Heteroaryl piperazine antipsychotic agents
First Claim
Patent Images
1. A compound having the formula ##STR6## wherein W1 is CR2 R3, W2 is CR4 R5, W3 is CR6 R7, and one of W1, W2 and W3 may be absent, and wherein the broken line extending from W1 to W3 represents an optional double bond between either W1 and W2 or W2 and W3, in which case two of R2, R3, R4, R5, R6 and R7 are absent;
- and wherein X1 is hydrogen, halogen (C1 -C4) alkyl, (C1 -C4) alkoxy, nitro, cyano, trifluoromethyl, or pentafluoroethyl;
Y1 is hydrogen, (C1 -C4) 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, (C1 -C4) alkyl, (C1 -C4) alkoxy, nitro, cyano, trifluoromethyl or pentafluoroethyl, or when X1 is attached to the carbon atom ortho to the carbon atom to which N-Y1 is attached then X1 and Y6 together may optionally form a saturated heterocyclic ring selected from pyrrolidine, piperidine, perhyddroazepine, 3-oxazolane and morpholine;
R1 is ##STR7## wherein B is selected from the group consisting of S, O and NY2 ;
X2 is hydrogen, halogen, (C1 -C4) alkyl, (C1 -C4) alkoxy, nitro, cyano, trifluoromethyl or pentafluoroethyl;
Y2 is hydrogen, (C1 -C4) 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, (C1 -C4) alkyl, (C1 -C4) alkoxy, nitro, cyano, trifluoromethyl or trifluoroethyl;
R2, R3, R4, R5, R6 and R7 are independently selected from the group consisting of hydrogen and lower alkyl, or any two of R2, R3, R4, R5, R6 and R7 taken together with the carbon or carbons to which they are attached form a (C3 -C7) saturated or unsaturated carbocyclic ring; and
Z is (C1 -C6) alkyl, branched (C1 -C6) alkyl, (C1 -C.sub.
6) alkenyl or branched (C1 -C6) alkenyl,and the pharmaceutically acceptable salts thereof.
1 Assignment
0 Petitions
Accused Products
Abstract
Compounds of the formula ##STR1## and pharmaceutical compositions comprising them, wherein R1, Z, X, W and Y are as defined below. The compounds are useful in the treatment of psychosis and anxiety.
-
Citations
6 Claims
-
1. A compound having the formula ##STR6## wherein W1 is CR2 R3, W2 is CR4 R5, W3 is CR6 R7, and one of W1, W2 and W3 may be absent, and wherein the broken line extending from W1 to W3 represents an optional double bond between either W1 and W2 or W2 and W3, in which case two of R2, R3, R4, R5, R6 and R7 are absent;
- and wherein X1 is hydrogen, halogen (C1 -C4) alkyl, (C1 -C4) alkoxy, nitro, cyano, trifluoromethyl, or pentafluoroethyl;
Y1 is hydrogen, (C1 -C4) 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, (C1 -C4) alkyl, (C1 -C4) alkoxy, nitro, cyano, trifluoromethyl or pentafluoroethyl, or when X1 is attached to the carbon atom ortho to the carbon atom to which N-Y1 is attached then X1 and Y6 together may optionally form a saturated heterocyclic ring selected from pyrrolidine, piperidine, perhyddroazepine, 3-oxazolane and morpholine;R1 is ##STR7## wherein B is selected from the group consisting of S, O and NY2 ;
X2 is hydrogen, halogen, (C1 -C4) alkyl, (C1 -C4) alkoxy, nitro, cyano, trifluoromethyl or pentafluoroethyl;
Y2 is hydrogen, (C1 -C4) 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, (C1 -C4) alkyl, (C1 -C4) alkoxy, nitro, cyano, trifluoromethyl or trifluoroethyl;
R2, R3, R4, R5, R6 and R7 are independently selected from the group consisting of hydrogen and lower alkyl, or any two of R2, R3, R4, R5, R6 and R7 taken together with the carbon or carbons to which they are attached form a (C3 -C7) saturated or unsaturated carbocyclic ring; and
Z is (C1 -C6) alkyl, branched (C1 -C6) alkyl, (C1 -C.sub.
6) alkenyl or branched (C1 -C6) alkenyl,and the pharmaceutically acceptable salts thereof. - View Dependent Claims (2, 3, 4, 5, 6)
- and wherein X1 is hydrogen, halogen (C1 -C4) alkyl, (C1 -C4) alkoxy, nitro, cyano, trifluoromethyl, or pentafluoroethyl;
Specification
-
- Resources
Litigation Campaign Assessment
Thank you for your request. You will receive a custom alert email when the Litigation Campaign Assessment is available.
×
-
Current AssigneePfizer Inc.
-
Original AssigneePfizer Inc.
-
InventorsHoward, Harry R.
-
Primary Examiner(s)Bond, Robert T.
-
Application NumberUS07/836,019Time in Patent Office950 DaysField of Search540/523, 544/363, 544/364, 544/121, 514/213, 514/255, 514/235.2US Class Current514/212.07CPC Class CodesC07D 417/12 linked by a chain containin...
