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Details for Patent: 4,883,795

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Details for Patent: 4,883,795

Title: Piperazinyl-heterocyclic compounds
Abstract:Arylpiperazinyl-ethyl (or butyl)-heterocyclic compounds and their pharmaceutically acceptable acid addition salts are neuroleptic agents. They are useful in the treatment of psychotic disorders.
Inventor(s): Lowe, III; John A. (Stonington, CT), Nagel; Arthur A. (Gales Ferry, CT)
Assignee: Pfizer Inc. (New York, NY)
Filing Date:Jan 23, 1989
Application Number:07/300,995
Claims:1. A compound of the formula ##STR4## or a pharmaceutically acceptable acid addition salt thereof, wherein Ar is naphthyl optionally substituted by fluoro, chloro, trifluoromethyl, methoxy, cyano or nitro; quinolyl; 6-hydroxy-8-quinolyl; isoquinolyl; quinazolyl; benzothiazolyl; benzothiadiazolyl; benzotriazolyl; benzoxazolyl;, benzoxazolonyl; indolyl; indanyl optionally substituted by one or two fluoro; 3-indazolyl optionally substituted by 1-trifluoromethylphenyl; or phthalazinyl;

n is 1 or 2; and

X and Y together with the phenyl to which they are attached form quinolyl; 2-hydroxyquinolyl; benzothiazolyl; 2-aminobenzothiazolyl; benzoisothiazolyl; indazolyl; 2-hydroxyindazolyl; indolyl; spiro; oxindolyl optionally substituted by one to three of (C.sub.1 -C.sub.3)alkyl, or one of chloro, fluoro or phenyl, said phenyl optionally substituted by one chloro or fluoro; benzoxazolyl; 2-aminobenzoxazolyl; benzoxazolonyl; 2-aminobenzoxazolinyl; benzothiazolonyl; benzoimidazolonyl; or benzotriazolyl.

2. A compound according to claim 1 wherein X and Y together with the phenyl to which they are attached form benzoxazolonyl.

3. A compound according to claim 2 wherein Ar is naphthyl and n is 1.

4. A compound according to claim 1 wherein X and Y together with the phenyl to which they are attached form oxindole.

5. A compound according to claim 5 wherein Ar is naphthyl and n is 1.

6. A pharmaceutical composition having neuroleptic activity comprising a compound according to claim 1 in an amount effective in the treatment of neuroleptic diseases, and a pharmaceutically acceptable carrier.

7. A composition according to claim 6 wherein X and Y together with the phenyl to which they are attached form benzoxazolonyl.

8. A composition according to claim 7 wherein Ar is naphthyl and n is 1.

9. A composition according to claim 6 wherein X and Y together with the phenyl to which they are attached form oxindole.

10. A composition according to claim 9 wherein Ar is naphthyl and n is 1.

11. A method of treating neuroleptic diseases which comprises administering to a subject in need of treatment a neuroleptic amount of a compound according to claim 1.

12. A compound of the formula ##STR5## or a pharmaceutically acceptable acid addition salt thereof, wherein Ar is naphthyl optionally substituted by fluoro, chloro, trifluoromethyl, methoxy, cyano or nitro; quinolyl; 6-hydroxy-8-quinolyl; isoquinolyl; quinazolyl; benzoisothiazolyl or an oxide or dioxide thereof each optionally substituted by fluoro, chloro, trifluoromethyl, methoxy, cyano, or nitro; benzothiazolyl; benzothiadiazolyl; benzotriazolyl; benzoxazolyl; benzoxazolonyl; indolyl; indanyl optionally substituted by one or two fluoro; 3-indazolyl optionally substituted by 1-trifluoromethylphenyl; or phthalazinyl;

n is 1 or 2; and

X and Y together with the phenyl to which they are attached form quinolyl; 2-hydroxyquinolyl; or spiro.

13. A compound according to claim 12 wherein Ar is benzoisothiazolyl and n is 1.

14. A pharmaceutical composition having neuroleptic activity comprising a compound according to claim 12 in an amount effective in the treatment of neuroleptic diseases, and a pharmaceutically acceptable carrier.

15. A composition according to claim 12 wherein Ar is benzoisothiazolyl and n is 1.

16. A method of treating neuroleptic diseases which comprises administering to a subject in need of treatment a neuroleptic amount of a compound according to claim 12.
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