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Buprenorphine analogues
专利权人:
PURDUE PHARMA LP
发明人:
KYLE, DONALD,GOEHRING, R.,FUNDYTUS, MARIAN
申请号:
ES09789036
公开号:
ES2449222T3
申请日:
2009.07.30
申请国别(地区):
ES
年份:
2014
代理人:
摘要:
Compound of Formula III: ** Formula ** in which R1 is selected from -C1-C10 alkyl, -C2-C12-alkenyl, C2-C12-alkynyl, -C3-C12-alkyl-alkyl, - (C4-C12) cycloalkenyl, ((C3-C12) cycloalkyl) - (C1-C6) alkyl -, ((C4-C12) cycloalkenyl) - (C1-C6) alkyl -, -aryl (5 to 12 members), (aryl (5 to 12 members)) - (C1-C6) alkyl -, - heteroaryl (5 to 12 members) and - heterocycle (3 to 12 members); any of which is optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of -C1-C6 alkyl, OH, halo, -C (halo) 3, -CH (halo) 2, -CH2 (halo) , NH2, -NH-(C1-C6) alkyl, CN, SH, -carbocyclic ring (5 to 12 members), -heterocycle (5 to 12 members), phenyl, and benzyl; R2 and R8 are each independently hydrogen, -C1-C10-alkyl, -C2-C12-alkenyl, -C2-C12-alkynyl, -C3-C12-cycloalkyl, - (C3-C12-alkyl )) - (C1-C6) alkyl, -C-cycloalkenyl (C4-C12), -bicycloalkyl (C6-C14), -trichloralkyl (C8-C20), -bicycloalkenyl (C7-C14), -cycloalkenyl (C8-C20), -aryl (5 to 12 members), (aryl (5 to 12 members)) - alkyl (C1-C6) -, -cyclic ring system (7 to 12 members), -cyclic aryl (7 to 12 members), -heteroaryl (5 to 12 members), -heterocycle (3 to 12 members), or -bicycloheterocycle (7 to 12 members); any of which is optionally substituted with one or two substituents independently selected from the group consisting of OH, (>; = O), halo, -C (halo) 3, -CH (halo) 2, -CH2 (halo), -alkyl (C1 -C6), halo (C1-C6) alkyl -, - (C2-C6) alkenyl, - (C2-C6) alkynyl, hydroxy (C1-C6) alkyl -, phenyl, benzyl, NH2, -NH-alkyl (C1-C6), CN, SH, OR4, CONR5R6 and COOR7; R3a and R3b are each independently selected from hydrogen, -alkyl (C1-C6), -alkenyl (C2-C6), -alkynyl (C2-C6), OH, hydroxy-alkyl (C1-C6) - , -C (halo) 3, -CH (halo) 2, and -CH2 (halo), or together form (>; = O); R4 is selected from -alkyl (C1-C6), -alkenyl (C2-C6) , - (C2-C6) alkynyl, -C (halo) 3, hydroxy (C1-C6) alkyl -, - (C3-C12) cycloalkyl, (C6-C14) alkylcycloalkyl (C8-C20) alkyl, -Cycloalkenyl (C4-C12), -bicycloalkenyl (C7-C14
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