Claims
- 1. A 2,6-substituted piperidino compound and pharmaceutically effective salts thereof, including resolved diasteriomers, enantiomers thereof, comprising the following formula:
- 2. The compound of claim 1, wherein R2 and R3 are benzene rings.
- 3. The compound of claim 2, wherein R1 is hydrogen, methyl, ethyl or propyl.
- 4. The compound of claim 1, wherein R2 and R3 are substituted benzenes containing at least one substituent selected from the group consisting of methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, isobutyl, carboxaldehyde, acetoxy, propionyloxy, isopropionyloxy, acetyl, propionyl, formyl, benzoyl, hydroxyl, methoxy, ethoxy, propoxy, isopropoxy, fluoro, chloro, bromo, iodo, and trifluoromethyl.
- 5. The compound of claim 1, wherein said compound is selected from the group consisting of N-methyl-2R-phenacyl-6S-trans-styrylpiperdine, cis-10R,2S,6R—N-methyl-6-[1-(2-hydroxy-2-phenyl)-ethyl]-2-trans-styrylpiperidine, cis-10S ,2S,6R—N-methyl-6-[1-(2-hydroxy-2-phenyl)-ethyl]-2-trans-styrylpiperidine, N-methyl-2R-phenacyl-6S-trans-styrylpiperidine, N-Methyl-2R-(2R-hydroxy-2-phenethyl)-6S-trans-styrylpiperidine, N-methyl-2R-(2S-hydroxy-2-phenethyl)-6S-trans-styrylpiperidine, and N-methyl-2R-(2-phenethyl)-6S-trans-styrylpiperidine.
- 6. A 2,6-substituted piperidino compound and pharmaceutically effective salts thereof, including resolved diasteriomers, enantiomers thereof, comprising the following formula:
- 7. The compound of claim 6, wherein R2 and R3 are benzene rings.
- 8. The compound of claim 6, wherein R1 is hydrogen, methyl, ethyl or propyl.
- 9. The compound of claim 6, wherein R1 is hydrogen, methyl, ethyl or propyl.
- 10. The compound of claim 6, wherein R2 and R3 are substituted benzenes containing at least one substituent selected from the group consisting of methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, isobutyl, carboxaldehyde, acetoxy, propionyloxy, isopropionyloxy, acetyl, propionyl, formyl, benzoyl, hydroxyl, methoxy, ethoxy, propoxy, isopropoxy, fluoro, chloro, bromo, iodo, and trifluoromethyl.
- 11. The compound of claim 6, wherein the compouond is selected from the group consisting of N-methyl-2R-trans-styryl-6S-(2-phenethyl)piperidine and N-methyl-2S-trans-styryl-6S-(2-phenethyl)piperidine.
- 12. A 2.6-substituted piperdino compound and pharmaceutically effective salts thereof following formula:
- 13. The compound of claim 12, wherein R1 is hydrogen, methyl, ethyl or propyl.
- 14. The compound of claim 12, wherein the compouond is selected from the group consisting of N-methyl-2,6-cis-di-trans-styrylpiperidine, N-methyl-2S,6S-trans-di-trans-styrylpiperidine, and N-methyl-2R,6R—trans-di-trans-styryl piperidine.
- 15. A 2,6-substituted piperidino or a 2,6-substituted piperazino compound and pharmaceutically effective salts thereof, including resolved diasteriomers, enantiomers thereof, comprising the following formula:
- 16. The compound of claim 15, wherein R1 is hydrogen, methyl, ethyl or propyl.
- 17. The compound of claim 15, wherein R2 and R3 are benzene rings.
- 18. The compound of claim 15, wherein R2 and R3 are substituted benzenes containing at least one substituent selected from the group consisting of methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, isobutyl, carboxaldehyde, acetoxy, propionyloxy, isopropionyloxy, acetyl, propionyl, formyl, benzoyl, phenyl, hydroxyl, methoxy, ethoxy, propoxy, isopropoxy, fluoro, chloro, bromo, iodo, and trifluoromethyl.
- 19. The compound of claim 15, wherein R2 and R3 are napthyl or diphenyl groups.
- 20. The compound of claim 15, wherein Z is N—R4.
- 21. The compound of claim 15, wherein Z is CH—R4.
