COMPOUND OF BRD4 INHIBITOR IN SOLID FORM, METHOD FOR ITS PRODUCTION AND APPLICATION Russian patent published in 2023 - IPC C07D495/14 C07D243/06 A61K31/55 A61K45/00 A61P35/00 A61P43/00 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a compound of formula (I) wherein the compound is in crystalline form, wherein the crystalline form of the compound of formula (I) is crystalline form A or crystalline form B. Crystalline form A has an X-ray powder diffraction pattern having characteristic X-ray diffraction peaks at the following angles 2θ: 7.03±0.2°, 11.28±0.2°, 14.00±0.2°, 15.11±0.2°, 17.31±0.2°, 19.48±0.2°, 20.07±0.2°, 22.86±0.2°. Crystal Form B has an X-ray powder diffraction pattern with the characteristic X-ray diffraction peaks at the following angles 2θ: 5.50±0.2°, 8.36±0.2°, 11.87±0.2°, 12.39±0.2°, 12.66±0.2°, 15.11±0.2°, 17.35±0.2°, 18.70±0.2°. A process for preparing a compound of formula (I) in crystalline form A comprises (1) adding a compound of formula (I) to a solvent to form a suspension or solution; where the solvent is selected from the group consisting of methyl tert-butyl ether, ethyl acetate, acetonitrile, ethanol, acetone, methanol, methyl ethyl ketone, a mixed solvent of acetone-water with a volume ratio of 2:1 and a mixed solvent of ethanol-water with a ratio of volumes of 3:1; (2) mixing the suspension or solution in a thermomixer while maintaining a constant temperature at 25–45°C followed by centrifugation and drying to obtain crystalline form A of the compound of formula (I). A process for preparing a compound of formula (I) in crystalline form B comprises (1) adding a compound of formula (I) to tetrahydrofuran to form a suspension or solution; (2) mixing the suspension or solution in a thermomixer while maintaining a constant temperature at 25–45°C followed by centrifugation and drying to obtain crystalline form B of the compound of formula (I).

EFFECT: compound of formula (I) in crystalline form for the treatment of diseases associated with BRD4.

13 cl, 5 dwg, 10 tbl, 9 ex