BUPRENORPHINE ANALOGUES Russian patent published in 2014 - IPC C07D489/12 A61K31/485 A61P25/04 

FIELD: chemistry.

SUBSTANCE: invention relates to buprenorphine analogues of formula , where R¹ is selected from -(C₁-C₁₀)alkyl, -(C₂-C₁₂)alkenyl, -(C₃-C₁₂)cycloalkyl, ((C₃-C₁₂)cycloalkyl)-(C₁-C₆)alkyl-; any of which is optionally substituted with 1 or 2 substitutes selected from OH and -(5-12-member)heterocycle, wherein at least one carbon atom is substituted with a nitrogen heteroatom; R² and R⁸ each independently is hydrogen, -(C₁-C₁₀)alkyl, -(C₂-C₁₂)alkenyl, -(C₂-C₁₂)alkynyl, -(C₃-C₁₂)cycloalkyl, -(5-9-member)heteroaryl, where in the 5-9-member heteroaryl, at least one carbon atom is substituted with a nitrogen, oxygen or sulphur heteroatom, phenyl and naphthyl; any of which is optionally substituted with one or two substitutes selected from OH, halo, -C(halo)₃, -(C₁-C₆)alkyl, phenyl, NH₂, CN, OR⁴ and COOR⁷; at least one of R² or R⁸ is not hydrogen; R^3a and R^3b are independently selected from hydrogen and -(C₁-C₆)alkyl; R⁴ is selected from -(C₁-C₆)alkyl, -C(halo)₃ and phenyl; R⁷ is hydrogen; X is selected from (C₁-C₆)alkoxy or OH; Z is (CH₂)_m; Y is (CH₂)_n-CH or a direct bond, under the condition that when Y is a direct bond, R⁸ is absent; m equals 1 and n equals 0. The invention also relates to a pharmaceutical composition which modifies opioid receptor function and is intended to treat pain, which contains compounds of formula I, a method of preparing said composition, a method of modulating an opioid receptor and a method of treating pain.

EFFECT: compounds of formula I as opioid receptor function modulators.

37 cl, 11 dwg, 7 tbl, 6 ex