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Benzimidazole derivative with cardiovascular activity and preparing method and application thereof

A compound and medicinal salt technology, applied in the fields of benzimidazole derivatives with cardiovascular activity, their preparation and application, can solve the problem that the condition has not been significantly improved

Inactive Publication Date: 2010-09-22
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, one-third of hypertensive patients have not been significantly improved after taking medication, and the development of antihypertensive drugs will still be a hot spot of concern

Method used

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  • Benzimidazole derivative with cardiovascular activity and preparing method and application thereof
  • Benzimidazole derivative with cardiovascular activity and preparing method and application thereof
  • Benzimidazole derivative with cardiovascular activity and preparing method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] 1H-benzimidazole

[0057] Mix o-phenylenediamine (1) (5.40g, 0.05mol) and formic acid (2.64g, 0.06mol), add 4mol / L hydrochloric acid (60ml) to reflux for 2h, add ammonia water to adjust pH to alkaline, filter, wash with water, 95% Recrystallized from ethanol to obtain 2.65 g of white solid, yield: 45.0%, m.p.172-173°C. (Document: mp: 172-173℃)

Embodiment 2

[0059] 2-Methyl-1H-benzimidazole

[0060] Referring to the preparation method of 1H-benzimidazole, white crystals were obtained, yield: 53.7%, m.p.176-178°C. (Document: m.p.177-177.5℃)

Embodiment 3

[0062] 2-Ethyl-1H-benzimidazole

[0063] Referring to the preparation method of 1H-benzimidazole, white crystals were obtained, yield: 48.7%, m.p.173-175°C. (Document: m.p.174.5℃)

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Abstract

The invention discloses benzimidazole derivative, belonging to the field of the medicinal chemistry. The invention also discloses a preparation method of the benzimidazole derivative, the medicinal composition containing the compound of benzimidazole derivative and the application of the compound of benzimidazole derivative to the treatment of hypertension and congestive heart failure and the treatment of other diseases through doubly blocking angiotensin II (AT1) receptor and endothelin (ETA) receptors.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a class of benzimidazole derivatives. The invention also discloses a preparation method of these benzimidazole derivatives, a pharmaceutical composition containing the compound and the use of the compound in the treatment of hypertension , congestive heart failure, and through dual blockade of angiotensin II (AT 1 ) receptors and endothelin (ET A ) receptors to treat other diseases or conditions. Background technique [0002] Hypertension is a common disease that seriously endangers human health in the 21st century, and it is also the cause of many other cardiovascular and cerebrovascular diseases. At present, one-third of hypertensive patients have not been significantly improved after taking medication, and the research and development of antihypertensive drugs will still be a hot spot of concern. [0003] The renin-angiotensin system (RAS) plays an important role in blood...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D413/12A61K31/422A61P9/12A61P9/04A61P9/00A61P43/00
Inventor 徐进宜吴晓明杨治华魏臻王秋娟朱培清许晓乐
Owner CHINA PHARM UNIV
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