DIARYLTHIOHYDANTOIN COMPOUND CRYSTAL Russian patent published in 2023 - IPC C07D471/04 A61K31/4184 A61P35/00 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a crystal of a diarylthiohydantoin compound of formula I, where the X-ray powder diffraction pattern using Cu Kα radiation diffraction peaks are located at the following values of angle 2θ: 13.47±0.2°, 15.32±0.2°, 15.98±0.2°, 18.68±0.2°, 23.11±0.2° and 26.41±0.2°. A crystal of the compound of formula I has an absorption peak at 238.92°C as analyzed by differential scanning calorimetry. The method of obtaining a crystal of a compound of formula I is performed by mixing a compound of formula I with a solvent at a temperature of 35–70°C for crystal precipitation, wherein the solvent is selected from the group consisting of methanol, ethanol, ethyl acetate, tetrahydrofuran, acetonitrile, acetone, a mixture of methanol and water, a mixture of ethanol and water, and a mixture of acetone and water. The invention relates to a pharmaceutical composition for the treatment of androgen-mediated cancer containing a therapeutically effective amount of a crystal of a compound of formula I according to the invention and a pharmaceutically acceptable excipient. The invention also relates to a method of treating androgen-mediated cancer in mammals, comprising administering to a mammal, preferably a human, in need of such treatment, a therapeutically effective amount of a crystal of a compound of Formula I or a pharmaceutical composition of the invention. A crystal of a compound of Formula I or a pharmaceutical composition of the invention is used for the treatment of androgen-mediated cancer.

EFFECT: crystal of a diarylthiohydantoin compound for the treatment of androgen-mediated cancer, which is stable and low hygroscopic.

15 cl, 4 dwg, 6 tbl, 8 ex