2,6-Methano-1,3-benzodiazocines, a process for their preparation and their use as medicaments
申请人:HOECHST-ROUSSEL
PHARMACEUTICALS INCORPORATED
公开号:EP0335292A2
公开(公告)日:1989-10-04
The present invention relates to compounds of the formula I
wherein R¹ is hydrogen, loweralkyl, loweralkylcarbonyl, loweralkylaminocarbonyl, cycloalkylaminocarbonyl, loweralkoxycarbonyl, aryloxycarbonyl, or arylaminocarbonyl; R² and R³ are independently hydrogen, loweralkyl, cycloalkylloweralkyl, arylloweralkyl, or loweralkenyl; R⁴ and R⁵ are independently hydrogen or loweralkyl; Y is halogen, loweralkyl, nitro, amino, loweralkylcarbonylamino, arylcarbonylamino, formyl or loweralkylaminocarbonyl; and n is an integer having a value of zero or 1; the geometrical isomers, optical antipodes or pharmaceutically acceptable acid addition salts thereof, and to a process for their preparation.
The compound have analgesic acetivities, and can, therefore, be used as medicaments.
本发明涉及式 I 的化合物
其中R¹是氢、低级烷基、低级烷基羰基、低级烷基氨基羰基、环烷基氨基羰基、低级烷氧基羰基、芳氧基羰基或芳基氨基羰基;R²和R³独立地是氢、低级烷基、环烷基低级烷基、芳基低级烷基或低级烯基;R⁴和R⁵独立地是氢或低级烷基;Y 是卤素、低级烷基、硝基、氨基、低级烷基羰基氨基、芳基羰基氨基、甲酰基或低级烷基氨基羰基;n 是数值为 0 或 1 的整数;其几何异构体、光学对映异构体或药学上可接受的酸加成盐,以及其制备方法。
这些化合物具有镇痛乙酰活性,因此可用作药物。