- 22. The compound of claim 14, wherein the compound is selected from the group consisting of cis-10R,2S,6R— and cis-10S,2S,6R—N-methyl-6-[1-(2-hydroxy-2-phenyl)-ethyl]-2-trans-styrylpiperidine, cis-2S,6R—N-methyl-6-[1-(2-hydroxy-2-phenyl)ethyl]-2-phenylethylpiperidine, 2S,6R, 8S-2-[6-(β-para-toluenesulfonyloxyphenethyl)-1-methyl-2-piperidyl]-acetophenone, N-Methyl-2R-(2R-hydroxy-2-phenethyl)-6S-(2-phenethyl) piperidine, N-Methyl-2R-(2S-hydroxy-2-phenethyl)-6S-(2-phenethyl) piperidine, N-methyl-2,6-cis-di-(2-phenethyl)piperdine, 2,6-cis-diphenethylpiperidine, N-ethyl-2,6-cis-diphenethylpiperidine, N-(n-propyl)-2,6-cis-diphenethylpiperidine, 2,6-cis-di-(3,4-methylenedioxyphenethylpiperidine, N-methyl-2,6-cis-di-(3,4-methylenedioxyphenethyl-piperidine, N-methyl-2S,6S-trans-di-(2-phenethyl)piperidine, N-methyl-2R,6R-trans-di-(2-phenethyl)piperidine, 2,6-cis-di-(o-fluorophen-ethyl)piperidine, N-methyl-2,6-cis-di-(o-fluorophenethyl)-piperidine, 2,6-cis-di-(m-fluorophenethyl)piperidine, N-methyl-2,6-cis-di-(m-fluorophenethyl)-piperidine, 2,6-cis-di-(p-fluorophenethyl)piperidine, N-methyl-2,6-cis-di-(p-fluorophenethyl)-piperidine, 2,6-cis-di-(o-methoxyphenethyl)piperidine, N-methyl-2,6-cis-di-(o-methoxyphen-ethyl)piperidine, 2,6-cis-di-(m-methoxyphenethyl)piperidine, N-methyl-2,6-cis-di-(m-methoxyphenethyl)piperidine, 2,6-cis-di-(p-methoxyphenethyl)piperidine, N-methyl-2,6-cis-di-(p-methoxyphenethyl)piperidine, 2,6-cis-di-(p-methylphenethyl)piperidine, N-methyl-2,6-cis-di-(p-methylphenethyl)piperidine, 2,6-cis-di-(m-trifluoromethylphenethyl)piperidine, N-methyl-2,6-cis-di-(m-trifluoromethylphenethyl)piperidine, 2,6-cis-di-(p-phenylphenethyl)piperidine, N-methyl-2,6-cis-di-(p-phenylphenethyl)piperidine, 2,6-cis-di-(p-hydroxymethylphenethyl)-piperidine, 2,6-cis-di-(p-acetoxymethylphenethyl)piperidine, 2,6-cis-di-(2,4-dichlorophenethyl)-piperidine, N-methyl-2,6-cis-di-(2,4-dichlorophenethyl)piperidine, 2,6-cis-di-(1-naphthalen-ethyl)piperidine, N-methyl-2,6-cis-di-(1-naphthalenethyl)piperidine, 2,6-cis-di-(2-naphthalen-ethyl)piperidine, N-methyl-2,6-cis-di-(2-naphthalenethyl)piperidine, 2,6-cis-diphenethyl-piperazine, and 1,4-dimethyl-2,6-cis-diphenethylpiperazine.
- 23. A 2,6-substituted piperidino or a 2,6-substituted piperazino compound and pharmaceutically effective salts thereof, including resolved diasteriomers, enantiomers thereof, comprising the following formula:
- 24. The compound of claim 23, wherein R2 and R3 are benzene rings.
- 25. The compound of claim 23, wherein R2 and R3 are substituted benzenes containing at least one substituent selected from the group consisting of methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, isobutyl, carboxaldehyde, acetoxy, propionyloxy, isopropionyloxy, acetyl, propionyl, formyl, benzoyl, hydroxyl, methoxy, ethoxy, propoxy, isopropoxy, fluoro, chloro, bromo, iodo, and trifluoromethyl.
- 26. The compound of claim 23, wherein the compound is 2,6-cis-2-phenethynyl-6-phenethylperidin-4-one or 2,6-trans-2-phenethynyl-6-phenethylperidin-4-one
- 27. A method of treating an individual for dependence on a drug of abuse, withdrawal from a drug of abuse, an eating disorder, or a CNS disease or pathology comprising administering to the individual a therapeutically effect amount of a compound of claim 1.
- 28. A method of treating an individual for dependence on a drug of abuse, withdrawal from a drug of abuse, an eating disorder, or a CNS disease or pathology comprising administering to the individual a therapeutically effect amount of a compound of claim 5.
- 29. A method of treating an individual for dependence on a drug of abuse, withdrawal from a drug of abuse, an eating disorder, or a CNS disease or pathology comprising administering to the individual a therapeutically effect amount of a compound of claim 6.
- 30. A method of treating an individual for dependence on a drug of abuse, withdrawal from a drug of abuse, an eating disorder, or a CNS disease or pathology comprising administering to the individual a therapeutically effect amount of a compound of claim 11.
- 31. A method of treating an individual for dependence on a drug of abuse, withdrawal from a drug of abuse, an eating disorder, or a CNS disease or pathology comprising administering to the individual a therapeutically effect amount of a compound of claim 15.
- 32. A method of treating an individual for dependence on a drug of abuse, withdrawal from a drug of abuse, an eating disorder, or a CNS disease or pathology comprising administering to the individual a therapeutically effect amount of a compound of claim 22.
- 33. A method of treating an individual for dependence on a drug of abuse, withdrawal from a drug of abuse, an eating disorder, or a CNS disease or pathology comprising administering to the individual a therapeutically effect amount of a compound of claim 23.
- 34. A method of treating an individual for dependence on a drug of abuse, withdrawal from a drug of abuse, an eating disorder, or a CNS disease or pathology comprising administering to the individual a therapeutically effect amount of a compound of claim 26.
Parent Case Info
[0001] This application is a continuation-in-part of Application Ser. No. 10/231,156 filed Aug. 30, 2002, which in turn is a divisional of Application Ser. No. 09/628,557 filed Jul. 28, 2000, now U.S. Pat. No. 6,455,543 B1, which in turn claims priority under 35 U.S.C. § 119(e)(1) to provisional Application No. 60/146,144 filed Jul. 30, 1999, all of which is incorporated herein by reference.
Provisional Applications (1)
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Number |
Date |
Country |
|
60146144 |
Jul 1999 |
US |
Divisions (1)
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Number |
Date |
Country |
Parent |
09628557 |
Jul 2000 |
US |
Child |
10231156 |
Aug 2002 |
US |
Continuation in Parts (1)
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Number |
Date |
Country |
Parent |
10231156 |
Aug 2002 |
US |
Child |
10813647 |
Mar 2004 |
US |