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ANALOGOS DE BUPRENORFINA
专利权人:
PURDUE PHARMA L.P.
发明人:
KYLE, DONALD J.,TAFESSE, LAYKEA
申请号:
PE0005482013
公开号:
PE00202014A1
申请日:
2011.09.20
申请国别(地区):
PE
年份:
2014
代理人:
摘要:
Refers to the analogues of buprenorphine compounds of formula I, Ia, IB, where R1 is H, heteroaryl phenyl, Benzyl, among others R2 is H, (C1 - C10 alkyl (C12), C2) alquenil, among others R8 is H, phenyl, Benzyl, among others, R3A and R2H are independently (C2 C10) alquenil (C1 - C6), Hydroxy alkyl at Tre X is - Oh, dihydroxy (C1 - C6 alkyl Halogen), among others Q is - (C1 - C10 alkoxy),- (C1 - C10 alkyl) Z is (CH2) m, where M is 1 - 6 - 8 -, G, S, SW, among others and it is CH - (CH2) n, where n is 0 - 6.Preferred compounds are: (4aS, 4R, 6R, 7R, 7aR, 12bs) - 6 - [(Benzyloxy) methyl) - 7 - methoxy - 3 - methyl - 4 - 1,2,3,4,5,6,7,7 to octahidro -, 7 -, 12 - metanbenzofuro ethane - [3,2 -? Isoquinolin - amino] - 9 (4aS, 4R, 6R, 7R, 7aR, 12 (BS) - 6 - (Benzyloxy) methyl) - 7 - methoxy - 3 - methyl - 1 - Vinyl - 1,2,3,4,5,6,7,7 octahidro - to - 4 -, 7 -, 12 - metanbenzofuro ethane [3,2 -? ] isoquinoline among others. In addition to such a Pharmaceutical composition.Said composition is useful in the treatment of Pain, constipation and other conditions Modulated by the activity of Opioid Receptors and orl-1SE REFIERE A LOS COMPUESTOS ANALOGOS DE BUPRENORFINA DE FORMULA I, IA, IB, DONDE: R1 ES H, HETEROARIL, FENIL, BENCIL ENTRE OTROS R2 ES H, (C1-C10) ALQUIL, (C2-C12) ALQUENIL, ENTRE OTROS R8 ES H, FENIL, BENCIL ENTRE OTROS, R3A Y R3B SON INDEPENDIENTEMENTE (C2-C10) ALQUENIL, HIDROXI(C1-C6)ALQUIL ENTRE OTROS X ES -OH,DIHIDROXI(C1-C6)ALQUIL, HALOGENO ENTRE OTROS Q ES -(C1-C10)ALCOXI,-(C1-C10)ALQUIL Z ES (CH2) m, DONDE m ES 1-6, G ES -OCO-, S, SO ENTRE OTROS Y ES (CH2)n-CH, DONDE n ES 0-6 . SON COMPUESTOS PREFERIDOS: (4R, 4aS,6R,7R,7aR,12bS)-6-((BENCILOXI)METIL)-7-METOXI-3-METIL-1,2,3,4,5,6,7,7 a-OCTAHIDRO-4 a, 7-ETANO-4,12-METANBENZOFURO[3,2- ? ] ISOQUINOLIN-9-AMINO (4R, 4aS,6R,7R,7aR,12 bS)-6-((BENCILOXI)METIL)-7-METOXI-3-METIL-9-VINIL-1,2,3,4,5,6,7,7 a-OCTAHIDRO-4 a, 7-ETANO-4,12-METANBENZOFURO[3,2- ? ] ISOQUINOLINA ENTRE OTROS. REFERIDA ADEMAS A UNA COMPOSICION FARMACE
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