COMPOUND OF FGFR INHIBITOR IN SOLID FORM AND METHOD OF ITS PREPARATION Russian patent published in 2023 - IPC C07D487/04 C07D495/00 A61K31/53 A61P35/00 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to the compound represented by formula (I) in solid form, which represents crystalline Form A of the compound represented by formula (I) with diffraction peaks at an angle of 2θ 6.37± 0.2°, 9.90± 0.2°, 12.74± 0.2°, 13.35± 0.2°, 14.26± 0.2°, 16.31± 0.2°, 19.07± 0.2° and 21.83± 0.2° in a powder X-ray diffraction pattern or represents the crystalline form B of the compound represented by formula (I), which has diffraction peaks at an angle of 2θ 9.14± 0.2°, 11.05± 0.2°, 13.25± 0.2°, 15.07± 0.2°, 16.47± 0.2°, 18.31± 0.2° and 22.29± 0.2° on a powder X-ray diffraction pattern. The invention relates to a method of obtaining crystalline form A of the compound represented by formula (I), comprising (a) adding the compound represented by formula (I) to acetonitrile; (b) stirring at a temperature of 30–50°C for 40–55 hours and (c) separating crystalline form A of the compound represented by formula (I). The invention relates to a method of producing crystalline form B of a compound represented by formula (I), comprising (a) adding crystalline form A of a compound represented by formula (I) to ethanol; (b) stirring at a temperature of 30–50°C for 5–30 hours; (c) standing at a temperature of 10–20°C for 3–10 hours and (d) separating crystalline form B of the compound represented by formula (I). The invention also relates to the use of a compound represented by formula (I) in solid form, which is crystalline form A or crystalline form B, for the production of a medicinal product for treating a disease associated with FGFR.

EFFECT: compound of formula (I) exhibited good inhibitory ability against wild-type FGFR, and the crystalline form B of the compound of formula (I) does not exhibit hygroscopicity and shows good prospects for the manufacture of medicinal products.

15 cl, 7 dwg, 7 tbl, 4 ex