Granted Patent
B2
US 12,201,634 · App. 17/551,955 · Granted Jan 21, 2025
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
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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 (28)
1. A method of adjunctively treating major depressive disorder in a human patient, wherein the patient is being treated with a first antidepressant and is in need of additional treatment for the major depressive disorder, comprising administering to the patient in need thereof about 10 to about 40 mg of a compound that 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, wherein the compound is administered once daily and prior to sleep, and wherein the compound treats a psychic symptom of the depression.
2. 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.
3. The method of claim 1 , wherein the compound [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.
4. The method of claim 1 , wherein the compound is administered at night.
5. The method of claim 4 , wherein antidepressant effect from the compound is maintained when the patient is awake the next day.
6. The method of claim 1 , wherein the once daily administration is repeated.
7. The method of claim 6 , wherein the compound is administered for at least four weeks.
8. The method of claim 1 , wherein the compound is administered in the form of a tablet.
9. The method of claim 1 , wherein the first antidepressant is a selective serotonin reuptake inhibitor, serotonin and noradrenaline reuptake inhibitor, or combinations thereof.
10. The method of claim 1 , wherein the effective amount of the compound is about 20 mg.
11. The method of claim 10 , wherein the once daily administration is repeated.
12. The method of claim 11 , wherein the compound is administered for at least four weeks.
13. The method of claim 10 , wherein the compound is administered in the form of a tablet.
14. The method of claim 10 , wherein the first antidepressant is a selective serotonin reuptake inhibitor, serotonin and noradrenaline reuptake inhibitor, or combinations thereof.
15. The method of claim 1 , wherein the compound is a hydrate of the pharmaceutical salt.
16. The method of claim 1 , wherein the compound is a hydrate of [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.
17. A method of adjunctively treating major depressive disorder in a human patient, wherein the patient is being treated with a first antidepressant and is in need of additional treatment for the major depressive disorder, comprising administering to the patient in need thereof about 20 mg of a compound that 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, wherein the compound is administered once daily, prior to sleep, and at night, and wherein the compound treats a psychic symptom of the depression.
18. The method of claim 17 , wherein antidepressant effect from the compound is maintained when the patient is awake the next day.
19. The method of claim 17 , 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.
20. The method of claim 17 , wherein the compound [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.
21. The method of claim 17 , wherein the compound is a hydrate of the pharmaceutical salt.
22. The method of claim 17 , wherein the compound is a hydrate of [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.
23. The method of claim 17 , wherein the once daily administration is repeated.
24. The method of claim 23 , wherein the compound is administered for at least four weeks.
25. The method of claim 17 , wherein the compound is administered in the form of a tablet.
26. The method of claim 17 , wherein the first antidepressant is a selective serotonin reuptake inhibitor, serotonin and noradrenaline reuptake inhibitor, or combinations thereof.
Continuity (4)
Provisional Application
62306487
· Mar 10, 2016
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