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Azilsartan medoxomil compound, preparation method and medicinal composition thereof

A technology for azilsartan medoxomil and a compound, which is applied in the field of new benzimidazole derivatives, can solve problems such as lack of research, and achieve the effects of fewer types of use, easy operation, and benefits for production and storage

Active Publication Date: 2014-03-12
CSPC OUYI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, the patent application only mentions that azilsartan medoxomil can be a solvate, such as a hydrate, etc., but unfortunately, no in-depth research has been carried out on related hydrates

Method used

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  • Azilsartan medoxomil compound, preparation method and medicinal composition thereof
  • Azilsartan medoxomil compound, preparation method and medicinal composition thereof
  • Azilsartan medoxomil compound, preparation method and medicinal composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Embodiment 1: the preparation of azilsartan medoxomil potassium salt:

[0030] Dissolve 56.8g (0.1mol) of azilsartan medoxomil in 400ml of methanol, add 40ml of KCL7.45g (0.1mol) of methanol solution while stirring at room temperature, continue stirring for 60 minutes after the addition, and then put it in an ice bath Stir for another 40 minutes, filter, wash the filter cake with 80ml of methanol, and dry in a circulating air dryer at 55°C for 3h to obtain 58.36g of anhydrous azilsartan medoxomil potassium salt, with a yield of 96.3%.

[0031] Elemental analysis:

[0032] Elemental analysis Actual value% Theoretical value% C 59.34 59.41 H 3.68 3.79 N 9.18 9.24 O 20.98 21.12 K 6.41 6.44

Embodiment 2

[0033] Embodiment 2: the preparation of azilsartan medoxomil compound of the present invention:

[0034] Take 30g of azilsartan medoxomil potassium salt in Example 1, add 500ml of hot water at 80°C to dissolve, cool to 20-30°C and stir for 1 hour, then cool to 10-15°C and stir for 1 hour, and finally cool to 0-5°C , stirred for 10 hours, crystals were precipitated, filtered, and the filter cake was dried at 35°C and 35% relative humidity for 5 hours to obtain 30.51 g of the azilsartan medoxomil compound of the present invention (theoretical yield: 30.89 g), the yield 98.77%.

[0035] Elemental analysis:

[0036] Elemental analysis Actual value% Theoretical value% C 57.64 57.69 H 3.97 4.01 N 8.89 8.97 O 23.15 23.08 K 6.23 6.25

[0037] . The water in the azilsartan medoxomil compound of the present invention measured by the Karl Fischer method is 2.82% (theory: 2.88%); the thermogravimetric analysis result shows that it is the ...

Embodiment 3

[0038] Embodiment 3: the preparation of azilsartan medoxomil compound of the present invention:

[0039] Take 20g of azilsartan medoxomil potassium salt in Example 1, add 300ml of 80°C hot water to dissolve, cool to 20-30°C and stir for 1 hour, then cool to 10-15°C and stir for 1 hour, and finally cool to 0-5°C , stirred for 10 hours, crystals were precipitated, filtered, and the filter cake was dried at 35°C and 35% relative humidity for 5 hours to obtain 19.91 g of the azilsartan medoxomil compound of the present invention (theoretical yield: 20.59 g), the yield 96.69%.

[0040] Elemental analysis:

[0041] Elemental analysis Actual value% Theoretical value% C 57.68 57.69 H 4.12 4.01 N 8.86 8.97 O 23.01 23.08 K 6.19 6.25

[0042] . The water in the azilsartan medoxomil compound of the present invention measured by the Karl Fischer method is 2.85% (theory: 2.88%); the result of thermogravimetric analysis shows that it is the c...

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Abstract

The invention relates to an azilsartan medoxomil compound, a preparation method and a medicinal composition thereof, and belongs to the technical field of medicine. The azilsartan medoxomil compound is (5-methyl-2-oxo-1,3-m-dioxole-4-group) methyl-2-ethoxy-1-{[2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazole-3-group) biphenyl-4-group] methyl}-1H-benzimidazole-7-carboxylate sylvite monohydrate. The invention also relates to the preparation method of the compound and the medicinal composition using the compound as an active substance. Compared with an azilsartan medoxomil sylvite, the compound has the advantages of better stability, suitability for preparing medicinal preparations of various forms and suitability for storage and use.

Description

technical field [0001] The present invention relates to a kind of novel benzimidazole derivatives, specifically relate to (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 2-ethoxy Base-1-{[2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl}-1H-benzene The invention relates to a metal salt of imidazole-7-carboxylate, that is, a hydrate of azilsartan medoxomil metal salt, a preparation method thereof, and a pharmaceutical composition containing the same, belonging to the field of medicine. Background technique [0002] The drug treatment of hypertension began in the 1940s. It has developed from the application of central sedatives and thiocyanate drugs to the present, and has formed a series of drugs including diuretics, β-blockers (β-RB), and calcium antagonists. Antihypertensive drug families mainly include antihypertensive agents (CCB), angiotensin-converting enzyme inhibitors (ACEI), angiotensin II receptor blockers (ARB), peripheral vasodilators, etc. Among them, ARB...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D413/14A61K31/4245A61P9/12A61P5/50
Inventor 张育高志峰韩彩霞刘磊马园园董新明王炫
Owner CSPC OUYI PHARM CO LTD
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