1,2,4,5-Tetra-alkyl-4-arylpiperidines, their production and pharmaceutical preparations containing same
申请人:ELI LILLY AND COMPANY
公开号:EP0013078A2
公开(公告)日:1980-07-09
Compounds of formula
wherein
R' is hydrogen, hydroxy or methoxy,
R2, R3 and R4 independently are C1-C5 alkyl;
R. is C1-C10 alkyl, benzyl or CH2R6, in which R6 is C2-7 alkenyl or C3-C6 cycloalkyl; the pharmaceutically acceptable acid addition and quaternary piperidinium salts thereof, are potent analgesics. Pharmaceutical formulations containing such compounds, a method for effecting anaigesia, intermediates and a process for preparing such compounds, are provided.
式中 R' 为氢、羟基或甲氧基,R2、R3 和 R4 独立地为 C1-C5 烷基;R. 为 C1-C10 烷基、苄基或 CH2R6,其中 R6 为 C2-7 烯基或 C3-C6 环烷基;其药学上可接受的酸加成盐和季哌啶盐的化合物是强效镇痛剂。 本研究提供了含有此类化合物的药物制剂、实现镇痛的方法、中间体以及制备此类化合物的工艺。