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Details for Patent: 6,420,390

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Details for Patent: 6,420,390

Title: Heteroarylpiperidines and their use as antipsychotics
Abstract:Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Inventor(s): Strupczewski; Joseph T. (Flemington, NJ), Glamkowski; Edward J. (Warren, NJ), Chiang; Yulin (Covent Station, NJ), Bordeau; Kenneth J. (Kintnersville, PA), Nemoto; Peter A. (Raritan, NJ), Tegeler; John J. (Bridgewater, NJ)
Assignee: Aventis Pharmaceuticals Inc. (Bridgewater, NJ)
Filing Date:Apr 19, 2000
Application Number:09/556,116
Claims:1. N-(2,3-Epoxypropyl)4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidine and its pharmaceutically acceptable acid addition salts.

2. 1-[4-(6-Fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]-2-propanone and its pharmaceutically acceptable acid addition salts.

3. 1-[4-[3-[4-(6-Fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]propoxy]-3-metho xyphenyl]-2-hydroxyethanone and its pharmaceutically acceptable acid addition salts.

4. A pharmaceuticlal composition which comprises a pharmaceutically acceptable carrier and a therapeutically effective amount of the compound of claim 3.

5. A depot pharmaceutical composition which comprises a pharmaceutically acceptable carrier and a therapeutically effective amount of the compound of claim 3 wherein the compound contains a hydroxy group which has been acylated.

6. The depot pharmaceutical composition of claim 5, wherein the hydroxy group is acylated with a (C.sub.4 -C.sub.18)alkanoyl group or a (C.sub.4 -C.sub.18)alkoxycarbonyl group.

7. The depot pharmaceutical composition of claim 5 which contains a pharmaceutically acceptable oil.

8. The depot pharmaceutical composition of claim 7, wherein the oil is selected from the group consisting of coconut oil, peanut oil, sesame oil, cotton seed oil, corn oil, soybean oil, olive oil and esters of fatty acids and polyfunctional alcohols.

9. The depot pharmaceutical composition of claim 6 which contains a pharmaceutically acceptable oil.

10. The depot pharmaceutical composition of claim 9, wherein the oil is selected from the group consisting of coconut oil, peanut oil, sesame oil, cotton seed oil, corn oil, soybean oil, olive oil and esters of fatty acids and polyfunctional alcohols.

11. A method for providing a long acting antipsychotic effect which comprises injecting into a mammal an amount of the composition of claim 5 sufficient to produce a long acting antipsychotic effect.

12. An antipsychotic composition which comprises the compound of claim 3 in an amount sufficient to produce an antipsychotic effect and a pharmaceutically acceptable carrier.

13. A method of treating psychoses which comprises administering to a mammal a psychoses-treating amount of a compound of claim 3.

14. An antipsychotic composition which comprises the compound of claim 1 in an amount sufficient to produce an antipsychotic effect and a pharmaceutically acceptable carrier.

15. A method of treating psychoses which comprises administering to a mammal a psychoses-treating amount of a compound of claim 1.

16. An antipsychotic composition which comprises the compound of claim 2 in an amount sufficient to produce an antipsychotic effect and a pharmaceutically acceptable carrier.

17. A method of treating psychoses which comprises administering to a mammal a psychoses-treating amount of a compound of claim 2.
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