SULFONAMIDE COMPOUNDS AND THEIR USE Russian patent published in 2022 - IPC C07D271/113 C07D413/12 A61K31/4245 A61P35/00 

FIELD: biotechnology.

SUBSTANCE: invention relates to a cocrystal of benzoic acid and 5-chloro-2-(N-((1S,2R)-2-(6-fluoro-2,3-dimethylphenyl)-1-(5-oxo-4,5-dihydro-1,3,4-oxadiazole-2-yl)propyl)sulfamoyl)benzamide, where the powder X-ray diffractogram of the cocrystal contains five or more peaks at (2θ ± 0.2°) 6.8°, 7.8°, 11.2°, 13.4°, 13.7°, 16.0°, 17.1°, 17.8°, and 23.2°. The invention also relates to a pharmaceutical composition having inhibitory activity against ribonucleotide reductase, containing (i) a cocrystal of benzoic acid and 5-chloro-2-(N-((1S,2R)-2-(6-fluoro-2,3-dimethylphenyl)-1-(5-oxo-4,5-dihydro-1,3,4-oxadiazole-2-yl)propyl)sulfamoyl)benzamide, and (ii) a pharmaceutically acceptable carrier. The invention relates to a method for inhibition of ribonucleotide reductase in vivo, including the administration of therapeutically effective amount of a pharmaceutical composition according to the invention to a human subject who needs it. A cocrystal of benzoic acid and 5-chloro-2-(N-((1S,2R)-2-(6-fluoro-2,3-dimethylphenyl)-1-(5-oxo-4,5-dihydro-1,3,4-oxadiazole-2-yl)propyl)sulfamoyl)benzamide is used for the production of a ribonucleotide reductase inhibitor as a drug for inhibition of activity against ribonucleotide reductase.

EFFECT: cocrystal of benzoic acid and 5-chloro-2-(N-((1S,2R)-2-(6-fluoro-2,3-dimethylphenyl)-1-(5-oxo-4,5-dihydro-1,3,4-oxadiazole-2-yl)propyl)sulfamoyl)benzamide, which has properties of stability, lower electrostatic character, which is a powerful and selective inhibitor of ribonucleotide reductase.

18 cl, 20 tbl, 12 dwg, 10 ex