4-Pentafluorophenoxypiperidines, a process for their preparation and their use as medicaments
申请人:HOECHST-ROUSSEL
PHARMACEUTICALS INCORPORATED
公开号:EP0333027A1
公开(公告)日:1989-09-20
This invention relates to 4-pentafluorophenoxypiperidines of formula I
wherein R¹ is hydrogen or aryl; and R is a monovalent radical selected from the group consisting of hdyrogen, cyano, loweralkyl, arylloweralkyl, bis-(aryl)loweralkyl, aminoloweralkyl, (loweralkylamino)loweralkyl, (diloweralkylamino)loweralkyl, (diloweralkylphosphinyl)loweralkyl, heteroarylloweralkyl, and a group of the formula
wherein A is a loweralkylene, loweralkenylene or loweralkynylene, m is an integer having a value of zero or 1, W is CH₂ or NR⁷ wherein R⁷ is hydrogen, loweralkyl or aryl, and p is an integer having a value of zero or 1, and to a process for their preparation. The compounds, alone or in combination with one ore more pharmaceutically acceptable carriers, are useful for alleviating pain, treating depression, reducing blood pressure, and treating convulsions, and can, therefore, be used as medicaments.
本发明涉及式 I 的 4-五氟苯氧基哌啶类化合物。
其中 R¹ 为氢或芳基;R 为选自以下组别的单价基团:氢基、氰基、低级烷基、芳基低级烷基、双(芳基)低级烷基、氨基低级烷基、(低级烷基氨基)低级烷基、(稀低级烷基氨基)低级烷基、(稀低级烷基膦基)低级烷基、杂芳基低级烷基,以及式 I 所列的基团
其中 A 是低级烷基、低级烯基或低级炔基,m 是数值为 0 或 1 的整数,W 是 CH₂ 或 NR⁷,其中 R⁷ 是氢、低级烷基或芳基,p 是数值为 0 或 1 的整数。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、治疗抑郁症、降低血压和治疗抽搐,因此可用作药物。