CHEMICAL COMPOUNDS Russian patent published in 2012 - IPC C07D417/04 C07D401/04 C07D471/04 C07D417/14 C07D213/75 C07D239/42 A61K31/427 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention describes compounds of formula (I) wherein: R¹ means C_1-6alkyl or C_3-6cycloalkyl; wherein R¹ may be optionally carbon-substituted by one or more R⁶; R² means hydrogen; R³ and R⁴ are carbon substitutes, and each is independently specified in carboxy, carbamoyl, N-(C_1-6alkyl)amino, N,N-(C_1-6alkyl)₂amino, C_1-6alkanoylamino, N-(C_1-6alkyl)carbamoyl, N,N-(C_1-6alkyl)₂carbamoyl, N-(C_1-6alkoxy)carbamoyl, phenyl-R⁹ - or heterocyclyl-R¹⁰-; wherein R³ and R⁴ may be independently carbon-substituted by one or more R¹¹; and wherein provided said heterocyclyl contains -NH - residue, then nitrogen may be optionally substituted by a group specified in R¹²; m has the value of 0, 1 or 2; wherein the values R³ may be equal or different; p has the value of 0, 1 or 2; wherein the values R⁴ may be equal or different; the ring A means nitrogen-containing 5- or 6-member heterocyclic group; wherein drawn nitrogen represents = N- and is found in an ortho-position to R¹R²NC(O)NH group in formula (I); the ring B means phenyl or heterocyclyl; wherein provided said heterocyclyl contains -NH- residue, then nitrogen may be optionally substituted by a group specified in R¹⁴; R⁵ is specified in hydroxy, C_1-6alkoxy or -N(R¹⁵)(R¹⁶); R⁶ and R¹¹ are carbon substitutes and each is independently specified in halo, C_1-6alkyl or C_1-6alkoxy; R¹⁵ and R¹⁶ are independently specified in hydrogen, C_1-6alkyl, C_1-6alkoxy, cyclopropyl or cyclopentyl; R¹² and R¹⁴ mean C_1-6alkyl; wherein R¹⁴ may be optionally carbon specified by one or more R²³; R⁹ and R¹⁰ mean a direct link; and R²³ means halo or methoxy; wherein said heterocyclyl means pyridine, imidazole, triazole, thiazole, benzothiazole, imodazolepyridine, dihydroquinoline or thiadiazole, or its pharmaceutically acceptable salt; provided said compound represents other than ethyl ester of 5-[2-[[(ethylamino)carbonyl]amino]pyridin-4-yl]-4-methyl-4H-1,2,4-triazole-3-carboxylic acid or their pharmaceutically acceptable salts. There are also described pharmaceutical compositions on the basis of said compounds, a method for bacterial DNA-hydrase and/or bacterial topoisomerase IV inhibition in a homoiothermal animal, as well as a method of treating an infection in a homoiothermal animal.

EFFECT: there are prepared and described new compounds showing antibacterial activity.

24 cl, 165 ex