CARROLL, FRANK IVY,NAVARRO, HERMAN A.,BRIEADDY, LAWRENCE E.,RUNYON, SCOTT P.
申请号：
ES06735365
公开号：
ES2383322T3
申请日:
2006.02.17
申请国别(地区):
ES
年份:
2012
代理人:
摘要：
A kappa opioid receptor antagonist compound represented by the formula (I): in which G is H, OH, OCO C1-8 alkyl, CONH2, NHCHO, NH2, NHSO2 C1-8 alkyl, or NHCO2 C1-8 alkyl； R1 it is C1-8 alkyl, or one of the following structures: Y1 is H, OH, Br, Cl, F, CN, CF3, NO2, N3, OR8, CO2R9, C1-6 alkyl, NR10R11, NHCOR12, NHCO2R12, CONR13R14, or CH2 (CH2) nY2； Y2 is H, CF3, CO2R9, C1-6 alkyl, NR10R11, NHCOR12, NHCO2R12, CONR13R14, CH2OH, CH2OR8, or COCH2R9； Y3 is H, OH, Br, Cl, F, CN, CF3 , NO2, N3, OR8, CO2R9, C1-6 alkyl, NR10R11, NHCOR12, NHCO2R12, CONR13R14, or CH2 (CH2) nY2； R2 is H, C1-8 alkyl, C3-8 alkenyl, C3-8 alkynyl or CH2 aryl substituted by one or more groups Y1； R3 is H, C1-8 alkyl, C3-8 alkenyl, C3-8 alkynyl or aryl CH2 substituted by one or more groups Y1； wherein R2 and R3 can be joined together to form a C2-8 alkyl group； R4 is hydrogen, C1-8 alkyl, CO2 C1-8 alkylaryl substituted by one or more Y1 groups, CH2 aryl substituted by one or more Y1 or CO2 groups C1-8 alkyl； Z is N, O or S； when Z is O or S, there is no R5； R5 is H, C1-8 alkyl, C3-8 alkenyl, C3-8 alkynyl, CH2CO2 C1-8 alkyl, CO2 C1-8 alkyl or aryl CH2 substituted by one or more groups Y1 ； (when Z is O or S, there is no R5): n is 0, 1, 2 or 3； R6 is a group selected from the group consisting of structures (a) - (p):Un compuesto antagonista del receptor opioide kappa representado por la fórmula (I):5en la que G es H, OH, OCO alquilo C1-8, CONH2, NHCHO, NH2, NHSO2 alquilo C1-8, o NHCO2 alquilo C1-8；R1 es alquilo C1-8, o una de las siguientes estructuras:Y1 es H, OH, Br, Cl, F, CN, CF3, NO2, N3, OR8, CO2R9, alquilo C1-6, NR10R11, NHCOR12, NHCO2R12, CONR13R14,o CH2(CH2)nY2；Y2 es H, CF3, CO2R9, alquilo C1-6, NR10R11, NHCOR12, NHCO2R12, CONR13R14, CH2OH, CH2OR8, o COCH2R9；Y3 es H, OH, Br, Cl, F, CN, CF3, NO2, N3, OR8, CO2R9, alquilo C1-6, NR10R11, NHCOR12, NHCO2R12, CONR13R14,o CH2(CH2)nY2；R2 es H, alquilo C1-8, alquenilo C3-8, alquinilo C3-8 o arilo CH2 sustituido por uno o más grupos Y1；R3 es H, alquilo C
