TRI- OR TETPA-SUBSTITUTED-3-AMINOPYRROLIDINE DERIVATIVES Russian patent published in 2011 - IPC C07D401/04 C07D498/06 A61K31/4709 A61K31/5383 A61P31/04 A61P31/00 

FIELD: medicine.

SUBSTANCE: invention refers to a compound of formula to its salt or hydrate where R¹ represents hydrogen atom, alkyl group containing 1-6 carbon atoms or cycloalkyl group containing 3-6 carbon atoms; and alkyl group is optionally substituted by halogen atom; R² represents hydrogen atom or alkyl group containing 1-6 carbon atoms; R³ represents alkyl group containing 1-6 carbon atoms or cycloalkyl group containing 3-6 carbon atoms; and alkyl group is optionally substituted by halogen atom; R⁴ and R⁵ independently represent hydrogen atom, halogen atom, alkyl group containing 1-6 carbon atoms, alkoxygroup containing 1-6 carbon atoms or alkenyl group containing 2-6 carbon atoms; and alkyl group is optionally substituted by halogen atom; and provided R⁴ and R⁵ are not hydrogen atoms simultaneously; or substitutes R⁴ and R⁵ together represent (a) 3-6-members cyclic compound including carbon atom, common for R⁴ and R⁵, with formation of a spirocyclic compound with a pyrrolidine ring; or (b) exomethylene group bound with the pyrrolidine ring by a double bond; R⁶ and R⁷ independently represent hydrogen atom or alkyl group containing 1-6 carbon atoms; R⁸ represents halogen-substituted alkyl group containing 1-6 carbon atoms or cycloalkyl group containing 3-6 carbon atoms; and cycloalkyl group can be substituted by halogen atom; R⁹ represents hydrogen atom; X¹ represents hydrogen atom or halogen atom; and A represents nitrogen atom or a fragment presented by formula , where X² represents hydrogen atom, alkyl group containing 1-6 carbon atoms or alkoxygroup containing 1-6 carbon atoms; or X² together with R⁸ represents a cyclic compound containing a portion of a nucleus, and the ring formed thereby optionally contains oxygen atom and is substituted by alkyl group containing 1-6 carbon atoms. Besides, the invention refers to an antibacterial agent based on the compound of formula I, to a therapeutic agent for infections, to a method of treating an infectious disease and an application of said compounds for preparing an antibacterial drug.

EFFECT: there are produced and described new compounds showing strong antibacterial activity in relation to gram-positive and gram-negative bacteria.

30 cl, 112 ex, 10 tbl, 4 dwg