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Angiotensin receptor antagonist and milrinone compound and use thereof

A technology of receptor antagonists and angiotensin, which is applied in the fields of cardiovascular system diseases, active ingredients of heterocyclic compounds, medical preparations containing active ingredients, etc., can solve the problem that the crystal structure of the compound is not determined and the property of the compound is unstable , no antihypertensive and other problems, to achieve the effect of providing pharmacokinetic properties, stable properties, and significant therapeutic effects

Active Publication Date: 2016-12-21
赛隆药业集团股份有限公司(长沙)医药研发中心
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] However, there are currently no clinically effective drugs for the treatment of heart failure and hypertension, and most drugs have unavoidable side effects while relieving symptoms of heart failure and hypertension
And the order of a single drug is prone to tolerance. In order to treat heart failure and hypertension more effectively, some compounds have been developed in the prior art, such as the drug compound containing valsartan disclosed in CN1816533, which contains valsartan Tan and positive inotropes, the drug complex is mainly used for the treatment of heart failure, but the valsartan and positive inotropes disclosed in the prior art do not have antihypertensive effect, and valsartan and positive inotropes consist of The complex has no definite crystal structure, resulting in unstable properties of the complex composed of valsartan and positive inotropic drugs

Method used

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  • Angiotensin receptor antagonist and milrinone compound and use thereof
  • Angiotensin receptor antagonist and milrinone compound and use thereof
  • Angiotensin receptor antagonist and milrinone compound and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Embodiment 1 A compound of angiotensin receptor antagonist and milrinone

[0036] The complex includes 1 mol of telmisartan and 1 mol of milrinone.

Embodiment 2

[0037] Embodiment 2 A compound of angiotensin receptor antagonist and milrinone

[0038] The complex includes 1 mol of irbesartan and 1 mol of milrinone.

Embodiment 3

[0039] Embodiment 3 A compound of angiotensin receptor antagonist and milrinone

[0040] The complex includes 1 mol of valsartan and 1 mol of milrinone.

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Abstract

The invention provides an angiotensin receptor antagonist and milrinone compound and a use thereof. The compound comprises an angiotensin receptor antagonist and milrinone, the angiotensin receptor antagonist and milrinone can be directly mixed, or can be indirectly connected through hydrogen bonds, and cocrystallized sodium hydrate formed by using the hydrogen bonds have stable properties and substantially improved pharmacokinetic properties. The action mechanisms of the angiotensin receptor antagonist and milrinone are different, but the compound formed by the angiotensin receptor antagonist and milrinone have unexpected synergism, so the compound has positive application prospect in the anti-heart failure and anti-hypertension field.

Description

technical field [0001] The invention belongs to the field of drugs for treating diseases of the cardiovascular system, in particular to a compound of angiotensin receptor antagonist and milrinone and its application. Background technique [0002] Heart failure (referred to as heart failure) is a complex clinical symptom group, which is a severe stage of various heart diseases. Its incidence rate is high, and its 5-year survival rate is similar to that of malignant tumors. The incidence of heart failure will continue to increase in the near future, and it is becoming the most important cardiovascular disease in the 21st century. [0003] According to foreign statistics, the prevalence of heart failure in the population is about 1.5% to 2.0%, and it can reach 6% to 10% for those over 65 years old. In the past 40 years, the death rate caused by heart failure has increased by 6 times. Heart failure is the initial myocardial injury due to any cause (such as myocardial infarction...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/06A61K31/444A61K9/48A61P3/06A61P9/12A61P9/04A61K31/4184A61K31/41A61K31/4178
CPCA61K9/1652A61K31/41A61K31/4178A61K31/4184A61K31/444A61K45/06A61K2300/00
Inventor 李剑峰周文吴彪
Owner 赛隆药业集团股份有限公司(长沙)医药研发中心
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