ADDITION SALT OF THE S1P1 RECEPTOR AGONIST AND ITS CRYSTALLINE FORM AND PHARMACEUTICAL COMPOSITION BASED ON IT Russian patent published in 2024 - IPC C07D413/10 A61K31/4245 A61P37/06 

Abstract RU 2822288 C2

FIELD: the method of obtaining maleate.

SUBSTANCE: method is carried out by obtaining a suspension or solution of the compound represented by formula A and a suspension or solution of maleic acid in a solvent selected from a group consisting of ethanol, acetone, diethyl ether, water, ethyl acetate, 1,4-dioxane or a mixture thereof, respectively, by mixing a suspension or solution of the compound represented by formula A and maleic acid acids in a molar ratio of 1:1.0-1:2.6 to carry out the reaction; in this case, the reaction is carried out at 10-40°C with stirring, for 10-24 hours. Then the solvent is removed after the reaction is completed; and drying is performed at 10-40°C, for 1-24 hours, and the ratio of the mass of the compound represented by formula A to the volume of the solvent in this method is 4 mg:1 ml - 26 mg:1 ml.

EFFECT: production of 1–{2-fluoro-4-[5-(4-isobutylphenyl)-1,2,4-oxadiazole-3-yl]benzyl}-3-azetidine carboxylic acid maleate, characterized by significantly improved solubility in water and better bioavailability.

4 cl, 12 dwg, 7 tabl, 36 ex

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RU 2 822 288 C2

Authors

Zheng, Wei

Pan, Wubin

Guo, Jiawang

Dates

2024-07-03Published

2018-05-04Filed