1-Carbonylderivatives of 4-aryl-4-aryloxypiperidines, a process for their preparation and their use as medicaments
申请人:HOECHST-ROUSSEL
PHARMACEUTICALS INCORPORATED
公开号:EP0333025A1
公开(公告)日:1989-09-20
This invention relates to 1-carbonyl and 1-thiocarbonyl derivatives of 4-aryl-4-aryloxypiperidines of the formula I
wherein Ar is phenyl optionally substituted by one or more loweralkyl, loweralkoxy, halogen, or trifluoromethyl groups; Ar¹ is phenyl optionally substituted by one or more halogen, nitro, amino or trifluoromethyl groups; A is oxygen or sulfur; and R is hydrogen, loweralkyl, arylloweralkyl, heteroarylloweralkyl, amino, loweralkylamino, diloweralkylamino, or arylamino, which compounds, alone or in combination with one or more pharmaceutically acceptable carriers, are useful for alleviating pain, and treating convulsions.
The invention relates, furthermore, to a process for the preparation of the above compounds.
本发明涉及式 I 的 4-芳基-4-芳氧基哌啶的 1-羰基和 1-硫代羰基衍生物
其中 Ar 是可选被一个或多个低级烷基、低级烷氧基、卤素或三氟甲基取代的苯基;Ar¹ 是可选被一个或多个卤素、硝基、氨基或三氟甲基取代的苯基;A 是氧或硫;这些化合物单独或与一种或多种药学上可接受的载体结合,可用于减轻疼痛和治疗抽搐。
此外,本发明还涉及上述化合物的制备工艺。