NOVEL FORMS OF (1R,2S,5S)-N-[(1S)-1-CYANO-2-[(3S)-2-OXOPYRROLIDIN-3-YL]ETHYL]-3-[(2S)-3,3-DIMETHYL-2-[(2,2,2-TRIFLUOROACETYL)AMINO]BUTANOYL]-6,6-DIMETHYL-3-AZABICYCLO[3.1.0]HEXANE-2-CARBOXAMIDE Russian patent published in 2024 - IPC C07D403/12 A61K31/403 A61P31/14 A61P31/12 

FIELD: chemistry.

SUBSTANCE: invention relates to a crystalline form of an isobutyl acetate solvate (1R,2S,5S)-N-[(1S)-1-cyano-2-[(3S)-2-oxopyrrolidin-3-yl]ethyl]-3-[(2S)-3,3-dimethyl-2-[(2,2,2-trifluoroacetyl)amino]butanoyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide (1:1), characterized by the fact that it has peaks on the powder diffractogram at following angles 2θ, ° (± 0.20°): 11.99, 12.65, 18.34, 19.05, 20.11, and the powder diffractogram was obtained using a diffractometer using a monochromatic Kα-radiation of copper. Invention relates to a pharmaceutical composition for treating and / or preventing viral diseases by blocking activity of 3C-like viral proteases, containing an effective amount of the crystalline form according to the invention and at least one pharmaceutically acceptable excipient. Invention also relates to a drug for treating and/or preventing viral diseases by blocking activity of 3C-like viral proteases, containing in an effective amount a crystalline form according to the invention and at least one pharmaceutically acceptable excipient. Crystalline form of isobutyl acetate solvate (1R,2S,5S)-N-[(1S)-1-cyano-2-[(3S)-2-oxopyrrolidin-3-yl]ethyl]-3-[(2S)-3,3-dimethyl-2-[(2,2,2-trifluoroacetyl)amino]butanoyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide according to the invention is used to produce a pharmaceutical composition for treating and/or preventing viral diseases by blocking activity of 3C-like viral proteases. Viral disease is caused by the SARS-CoV-2 virus.

EFFECT: crystalline form of isobutyl acetate solvate (1R,2S,5S)-N-[(1S)-1-cyano-2-[(3S)-2-oxopyrrolidin-3-yl]ethyl]-3-[(2S)-3,3-dimethyl-2-[(2,2,2-trifluoroacetyl)amino]butanoyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide (1:1), exhibiting antiviral activity, reducing the severity of the clinical course of the viral infection, having storage stability and reduced hygroscopicity.

29 cl, 8 dwg, 10 tbl, 7 ex