ANTIBACTERIAL PIPERIDINE DERIVATIVES Russian patent published in 2011 - IPC C07D417/14 A61K31/4523 A61K31/4709 A61K31/5377 A61P31/04 

FIELD: chemistry.

SUBSTANCE: formula (I) compound has antibacterial activity and can be used as a medicinal agent. In formula ,

R¹ is hydrogen, halogen, C_1-4alkyl; R² is selected from hydrogen, halogen, C_1-4alkyl; R³ is selected from hydrogen, halogen, cyano, C_1-4alkyl; W is -N(R⁶)-; X is a single bond; ring A is an unsaturated or partially saturated ring containing 5-6 atoms, one or two of which are independently selected from nitrogen and sulphur; or an unsaturated or partially saturated bicyclic ring containing 9-10 atoms, one, two or three of which are selected from nitrogen and sulphur; R⁴ and R⁵ are substitutes on a carbon atom and are independently selected from a halogen, nitro, cyano, hydroxy, amino, carboxy, carbamoyl, formyl, hydroxy iminomethyl, C1-4alkoxyminomethyl, C₁-₄alkyl, C_1-4alkoxy, C₁-₄alkanoyl, C₁-₄alkoxy)carbamoyl, N-(C₁-₄alkyl)-N-(C₁-₄alkoxy)carbamoyl, C₁-₄alkylS(O)_a, where a equals 0-2, C₁-₄alkoxycarbonyl, C₁-₄alkoxycarbonylamino, C₁-₄alkylsulphonylamino, (saturated or unsaturated carbocycle containing 3-7 atoms)-R¹⁰- or (saturated, partially saturated or unsaturated ring containing 5-6 atoms, one or two of which are selected from nitrogen, oxygen and sulphur)-R¹¹-; where R⁴ and R⁵ can independently and optionally substituted at the carbon atom with one or more R¹²; R⁶ is hydrogen; n equals 1-4; where values of R⁴ can be identical or different; m equals 0-4; where values of R⁵ can be identical or different; R¹² is selected from azido, halogen, cyano, hydroxy, amino, carboxy, C_1-4alkyl, C_2-4alkenyl, C_2-4alkynyl, C_1-4alkoxy, C_1-4alkanoyl, N-(C_1-4alkyl)amino, N,N-(C_1-4alkyl)₂amino, C_1-4alkylS(O)_a, where a equals 0-2, (saturated or unsaturated cabocycle containing 3-7 atoms)-R¹⁴- or (saturated, partially saturated or unsaturated ring containing 5 or 6 atoms, one or two of which are selected from nitrogen, oxygen and sulphur)-R¹⁵-; where R¹² can independently and optionally be substituted at the carbon atom with one or more R⁹; R¹⁰, R¹¹, R¹⁴ and R¹⁵ are independently selected from a single bond, -C(O)-, -N(R¹⁹)C(O)- or -C(O)N(R²⁰)-; where R¹⁹ and R²⁰ are independently selected from hydrogen or C_1-4alkyl; R¹⁶ is selected from halogen, cyano, hydroxy, carboxy, methyl and methoxy. The invention also relates to a pharmaceutical composition, having antibacterial activity, containing the disclosed compound as an active ingredient, use of the disclosed compound to prepare a medicinal agent and a method of producing the compound of formula (I).

EFFECT: high activity of the compounds.

22 cl, 52 tbl, 721 ex