申请人:PFIZER INC.
公开号:EP0175452A1
公开(公告)日:1986-03-26
1,3-Disubstituted piperidine compounds of the formula
and the pharmaceutically-acceptable acid-addition salts thereof; wherein
X and Y are each hydrogen, fluoro, chloro or bromo;
Z is hydrogen, fluoro or chloro;
Q represents a chemical bond, a divalent group of the formula -C(=O)- or a divalent group of the formula -CH(OH)-;
and n is an integer from 3 to 5.
The compounds possess pharmaceutical activity as neuroleptic agents, and they are useful for treating psychotic disorders, e.g. schizophrenia, in human subjects. In particular, they are useful for alleviating such symptoms as anxiety, agitation, excessive aggression, tension and social or emotional withdrawal in psychotic patients.
Certain 3-(3-methoxyphenyl)-piperidine compounds are useful as chemical intermediates to the aforementioned neuroleptic agents are also described.
式中的 1,3-二取代哌啶化合物
及其药学上可接受的酸加成盐; 其中
X 和 Y 分别为氢、氟、氯或溴;
Z 是氢、氟或氯;
Q 代表化学键、式 -C(=O)- 的二价基团或式 -CH(OH)- 的二价基团;
n 是 3 至 5 的整数。
这些化合物作为神经安定剂具有药物活性,可用于治疗人类的精神障碍,如精神分裂症。特别是,它们有助于减轻精神病患者的焦虑、激动、过度攻击、紧张和社交或情感退缩等症状。
此外,还介绍了某些 3-(3-甲氧基苯基)-哌啶化合物可用作上述神经安定剂的化学中间体。