BICYCLIC NITROIMIDAZOLES COVALENTLY CONNECTED TO REPLACED PHENYLOXAZOLYDINONES Russian patent published in 2014 - IPC C07D498/04 A61K31/06 A61P31/04 A61P31/06 

FIELD: biotechnologies.

SUBSTANCE: invention refers to a number of bicyclic nitroimidazole-replaced phenyloxazolydinones of the following structural formula (I):

,

containing nitroimidazole circle, or to its pharmaceutically acceptable salt; where R₁ represents hydrogen, (C₁-C₆)alkyl or aryl; n is equal to 0, 1 or 2; X₁ and X₂ independently represent H, CF₃, CI, OCF₃ or F; G represents -OH, triazole or -NHCOR₂; R₂ represents (C₁-C₆)alkyl, cycloalkyl or aryl; and L represents a bond or a linker group chosen from any combination 2-3 of the following groups: 1) (C₁-C₆)alkylene, 2) (C₃-C₈)cycloalkylene, 3) arylene, arylene-replaced CN, ore arylene-replaced F, 4) group chosen from the group consisting of

,

where R₁₀ represents H, CF₃, hydroxyl, amino, alkyl, alkylamino, alkoxy or aryl, and R₁₃ represents H, hydroxyl, amino, alkyl, alkyl amino, alkoxy or aryl, or R₁₃ in combination with nitroimidazole circle can form spiral-shaped structure, 5) -C(=O)-, 6) -O-, 7) -S(O)_n-, in which n is equal to 0.1 or 2, 8) -N(R₃)-, 9) -C(R₄)=C(R₅)-, R₃ represents hydrogen, (C₁-C₆) alkyl or aryl, and R₄ and R₅ represent hydrogen, (C₁-C₆) alkyl or aryl, or R₄ and R₅ can be combined together so that they can form a bond. Besides, the invention refers to pharmaceutical composition for treatment of bacterial infection based on compounds of formula I, as well as to a bacterial infection treatment method.

EFFECT: invention describes new compounds that have antibacterial activity against a line of wild type and stable lines of pathogenic microorganisms, and as a result, are suitable for prevention, control and treatment of a number of human and mammal bacterial infections caused by these pathogenic microorganisms such as bacillus Kochii.

15 cl, 93 ex, 1 tbl, 22 dwg