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N- [4- (2-Oxo-1,2-dihydro-pyridin-4-yl) -benzyl] -benzamide derivatives as ALDH-2 inhibitors for the treatment of addiction
专利权人:
Amygdala Neurosciences; Inc.
发明人:
CANNIZZARO, Carina E.,GRAUPE, Michael,GUERRERO, Juan,LU, Yafan,STICKLEY, Robert,VENKATARAMANI, Chandrasekar,ZABLOCKI, Jeff
申请号:
ES15184883
公开号:
ES2656716T3
申请日:
2012.06.29
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
A compound of formula II: ** Formula ** in which: R1 is hydrogen, -CH2OH, -CH2OP (O) (OR20) (OR21) or optionally substituted C1-6 alkyl; R2 is hydrogen, halo, optionally substituted C1-6 lower alkyl or optionally substituted cycloalkyl; each of R3, R4, R5, R6, R9, R10, R11, R12 and R13 is independently hydrogen, hydroxyl, -OP (O) (OR20) (OR21), -CH2OH, -CH2OP (O) (OR20) ( OR21), aminocarbonyl, acyl, acylamino, -O- (C1 to C6 alkyl) -O- (C1 to C6 alkyl), cyano, halo, -SO2NR24R25, -NR24R25, optionally substituted alkyl, optionally substituted alkylene, optionally substituted alkynyl, optionally substituted alkoxy, optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted heteroaralkyl or optionally substituted heterocyclyl; R7 is hydrogen or optionally substituted C1-6 alkyl; each of R20 and R21 is independently Na +, Li +, K +, hydrogen, C1-6 alkyl; or R20 and R21 can be combined to represent a single divalent cation of Zn2 +, Ca2 + or Mg2 +. each of R24 and R25 is independently selected from hydrogen or C1-6 alkyl or when combined together with the nitrogen to which they are attached form a heterocycle; or a salt, an ester, an individual stereoisomer, a mixture of stereoisomers or a pharmaceutically acceptable tautomer thereof.Un compuesto de fórmula II:**Fórmula** en la que: R1 es hidrógeno, -CH2OH, -CH2OP(O)(OR20)(OR21) o alquilo C1-6 opcionalmente sustituido; R2 es hidrógeno, halo, alquilo C1-6 inferior opcionalmente sustituido o cicloalquilo opcionalmente sustituido; cada uno de R3, R4, R5, R6, R9, R10, R11, R12 y R13 es independientemente hidrógeno, hidroxilo, -OP(O)(OR20)(OR21), -CH2OH, -CH2OP(O)(OR20)(OR21), aminocarbonilo, acilo, acilamino, -O-(alquilo C1 a C6)-O- (alquilo C1 a C6), ciano, halo, -SO2NR24R25, -NR24R25, alquilo opcionalmente sustituido, alquileno opcionalmente sustituido, alquinilo opcionalmente sustituido, alcoxi opcionalmente sustituido, cicloalqui
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