DERIVATIVES OF DIHYDROBENZO[b][1,4]DIAZEPINE-2-ONE AS I mGluR2 ANTAGONISTS Russian patent published in 2006 - IPC C07D403/10 C07D401/04 C07D403/14 C07D417/10 A61K31/5513 A61P25/00 

FIELD: organic chemistry, medicine.

SUBSTANCE: invention relates to new biologically active compounds that act as I mGluR2 antagonists. Invention describes compounds of the general formula (I): wherein R' means cyano-group, fluoro(lower)alkyl, (lower)alkoxy-group or pyrrole-1-yl that can be unsubstituted or comprising from 1 to 3 substituted taken among the group involving fluorine, chlorine atom, cyano-group, phenyl optionally substituted with halogen atom, -(CH₂)_1-4-hydroxy-group, (lower)alkyl, -(CH₂)_n-lower(alkoxy)-group, -(CH₂)_n-C(O)O-R''; R² means hydrogen atom if R¹ means optionally substituted pyrrole-1-yl as indicated above; or R² means halogen atom, hydroxy-group, (lower)alkyl, fluoro(lower)alkyl, (lower)alkoxy-, (lower)alkoxy(ethoxy)_n-group (wherein n means a whole number from 1 to 4), (lower)alkoxymethyl, morpholine-4-yl, 1-oxothiomorpholine-4-yl, 1,1-dioxothiomorpholine-4-yl, thiomorpholine-4-yl; Y means -CH= or =N-; R³ means halogen atom, (lower)alkyl, cyano-group, -(CH₂)_n-C(O)-NR'R'', or R³ means optionally substituted 5-membered aromatic heterocycle that can be substituted with the group representing halogen atom, -(CH₂)_n-NR'R'', -(CH₂)_n-C(O)-OR'', -(CH₂)_n-C(O)-NR'R'', hydroxy-, (lower)alkoxy-group or (lower)alkyl optionally substituted with hydroxy-group; R' means hydrogen atom, (lower)alkyl, (C₃-C₆)-cycloalkyl, fluoro(lower)alkyl; R'' means hydrogen atom, (lower)alkyl, (C₃-C₆)-cycloalkyl, fluoro(lower)alkyl or 3-hydroxy(lower)alkyl; n = 0, 1, 2, 3 or 4, and to their pharmaceutically acid-additive salts. Also, invention describes a medicinal agent representing antagonist of metabotropic glumatate receptors, a method for preparing compounds of the formula (I) (variants), using one or more compounds by claim 1, and/or one or more their pharmaceutically acceptable acid-additive salts for preparing medicinal agents designated for treatment or prophylaxis of Alzheimer's disease. Invention provides preparing new compounds possessing useful biological properties.

EFFECT: valuable medicinal properties of compounds and medicines.

26 cl, 88 ex