QUINOLINE AS ALLOSTERIC ENHENCER OF GABA-B RECEPTORS Russian patent published in 2010 - IPC C07D215/18 C07D215/20 C07D491/04 C07D215/38 C07D401/04 A61K31/4738 A61P25/22 

FIELD: chemistry.

SUBSTANCE: present invention relates to compounds of formula (I) , where R¹ is hydrogen, C₁-C₇ alkyl; R² is C₁-C₇ alkyl, aryl, C₁-C₇ haloalkyl or C₃-C₈ cycloalkyl; R³, R⁴ each independently represents hydrogen, halogen, C₁-C₇ alkoxy, C₁-C₇ alkylsuphonyl; R⁵ is hydrogen, halogen, C₁-C₇ alkyl, C₁-C₇ haloalkoxy, or aryloxy, or is -NR⁷R⁸, where R⁷ and R⁸ represent C₁-C₇ alkyls, or R⁷ and R⁸ together with the nitrogen atom to which they are bonded can form a 4-7-member heterocycloalkyl group, which can be substituted with one or more substitutes selected from a group consisting of halogen, C₁-C₇ alkyl, C₁-C₇ alkoxy, hydroxyl, phenyl and di(C₁-C₇)alkylamino; R⁶ is hydrogen or together with R⁵ can form a 5- or 6-member heterocycloalkyl group which can be substituted with one or more halogens; and their pharmaceutically acceptable salts of acid compound, except the range of compounds given in paragraph 1 of the formula of invention. The invention also relates to medicine based on said compounds, with activity of allosteric enhancer of GABA-B receptors and use of compounds of the formula to prepare medicines used in treating central nervous system disorders, including anxiety and depression.

EFFECT: novel compounds are obtained and described, which can be used for preparing medicines used in treating central nervous system disorders, including anxiety and depression.

14 cl, 58 ex, 1 tbl