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Claims for Patent: 5,256,664

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Claims for Patent: 5,256,664

Title: Antidepressant 3-halophenylpiperazinylpropyl derivatives of substituted triazolones and triazoldiones
Abstract:2-(3-[4-(3-Halophenyl)-1-piperazinyl]propyl derivatives of certain 4-alkyl- or 4-phenoxyalkyl-2,4-dihydro-3H-1,2,4-triazol-3-ones and triazol-3,5-diones are psychotropic agents having promise as antidepressants by virtue of their receptor site binding affinity profiles and animal pharmacology.
Inventor(s): Mayol; Robert F. (Durham, CT), Luke; George M. (LaFayette, NY)
Assignee: Bristol-Myers Squibb Company (New York, NY)
Application Number:07/875,044
Patent Claims: 1. A compound of Formula I ##STR10## or a pharmaceutically acceptable acid addition salt and/or hydrate thereof wherein

R is halogen or trifluoromethyl;

X is oxygen or acetyl;

the single and dotted lines represent either a covalent single or double bond;

n is an integer from 2 to 4; and

Z is hydrogen or ##STR11## in which R.sup.1 is hydrogen, halogen, C.sub.1-4 alkoxy or trifluoromethyl.

2. The compound of claim 1 wherein X is acetyl.

3. The compound of claim 1 wherein X is oxygen.

4. The compound of claim 1 wherein Z is ##STR12##

5. The compound of claim 1 wherein R is 3-chloro.

6. The compound of claim 4 wherein R.sup.1 is hydrogen.

7. The compound of claim 2, 2-(3-[4-(3-chlorophenyl)-1-piperazinyl]propyl)-5-acetyl-2,4-dihydro-4-(2-p henoxyethyl)-3H-1,2,4-triazol-3-one hydrochloride.

8. The compound of claim 3, 2-(3-[4-(3-chlorophenyl)-1-piperazinyl]propyl)-4-(2-phenoxyethyl)-4H-1,2,4 -triazole-3,5(1H,2H)-dione hydrochloride.

9. The antidepressant method which comprises administering to a mammalian host with depression, an effective antidepressant dose of a compound claimed in claim 1.

10. The antidepressant method which comprises administering to a mammalian host with depression, an effective antidepressant dose of a compound claimed in claim 7.

11. The antidepressant method which comprises administering to a mammalian host with depression, an effective antidepressant dose of a compound claimed in claim 8.

12. A pharmacological composition in unit dosage form suitable for systemic administration to a mammalian host comprising a pharmaceutical carrier and an effective antidepressant amount of a compound claimed in claim 1.

13. A pharmacological composition in unit dosage form suitable for systemic administration to a mammalian host comprising a pharmaceutical carrier and an effective antidepressant amount of a compound claimed in claim 7.

14. A pharmacological composition in unit dosage form suitable for systemic administration to a mammalian host comprising a pharmaceutical carrier and an effective antidepressant amount of a compound claimed in claim 8.
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