APPLICATION OF A DERIVATIVE OF 1,3,5-TRIAZINE-2,4-DIAMINE FOR INHIBITING THE REPLICATION OF BETACORONAVIRUSES, INCLUDING SARS-COV-2 Russian patent published in 2022 - IPC A61K31/53 A61P31/14 C07D251/54 C07D253/02 

Abstract RU 2780249 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 a derivative of 1,3,5-triazine-2,4-diamine by the general formula I, wherein R1 and R2 constitute a substituent selected from hydrogen; an alkyl (C1-C10) of an unbranched or branched structure; an aryl without substituents or substituted in positions 2,3,4,5,6; a hetaryl constituting a nitrogen-, and/or sulphur-, and/or oxygen-containing five- or six-membered heterocycle; R3 constitutes a substituent selected from hydrogen; or an alkyl (C1-C10) of an unbranched or branched structure; or an aryl without substituents or substituted in positions 2,3,4,5,6; or a hetaryl, wherein the hetaryl is a nitrogen-, and/or sulphur-, and/or oxygen-containing five- or a six-membered heterocycle; or an alkylNH, wherein the alkyl(C1-C10) is of an unbranched or branched structure; or an arylNH-, wherein the aryl is without substituents or is substituted in positions 2,3,4,5,6; or a hetarylNH-, wherein the hetaryl constitutes a nitrogen-, and/or sulphur-, and/or an oxygen-containing five- or six-membered heterocycle; or pyrrolidine-1-yl, piperidine-1-yl, morpholine-4-yl-, piperazine-1-yl-, homopiperazine-1-yl-, tetrahydroquinoline-1-yl-, tetrahydroisoquinoline-2-yl-, hexamethyleneiminyl; or R4CH2-, wherein R4 is selected from an alkyl (C1-C10) of an unbranched or branched structure; an aryl without substituents or substituted in positions 2,3,4,5,6; a hetaryl, wherein the hetaryl constitutes a nitrogen-, and/or sulphur-, and/or oxygen-containing five- or six-membered heterocycle; pyrrolidine-1-yl, piperidine-1-yl, morpholine-4-yl-, piperazine-1-yl-, homopiperazine-1-yl-, tetrahydroquinoline-1-yl-, tetrahydroisoquinoline-2-yl, hexamethyleneiminyl for suppressing the replication of betacoronavirus.

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, 7 ex

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RU 2 780 249 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