1,4 THIAZEPINES/SULPHONES AS BACE1 AND/OR BACE2 INHIBITORS Russian patent published in 2016 - IPC C07D417/12 C07D513/04 A61K31/554 A61P25/16 A61P3/10 

FIELD: pharmaceutics.

SUBSTANCE: invention relates to compounds of formula I, having inhibitory activity on BACE1 and/or BACE2, pharmaceutical compositions based thereon and method for use thereof. In general formula I R¹ represents a halogen, R² is selected from a group consisting of i) C_1-6-alkyl and ii) a halogen-C-_1-6-alkyl; R³ is selected from group consisting of i) hydrogen and ii) C_1-6-alkyl; R⁴ is selected from a group consisting of i) hydrogen and ii) C_1-6-alkyl; R⁵ is a 5-6-member heteroaryl with 1-2 nitrogen atoms, substituted with halogen, R⁶ represents hydrogen; R⁷ represents hydrogen; R⁸ represents hydrogen; R⁹ represents hydrogen; or R⁶ and R⁸ together form a 5-6-member heterocyclyl containing 1 oxygen atom, X is selected from a group consisting of i) -S and ii) -SO₂.

EFFECT: compounds are useful in therapeutic and/or preventive treatment, for example, Alzheimer's disease and diabetes type 2.

29 cl, 8 tbl, 14 ex