INDOLE AND BENZOXAZINE DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS Russian patent published in 2014 - IPC C07D471/04 C07D265/34 A61K31/437 A61K31/506 A61K31/538 A61P25/00 

FIELD: chemistry.

SUBSTANCE: invention relates to novel derivatives of indole and benzoxazine, possessing positive allosteric modulating activity with respect to mGluR2 receptor. In formula (I) R¹ represents C_1-3alkyl, substituted with trifluoromethyl, R² represents cyano or halogeno, R³ represents hydrogen, C_1-3alkyl, C_1-3alkyl, substituted with C_3-7cycloalkyl, pyridinyl, hydroxy C_2-4alkyl, C_1-3alkyloxyC_2-4alkyl, 4-tetrahydropyranyl, 4-(hydroxy)-cyclohexanyl, 4-(hydroxy)-4-(C_1-3alkyl)cyclohexanyl, phenyl, pyridinyl methyl, pyridinyl methyl, substituted with one C_1-3alkyl group, or phenyl or pyridinyl, substituted with one or two substituents, selected from group, consisting of halogeno and C_1-3alkyl, R⁴ represents hydrogen or halogeno, A represents radical of formula -CH=CH-(a) or -CH₂-CH₂-O-(b), where one or two hydrogen atoms can be substituted with C_1-3alkyl. Invention also relates to pharmaceutical composition, containing claimed compounds, and to compound for application in treatment or prevention of central nervous system disorder, selected from the group: anxiety disorders, psychotic disorders, personality disorders, mood disorders, migraine, epilepsy or convulsive disorders, cognitive disorders, attention deficit/hyperactivity syndrome, nervous anorexia, neurogenic bulimia, neurodegeneration, neurotoxicity, ischemia, alcohol addiction, cocaine addiction, nicotine addiction, opioid addiction.

EFFECT: obtaining novel indole and benzoxazine derivatives.

15 cl, 3 tbl, 6 ex