NOVEL CRYSTALLINE FORM OF [(2R,3S,4R,5R)-3,4-DIHYDROXY-5-[4-(HYDROXYAMINO)-2-OXOPYRIMIDIN-1-YL]OXOLAN-2-YL]METHYL-2-METHYLPROPANOATE Russian patent published in 2025 - IPC C07H19/67 C07D487/04 A61K31/7068 A61P31/16 

FIELD: chemistry.

SUBSTANCE: invention relates to a crystalline form [(2R,3S,4R,5R)-3,4-dihydroxy-5-[4-(hydroxyamino)-2-oxopyrimidin-1-yl]oxolan-2-yl]methyl 2-methylpropanoate, characterized by the fact that it has peaks on the powder diffractogram at following angles 2θ (±0.2°): 6.15°, 8.30°, 10.35°, 11.10°, 12.90°, where the powder diffractogram was obtained using a diffractometer using a monochromatic Kα-radiation of molybdenum. Invention relates to a pharmaceutical composition exhibiting preventive and/or therapeutic antiviral activity with respect to RNA-containing viruses, containing an effective amount of the crystalline form according to the invention and at least one pharmaceutically acceptable excipient. Invention also relates to a medicinal agent exhibiting preventive and/or therapeutic antiviral activity with respect to RNA-containing viruses, containing the pharmaceutical composition according to the invention in an effective amount. Virus is a virus, the genome of which is encoded by a single-stranded sense (+)-strand, as well as an antisense RNA (-)-strand, and which uses viral RNA-dependent-RNA-polymerase for its replication.

EFFECT: crystalline form IV [(2R,3S,4R,5R)-3,4-dihydroxy-5-[4-(hydroxyamino)-2-oxopyrimidin-1-yl]oxolan-2-yl]methyl-2-methylpropanoate, having antiviral activity, stability and reduced hygroscopicity.

16 cl, 3 tbl, 2 dwg, 4 ex