SOLID FORM, CRYSTALLINE, AND CRYSTALLINE A OF FXR AGONIST AND METHOD FOR THEIR PRODUCTION AND THEIR APPLICATION Russian patent published in 2023 - IPC C07D413/14 A61K31/4709 A61P1/16 

FIELD: pharmaceutics.

SUBSTANCE: crystalline form A of the compound of formula (I), characterized by a powder X-ray pattern with characteristic diffraction peaks at the following angles 2θ: 11.86±0.2°, 12.72±0.2°, 16.15±0.2°, 17.40±0.2°, 19.72±0.2°, 24.18±0.2°, and 25.27±0.2°. The method for obtaining crystalline Form A of the compound of formula (I) according to the invention is carried out by (a) adding a compound of formula (I) to a solvent; (b) stirring at 30-50°C for 40-55 hours and (c) centrifugation and subsequent evaporation of the solvent to obtain crystalline form A of the compound of formula (I); where the solvent is alcohol, tetrahydrofuran, water, acetone, acetonitrile, ethyl acetate, a mixed solvent of alcohol and water, where the volume ratio of alcohol to water is 1:0.6 - 1:1.5, or a mixed solvent of acetone and water, where the volume ratio of acetone to water is 1:1.5 - 1:2.5 and the alcohol is selected from methanol, ethanol, isopropanol and n-propanol. The invention also relates to a process for the preparation of a compound of formula (I) comprising the steps of reacting compounds designated by the structures a, b, c, d, e (given in the claims). The invention also relates to a compound represented by the formula e, where R₁ is CH₃. The crystalline form A of the compound of formula (I) of the invention is used in the manufacture of a medicament for treatment of FXR-associated diseases, where the FXR-associated disease is a non-alcoholic fatty liver disease.

EFFECT: stable, slightly hygroscopic, and less susceptible to light damage, crystalline form A of compound (I).

18 cl, 5 dwg, 9 tbl, 6 ex