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Compound of angiotensin receptor blocker and levosimendan and use of compound

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 improving stability

Active Publication Date: 2016-12-14
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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  • Compound of angiotensin receptor blocker and levosimendan and use of compound
  • Compound of angiotensin receptor blocker and levosimendan and use of compound
  • Compound of angiotensin receptor blocker and levosimendan and use of compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1 A complex of angiotensin receptor antagonist and levosimendan

[0035] The complex includes 1 mol of valsartan and 1 mol of levosimendan.

Embodiment 2

[0036] Example 2 A complex of angiotensin receptor antagonist and levosimendan

[0037] The complex includes 1 mol of Olmesartan and 1 mol of Levosimendan.

Embodiment 3

[0038] Example 3 A complex of angiotensin receptor antagonist and levosimendan

[0039] The complex includes 1 mol of Telmisartan and 2 mol of Levosimendan.

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PUM

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Abstract

The invention provides a compound of an angiotensin receptor blocker and levosimendan and use of the compound. The compound is composed of the angiotensin receptor blocker and levosimendan, which can be mixed directly or be connected indirectly through a hydrogen bond, wherein a co-crystallized sodium hydrate formed by connection through hydrogen bond is more stable in property; and the pharmacokinetic properties are improved significantly; the action mechanisms of the angiotensin receptor blocker and the levosimendan are different, but the formed compound has an unexpected synergistic effect and has positive application prospects in the anti-heart failure and anti-hypertensive treatment field.

Description

Technical field [0001] The invention belongs to the field of medicines for treating cardiovascular diseases, and particularly relates to a complex of an angiotensin receptor antagonist and levosimendan and its use. Background technique [0002] Heart failure (abbreviated as heart failure) is a complex group of clinical symptoms, which is a severe stage of various heart diseases, with a high incidence rate and a 5-year survival rate similar to that of malignant tumors. The incidence of heart failure in the near future will continue to increase, and it is becoming the most important cardiovascular disease in the 21st century. [0003] According to foreign statistics, the prevalence of central failure in the population is about 1.5% to 2.0%, and it can reach 6% to 10% for people over 65. In the past 40 years, deaths caused by heart failure have increased by 6 times. Heart failure is due to any initial myocardial damage (such as myocardial infarction, cardiomyopathy, hemodynamic overl...

Claims

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Application Information

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IPC IPC(8): A61K31/50A61K31/41A61K31/4178A61K31/4184A61K31/519A61P9/00A61P9/12A61P3/06
CPCA61K31/41A61K31/4178A61K31/4184A61K31/50A61K31/519A61K2300/00
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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