INDOLE-3-CARBOXYLIC ACID DERIVATIVE HAVING ANTIVIRAL ACTIVITY ON SARS-CoV-2 Russian patent published in 2024 - IPC A61K31/454 C07D403/06 A61P31/12 

Abstract RU 2820633 C1

FIELD: virology; medicine.

SUBSTANCE: invention relates to a compound having high antiviral activity of anti-SARS-CoV-2 (Severe acute respiratory syndrome-related coronavirus 2, formerly 2019-nCoV). Disclosed is the use of a water-soluble dihydrochloride compound of 6-bromo-1-methyl-5-methoxy-2-(1-piperidinomethyl)-3-(2-diethylaminoethoxy)carbonylindole of general formula (II), having in vitro dose-dependent activity on SARS-CoV-2, which at concentration of 30 mcg/ml completely inhibits coronavirus infection SARS-CoV-2. Compound II has IFN-inducing activity and inhibits syncytium formation mediated by the spinous protein (S-glycoprotein) SARS-CoV-2, and also has high activity (IC50=1.06 mcg/ml) and selectivity (selectivity index SI=78.6).

EFFECT: using the invention enables to effectively suppress the reproduction of SARS-CoV-2.

1 cl, 1 dwg, 3 tbl, 4 ex

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Authors

Narovlyanskij Aleksandr Naumovich

Filimonova Marina Vladimirovna

Tsyshkova Nina Gavrilovna

Pronin Aleksandr Vasilevich

Grebennikova Tatyana Vladimirovna

Karamov Eduard Vladimirovich

Larichev Viktor Filippovich

Kornilaeva Galina Vladimirovna

Fedyakina Irina Timofeevna

Dolzhikova Inna Vadimovna

Mezentseva Marina Vladimirovna

Poloskov Vladislav Vasilevich

Koval Lidiya Semenovna

Marinchenko Valentina Pavlovna

Surinova Valentina Ivanovna

Filimonov Aleksandr Sergeevich

Shitova Anna Andreevna

Soldatova Olga Vasilevna

Ivanov Sergej Anatolevich

Sanin Aleksandr Vladimirovich

Zubashev Igor Konstantinovich

Veselovskij Vladimir Vsevolodovich

Kozlov Vyacheslav Vladimirovich

Stepanov Andrej Valentinovich

Khomich Aleksandr Vladimirovich

Kozlov Vasilij Sergeevich

Shegaj Petr Viktorovich

Kaprin Andrej Dmitrievich

Ershov Feliks Ivanovich

Gintsburg Aleksandr Leonidovich

Dates

2024-06-06Published

2022-12-16Filed