AMORPHOUS 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 A61K31/7068 A61P31/14 A61P31/20 

FIELD: medicine; pharmacology.

SUBSTANCE: invention relates to medicine, pharmacology and chemical-pharmaceutical industry, namely to amorphous form [(2R,3S,4R,5R)-3,4-dihydroxy-5-[4-(hydroxyamino)-2-oxopyrimidin-1-yl]oxolan-2-yl]methyl-2-methylpropanoate has a diffraction maximum on the X-ray powder pattern in the form of one wide halo in range of 10–30° 2θ (±2°). Invention relates to a pharmaceutical composition exhibiting preventive and/or therapeutic antiviral activity with respect to viruses, the genome of which is encoded by a single-stranded sense (+)-thread, as well as an antisense (-)-RNA strand, and which use viral RNA-dependent-RNA polymerase for their replication, containing an amorphous form in an effective amount [(2R,3S,4R,5R)-3,4-dihydroxy-5-[4-(hydroxyamino)-2-oxopyrimidin-1-yl]oxolan-2-yl]methyl-2-methylpropanoate and at least one pharmaceutically acceptable excipient. Invention also relates to a medicinal agent exhibiting preventive and/or therapeutic antiviral activity with respect to viruses, the genome of which is encoded by a single-stranded sense (+)-thread, as well as an antisense (-)-RNA strand, and which use viral RNA-dependent-RNA polymerase for their replication, containing an effective amount of the pharmaceutical composition according to the invention.

EFFECT: longer antiviral activity, as well as improved physical and chemical and technological properties of the amorphous form [(2R,3R,4R,5R)-3,4-dihydroxy-5-[4-(hydroxyamino)-2-oxopyrimidin-1-yl]oxolan-2-yl]methyl-2-methylpropanoate.

13 cl, 2 dwg, 3 ex