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BUPRENORPHINE ANALOGS AS OPIOID RECEPTOR AGONISTS AND/OR ANTAGONISTS
专利权人:
PURDUE PHARMA L.P.
发明人:
KYLE, Donald J.,TAFESSE, Laykea
申请号:
RSP20160119
公开号:
RS54579B1
申请日:
2011.09.20
申请国别(地区):
RS
年份:
2016
代理人:
摘要:
The compound, pharmaceutical composition, method of treatment of a disorder, and use of a compound.A compound represented by the following formula (ciclopropano) or a pharmacologically acceptable salt of the same displays antagonism of receptor OrexinA, and thus has a potential utility for the treatment of a sleep disorder for which is effective anagonismo recipients of OrexinA, Po. R example, insomnia: where Q represents - CH or a nitrogen atom, R ~ 1A ~ and R ~ 1b ~.Each independently represent a group C ~ 1 - 6 ~ alkyl and the like, R ~ C ~ represents a hydrogen atom and the like, R ~ 2 ~ R ~ 2B ~ R ~ 2C and 2D ~ R ~ ~ each independently represent a hydrogen atom, a halogen atom, a group C (1 - 6 ~ alkyl and the like, R ~ 3A ~ R ~ B ~ R ~ 3C ~, each independently represent a hydrogen atom,A halogen atom and the like and R ~ 3d ~ represents a hydrogen atom, and so on.Jedinjenje formule Inaznačeno time što jeR1 izabran od vodonika, -(C1-C10)alkila, -(C2-C12)alkenila, -(C2-C12)alkinila, -(C1-C10)alkoksi, -(C3-C12)cikloalkila, ((C3-C12)cikloalkil)-(C1-C6)alkil-, -(5- do 12-članog)heteroarila i ((5- do 12-članog)heteroaril)-(C1-C6)alkil-; od kojih je bilo koji izborno supstituisan sa 1, 2 ili 3 supstituenta nezavisno izabrana iz grupe koja se sastoji od -(C1-C6)alkila, -COOR7 i -CONR9R10;R2 i R8 svaki su nezavisno vodonik, -(C1-C10)alkil, -(C2-C12)alkinil, -(C1-C10)alkoksi, -(OCH2CH2)s-O(C1-C6)alkil, -(CH2CH2O)s-(C1-C6)alkil, -NH2, -NH(C1-C6)alkil, -CONR5R6, -(C1-C6)alkil-CO-NR5R6, -COOR7, -(C1-C6)alkil-CO-OR7, -(C3-C12)cikloalkil, -(5- do 12-člani)aril, ((5- do 12-člani)aril)-(C1-C6)alkil-, -(5- do 12-člani)heteroaril, -(7- do 12-člani)bicikloheterocikl, fenil, benzil ili naftil; od kojih je svaki izborno supstituisan sa jednim ili dva supstituenta nezavisno izabrana iz grupe koja se sastoji od -OH, halo, -C(halo)3. -CH(halo)2, -CH2(halo), -(C1-C6)alkila, -(C2-C6)alkenila, -(C2-C6)alkinila, hidroksi(C1-C6)alkil-, dihidroksi (C1-C6)alkil-, -(C1-C6)alkoksi, ((C1-C6)alk
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