AZILSARTAN ORGANIC AMINE SALTS, METHOD FOR THEIR PRODUCTION AND USE Russian patent published in 2016 - IPC C07D413/10 A61K31/4245 A61P9/12 

FIELD: pharmaceutics.

SUBSTANCE: invention relates to azilsartan organic amine salts, where the ratio of azilsartan to organic amin is 2:1, and an organic amine is represented by ethanolamine or choline. Azilsartan organic amine salt exists in the form of complex and is represented by formulae (I) and (III), where M^⊕ is a choline cation or cation formed by ethanolamine and H⁺. Invention also relates to methods of azilsartan organic amine salts producing. Azilsartan organic amine salt of formula (I) is obtained by adding azilsartan acid and organic amine to alcoholic solvent in specific order to obtain the respective salts at room temperature or under heating, wherein mentioned reaction is carried out in water-free conditions and the molar ratio of azilsartan acid to organic amin is 2:1. Azilsartan organic amine salt of formula (III) is obtained by adding azilsartan acid and alcohol solution of choline in alcohol solvent, wherein this mentioned alcohol solution of choline is a solution of choline in methanol with concentration of 45 % and the molar ratio of azilsartan to choline is 1:1-2:1. Azilsartan organic amine salts are intended for preparation of a pharmaceutical composition or a medicament for hypertension treatment.

EFFECT: azilsartan organic amine salt with an organic amine possessing good pharmacokinetic properties high bioavailability, low drug toxicity.

9 cl, 4 dwg, 1 tbl, 11 ex