APPLICATION OF AN OXYGEN-CONTAINING DERIVATIVE OF 6-HALOQUINOLINE FOR INHIBITING THE REPLICATION OF BETACORONAVIRUSES, INCLUDING SARS-COV-2, AND METHOD FOR PRODUCTION THEREOF Russian patent published in 2022 - IPC A61K31/53 A61P31/14 C07D215/28 C07D215/38 

Abstract RU 2780245 C1

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to the field of pharmacology and medicine and is aimed at treating diseases caused by betacoronaviruses, including SARS-CoV-2. Described is an application of an oxygen-containing derivative of 6-haloquinoline by the general formula I, wherein Hal constitutes a substituent selected from bromine, fluorine, chlorine; R1 constitutes a substituent selected from hydrogen, an alkyl (C1-C10) of a normal or branched structure, an aryl without substituents or substituted in positions 2, 3, 4, 5, 6; R2 constitutes a substituent selected from hydrogen, NHalkyl-, NHaryl-, NHhetaryl-, pyrrolidinyl-, piperidinyl-, morpholinyl-, piperazinyl-, homopiperazinyl-, tetrahydroquinolinyl-, tetrahydroisoquinolinyl-, hexamethyleneiminyl-; -SC(S)X, wherein X=NHalkyl-, NHaryl-, NHhetaryl-, pyrrolidinyl-, piperidinyl-, morpholinyl-, piperazinyl-, homopiperazinyl-, tetrahydroquinolinyl-, tetrahydroisoquinolinyl-, hexamethyleneinyl-; R3 constitutes a substituent selected from hydrogen, alkyl (C1-C10) of a normal or branched structure, alkylaryl, aryl without substituents or substituted in positions 2, 3, 4, 5, 6, for suppressing the replication of betacoronaviruses.

EFFECT: ensured effective suppression of the replication of betacoronaviruses, including SARA-CoV-2, at low values of the effective concentration of EC50, low cytotoxicity, and high value of selectivity index.

5 cl, 1 tbl, 8 ex

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RU 2 780 245 C1

Authors

Shikhaliev Khidmet Safarovich

Medvedeva Svetlana Mikhajlovna

Zorina Anna Vyacheslavovna

Stolpovskaya Nadezhda Vladimirovna

Sulimov Vladimir Borisovich

Sulimov Aleksej Vladimirovich

Kutov Danil Konstantinovich

Pyankov Oleg Viktorovich

Shcherbakov Dmitrij Nikolaevich

Dates

2022-09-21Published

2021-04-30Filed