COMPOSITIONS COMPRISING ENZYME-CLEAVABLE KETONE-MODIFIED OPIOID PRODRUGS AND OPTIONAL INHIBITORS THEREOF Russian patent published in 2016 - IPC C07D489/02 A61K31/485 A61P25/00 

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula KC-(II), use thereof in treating or preventing pain, method for production thereof, pharmaceutical compositions based thereon, single dose containing same, method for production thereof, method of identifying a compound of formula KC-(II), method of reducing potential abuse of composition containing a compound of formula KC-(II). In general formula KC-(II), R^a is hydrogen or hydroxyl; R⁵ is selected from (1-6C)alkyl and (1-6C) alkyl, substituted with (1-6C)alkxoycarbonyl group; each R¹ is independently selected from hydrogen and (1-6C)alkyl; each R² is independently selected from hydrogen, (1-6C)alkyl, and-C(O) NR²¹R²², where R²¹ and R²² are independently selected from a group consisting of hydrogen, (1-6C)alkyl and (1-6C)alkyl, substituted -C(O)OR⁶⁰, where R⁶⁰ is hydrogen; n equals a whole number from 2 to 4; R³ is hydrogen; R⁴ is , where each R⁶ is independently selected from hydrogen and (1-6C)alkyl, substituted guanidyl group or an amino group; W is -NR⁸-; R⁸ is hydrogen; p equals 1 or 2; and R⁷ is selected from acyl and acyl substituted with -COOH or-NHCOCH₃.

EFFECT: novel pharmaceutical compositions.

18 cl, 20 dwg, 25 tbl, 41 ex