DERIVATIVES OF DIHYDROBENZODIAZEPIN-2-ONE FOR TREATMENT OF NEUROLOGICAL DISORDERS Russian patent published in 2008 - IPC C07D401/10 C07D401/14 C07D403/10 C07D243/00 A61K31/5513 A61P25/00 A61P25/28 

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to derivatives of dihydrobenzodiazepin-2-one represented by the formula (I): wherein X means a simple bond or ethynediyl group; if X means a simple bond then R¹ means hydrogen atom, halogen atom, (lower)-alkyl, (lower)-alkoxy-group, fluoro-(lower)-alkyl, fluoro-(lower)-alkoxy-group, pyrrol-1-yl or unsubstituted phenyl or phenyl substituted with one or two substitutes chosen from group comprising halogen atom, (lower)-alkyl; if X means ethynediyl group then R¹ means unsubstituted phenyl, phenyl substituted with one or two substitutes chosen from group comprising halogen atom, (lower)-alkyl or fluoro-(lower)-alkyl; R² means hydrogen atom, (lower)-alkyl, (lower)-alkenyl, (lower)-alkoxy-group, -NR'R'', pyrrolidin-1-yl, morpholin-4-yl, fluoro-(lower)-alkyl, fluoro-(lower)-alkoxy-group, (C₃-C₆)-cycloalkyl, (C₃-C₆)-cycloalkyl-(lower)-alkoxy-group, hydroxy-(lower)-alkyl or (lower)-alkoxy-(ethoxy)_m-group wherein m = 1, 2, 3 or 4; R' means hydrogen atom, (lower)-alkyl or (C₃-C₆)-cycloalkyl; R'' means hydrogen atom, (lower)-alkyl or (C₃-C₆)-cycloalkyl; Y means -CH= or =N-; R³ means six-membered aromatic heterocycle comprising from 1 to 3 nitrogen atoms or pyridine-N-oxide wherein indicated cycles are unsubstituted or substituted with one or two substitutes chosen from group comprising fluoro-(lower)-alkyl, amino-, (lower)-alkylamino-, (lower)-alkoxy-(lower)-alkylamino- (lower)-hydroxy-(lower)-alkylamino-, hydroxy-, (lower)-alkoxy-group, (C₃-C₆)-cycloalkyl, morpholin-4-yl and (lower)-alkyl that is substituted optionally with fluorine atom, -NR'R'', hydroxy-, (lower)-alkoxy-group, pyrrolidin-1-yl, azethidin-1-yl wherein R' and R'' have values given above; n = 0, 1, 2, 3 or 4, and to their pharmaceutically acceptable additive salts possessing antagonistic activity with respect to metabotropic glutamate receptor (mGluR). Also, invention describes a medicinal agent comprising indicated compounds. Invention provides synthesis of novel compounds possessing useful biological properties, and a medicinal agent based on thereof.

EFFECT: valuable medicinal properties of compound and pharmaceutical composition.

28 cl, 1 tbl, 417 ex