CRYSTAL FORM OF 1,4-BIS[1,2-BENZISOSELENAZOL-3(2H)-OH]-BUTANE, METHOD OF ITS PREPARATION AND USE Russian patent published in 2023 - IPC C07D293/12 A61K31/41 A61K9/00 A61K39/29 A61P1/16 A61P35/00 A61P17/16 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a method of obtaining a crystalline form I of 1,4-bis[1,2-benzisoselenazol-3(2H)-one]-butane, which has characteristic peaks at angles 2θ making 6.15 ± 0.20°, 12.28 ± 0.20°, 18.44 ± 0.20°, 19.09 ± 0.20°, 21.89 ± 0.20°, 22.20 ± 0.20°, 23.68 ± 0.20°, 25.92 ± 0.20°, 27.50 ± 0.20°, 30.95 ± 0.20°, 32.45 ± 0.20°, 35.79 ± 0.20°, 37.37 ± 0.20° and 37.72 ± 0.20°, using X-ray powder diffraction with Cu-Kα radiation α. The method involves dissolving 1,4-bis[1,2-benzisoselenazol-3(2H)-one]-butane in solvent S1 and adding antisolvent S2 to obtain crystalline form I. Solvent S1 is selected from DMSO and a mixture consisting of DMSO and 1–10% acetone or tetrahydrofuran (v/v); solvent S2 is selected from water, acetonitrile, MTBE, isopropyl acetate, methanol and ethyl acetate. Moreover, when the solvent S1 is DMSO, the solvent S2 is not ethyl acetate; the volume ratio of solvent S1 to solvent S2 is 1:0.5–1:2; and the method is performed at a temperature of 30–70°C.

EFFECT: obtaining of crystalline form I of 1,4-bis[1,2-benzisoselenazol-3(2H)-one]-butane with good stability, low toxicity and inhibitory activity against liver cancer associated with HBV.

3 cl, 10 dwg, 1 tbl, 9 ex