Use of D4 and 5-HT2A antagonists, inverse agonists or partial agonists

• US 8,304,431 B2
• Filed: 12/02/2004
• Issued: 11/06/2012
• Est. Priority Date: 12/02/2003
• Status: Expired due to Fees

• Current Assignee: Pharmaneuroboost N.V.
• Original Assignee: Pharmaneuroboost N.V.
• Inventors: Buntinx, Erik
• Primary Examiner(s): Wang, Shengjun
• Assistant Examiner(s): Pihonak, Sarah
• Application Number:
  US10/580,962
• Publication Number:
  US 20070078162A1
• Time in Patent Office: 2,896 Days
• Field of Search: 514/316, 514/469, 546/186, 549/469
• US Class Current: 514/316
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/343 condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
• CPC Class Codes: A61K 31/4545 containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/16 Anti-Parkinson drugs
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
• CPC Class Codes: A61P 25/22 Anxiolytics
• CPC Class Codes: A61P 25/24 Antidepressants
• CPC Class Codes: A61P 25/28 for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

Abstract

The present invention relates to the use of compounds and compositions of compounds having D4 and 5-HT2A antagonistic, partial agonistic or inverse agonistic activity for the treatment of the underlying dysregulation of the emotional functionality of mental disorders (i.e. affect instability-hypersensitivity-hyperaesthesia-dissociative phenomena-etc). The invention also relates to methods comprising administering to a patient diagnosed as having a neuropsychiatric disorder a pharmaceutical composition containing (i) compounds having D4 antagonistic, partial agonistic or inverse agonistic activity and (ii) compounds having 5-HT2A antagonistic, partial agonistic or inverse agonistic, and (iii) any known medicinal compound and compositions of said compounds. The combined D4 and 5-HT2A antagonistic, partial agonistic or inverse agonistic effects may reside within the same chemical or biological compound or in two different chemical and/or biological compounds.

Claims

1. A pharmaceutical composition for treating a mood disorder or an anxiety disorder comprising:

(a) pipamperone in a dose of 5-15 mg,

(b) escitalopram in a dose of 10-20 mg,

or a pharmaceutically acceptable salt of pipamperone and/or escitalopram, and

(c) a pharmaceutically acceptable carrier.

2. The pharmaceutical composition of claim 1 for treating a mood disorder.

3. The pharmaceutical composition of claim 1 for treating an anxiety disorder.

7. The pharmaceutical composition of claim 1 comprising pipamperone in a dose of 15 mg.

9. The pharmaceutical composition of claim 1 comprising escitalopram in a dose of 10 mg.

11. The pharmaceutical composition of claim 1 comprising pipamperone in a dose of 15 mg and escitalopram in a dose of 10 mg.

13. The pharmaceutical composition of claim 1 formulated for daily administration.

15. The pharmaceutical composition of claim 1, wherein the daily dose of pipamperone is 5-15 mg per day.

17. The pharmaceutical composition of claim 1, wherein the daily dose of pipamperone is 15 mg per day.

19. The pharmaceutical composition of claim 1, wherein the daily dose of escitalopram is 10-20 mg per day.

21. The pharmaceutical composition of claim 1, wherein the daily dose of escitalopram is 10 mg per day.

23. The pharmaceutical composition of claim 1, wherein the daily dose of pipamperone is 15 mg per day and the daily dose of escitalopram is 10 mg per day.

25. The pharmaceutical composition of claim 1, wherein pipamperone is provided as a pharmaceutically acceptable salt.

27. The pharmaceutical composition of claim 1, wherein escitalopram is provided as a pharmaceutically acceptable salt.

29. The pharmaceutical composition of claim 1 formulated for twice daily administration.

32. A method of treating an anxiety disorder in a patient comprising administering to the patient the pharmaceutical composition of any of claim 1, 3-4 or 6-31.

33. A method of treating a mood disorder in a patient comprising administering to the patient the pharmaceutical composition of any of claim 1-2, 4-5 or 7-31.

4. A pharmaceutical composition comprising:

(a) pipamperone in a dose of 5-15 mg,

(b) escitalopram in a dose of 10-20 mg,

or a pharmaceutically acceptable salt of pipamperone and/or escitalopram, and

(c) a pharmaceutically acceptable carrier.

5. The pharmaceutical composition of claim 4, wherein pipamperone and escitalopram are present in an amount effective to treat a mood disorder.

6. The pharmaceutical composition of claim 4, wherein pipamperone and escitalopram are present in an amount effective to treat an anxiety disorder.

8. The pharmaceutical composition of claim 4 comprising pipamperone in a dose of 15 mg.

10. The pharmaceutical composition of claim 4 comprising escitalopram in a dose of 10 mg.

12. The pharmaceutical composition of claim 4 comprising pipamperone in a dose of 15 mg and escitalopram in a dose of 10 mg.

14. The pharmaceutical composition of claim 4 formulated for daily administration.

16. The pharmaceutical composition of claim 4, wherein the daily dose of pipamperone is 5-15 mg per day.

18. The pharmaceutical composition of claim 4, wherein the daily dose of pipamperone is 15 mg per day.

20. The pharmaceutical composition of claim 4, wherein the daily dose of escitalopram is 10-20 mg per day.

22. The pharmaceutical composition of claim 4, wherein the daily dose of escitalopram is 10 mg per day.

24. The pharmaceutical composition of claim 4, wherein the daily dose of pipamperone is 15 mg per day and the daily dose of escitalopram is 10 mg per day.

26. The pharmaceutical composition of claim 4, wherein pipamperone is provided as a pharmaceutically acceptable salt.

28. The pharmaceutical composition of claim 4, wherein escitalopram is provided as a pharmaceutically acceptable salt.

30. The pharmaceutical composition of claim 4 formulated for twice daily administration.

31. A pharmaceutical composition for treating a mood disorder or an anxiety disorder comprising pipamperone in a dose of 5-15 mg and escitalopram in a dose of 10-20 mg.