Crystalline ARB-NEPi dicationic compound and preparation method and application thereof

A dual-cation, crystalline technology, applied in organic chemical methods, active ingredients of heterocyclic compounds, drug combinations, etc., can solve problems such as increasing the risk of cardiovascular burden
CN105503760AInactive Publication Date: 2016-04-20SHANGHAI HANSOH BIOMEDICAL +1
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Patent Information

Authority / Receiving Office
CN Β· China
Patent Type
Applications(China)
Current Assignee / Owner
SHANGHAI HANSOH BIOMEDICAL
Publication Date
2016-04-20
Estimated Expiration
Not applicable Β· inactive patent

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Abstract

The present invention discloses a crystalline ARB-NEPi dicationic compound and a preparation method and application thereof. In particular, the present invention relates to the crystalline ARB-NEPi dicationic compound having the formula of NEPi.Nax.Ky.ARB.ZH2O. The present invention also relates to a pharmaceutical composition containing an effective amount of the crystalline dicationic compound and application of the pharmaceutical composition in the preparation of drugs for treatment or prevention of neutral-endopeptidase-related diseases, cardiovascular diseases, hypertension, acute and chronic heart failures, congestive heart failure, left ventricular dysfunction, hypertrophic cardiomyopathy, diabetic cardiomyopathy, supraventricular arrhythmia and ventricular arrhythmia, atrial fibrillation, atrial flutter or detrimental vascular remodeling, and the like, and the pharmaceutical composition has broad application prospects.
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Description

technical field

[0001] The invention belongs to the technical field of medicines, and in particular relates to a crystalline ARB-NEPi dication complex with dual functions and a preparation method and application thereof. Background technique

[0002] Neutral endopeptidase (EC 3.4.24.11; neprilysin; neprilysin; NEP) is a zinc-containing metalloprotease that cleaves various peptide substrates at the amino terminus of aromatic amino acids. Substrates for this enzyme include, but are not limited to, atrial natriuretic peptide (ANF, also known as ANP), brain natriuretic peptide (BNP), met and leu enkephalins, bradykinin, neurokinin A and substance P.

[0003] ANF ​​is a family of vasodilatory, diuretic and antihypertensive peptides, and one form, ANF99-126, is a circulating peptide hormone released by the heart during cardiac dilation. The function of ANF is to maintain salt and water homeostasis and to regulate blood pressure. ANF ​​is rapidly inactivated in circulation by at ...

Claims

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