Methods of treating Alzheimer's disease and pharmaceutical compositions thereof

Patent metadata

Field	Value
Publication number	US-9687473-B2
Application number	US-201615084712-A
Country	US
Kind code	B2
Filing date	Mar 30, 2016
Priority date	Sep 9, 2012
Publication date	Jun 27, 2017
Grant date	Jun 27, 2017

Abstract

The present invention describes methods of treating dementia comprising administering an effective daily dose of N-[2-(6-fluoro-1H-indol-3-yl)ethyl]-3-(2,2,3,3-tetrafluoropropoxy)benzylamine to improve or augment the effect of an acetylcholinesterase inhibitor.

First claim

What is claimed:

1. A method of treating Alzheimer's disease, comprising administering to a patient in need of such treatment and undergoing treatment with an acetylcholinesterase inhibitor a daily dose of N-[2-(6-fluoro-1H-indol-3-yl)ethyl]-3-(2,2,3,3-tetrafluoropropoxy)benzylamine or a pharmaceutically acceptable salt thereof effective for treating Alzheimer's disease, wherein the daily dose administered to the patient is between 10 and 50 mg and the dose is administered once daily.

2. The method of claim 1 , wherein the pharmaceutically acceptable salt is the hydrochloride.

3. The method of claim 1 , wherein the dose is administered as an immediate release formulation.

4. The method of claim 1 , wherein the Alzheimer's disease is mild to moderate Alzheimer's disease.

5. The method of claim 1 , wherein the acetylcholinesterase inhibitor is donepezil.

6. The method of claim 1 , wherein the acetylcholinesterase inhibitor is rivastigmine.

7. The method of claim 1 , wherein the administration of N-[2-(6-fluoro-1H-indol-3-yl)ethyl]-3-(2,2,3,3-tetrafluoropropoxy)benzylamine improves or augments the effect of the acetylcholinesterase inhibitor.

8. The method of claim 1 , wherein the dose is administered orally.

9. A method of treating Alzheimer's disease as adjunctive therapy to acetylcholinesterase inhibitor treatment, comprising:
administering an effective daily dose of N-[2-(6-fluoro-1H-indol-3-yl)ethyl]-3-(2,2,3,3-tetrafluoropropoxy)benzylamine or a pharmaceutically acceptable salt thereof to a patient in need of such treatment, wherein the daily dose administered to the patient is between 10 and 50 mg and the dose is administered once daily; and
administering an acetylcholinesterase inhibitor to the patient.

10. The method of claim 9 , wherein the pharmaceutically acceptable salt is the hydrochloride.

11. The method of claim 9 , wherein the dose is administered as an immediate release formulation.

12. The method of claim 9 , wherein the Alzheimer's disease is mild to moderate Alzheimer's disease.

13. The method of claim 9 , wherein the acetylcholinesterase inhibitor is donepezil.

14. The method of claim 9 , wherein the acetylcholinesterase inhibitor is rivastigmine.

15. The method of claim 9 , wherein the administration of N-[2-(6-fluoro-1H-indol-3-yl)ethyl]-3-(2,2,3,3-tetrafluoropropoxy)benzylamine improves or augments the effect of the acetylcholinesterase inhibitor.

16. The method of claim 9 , wherein the dose is administered orally.

17. A method of treating Alzheimer's disease, comprising administering to a patient in need of such treatment and undergoing treatment with an acetylcholinesterase inhibitor a daily dose of N-[2-(6-fluoro-1H-indol-3-yl)ethyl]-3-(2,2,3,3-tetrafluoropropoxy)benzylamine or a pharmaceutically acceptable salt thereof effective for treating Alzheimer's disease, wherein the daily dose administered to the patient is 10 mg once daily.

18. The method of claim 17 , wherein the pharmaceutically acceptable salt is the hydrochloride.

19. The method of claim 17 , wherein the dose is administered as an immediate release formulation.

20. The method of claim 17 , wherein the Alzheimer's disease is mild to moderate Alzheimer's disease.

21. The method of claim 17 , wherein the acetylcholinesterase inhibitor is donepezil.

22. The method of claim 17 , wherein the acetylcholinesterase inhibitor is rivastigmine.

23. The method of claim 17 , wherein the administration of N-[2-(6-fluoro-1H-indol-3-yl)ethyl]-3-(2,2,3,3-tetrafluoropropoxy)benzylamine improves or augments the effect of the acetylcholinesterase inhibitor.

24. The method of claim 17 , wherein the dose is administered orally.

25. A method of treating Alzheimer's disease as adjunctive therapy to acetylcholinesterase inhibitor treatment, comprising administering an effective daily dose of N-[2-(6-fluoro-1H-indol-3-yl)ethyl]-3-(2,2,3,3-tetrafluoropropoxy)benzylamine or a pharmaceutically acceptable salt thereof to a patient in need of such treatment, wherein the daily dose administered to the patient is 10 mg and the dose is administered once daily;
and administering an acetylcholinesterase inhibitor to the patient.

26. The method of claim 25 , wherein the pharmaceutically acceptable salt is the hydrochloride.

27. The method of claim 25 , wherein the dose is administered as an immediate release formulation.

28. The method of claim 25 , wherein the Alzheimer's disease is mild to moderate Alzheimer's disease.

29. The method of claim 25 , wherein the acetylcholinesterase inhibitor is donepezil.

30. The method of claim 25 , wherein the acetylcholinesterase inhibitor is rivastigmine.

31. The method of claim 25 , wherein the administration of N-[2-(6-fluoro-1H-indol-3-yl)ethyl]-3-(2,2,3,3-tetrafluoropropoxy)benzylamine improves or augments the effect of the acetylcholinesterase inhibitor.

32. The method of claim 25 , wherein the dose is administered orally.

Assignees

• H Lundbeck As

Inventors

• Schmidt Ellen
• Areberg Johan

Classifications

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P25/28

  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 · CPC title

• A61P25/00

  Drugs for disorders of the nervous system · CPC title

• A61K31/27

  of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine · CPC title

• A61K45/06 Primary

  Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · CPC title