DERIVATIVES OF DIHYDROBENZO[b][1,4]DIAZEPINE-2-ONE AS ANTAGONISTS OF MGLUR2 II Russian patent published in 2005 - IPC

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new biologically active derivatives of dihydrobenzo[b][1,4]diazepine-2-one. Invention describes derivatives of dihydrobenzo[b][1,4]diazepine-2-one of the general formula (I): wherein X means a simple bond or ethynediyl group wherein if X means a simple bond then R¹ means cyano-group, halogen atom, lower alkyl, (C₁-C₃)-cycloalkyl, (lower)-alkoxyl, fluoro-(lower)-alkyl or it means pyrrole-1-yl that may be free or substituted with 1-3 substitutes taken among the group consisting of fluorine, chlorine atom, cyano-group, -(CH₂)_1-4-hydroxyl group, fluoro-(lower)-alkyl, lower alkyl, -(CH₂)_n-(lower)-alkoxyl, -(CH₂)_n-C(O)OR'', -(CH₂)_1-4-NR'R'', hydroxy-(lower)-alkoxyl and -(CH₂)_n-COR'R'', or it means free phenyl or phenyl substituted with one or two substitutes taken among the group consisting of halogen atom, lower alkyl, fluoro-(lower)-alkyl, (lower)-alkoxyl, fluoro-(lower)-alkoxyl and cyano-group; if X means ethynediyl group then R¹ means free phenyl or phenyl substituted with 1-3 substituted taken among the group consisting of halogen atom, lower alkyl, fluoro-(lower)-alkyl, (C₃-C₆)-cycloalkyl, (lower)-alkoxyl and fluoro-(lower)-alkoxyl; R² means -NR'R'', fluoro-(lower)-alkoxyl or 3-oxopiperazin-1-yl, pyrrolidin-1-yl, or piperidin-1-yl wherein their rings are substituted optionally with R''; R' means hydrogen atom, lower alkyl, (C₃-C₆)-cycloalkyl, fluoro-(lower)-alkyl or 2-(lower)-alkoxy-(lower)-alkyl; R'' means hydrogen atom, lower alkyl, (C₃-C₆)-cycloalkyl, fluoro-(lower)-alkyl, 2-(lower)-alkoxy-(lower)-alkyl, -(CH₂)_2-4-di-(lower)-alkylamino-group, -(CH₂)_2-4-morpholinyl, -(CH₂)_2-4-pyrrolidinyl, -(CH₂)_2-4-piperidinyl or 3-hydroxy-(lower)-alkyl; Y means -CH= or =N-; R³ means halogen atom, lower alkyl, fluoro-(lower)-alkyl, (lower)-alkoxyl, cyano-group, -(CH₂)_n-C(O)OR'', -(CH₂)_1-4-NR'R'' or it means optionally substituted 5-membered aromatic heterocycle that can be substituted with halogen atom, fluoro-(lower)-alkyl, fluoro-(lower)-alkoxyl, cyano-group, -(CH₂)_n-NR'R'', -(CH₂)_n-C(O)OR'', -(CH₂)_n-C(O)NR'R'', -(CH₂)_n-SO₂NR'R'', -(CH₂)_n-C(NH₂)=NR'', hydroxyl, (lower)-alkoxyl, (lower)-alkylthio-group or lower alkyl that is optionally substituted with fluorine atom, hydroxyl, (lower)-alkoxyl, cyano-group or carbamoyloxy-group; n means 0, 1, 2, 3 or 4, and their pharmaceutically acceptable additive salts. Also, invention describes a medicinal agent as antagonist of mGlu receptors of group II based on compounds of the formula (I). Invention provides preparing new compounds eliciting valuable biological properties.

EFFECT: valuable medicinal properties of compounds.

17 cl, 496 ex