Show metadata Hide metadata

(19)

(11)

2 811 800

(13)

(51)

IPC

C07D403/12(2006-01-01)

A61K31/403(2006-01-01)

A61P31/12(2006-01-01)

A61P31/14(2006-01-01)

(21) (22)

Application

2023112257, 2023-05-12

(24)

Start date

2023-05-12

(22)

Actual filing date

2023-05-12

(45)

Published

2024-01-17

(72)

Inventor

Belyi Petr AleksandrovichLopatukhin Eduard IurevichKorolev Vladimir LvovichZaslavskaia Kira IakovlevnaKorliukov Aleksandr AleksandrovichBuikin Petr Alekseevich

(73)

Holder

Obshchestvo S Ogranichennoi Otvetstvennostiu Rus"

NEW AZABICYCLOHEXANE DERIVATIVES Russian patent published in 2024 - IPC C07D403/12 A61K31/403 A61P31/12 A61P31/14

Abstract RU 2811800 C1

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

Similar patents RU2811800C1

Title	Year	Author	Number
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	2023	Belyi Petr Aleksandrovich Lopatukhin Eduard Iurevich Korolev Vladimir Lvovich Zaslavskaia Kira Iakovlevna Korliukov Aleksandr Aleksandrovich Buikin Petr Alekseevich	RU2827154C1
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	2023	Belyi Petr Aleksandrovich Lopatukhin Eduard Iurevich Korolev Vladimir Lvovich Zaslavskaia Kira Iakovlevna Korliukov Aleksandr Aleksandrovich Buikin Petr Alekseevich	RU2827358C1
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	2023	Belyi Petr Aleksandrovich Lopatukhin Eduard Iurevich Korolev Vladimir Lvovich Zaslavskaia Kira Iakovlevna Korliukov Aleksandr Aleksandrovich Buikin Petr Alekseevich	RU2827158C1
NITRILE-CONTAINING ANTIVIRAL COMPOUNDS	2021	Owen, Dafydd Rhys Pettersson, Martin Youngjin Reese, Matthew Richard Sammons, Matthew Forrest Tuttle, Jamison Bryce Verhoest, Patrick Robert Wei, Liuqing Yang, Xiaojing Yang, Qingyi	RU2786722C1
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	2023	Belyi Petr Aleksandrovich Lopatukhin Eduard Iurevich Korolev Vladimir Lvovich Zaslavskaia Kira Iakovlevna Korliukov Aleksandr Aleksandrovich Buikin Petr Alekseevich	RU2827357C1
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	2023	Belyi Petr Aleksandrovich Lopatukhin Eduard Iurevich Korolev Vladimir Lvovich Zaslavskaia Kira Iakovlevna Korliukov Aleksandr Aleksandrovich Buikin Petr Alekseevich	RU2827157C1
NITRILE-CONTAINING ANTIVIRAL COMPOUNDS	2021	Ouen, Defidd Ris Pettersson, Martin Yungchin Riz, Mettyu Richard Semmons, Mettyu Forrest Tattl, Dzhejmison Brajs Verkhust, Patrik Robert Vej, Lyutsin Yan, Syaotszin Yan, Tsingyuj	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	Belyj Petr Aleksandrovich Lopatukhin Eduard Yurevich Korolev Vladimir Lvovich Zaslavskaya Kira Yakovlevna Belov Evgenij Yurevich	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	Belyj Petr Aleksandrovich Lopatukhin Eduard Yurevich Korolev Vladimir Lvovich Zaslavskaya Kira Yakovlevna Belov Evgenij Yurevich	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	Belyj Petr Aleksandrovich Lopatukhin Eduard Yurevich Korolev Vladimir Lvovich Zaslavskaya Kira Yakovlevna Belov Evgenij Yurevich	RU2794754C1

RU 2 811 800 C1

Authors

Belyi Petr Aleksandrovich

Lopatukhin Eduard Iurevich

Korolev Vladimir Lvovich

Zaslavskaia Kira Iakovlevna

Korliukov Aleksandr Aleksandrovich

Buikin Petr Alekseevich

Dates

2024-01-17—Published

2023-05-12—Filed