SELECTIVE GLYCOSIDASE INHIBITORS AND USE THEREOF Russian patent published in 2016 - IPC C07H9/06 C07D513/04 A61K31/7056 A61K31/429 A61P9/00 A61P11/06 A61P25/28 A61P29/00 A61P37/08 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, where each R represents H; R¹ and R² are independently selected from a group consisting of H, C_1-6alkyl, C_2-6alkenyl, C_1-6alkoxy and -(CH₂)_n-cyclopropyl, where n equals 1 or 2; or R¹ and R² can be bonded together with a nitrogen atom to which they are bonded to form azetidine, pyrrolidine or isoxazolidine, where said C_1-6alkyl is optionally substituted by fluorine or hydroxy; R³ is selected from a group consisting of C_1-8alkyl, C_2-8alkenyl, C_3-6cycloalkyl, phenyl and pyridine, each optionally substituted with 1-3 substitutes selected from fluorine and OH; R⁴ is selected from a group consisting of H, F or C_1-8alkyl; or R³ and R⁴ and a carbon atom to which they are bonded, can be combined together to form vinyl or 3-7-membered carbocyclic ring, wherein said 3-7-member carbocyclic ring optionally contains a double bond; and R⁵ is selected from H, F and OH; provided that when R⁴ represents F while R⁵ is other than OH. Invention also relates to specific derivatives of pirano[3,2d]thiazole. Disclosed compounds are intended for producing a pharmaceutical composition possessing inhibitory activity on O-GlcNAcase, containing an active ingredient in an effective amount of compound or its pharmaceutically acceptable salt in combination with pharmaceutically acceptable carrier.

EFFECT: technical result is a compound for selective inhibition of glycosidase.

15 cl, 1 tbl, 218 ex