New application of compound of angiotensin II receptor antagonist metabolite and NEP inhibitor

A receptor antagonist, angiotensin technology, applied in the field of drug application, can solve problems such as untargeted drugs, and achieve the effect of good antihypertensive effect

Active Publication Date: 2022-05-10
SHENZHEN SALUBRIS PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is currently no specific targeted drug

Method used

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  • New application of compound of angiotensin II receptor antagonist metabolite and NEP inhibitor
  • New application of compound of angiotensin II receptor antagonist metabolite and NEP inhibitor
  • New application of compound of angiotensin II receptor antagonist metabolite and NEP inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0091] Preparation of AHU377 free acid:

[0092] Add 2.1g of AHU377 calcium salt and 40mL of isopropyl acetate into a 250mL single-necked bottle, add 4.5mL of 2mol / L hydrochloric acid at room temperature and stir to dissolve. Separate the liquid, collect the organic layer, and wash the organic layer twice with 20 mL of water; desolvate under reduced pressure at 35°C to obtain the free acid of AHU377.

Embodiment 2

[0094] Preparation of complex:

[0095]

[0096] At room temperature, add 2.36g of AHU377 free acid, 2g of EXP3174 and 40mL of acetone obtained according to the method in Example 1 into a 250mL three-neck flask, and dissolve; add 1.3 equivalents of calcium hydroxide solid and 1mL of water relative to AHU377 at room temperature, and stir at room temperature 10h, add 40mL of acetone, react for another 8h, filter through a Buchner funnel under nitrogen protection, rinse the solid with acetone to obtain a white solid, dry in vacuum at 35°C for 8h, and dry to obtain 3.5g of solid, the purity of which is 99% by HPLC. %, the molar ratio of EXP3174 and AHU377 in the obtained product is 1:1 through content test calculation.

[0097] The X-ray powder diffraction spectrogram of gained product is as figure 1 As shown, the DSC spectrum is as figure 2 shown.

[0098] By comparing with the XRD patterns of EXP3174 and AHU377 calcium, it is found that there are obvious differences in t...

Embodiment 3

[0111] Preparation of complex:

[0112]

[0113] At room temperature, add 2.36g of AHU377 free acid, 2g of EXP3174 and 40mL of acetone obtained according to the method in Example 1 into a 250mL three-necked flask, and dissolve it; Stir at ℃ for 6 hours, add 40 mL of acetone, react for another 8 hours, filter through a Buchner funnel under nitrogen protection, rinse the solid with acetone to obtain a white solid, dry in vacuum at 50 °C for 8 hours, and dry to obtain 3.1 g of solid, which passed the content test The calculation shows that the molar ratio of EXP3174 and AHU377 in the obtained product is 1:1.

[0114] The DSC spectrogram of gained product is as Figure 5 shown.

[0115] Elemental analysis, found value: C: 58.51%; H: 5.41%; N: 10.25%. Theoretical value (according to (EXP3174·AHU377) 3-·1.5Ca2+·2H2O): C: 58.68%; H: 5.46%; N: 10.41%.

[0116] The TG spectrogram of gained product is as Image 6 As shown, the water content of the obtained product measured by th...

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Abstract

The invention belongs to the technical field of medicine application, and relates to a novel application of a compound of an angiotensin II receptor antagonist metabolite and an NEP inhibitor, in particular to an application of the compound in preparation of a medicine for salt-sensitive hypertension.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical application, and relates to a new application of a compound of an angiotensin II receptor antagonist metabolite and an NEP inhibitor, and specifically relates to the application of the compound in preparing medicine for salt-sensitive hypertension. Background technique [0002] Hypertension is a clinical syndrome mainly manifested by increased systemic arterial pressure, and is the most common cardiovascular disease. Moreover, the incidence of hypertension is on the rise. If high blood pressure is not effectively controlled and treated, it can cause coronary arteriosclerosis, coronary heart disease, angina pectoris, and serious complications such as hypertensive heart disease and heart failure. In addition, long-term high blood pressure can lead to kidney, brain, cardiovascular and other organ damage. [0003] Due to the various etiology and pathogenesis of hypertension, poor blood pressu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4178A61K31/216A61P9/12
CPCA61K31/4178A61K31/216A61K9/0053A61P9/12A61K31/41A61P9/04C07D403/10
Inventor 孙晶超景小龙肖瑛
Owner SHENZHEN SALUBRIS PHARMA CO LTD
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