C-ARYL GLUCOSIDE DERIVATIVES, PREPARATION PROCESS AND PHARMACEUTICAL USE THEREOF Russian patent published in 2017 - IPC C07D493/10 C07H7/04 A61K31/357 A61P3/10 A61P3/04 

FIELD: chemistry.

SUBSTANCE: present invention relates to compounds of formula (I), pharmaceutically acceptable salts or stereoisomers thereof, method for production and use thereof in medicine:

where A is phenyl , or thienyl, where phenyl is substituted with 1–5 halogen atoms and -OR⁷; R⁷ is C_1-6 alkyl, where C_1-6 alkyl is optionally substituted by one or more groups selected from a deuterium, halogen, C_1-6 alkoxy and C_1-6 cycloalkoxy; or said phenyl substituted only with -OR⁷, where R⁷ is C_1-6 alkyl, and said C_1-6 alkyl is additionally substituted with 1–3 groups selected from halogen and C_3-10 cycloalkoxy; or, if A represents or thienyl, thienyl is possibly substituted with one or more groups selected from halogen, C_1-6 alkyl and phenyl, optionally substituted with deuterium or a halogen; R¹, R², R³ or R⁴ are selected from hydrogen, C_1-6 alkyl or halogen; R⁵ and R⁶ are selected from hydrogen and deuterium. Disclosed method of producing a compound of formula (I) involves conversion of compound of formula (IA) into a compound of formula (IB)

removal of protection from compound of formula (IB) to obtain a compound of formula (I); where R¹-R⁶ and A are defined above, X and Y are protective hydroxyl groups.

EFFECT: disclosed are novelsodium-dependent glucose cotransporter (SGLT)-1 inhibitors and an efficient method for preparation thereof.

16 cl, 13 ex, 2 tbl