PHACETOPERANE FOR TREATING OF ATTENTION DEFICIT HYPERACTIVITY DISORDER

• US 20180214436A1
• Filed: 03/06/2018
• Published: 08/02/2018
• Est. Priority Date: 11/29/2011
• Status: Active Grant

• Current Assignee: NLS-1 Pharma AG
• Original Assignee: NLS Pharma AG
• Inventors: KONOFAL, Eric, FIGADERE, Bruno
• Granted Patent: US 10,456,387 B2
• Time in Patent Office: Days
• CPC Class Codes: A61K 31/445 Non condensed piperidines, e.g. piperocaine
• CPC Class Codes: A61K 31/4458 only substituted in position 2, e.g. methylphenidate
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/20 Hypnotics; Sedatives
• CPC Class Codes: C07D 211/22 by oxygen atoms
• CPC Class Codes: Y02P 20/55 Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Abstract

The invention relates to the treatment of an attention deficit hyperactivity disorder (ADHD) with alpha-phenyl(piperidin-2-yl)methanol, or the pharmaceutically acceptable salts and esters thereof, in particular the acetate derivative, more particularly dextrophacetoperane. The invention additionally provides a method of synthesis of the (S,S) enantiomer of alpha-phenyl(piperidin-2-yl)methanol as well as a method of synthesis of dextrophacetoperane.

Claims

1-10. -10. (canceled)

11. A method for treating an attention deficit hyperactivity disorder (ADHD) in a human, comprising administering to a human in need thereof levophacetoperane, or a pharmaceutically acceptable salt thereof, in an amount of about 5 mg to about 20 mg per day.

12. The method of claim 11, wherein levophacetoperane, or a pharmaceutically acceptable salt thereof, is administered orally.

13. The method of claim 12, wherein the amount of levophacetoperane, or a pharmaceutically acceptable salt thereof, administered ranges from about 5 mg to about 10 mg.

14. The method of claim 13, wherein the human is a child or an adolescent.

15. The method of claim 12, wherein the amount of levophacetoperane, or a pharmaceutically acceptable salt thereof, administered ranges from about 10 mg to about 20 mg.

16. The method of claim 15, wherein the human is an adolescent or an adult.

17. The method of any of claims 12-16, wherein the levophacetoperane, or a pharmaceutically acceptable salt thereof, is administered as a tablet.

18. The method of claim 11, wherein levophacetoperane, or a pharmaceutically acceptable salt thereof, is administered as the sole active pharmaceutical ingredient.

19. The method of claim 18, wherein levophacetoperane, or a pharmaceutically acceptable salt thereof, is administered orally.

20. The method of claim 19, wherein the amount of levophacetoperane, or a pharmaceutically acceptable salt thereof, administered ranges from about 5 mg to about 10 mg.

21. The method of claim 20, wherein the human is a child or adolescent.

22. The method of claim 19, wherein the amount of levophacetoperane, or a pharmaceutically acceptable salt thereof, administered ranges from about 10 mg to about 20 mg.

23. The method of claim 22, wherein the human is an adolescent or adult.

24. The method of any of claims 19-23, wherein levophacetoperane, or a pharmaceutically acceptable salt thereof, is administered as a tablet.

25. The method of claim 11, wherein levophacetoperane, or a pharmaceutically acceptable salt thereof, is administered in combination with a psychostimulant.

26. the method of claim 25, wherein the psychostimulant is methylphenidate or amphetamine.

27. The method of claim 25, wherein levophacetoperane, or a pharmaceutically acceptable salt thereof, and the psychostimulant are administered orally.

28. The method of claim 27, wherein levophacetoperane, or a pharmaceutically acceptable salt thereof, is administered from about 5 mg to about 10 mg.

29. The method of claim 28, wherein the human is a child or an adolescent.

30. The method of claim 27, wherein the amount of levophacetoperane, or a pharmaceutically acceptable salt thereof, administered ranges from about 10 mg to about 20 mg.

31. The method of claim 30, wherein the human is an adolescent or an adult.

32. The method of any of claims 27-31, wherein levophacetoperane, or a pharmaceutically acceptable salt thereof, is administered as a tablet.