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Buprenorphine analogs as agonists and / or opioid receptor antagonists
专利权人:
Purdue Pharma L.P.
发明人:
KYLE, Donald J.,TAFESSE, Laykea
申请号:
ES11776855
公开号:
ES2566828T3
申请日:
2011.09.20
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
A compound of Formula I: ** Formula ** in which R1 is selected from hydrogen, -alkyl- (C1-C10), alkenyl- (C2-C12), alkynyl- (C2-C12), alkoxy- (C1- C10), cycloalkyl- (C3-C12), (cycloalkyl (C3-C12)) - alkyl- (C1-C6), heteroaryl- (5 to 12 members) and (heteroaryl (10 to 12 members)) - alkyl - (C1-C6); any of which is optionally substituted with 1, 2, or 3 substituents that are independently selected from the group consisting of alkyl- (C1-C6), -COOR7 and -CONR9R10; R2 and R8 are each independently hydrogen, alkyl- (C1-C10), alkynyl- (C2-C12), alkoxy- (C1-C10), - (OCH2CH2) s-Oalkyl (C1-C6), - (CH2CH2O) s-(C1-C6) alkyl, -NH2, -NH (C1-C6) alkyl, -CONR5R6, alkyl- (C1-C6) -CO-NR5R6, -COOR7, alkyl- (C1-C6) -CO-OR7, cycloalkyl- (C3-C12), aryl- (5 to 12 members), (aryl (5 to 12 members)) - alkyl- (C1-C6), heteroaryl- (5 to 12 members), bicycloheterocycle- ( 7 to 12 members), phenyl, benzyl or naphthyl; each of which is optionally substituted with one or two substituents that are independently selected from the group consisting of -OH, halo, -C (halo) 3, -CH (halo) 2, - CH2 (halo), alkyl- ( C1-C6), alkenyl- (C2-C6), alkynyl- (C2-C6), hydroxyalkyl- (C1-C6), dihydroxyalkyl- (C1-C6), alkoxy- (C1-C6), (alkoxy (C1- C6)) CO-C1-C6 alkoxy, phenyl, benzyl, -NH2, -CN, -OR4, -CONR5R6, - (C1-C6 alkyl) -CO-NR5R6, -COOR7, alkyl- (C1-C6) - CO-OR7, alkoxy- (C1-C6) -COOR7, - (OCH2CH2) s-Oalkyl (C1-C6), -NH-SO2alkyl (C1-C6), -N (SO2alkyl (C1-C6)) 2, - C (>; = NH) NH2, -NH-CO-(C1-C6) alkyl, -NH-CO-NH2, - NH-C (>; = O) -NH-(C1-C6) alkyl, -NH-C (>; = O) aryl- (5 to 12 members), -NH-(C1-C6) alkyl -CO-OR7, -NH-C (>; = O) - (C1-C6) alkyl -CO-OR7, aryl- (5 to 12 members), -NH-(C1-C6) alkyl -C (O) -NR5R6, -C (O) NH-alkyl (C1-C6) - COOR7, heteroaryl- (5 to 12 members) and (heteroaryl (5 to 12 members)) - (C1-C6) alkyl -; wherein at least one of R2 and R8 is alkyl- (C1-C10), alkynyl- (C2-C12), alkoxy- (C1-C10), - (OCH2CH2) s- Oalkyl (C1-C6), - ( CH2CH2O) s-(C1-C6) alkyl, NH2, -NH (C1-C6) alkyl, -C
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