Substituted 3-(Pyridinylamino)-indoles and benzo[b]thiophenes, a process for their preparation and their use as medicaments
申请人:HOECHST-ROUSSEL PHARMACEUTICALS INCORPORATED
公开号:EP0509402A1
公开(公告)日:1992-10-21
The present invention relates to compounds of the formula I
where
R₁is hydrogen, loweralkyl, loweralkenyl, loweralkynyl, arylloweralkyl, aminoloweralkyl, loweralkylaminoloweralkyl, formyl, loweralkylcarbonyl, aminoloweralkylcarbonyl or loweralkoxycarbonyl;
the group -X-Y= is
R₂ and R₃ being independently hydrogen or loweralkyl;
Wis hydrogen, halogen, hydroxy, loweralkoxy, arylloweralkoxy or
where R₄ is hydrogen, loweralkyl or arylloweralkyl; R₅ is loweralkyl or arylloweralkyl; or alternatively the group
as a whole is
, R₆ being hydrogen, loweralkyl, aryl or arylloweralkyl; and
Zis hydrogen, halogen, loweralkyl, nitro or amino;
which are useful for alleviating various memory dysfunctions such as Alzheimer's disease, as modulators of neurotransmitter functions such as serotonergic and adrenergic, and as such are useful as antidepressants, anxiolytics, atypical antipsychotics, antiemetics, and for the treatment of personality disorders such as obsessive compulsive disorders.
本发明涉及式 I 的化合物
式中
R₁是氢、低级烷基、低级烯基、低级炔基、芳基低级烷基、氨基低级烷基、氨基低级烷基、甲酰基、低级烷基羰基、氨基低级烷基羰基或低级烷氧基羰基;
基团 -X-Y= 是
R₂ 和 R₃ 独立为氢或低级烷基;
是氢、卤素、羟基、低级烷氧基、芳基低级烷氧基或
其中 R₄ 是氢、低级烷基或芳基低级烷基; R₅ 是低级烷基或芳基低级烷基;或者,该基团
作为一个整体是
R₆ 是氢、低级烷基、芳基或芳基低级烷基;以及
Z 是氢、卤素、低级烷基、硝基或氨基;
这些物质可用于缓解各种记忆功能障碍,如阿尔茨海默氏症,作为神经递质功能的调节剂,如血清素能和肾上腺素能,因此可用作抗抑郁药、抗焦虑药、非典型抗精神病药、止吐药,以及用于治疗人格障碍,如强迫症。