FIELD: pharmaceuticals.
SUBSTANCE: invention relates to a compound characterized by formula II, in which X is selected from the group consisting of ethyl acetate, butyl acetate, tetrahydrofuran, isobutyl acetate, ethanol, water, diethyl ether, dimethylformamide, dimethyl sulfoxide and propyl acetate, R1 and R2 independently of each other represent C1 -alkyl, R3, R4, R5 independently of each other represent fluorine, R6 represents tert-butyl, m = 0.5–3.0, n = 1.0. The invention also relates to a pharmaceutical composition and a medicinal product based on the said compound.
Formula II
EFFECT: new forms of (1R,2S,5S)-N-[(1S)-1-cyano-2-[(3S)-2-oxopyrrolidin-3-yl]ethyl]-3-[(2S)- have been obtained 3,3-dimethyl-2-[(2,2,2-trifluoroacetyl)amino]butanoyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide, having improved physicochemical properties and antiviral activity, which can be used in medicine for the prevention or treatment of viral diseases by blocking the activity of 3C-like viral proteases, including those caused by the SARS-CoV-2 virus.
22 cl, 3 dwg, 19 tbl, 4 ex
Title | Year | Author | Number |
---|---|---|---|
NITRILE-CONTAINING ANTIVIRAL COMPOUNDS | 2021 |
|
RU2786722C1 |
NITRILE-CONTAINING ANTIVIRAL COMPOUNDS | 2021 |
|
RU2820150C2 |
SYNTHESIS OF (1R,2S,5S)-N-[(1S)-1-CYANO-2-[(3S)-2-OXOPYRRROLIDIN-3-YL]ETHYL]-3-[(2S)-3,3-DIMETHYL-2-[(2,2,2-TRIFLUOROACETIL)AMINO]BUTANOIL]-6,6-DIMETHYL-3-AZABICYCLO[3.1.0]HEXAN-2-CARBOXAMIDE | 2022 |
|
RU2794748C1 |
METHOD FOR PRODUCING (1R,2S,5S)-N-[(1S)-1-CYANO-2-[(3S)-2-OXOPYRRROLIDIN-3-YL]ETHYL]-3-[(2S)-3,3- DIMETHYL-2-[(2,2,2-TRIFLUORACETYL)AMINO]BUTANOYL]-6,6-DIMETHYL-3-AZABICYCLO[3.1.0]HEXAN-2-CARBOXAMIDE | 2022 |
|
RU2794750C1 |
METHOD FOR PRODUCING (1R,2S,5S)-N-[(1S)-1-CYANO-2-[(3S)-2-OXOPYRRROLIDIN-3-YL]ETHYL]-3-[(2S)-3,3- DIMETHYL-2-[(2,2,2-TRIFLUORACETYL)AMINO]BUTANOYL]-6,6-DIMETHYL-3-AZABICYCLO[3.1.0]HEXAN-2-CARBOXAMIDE | 2022 |
|
RU2794754C1 |
METHOD FOR PRODUCING (1R,2S,5S)-N-[(1S)-1-CYANO-2-[(3S)-2-OXOPYRRROLIDIN-3-YL]ETHYL]-3-[(2S)-3,3- DIMETHYL-2-[(2,2,2-TRIFLUORACETYL)AMINO]BUTANOYL]-6,6-DIMETHYL-3-AZABICYCLO[3.1.0]HEXAN-2-CARBOXAMIDE | 2022 |
|
RU2794746C1 |
METHOD FOR PRODUCING (1R,2S,5S)-N-[(1S)-1-CYANO-2-[(3S)-2-OXOPYRRROLIDIN-3-YL]ETHYL]-3-[(2S)-3,3- DIMETHYL-2-[(2,2,2-TRIFLUORACETYL)AMINO]BUTANOYL]-6,6-DIMETHYL-3-AZABICYCLO[3.1.0]HEXAN-2-CARBOXAMIDE | 2022 |
|
RU2794755C1 |
OXADIAZOLES AS MUSCARINIC RECEPTOR AGONISTS M AND/OR M | 2019 |
|
RU2817018C2 |
CYCLIC AMINE DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS | 2011 |
|
RU2565596C2 |
DERIVATIVES OF CYCLOHEXANE OR TETRAHYDROPYRANE OR THEIR PHARMACEUTICALLY ACCEPTABLE SALTS, OR HYDRATES, OR SOLVATES OF THESE COMPOUNDS, OR THEIR SALTS, INTERMEDIATE COMPOUNDS FOR THEIR SYNTHESIS AND FUNGICIDE AGENT | 1992 |
|
RU2084439C1 |
Authors
Dates
2024-01-17—Published
2023-05-12—Filed