This invention provides O-.alpha.-acyloxyalkyl ethers of the venlafaxine
metabolite 4-[2-(Dimethylamino-1-(1-hydroxycyclohexyl)ethyl]phenol,
represented by Formula (I):
##STR1##
wherein:
the configuration at the steriogenic center (*) may be R, S, or RS (the
racemate);
R.sub.1 is selected from C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy,
C.sub.3 -C.sub.6 cycloalkyl, or the moiety:
##STR2##
R.sub.2 is selected from H, or C.sub.1 -C.sub.6 alkyl; or,
R.sub.1 and R.sub.2 may be concatenated such that
##STR3##
form a moiety having formula (b):
##STR4##
R3 is selected from H or C.sub.1 -C.sub.6 alkyl; and
R4 and R5 are independently selected from H, C.sub.1 -C.sub.6 alkyl,
C.sub.3 -C.sub.6 cycloalkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6
thioalkoxy, --CN, --OH, --CF.sub.3, --OCF.sub.3, halogen, --NH.sub.2,
--NO.sub.2, 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.
