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US 5,350,747 AGranted
Heteroaryl piperazine antipsychotic agents
AssigneePfizer Inc.
InventorHarry R. Howard
Life of this patent
Estimating the term…
Abstract
Compounds of the formula ##STR1## and pharmaceutical compositions comprising them, wherein R.sup.1, Z, X, W and Y are as defined below. The compounds are useful in the treatment of psychosis and anxiety.
Claims6
A compound having the formula ##STR6## wherein W.sup.1 is CR.sup.2 R.sup.3, W.sup.2 is CR.sup.4 R.sup.5, W.sup.3 is CR.sup.6 R.sup.7, and one of W.sup.1, W.sup.2 and W.sup.3 may be absent, and wherein the broken line extending from W.sup.1 to W.sup.3 represents an optional double bond between either W.sup.1 and W.sup.2 or W.sup.2 and W.sup.3, in which case two of R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are absent;
- and wherein X.sup.1 is hydrogen, halogen (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkoxy, nitro, cyano, trifluoromethyl, or pentafluoroethyl;
- Y.sup.1 is hydrogen, (C.sub.1 -C.sub.4) alkyl, phenyl or substituted phenyl, wherein said substituted phenyl is substituted with one or more substituents that are independently selected from the group consisting of halogen, (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkoxy, nitro, cyano, trifluoromethyl or pentafluoroethyl, or when X.sup.1 is attached to the carbon atom ortho to the carbon atom to which N-Y.sup.1 is attached then X.sup.1 and Y.sup.6 together may optionally form a saturated heterocyclic ring selected from pyrrolidine, piperidine, perhyddroazepine, 3-oxazolane and morpholine;
- R.sup.1 is ##STR7## wherein B is selected from the group consisting of S, O and NY.sup.2 ;
- X.sup.2 is hydrogen, halogen, (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkoxy, nitro, cyano, trifluoromethyl or pentafluoroethyl;
- Y.sup.2 is hydrogen, (C.sub.1 -C.sub.4) alkyl, phenyl or substituted phenyl, wherein said substituted phenyl is substituted with one or more substituents that are independently selected from the group consisting of halogen, (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkoxy, nitro, cyano, trifluoromethyl or trifluoroethyl;
- R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are independently selected from the group consisting of hydrogen and lower alkyl, or any two of R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 taken together with the carbon or carbons to which they are attached form a (C.sub.3 -C.sub.7) saturated or unsaturated carbocyclic ring;
- and Z is (C.sub.1 -C.sub.6) alkyl, branched (C.sub.1 -C.sub.6) alkyl, (C.sub.1 -C.sub. 6) alkenyl or branched (C.sub.1 -C.sub.6) alkenyl,
- and the pharmaceutically acceptable salts thereof.
5 more elements
Dependencies are inferred from the claim text.