9-AZABICYCLO [3 . 3 . 1] NONANE DERIVATIVES AS MONOAMINE REUPTAKE INHIBITORS

摘要

The present invention relates to a 9-azabicyclo[3.3.1]nonane derivative of formula (I), wherein R¹ is H or C_1-5alkyl; X is O or NR², wherein R² is H, C_1-5alkyl or C_2-5acyl and Ar is C_6-10aryl or a 5-10 membered heteroaryl ring system, both being optionally substituted with one to three of R³-R⁵ independently selected from halogen, C_1-5alkyl, C_1-5alkoxy, C_3-6cycloalkyl, C_2-5alkenyl, C_2-5alkynyl, CN, NO₂, hydroxy, phenyl, phenoxy and phenylC_1-2alkoxy, wherein said C_1-5alkyl and C_1-5alkoxy are optionally substituted with one to three halogens and wherein said phenyl, phenoxy and phenylC_1-2alkoxy are optionally substituted with one to three substituents independently selected from halogen and methyl or two of R³-R⁵ at adjacent positions together form a methylenedioxy or propylene unit, with the proviso that the compounds exo-9-methyl-3-phenoxy-9-azabicyclo[3.3.1]nonane and N-(9-methyl-9-azabicyclo[3.3.1]non-3-yl)-1H indazole-5-amine are excluded, or a pharmaceutically acceptable salt or solvate thereof. The invention also relates to pharmaceutical compositions comprising said 9-azabicyclo[3.3.1]nonane derivatives and to their use in therapy.