THIENOPYRIDINE DERIVATIVES AS GABA-B ALLOSTERIC ENHANCERS Russian patent published in 2010 - IPC C07D495/04 C07D495/14 A61K31/4365 A61K31/435 A61K31/4427 A61P25/00 

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula I , where R¹ is C₁-C₇-alkyl; R² is C₁-C₇-alkyl, C₁-C₇-haloalkyl, C₃-C₈-cycloalkyl; R³ is -NR^aR^b; possibly substituted phenyl, thiophenyl, furanyl, where the substitutes are selected from a group consisting of halogen, C₁-C₇-alkoxy, C₁-C₇-alkylsulphonyl and -C(O)O-C₁-C₇-alkyl; R⁴ is hydrogen or C₁-C₇-alkyl; R⁵ is hydrogen, halogen, C₁-C₇-alkyl, phenyl; or R⁵ together with R⁴ can form a ring selected from a group consisting of C₅-C₇-cycloalkyl, tetrahydrofuranyl, piperidine, tetrahydropyran, phenyl or pyridinyl, which can possibly be substituted with -C(O)O-C₁-C₇-alkyl; R^a and R^b together with the nitrogen atom to which they are bonded form piperidine; and to pharmaceutically acceptable salts thereof. The invention also relates to a medicinal agent based on the said compounds which has GABA-B receptor allosteric enhancement effect.

EFFECT: obtaining novel compounds and a medicinal agent based on the said compounds, which can be used in medicine for treating central nervous system disorders.

13 cl, 42 ex