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Compound containing benzomorpholone-biphenyl skeleton and its preparation method and application

A technology of benzomorpholone and skeleton compound, which is applied in the field of medicinal chemistry, can solve the problems of low selectivity and lack of oral activity, and achieve the effects of simple synthesis method, vasodilation and high yield

Active Publication Date: 2022-05-31
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In 1971, the first angiotensin Ⅱ polypeptide analog, saraxin, was discovered, which can competitively inhibit AT 1 receptor, but low selectivity and lack of oral activity prompted the development of non-peptide angiotensin II type 1 receptor blockers

Method used

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  • Compound containing benzomorpholone-biphenyl skeleton and its preparation method and application
  • Compound containing benzomorpholone-biphenyl skeleton and its preparation method and application
  • Compound containing benzomorpholone-biphenyl skeleton and its preparation method and application

Examples

Experimental program
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Embodiment 1

Embodiment 2

[0046] Intermediate 4-1 is prepared in the same manner.

Embodiment 3

[0050] Intermediate 2 was prepared in the same manner.

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Abstract

The invention belongs to the field of medicinal chemistry and discloses a compound with a benzomorpholone-biphenyl skeleton, a preparation method and an application thereof. It has the following general structural formula: Ⅰ The preparation method of this type of compound is simple and reliable, and the total yield is over 40%. Preliminary pharmacological experiments show that these compounds have a certain relaxation effect on isolated rat arteries, and can inhibit the proliferation of mouse embryonic fibroblasts (NIH‑3T3) and the expression of type I collagen to a certain extent, and can be used for Development of antihypertensive drugs and anti-myocardial fibrosis drugs.

Description

Compound containing benzomorpholinone-biphenyl skeleton and preparation method and application thereof technical field The present invention relates to the field of medicinal chemistry, be specifically related to a class of compounds containing benzomorpholinone-biphenyl skeleton, preparation The method and its application as an active ingredient of blood pressure lowering and anti-myocardial fibrosis drugs. technical background [0002] Angiotensin II type 1 receptor blockers (ARBs) have been used clinically for several years to control cardiovascular disease. Widely used in the drug treatment of hypertension and anti-fibrosis. Compared with other antihypertensive drugs, the efficacy of ARBs in antihypertensive Better and safer, with high efficacy, high specificity, fewer side effects, high compliance, and protective effects on multiple organs pharmacological properties used. In terms of anti-myocardial fibrosis (MF), ARBs can effectively reverse hypertensive cardia...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D265/36C07D413/10C07D413/14C07D413/12A61P9/12A61P9/00A61P9/08
CPCC07D265/36C07D413/10C07D413/14C07D413/12A61P9/12A61P9/00A61P9/08
Inventor 施秀芳安义平李秀君张振中于震强陈海歌朱超然郭璇
Owner ZHENGZHOU UNIV
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