| 摘要 |
This invention provides O-alpha-acyloxyalkyl ethers of the venlafaxine metabolite 4-[2-(Dimethylamino-1-(1-hydroxycyclohexyl)ethyl]phenol, represented by Formula (I):wherein:the configuration at the steriogenic center (*) may be R, S, or RS (the racemate);R1 is selected from C1-C6 alkyl, C1-C6 alkoxy, C3-C6 cycloalkyl, or the moiety:R2 is selected from H, or C1-C6 alkyl; or,R1 and R2 may be concatenated such that form a moiety having formula (b):R3 is selected from H or C1-C6 alkyl; andR4 and R5 are independently selected from H, C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, C1-C6 thioalkoxy, -CN, -OH, -CF3, -OCF3, halogen, -NH2, -NO2, or mono or dialkylamino wherein each alkyl group has 1 to 6 carbon atoms, or pharmaceutically acceptable salts or hydrates thereof, R, S, or RS forms thereof; as well as pharmaceutical compositions and methods treating central nervous system disorders.
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