AMIDE DERIVATIVES OF 2,3,4,5-TETRAHYDROBENZO {f}-{1,4} OXAZEPINE-5-CARBOXYLIC ACID AS INHIBITOR OF Y-SECRETASE FOR TREATMENT OF ALZHEIMER'S DISEASE Russian patent published in 2008 - IPC C07D267/14 A61K31/553 A61P25/28 

FIELD: chemistry.

SUBSTANCE: claim describes benzoxazepinone derivatives of formula : wherein R¹ represents hydrogen, C₁-C₆ alkoxy, halogen or NR'R", n is 1 or 2, R', R" independently from each other represents hydrogen or C₁-C₆ alkyl; R² represents hydrogen, C₁-C₆ alkyl -(CH₂)_m-C₃-C₇-cycloalkyl, -(CH₂)_m-phenyl or -(CH₂)_m-O-C₁-C₆ alkyl; m is 0.1 or 2; R³ represents C₁-C₆ alkyl,-(CH₂)_m-C(O)O-C₁-C₆ alkyl, C₃-C₇ cycloalkyl or -(CH₂)_m-phenyl which is unsubstituted or substituted by one or two substituents, selected from the group consisting of halogen, trifluoromethyl, -NR'R", nitro and -SO₂NH₂, or represents -C₃-C₇ -cycloalkyl, unsubstituted or substituted by phenyl, or is -(CR′R″)_o-heterocyclyl, selected from the group consisting of tetrahydropyran-4-yl, pyridin-3-yl, indol-3-yl optionally substituted by halogen or C₁-C₆ alkoxy group, or thiophen-2-yl, furan-2-yl, NH-pyridin-2-yl optionally substituted by nitro group or benzoimidazol-2-yl, 2-oxo-tetrahydrofuran, and benzo[1,3]dioxol-5-yl and represents -tetrahydro-naphthalen-1-yl, -CHR′-naphthalen-2-yl, -fluoren-9-yl, -(CH₂)_o-S-lower alkyl, -(CH₂)_o-S-benzyl, -(CH₂)_o-C(O)NH₂, -(CH₂)_oNR′R″, -CH[C(O)NH₂]-(CH₂)_o-phenyl, -(CH₂)_o-CF₃, or -(CH₂)_o-CR′R″-CH₂-NR′R″; and o is 1 or 2; or their pharmaceutically suitable acid addition salts, excluding: phenetylamide 4-benzyl-3-oxo-2,3,4,5-tetrahydro-benzo[f][1,4]-oxazepine-5-carboxylic acid, butylamide 4-benzyl-3-oxo-2,3,4,5-tetrahydro-benzo[f][1,4]-oxazepine-5-carboxylic acid, phenetylamide 4-cyclohexyl-3-oxo-2,3,4,5-tetrahydro-benzo[f][1,4]-oxazepine-5-carboxylic acid, butylamide 4-cyclohexyl-3-oxo-2,3,4,5-tetrahydro-benzo[f][1,4]-oxazepine-5-carboxylic acid. The pharmaceutical on basis of the compounds of formula I aimed at the treatment of Alzheimer's disease is described.

EFFECT: production of the new compounds, benzoxazepinone derivatives having useful biological properties.

26 cl, 196 ex