Phacetoperane for treating of attention deficit hyperactivity disorder

• US 10,456,387 B2
• Filed: 03/06/2018
• Issued: 10/29/2019
• Est. Priority Date: 11/29/2011
• Status: Active Grant

• Current Assignee: NLS-1 Pharma AG
• Original Assignee: NLS-1 Pharma AG
• Inventors: Konofal, Eric, Figadere, Bruno
• Primary Examiner(s): Cornet, Jean P
• Application Number:
  US15/913,481
• Publication Number:
  US 20180214436A1
• Time in Patent Office: 602 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. A method for treating an attention deficit hyperactivity disorder (ADHD) in a human patient by at least reducing impulsivity, comprising orally administering to said patient levophacetoperane, or a pharmaceutically acceptable salt thereof, as the sole active ingredient in an amount effective to reduce impulsivity in said patient ranging from about 5 mg to about 20 mg per day.

2. The method of claim 1, wherein the administered amount of levophacetoperane, or a pharmaceutically acceptable salt thereof, ranges from about 5 mg to about 10 mg.

3. The method of claim 2, wherein the human is a child or an adolescent.

4. The method of claim 1, wherein the administered amount of levophacetoperane, or a pharmaceutically acceptable salt thereof, ranges from about 10 mg to about 20 mg.

5. The method of claim 4, wherein the human is an adolescent or an adult.

6. The method of any of claims 1 and 2-5, wherein the levophacetoperane, or a pharmaceutically acceptable salt thereof, is administered as a tablet.

7. The method of claim 1, wherein the administered amount of levophacetoperane, or a pharmaceutically acceptable salt thereof, ranges from about 5 mg to about 15 mg.

8. The method of claim 7, wherein the human is a child or an adolescent.

9. The method of any of claims 7-8, wherein the administered levophacetoperane, or a pharmaceutically acceptable salt thereof, is as a tablet.