DERIVATIVES OF SUBSTITUTED DIBENZOAZEPINE AND BENZODIAZEPINE, USEFUL AS INHIBITORS OF γ -SECRETASE Russian patent published in 2009 - IPC C07D223/18 C07D243/12 C07D409/12 A61K31/5513 A61P25/28 

FIELD: chemistry.

SUBSTANCE: present invention pertains to new compounds with general formula I, where R¹ represents -(CHR')_q-aryl or -(CHR')_q-thiophen, which are unsubstituted or mono-, di- or tri-substituted with (inferior)alkyl, (inferior)alkoxy, CF₃ or haloid, or represents (inferior)alkyl, (inferior)alkenyl, -(CH₂)_n-Si(CH₃)₃, -(CH₂)_n-O-(inferior)alkyl, -(CH₂)_n-S- (inferior)alkyl, -(CH₂)_q-cycloalkyl, -(CH₂)_n-[CH(OH)]_m-(CF₂)_p-CH_qF_(3-q), or represents -(CH₂)_n-CR₂-CF₃, where two radicals R together with a carbon atom form a cycloalkyl ring; R' represents hydrogen or (inferior)alkyl; n is 1, 2 or 3; m is 0 or 1; p is 0, 1,2, 3, 4, 5 or 6; q is 0, 1, 2 or 3; R² represents hydrogen or (inferior)alkyl; R³ represents hydrogen, (inferior)alkyl, CH₂F, aryl, optionally mono-, di- or tri-substituted with a haloid, or represents -(CH₂)_nNR⁵R⁶, where R⁵ and R⁶ independently represent hydrogen or (inferior)alkyl; R⁴ represents one of the following groups a) or b), where R⁷ represents inferior)alkyl or -(CH₂)_ncycloalkyl; R⁸ and R⁹ independently represent hydrogen, (inferior)alkyl, -(CH₂)_n-cycloalkyl or -C(O)-phenyl. The invention also relates to pharmaceutically used acid addition salts of these compounds, optically pure enantiomers, racemates or diastereomeric mixtures, as well as compounds with general formula I-1, and medicinal agent.

EFFECT: obtaining new biologically active compounds, designed for inhibiting γ-secretase.

16 cl, 83 ex