N-[3-(5-AMINO-3,3A,7,7A-TETRAHYDRO-1H-2,4-DIOXA-6-AZA-INDEN-7-YL)-PHENYL]-AMIDES AS INHIBITORS OF BACE1 AND(OR) BACE2 Russian patent published in 2016 - IPC C07D498/04 A61K31/5365 A61P25/28 

FIELD: pharmaceutics.

SUBSTANCE: invention relates to a compound of formula Ia, where R¹ represents a pyridinyl or pyridinyl, substituted with 1-2 substitutes, individually selected from a cyano, a halogen atom, halogen-C_1-6-alkoxy, or pyrazinyl, substituted by halogen-C_1-6-alkoxy or C_2-6-alkynyl-C_1-6-alkoxy; R² represents F; R³ is selected from a group consisting of i) methyl, ii) -CH₂CH₂F, iii) -CH₂CHF₂; R⁴ is hydrogen; and R⁵ is selected from a group consisting of i) a hydrogen atom, ii) -CF₃; or its pharmaceutically acceptable salts. Invention also relates to specific compounds of N-[3-(5-amino-3,3A,7,7A-tetrahydro-1H-2,4-dioxa-6-aza-inden-7-yl)phenyl]amide, given in claim. Compound according to invention is intended for use as a therapeutically active substance possessing inhibitory activity on BACE1 and/or BACE2, for preparing a pharmaceutical composition or a medicinal agent.

EFFECT: inhibiting properties of N-[3-(5-amino-3,3A,7,7A-tetrahydro-1H-2,4-dioxa-6-aza-inden-7-yl)phenyl]amide with respect to BACE1 and/or BACE2.

12 cl, 8 tbl, 22 ex