申请人:WARNER-LAMBERT COMPANY
公开号:EP0170460A1
公开(公告)日:1986-02-05
A compound having the following general formula I:
wherein A is the radical -NR1R2 in which R, and R2 are independently hydrogen, lower alkyl, or lower alkenyl; or wherein A is the radical -NHR3 in which R3 is phenyl, phenylmethyl, N,N-bis (1-methylethyl)- aminoethyl or 4-pyridyl; or wherein A is the radical -OR4 in which R4 is lower alkyl, phenyl (optionally substituted in the 2-, 3-, or 4- position with one or more of a chlorine, fluorine, lower alkoxy or phenylmethoxy), or phenylmethyl (optionally substituted in the 2-, 3-, or 4- position with one or more of a chlorine, fluorine, lower alkoxy or phenyl (methoxy); and the pharmaceutically acceptable salts of those compounds of formula I having a basic nitrogen atom. The compounds are effective as cognition activators for treating senility or for reversing the effects of electroshock induced amnesia. A process for producing the compounds, a useful intermediate in their preparation and pharmaceutical compositions are also disclosed.
具有以下通式 I 的化合物
其中 A 是基团-NR1R2,其中 R 和 R2 独立地为氢、低级烷基或低级烯基;或 其中 A 是基团-NHR3,其中 R3 为苯基、苯基甲基、N,N-双(1-甲基乙基)-氨基乙基或 4-吡啶基;或其中 A 是基团-OR4,其中 R4 是低级烷基、苯基(可选择在 2-、3-或 4-位被氯、氟、低级烷氧基或苯基甲氧基中的一种或多种取代)或苯基甲基(可选择在 2-、3-或 4-位被氯、氟、低级烷氧基或苯基(甲氧基)中的一种或多种取代);以及具有碱性氮原子的式 I 化合物的药学上可接受的盐。这些化合物作为认知激活剂可有效治疗老年痴呆症或逆转电击诱导的失忆症的影响。此外,还公开了生产这些化合物的工艺、制备这些化合物的有用中间体以及药物组合物。