IP Library Granted Patent US 11,241,432
Granted Patent B2
US 11,241,432 · App. 17/092,725 · Granted Feb 8, 2022

Methods of treating depression using orexin-2 receptor antagonists

Inventors: Peter De Boer (Breda, NL); Justine M. Kent (Titusville, NJ); Wayne C. Drevets (Titusville, NJ)
Assignee: Janssen Pharmaceutica NV
A61K31/506A61K9/0095A61K9/10A61K9/2018A61K9/2027A61K45/06A61K47/38A61K31/50A61K31/53
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Quick Facts
Patent No.
US 11,241,432
App. No.
17/092,725
Granted
Feb 8, 2022
Kind
B2
Abstract

The present disclosure is directed to, inter alia, methods of treating a subject suffering from or diagnosed with depression, comprising administering to a subject in need of such treatment an effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 1 to R 4 are described herein and wherein the compound is administered prior to sleep.

Claims (36)

1. A method of treating depression associated with bipolar disorder in a subject, comprising administering to the subject in need of such treatment an effective amount of a compound of formula (I):

wherein:

R 1 is C 1-4 alkyl;

R 2 is C 1-4 alkyl;

R 3 is H or halogen; and

R 4 is H or C 1-4 alkoxy:

or a pharmaceutically acceptable salt or hydrate thereof.

2. The method of claim 1 , wherein the subject is not suffering from or diagnosed with an insomnia disorder.

3. The method of claim 1 , wherein R 3 is halogen.

4. The method of claim 1 , wherein R 4 is H.

5. The method of claim 1 , wherein the compound is [5-(4,6-dimethyl-pyrimidin-2-yl)-hexahydro-pyrrolo[3,4-c]pyrrol-2-yl]-(2-fluoro-6-[1,2,3]triazol-2-yl-phenyl)-methanone or a pharmaceutically acceptable salt thereof.

6. The method of claim 1 , wherein the compound is [5-(4,6-dimethyl-pyrimidin-2-yl)-hexahydro-pyrrolo[3,4-c]pyrrol-2-yl]-(2-fluoro-6-[1,2,3]triazol-2-yl-phenyl)-methanone.

7. The method of claim 1 , wherein the compound is [5-(4,6-dimethyl-pyrimidin-2-yl)-hexahydro-pyrrolo[3,4-c]pyrrol-2-yl]-(2-fluoro-6-[1,2,3]triazol-2-yl-phenyl)-methanone hydrochloride.

8. The method of claim 1 , wherein the compound is (5-(4,6-dimethylpyrimidin-2-yl)hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)(4-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone or a pharmaceutically acceptable salt thereof.

9. The method of claim 1 , wherein the compound is (5-(4,6-dimethylpyrimidin-2-yl)hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)(4-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone.

10. The method of claim 5 , wherein the effective amount of the compound is about 10 to about 40 mg.

11. The method of claim 10 , wherein the compound is administered once daily.

12. The method of claim 11 , wherein the compound is administered at night.

13. The method of claim 11 , wherein the compound is administered prior to sleep.

14. The method of claim 12 , wherein the compound is administered prior to sleep.

15. The method of claim 5 , wherein the effective amount of the compound is about 20 mg.

16. The method of claim 15 , wherein the compound is administered once daily.

17. The method of claim 16 , wherein the compound is administered at night.

18. The method of claim 16 , wherein the compound is administered prior to sleep.

19. The method of claim 17 , wherein the compound is administered prior to sleep.

20. The method of claim 5 , wherein the compound is administered as an adjunctive treatment.

21. The method of claim 20 , wherein the effective amount of the compound is about 10 to about 40 mg.

22. The method of claim 21 , wherein the compound is administered once daily.

23. The method of claim 22 , wherein the compound is administered at night.

24. The method of claim 22 , wherein the compound is administered prior to sleep.

25. The method of claim 23 , wherein the compound is administered prior to sleep.

26. The method of claim 20 , wherein the effective amount of the compound is about 20 mg.

27. The method of claim 26 , wherein the compound is administered once daily.

28. The method of claim 27 , wherein the compound is administered at night.

29. The method of claim 27 , wherein the compound is administered prior to sleep.

30. The method of claim 28 , wherein the compound is administered prior to sleep.

Continuity (3)
Continuation 15454628 · Mar 9, 2017
Provisional Application 62306487 · Mar 10, 2016
Related Publication 20210052588A1 · Feb 25, 2021
Cited By (2)
US 12,201,634 US 12,378,254