for pulmonary artery disease. High blood pressure, and only in the Japanese market

Method used

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  • Use of 4,7-dihydrotetrazyl[1,5-alpha]pyrimidine compound and its derivatives in preparation of drug for prevention or treatment on cerebral hemorrhage
  • Use of 4,7-dihydrotetrazyl[1,5-alpha]pyrimidine compound and its derivatives in preparation of drug for prevention or treatment on cerebral hemorrhage
  • Use of 4,7-dihydrotetrazyl[1,5-alpha]pyrimidine compound and its derivatives in preparation of drug for prevention or treatment on cerebral hemorrhage

Examples

Experimental program
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Embodiment Construction

[0042] The present invention will be further described below in conjunction with experiments and experimental data.

[0043] The 4,7-dihydrotetrazol[1,5-α]pyrimidine compounds and their derivatives used in the following examples were all purchased from Chembridge Company (San Diego, USA).

[0044] In the following ROCK1 enzyme inhibitory activity experiments, zebrafish cerebral hemorrhage drug efficacy evaluation experiments, and mouse acute toxicity experiments, the compound with curative effect used is 7-(4-hydroxy-3-methoxyphenyl)-5- Methyl-6-carboxylate benzyl-4,7-dihydrotetrazole (1,5-α) pyrimidine, its structural formula is:

[0045]

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Abstract

The invention discloses a use of 4,7-dihydrotetrazyl[1,5-alpha]pyrimidine compound and its derivatives in preparation of a drug for prevention or treatment on cerebral hemorrhage. Through a self-created computer-assisted drug molecule design program and virtual screening, it is shown that the 4,7-dihydrotetrazyl[1,5-alpha]pyrimidine compound and its derivatives have a ROCK1 protein inhibitory activity and can be used for treating cerebral hemorrhage. Through further biological activity detection of the screened 4,7-dihydrotetrazyl[1,5-alpha]pyrimidine compound, it is shown that the screened 4,7-dihydrotetrazyl[1,5-alpha]pyrimidine compound has an obvious ROCK1 protein inhibitory activity and has good prevention and treatment effects in an atorvastatin-induced zebra fish cerebral hemorrhage model.

Description

technical field [0001] The novel application of a class of compounds of the present invention particularly relates to the application of 4,7-dihydrotetrazol[1,5-α]pyrimidine compounds and their derivatives in the preparation of drugs for treating cerebral hemorrhage. Background technique [0002] Cerebral hemorrhage refers to non-traumatic intraparenchymal hemorrhage, which can be caused by many reasons. Clinically, arteriole hemorrhage in the internal capsule area is the most common. Hemorrhagic hematoma (or blood clot) can split and compress nearby brain tissue, destroy or affect their normal functions (movement, sensation, memory, language, mental activity, etc.), resulting in symptoms such as hemiplegia, numbness of the side of the body, and slurred speech; bleeding When the amount is large, it can cause increased intracranial pressure, brain tissue displacement and even brain herniation. The disability rate and mortality rate are high, and it is one of the main diseas...

Claims

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Application Information

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IPC IPC(8): C07D487/04A61K31/519A61P9/10A61P7/04
Inventor 余慧东侯廷军沈明云潘培辰李铭源黎晌
Owner 深圳瀜新生物科技有限公司