Compound of angiotensin receptor inhibitor and enkephalinase inhibitor and usage thereof

Abstract

The invention provides a compound of an angiotensin receptor inhibitor and an enkephalinase inhibitor and a usage thereof. The compound is formed by the angiotensin receptor inhibitor and the enkephalinase inhibitor. The compound can be directly blended, or indirectly connected by a hydrogen bond, and cocrystallization sodium hydrate formed by the hydrogen bond connection is more stable in property, and the pharmacokinetics property is remarkably improved. Although the action mechanisms of the angiotensin receptor inhibitor and the enkephalinase inhibitor are different, the compound formed bythe both parties has an unexpected synergistic effect, and has the positive application prospect in the field of anti-heart-failure and anti-hypertension treatments.

Description

[0001] This application is a divisional application of a Chinese patent application with the application number 201610627302.0, the application date is August 1, 2016, and the invention title is "composite and use of angiotensin receptor antagonist and neprilysin inhibitor" . technical field [0002] The invention belongs to the field of drugs for treating diseases of the cardiovascular system, in particular to a compound of an angiotensin receptor antagonist and a neprilysin inhibitor and its application. Background technique [0003] 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. [0004] According to foreign statistics, the prevalence ...

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Problems solved by technology

[0010] 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 an angiotensin receptor antagonist and NEP inhibitor disclosed in CN101098689 The drug combination product, which consists of valsartan and (2R,4S)-5-biphenyl-4-yl-5-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester ( sacubitril), this combination product was listed in the United States and Europe in 2015, and is clinically used for the treatment of chronic heart failure; but the prior art has not yet disclosed the complex composed of angiotensin receptor antagonist and cansatril , and did not disclose whether the complex has the effect of anti-heart failure and hypertension. In addition, the complex composed of angiotensin receptor antagonist and canzatril has no definite crystal structure, resulting in unstable properties of the complex. low bioavailability

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