HYBRID DERIVATIVES OF (1H-1,2,4) TRIAZOLE AND SULPHUR-CONTAINING HETEROCYCLES: DERIVATIVES OF THIAZOLIDINE-2,4-DIONE, THIOMORPHOLINE-3-ONE, AND 1,4-THIAZEPAN-3-ONE, EXHIBITING ANTIMICROBIAL ACTIVITY Russian patent published in 2022 - IPC C07D417/06 C07D417/14 A61K31/381 A61K31/4196 A61P31/10 

Abstract RU 2771027 C1

FIELD: pharmaceuticals.

SUBSTANCE: group of inventions relates to pharmaceutical chemistry and includes a compound by the general formula (I) or a stereoisomer, enantiomer, diastereoisomer, racemate, pharmaceutically acceptable salt thereof. In the formula (I), R1 constitutes hydrogen or methyl; Q constitutes a covalent bond, -NH-, -NR5-, -(CH2)n-NH-, -(CH2)n-NR5- or -(CH2)n-, wherein n=0, 1 or 2; R5 constitutes a -C1-4-alkyl, benzyl or benzoyl, wherein the benzyl or benzoyl may optionally be substituted with 0 to 2 substituents, independently selected from a partially or fully halogenated -C1-4-alkyl, halogen; X constitutes -CH- or -N-; A is the fragment specified in the claim, R3 and R4 are independently selected from fluorine or chlorine. The group of inventions also relates to a pharmaceutical composition containing a compound by the formula (I) and to an application thereof.

EFFECT: compound by the general formula (I), applied as an antifungal agent for treating and/or preventiing an infectious disease of a microbial etiology in a subject, caused by a fungal infection, in particular, dermatophytosis, superficial mycosis, candidiasis of the skin and/or nails, vaginal candidiasis, candidiasis of internal organs, oral candidiasis, or endocarditis.

14 cl, 5 dwg, 1 tbl

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RU 2 771 027 C1

Authors

Levshin Igor Borisovich

Polshakov Vladimir Ivanovich

Simonov Aleksandr Yurevich

Grammatikova Nataliya Eduardovna

Dates

2022-04-25Published

2020-12-29Filed