NALMEFENE DI-ESTER PRODRUGS

• US 20110053971A1
• Filed: 04/23/2009
• Published: 03/03/2011
• Est. Priority Date: 04/24/2008
• Status: Abandoned Application

• Current Assignee: Janssen Pharmaceutica NV (Johnson & Johnson)
• Original Assignee: Janssen Pharmaceutica NV (Johnson & Johnson)
• Inventors: Guillaume, Michel Joseph Maurice André, Gaekens, Tim
• Application Number:
  US12/937,577
• Publication Number:
  US 20110053971A1
• Time in Patent Office: Days
• US Class Current: 514/282
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/30 for treating abuse or dependence
• CPC Class Codes: A61P 25/32 Alcohol-abuse
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: C07D 489/08 Oxygen atom

Abstract

The present invention relates to prodrugs of nalmefene of formula (I), pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of substance abuse disorders such as alcohol abuse and alcohol dependence and impulse control disorders such as pathological gambling and addiction to shopping.

Claims

1. A compound of formula (I)

2. The compound as claimed in claim 1 wherein R¹ is C₁₈alkyloxycarbonylC₃alkyl.

3. The compound as claimed in claim 2 wherein the compound is

4. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically active amount of the compound of claim 1.

5. A process for preparing a pharmaceutical composition, wherein a therapeutically active amount of the compound of claim 1 is intimately mixed with a pharmaceutically acceptable carrier.

6. The compound of claim 1 for use as a medicine.

7. The compound of claim 1 for the treatment of substance abuse disorders.

8. The compound as claimed in claim 7 for the treatment of substance abuse disorders wherein said disorder is alcohol abuse or alcohol dependence.

9. The compound of claim 1 for administration in decreasing alcohol craving and alcohol consumption in alcohol-dependent patients.

10. The compound of claim 1 for the treatment of impulse control disorders.

11. The compound as claimed in claim 10 for the treatment of impulse control disorders wherein said disorder is pathological gambling or addiction to shopping.

12. (canceled)

13. A process for preparing a compound of formula (I) by esterification methods comprising reacting nalmefene (II) with an acyl halide of formula (III) in the presence of a base to pick up the acid liberated during the reaction,