Proline sulfonamide derivatives as orexin receptor antagonists

Patent metadata

Field	Value
Publication number	US-9000029-B2
Application number	US-201414530532-A
Country	US
Kind code	B2
Filing date	Oct 31, 2014
Priority date	Aug 24, 2010
Publication date	Apr 7, 2015
Grant date	Apr 7, 2015

Abstract

The present invention relates to (S)-proline sulfonamide compounds of formula (I)

wherein R 1 and R 2 are as described in the description, or pharmaceutically acceptable salts thereof, for use in the prevention or treatment of diseases or disorders related to the orexin system. The present invention also relates to the use of (S)-proline sulfonamide compounds of formula (II) as pharmaceuticals, to pharmaceutical compositions comprising compounds of formula (II), and especially their use in the prevention or treatment of diseases or disorders related to the orexin system.

First claim

The invention claimed is:

1. A method for antagonizing an orexin receptor in a subject having an anxiety disorder, comprising administering to said subject a pharmaceutical composition comprising the compound (S)-1-(4-Methoxy-benzenesulfonyl)-pyrrolidine-2-carboxylic acid (3,5-dimethyl-phenyl)-amide.

2. A method according to claim 1 , wherein said anxiety disorder is selected from a phobic anxiety or a post-traumatic stress disorder.

3. A method according to claim 1 , wherein said pharmaceutical composition comprises a pharmaceutically acceptable carrier.

4. A method according to claim 2 , wherein said pharmaceutical composition comprises a pharmaceutically acceptable carrier.

5. A method according to claim 3 , wherein said compound is (S)-1-(4-Methoxy-benzenesulfonyl)-pyrrolidine-2-carboxylic acid (3,5-dimethyl-phenyl)-amide in free form.

6. A method according to claim 4 , wherein said compound is (S)-1-(4-Methoxy-benzenesulfonyl)-pyrrolidine-2-carboxylic acid (3,5-dimethyl-phenyl)-amide in free form.

7. A method according to claim 2 , wherein said anxiety disorder is a phobic anxiety.

8. A method according to claim 2 , wherein said anxiety disorder is a post-traumatic stress disorder.

9. A method according to claim 4 , wherein said anxiety disorder a phobic anxiety.

10. A method according to claim 4 , wherein said anxiety disorder is a post-traumatic stress disorder.

11. A method according to claim 6 , wherein said anxiety disorder is a phobic anxiety.

12. A method according to claim 6 , wherein said anxiety disorder is a post-traumatic stress disorder.

13. A method according to claim 1 , wherein said anxiety disorder is a circumscribed threat induced anxiety disorder.

Assignees

• Boss Christoph
• Brotschi Christine
• Gatfield John
• Gude Markus
• Heidmann Bibia
• Sifferlen Thierry
• Williams Jodi T
• Actelion Pharmaceuticals Ltd

Inventors

• Boss Christoph
• Brotschi Christine
• Gatfield John
• Gude Markus
• Heidmann Bibia
• Sifferlen Thierry
• Williams Jodi T

Classifications

• A61P25/00

  Drugs for disorders of the nervous system · CPC title

• A61P39/00

  General protective or antinoxious agents · CPC title

• A61K31/401 Primary

  Proline; Derivatives thereof, e.g. captopril · CPC title

• A61K31/40

  having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil · CPC title

• A61P25/30

  for treating abuse or dependence · CPC title