Novel use of complexes of metabolites of angiotensin II receptor antagonists with nep inhibitors

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: 2022-03-11
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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  • Novel use of complexes of metabolites of angiotensin II receptor antagonists with nep inhibitors
  • Novel use of complexes of metabolites of angiotensin II receptor antagonists with nep inhibitors
  • Novel use of complexes of metabolites of angiotensin II receptor antagonists with nep inhibitors

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, EXP31742g and 40mL of acetone obtained according to the method of 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 for 10h , add 40mL of acetone, and 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, dry to obtain 3.5g of solid, and the purity of HPLC is 99% , 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 the XRD...

Embodiment 3

[0111] Preparation of complex:

[0112]

[0113] At room temperature, add 2.36g of AHU377 free acid, EXP31742g and 40mL of acetone obtained according to the method of Example 1 into a 250mL three-necked flask, and dissolve it; Stir for 6 hours, add 40 mL of acetone, and react for another 8 hours. Under nitrogen protection, filter through a Buchner funnel, 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 the solid, which is calculated by the content test It can be seen 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 Figure 6 As shown, the water content of the obtained product measured by ...

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Abstract

The invention relates to a new application of a compound of an angiotensin II receptor antagonist metabolite and an NEP inhibitor, which belongs to the technical field of pharmaceutical application, and specifically relates to the application of the compound in the preparation of medicines 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. According to statistics, there are about 290 million people with cardiovascular disease in China ("China Cardiovascular Disease Report 2013"). 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 ...

Claims

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Application Information

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IPC IPC(8): C07D403/10A61K31/216A61K31/41A61K31/4178A61P9/12A61P9/04
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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