IP Library › Granted Patent US 7,973,049
Granted Patent B2
US 7,973,049 · App. 12/112,936 · Granted Jul 5, 2011

Morphinan compounds

Assignee: Concert Pharmaceuticals Inc.
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Quick Facts
Patent No.
US 7,973,049
App. No.
12/112,936
Granted
Jul 5, 2011
Kind
B2
Abstract

This disclosure relates to novel morphinan compounds and their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a σ 1 receptor agonist that also has NMDA antagonist activity.

Claims (36)

1. A compound having the formula:

or a pharmaceutically acceptable salt thereof.

2. The compound or pharmaceutically acceptable salt thereof of claim 1 , wherein any atom not designated as deuterium is present at its natural isotopic abundance.

3. The compound or pharmaceutically acceptable salt thereof of claim 2 , wherein the pharmaceutically acceptable salt is the HBr salt.

4. A pyrogen-free composition comprising the compound or pharmaceutically acceptable salt thereof of claim 2 formulated for pharmaceutical administration and a pharmaceutically acceptable carrier.

5. The composition of claim 4 , further comprising a second therapeutic agent useful in the treatment of a disease or condition selected from pseudobulbar affect and neuropathic pain.

6. The composition of claim 5 , wherein the second therapeutic agent is selected from quinidine or a salt thereof, oxycodone, and gabapentin.

7. The composition of claim 6 , wherein the second therapeutic agent is quinidine or a salt thereof.

8. The composition of claim 7 , wherein the second therapeutic agent is quinidine sulfate.

9. The composition of claim 4 or 5 , wherein the pharmaceutically acceptable salt is the HBr salt.

10. A method of treating a subject suffering from or susceptible to a disease or condition selected from pseudobulbar affect and neuropathic pain, comprising administering to the subject in need thereof a therapeutically effective amount of a pharmaceutical composition comprising a compound having the formula:

or a pharmaceutically acceptable salt thereof;

and a pharmaceutically acceptable carrier.

11. The method of claim 10 , wherein any atom not designated as deuterium in the compound is present at its natural isotopic abundance.

12. The method of claim 11 , comprising administering to the subject in need thereof a second therapeutic agent selected from quinidine or a salt thereof, oxycodone, and gabapentin.

13. The method of claim 11 , wherein the second therapeutic agent is quinidine or a salt thereof.

14. The method of claim 13 , wherein the subject is suffering from or susceptible to pseudobulbar affect and the second therapeutic agent is quinidine sulfate.

15. The method of claim 11 or 12 , wherein the pharmaceutically acceptable salt is the HBr salt.

16. A composition according to claim 7 , wherein the amount of compound is 10-60 mg and the amount of quinidine is 2.5-30 mg.

17. A composition comprising a compound having the formula:

or a pharmaceutically acceptable salt thereof, wherein the composition is formulated for pharmaceutical administration and wherein the carrier is a pharmaceutically acceptable carrier.

18. The composition of claim 17 , wherein any atom not designated as deuterium in the compound is present at its natural isotopic abundance.

19. The composition of claim 18 , further comprising a second therapeutic agent useful in the treatment of a disease or condition selected from pseudobulbar affect and neuropathic pain .

20. The composition of claim 19 , wherein the second therapeutic agent is selected from quinidine or a salt thereof, oxycodone, and gabapentin.

21. The composition of claim 20 , wherein the second therapeutic agent is quinidine or a salt thereof.

22. The composition of claim 21 , wherein the second therapeutic agent is quinidine sulfate.

23. The composition of claim 18 or 19 , wherein the pharmaceutically acceptable salt is the HBr salt.

24. A method of treating a subject suffering from or susceptible to a disease or condition selected from pseudobulbar affect and neuropathic pain, comprising administering to the subject in need thereof a therapeutically effective amount of a pharmaceutical composition comprising a compound having the formula:

or a pharmaceutically acceptable salt thereof;

and a pharmaceutically acceptable carrier.

25. The method of claim 24 , wherein any atom not designated as deuterium in the compound is present at its natural isotopic abundance.

26. The method of claim 25 , further comprising administering to the subject in need thereof a second therapeutic agent selected from quinidine or a salt thereof, oxycodone, and gabapentin.

27. The method of claim 26 , wherein the second therapeutic agent is quinidine or a salt thereof

28. The method of claim 27 , wherein the subject is suffering from or susceptible to pseudobulbar affect and the second therapeutic agent is quinidine sulfate.

29. The method of claim 25 or 26 , wherein the pharmaceutically acceptable salt is the HBr salt.

30. A composition according to claim 21 , comprising 10-60 mg of the compound and 2.5-30 mg of quinidine.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 17, 2008
From: TUNG, ROGER
To: CONCERT PHARMACEUTICALS INC.
Reel/Frame 021250/0269 →
Continuity (4)
Provisional Application 60915130 · May 1, 2007
Provisional Application 60916662 · May 8, 2007
Provisional Application 60976044 · Sep 28, 2007
Related Publication 20080280936A1 · Nov 13, 2008