KAJL Donal'd Dzh. (US),КАЙЛ Дональд Дж. (US),GERING R. Richard (US),ГЕРИНГ Р. Ричард (US),FANDITAS Mehrian E. (US),ФАНДИТАС Мэриан Е. (US),KAJL DONALD DZH.,КАЙЛ Дональд Дж.,GERING R. RICHARD,ГЕРИНГ Р. Ричард,FANDITAS MEHRIAN E.,ФАНДИТАС Мэриан Е.
申请号：
RU2011107440/04
公开号：
RU0002520222C2
申请日:
2009.07.30
申请国别(地区):
RU
年份:
2014
代理人:
摘要：
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； R3a and R3b 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 exИзобретение относится к аналогам бупренорфина Формулы I, где R1 выбран из -(С1-С10)алкила, -(С2-С12)алкенила, -(С3-С12)циклоалкила, ((С3-С12)циклоалкил)-(С1-С6)алкила-； любой из которых необязательно замещен 1 или 2 заместителями, выбранными из ОН и -(5-12-членного)гетероцикла, в котором, по крайней мере, один атом углерода замещен гетероатомом азота； R2 и R8 каждый независимо представляет собой водород, -(С1-С10)алкил, -(С2-С12)а
