PHARMACEUTICAL COMPOSITION, INCLUDING TRICYCLIC SULFUR-CONTAINING 1,2-DIHYDROQUINOLINE DERIVATIVE FOR INHIBITION OF REPLICATION OF BETA CORONAVIRUSES, INCLUDING SARS-CoV-2, AND METHOD OF ITS USE Russian patent published in 2024 - IPC C07D495/04 A61K31/4365 A61P31/14 

FIELD: pharmacology and medicine.

SUBSTANCE: invention relates to the use of a pharmaceutical composition for suppressing the replication of beta-coronavirus, including a therapeutically effective amount of a tricyclic sulfur-containing derivative of 1,2-dihydroquinoline of general formula I and pharmaceutically acceptable additives. In general formula I, R1 represents a substituent selected from methyl, ethyl, methoxy, ethoxy; R2 represents a substituent selected from methyl, ethyl, methoxy, ethoxy; R3 represents a substituent selected from methyl, ethyl, methoxy, ethoxy group; R4 is a substituent selected from methyl, benzyl, 3-phenylacryloyl-, 3-(4-methoxyphenyl)acryloyl-, 3-phenylpropanoyl-, phenylethyl, 2-(4-fluorophenoxy)acetyl-, 4-chlorophenoxyacetyl-, 2-(2,4-dichlorophenoxy)acetyl-, 4-nitrobenzoyl-, 2-(1,3-dioxoisoindolin-2-yl)-3-phenylpropanoyl-) groups; 3,4-dichlorophenylcarbamoyl-, furan-2-carbonyl-, ethylcarbamoyl-, 2-naphthyloxyacetyl-, 2-(1,3-dioxoisoindolin-2-yl)acetyl-, 2-(1,3-dioxohexahydro-1H-isoindole -2(3H)-yl)acetyl-, 2-morpholinoacetyl-, piperidin-1-ylacetyl-, 2-(4-carbamoylpiperidin-1-yl)acetyl-, 2-(2,5-dioxopyrrolidin-1-yl) acetyl-,2-phenoxyacetyl-,2-1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)acetyl-, 2-benzo[d]oxazol-2-ylthio)acetyl-, 2 -(benzo[d]thiazol-2-yloxy)acetyl-, benzoxazol-2-ylmercaptoacetyl-, furanoyl-, 2-naflinylioxymethylcarbonyl, 3,4-dichlorophenylcarbamoyl; X represents a substituent selected from 4-(4-chlorobenzyloxy)phenylimino-, 4-isopropylphenylimino-, 4-(6-methylbenzo[d]thiazol-2-yl)phenylimino-, 4-(N-benzoylsulfamoyl)phenylimino-, 4-ethoxyphenylimino-, 4-ethoxycarbonylphenylimino-, phenylimino-, 4-chlorophenylimino-, 3-chlorophenylimino-, 4-sulfamoylphenylimino-, 4-(N-acetylsulfamoyl)phenylimino-, 4-(N-(thiazol-2-yl) sulfamoyl)phenylimino-, 2-nicotinoylhydrazono-, 4-((4-chlorobenzyl)oxy)phenylimino-, 2-methoxyphenylimino-, 4-(N-(pyrimidin-2-yl)sulfamoyl)phenylimino-, 4-(N-(4,6-dimethylpyrimidin-2-yl)sulfamoyl)phenylimino-.

(I)

EFFECT: use of the invention makes it possible to effectively suppress the replication of beta-coronaviruses, such as SARS-CoV-2, with low toxicity, and can be used to treat diseases caused by beta-coronaviruses.

4 cl, 1 tbl, 20 ex