IP Library Granted Patent US 12,054,495
Granted Patent B2
US 12,054,495 · App. 17/991,899 · Granted Aug 6, 2024

Substituted macrocyclic compounds and related methods of treatment

Inventors: Lewis D. Pennington (Arlington, MA); Younggi Choi (Stow, MA); Hoan Huynh (Waltham, MA); Brian M. Aquila (Marlborough, MA); Ingo Andreas Mugge (Waltham, MA); Yuan Hu (Waltham, MA); James R. Woods (Waltham, MA); Roman A. Valiulin (Cambridge, MA); Brian Kenneth Raymer (Holliston, MA); Jörg Martin Bentzien (White Plains, NY); Michael R. Hale (Bedford, MA); Jonathan Ward Lehmann (Burlington, MA); Daljit Matharu (Lexington, MA); Srinivasa Karra (Pembroke, MA)
Assignee: Alkermes, Inc.
C07D498/08A61P25/26C07D498/18C07D498/22C07B2200/05
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Quick Facts
Patent No.
US 12,054,495
App. No.
17/991,899
Granted
Aug 6, 2024
Kind
B2
Abstract

The present invention provides compounds useful for the treatment of narcolepsy or cataplexy in a subject in need thereof. Related pharmaceutical compositions and methods are also provided herein.

Claims (73)

1. A compound of Formula I-A or a pharmaceutically acceptable salt thereof:

wherein:

ring A is selected from the group consisting of phenyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, and triazinyl;

n is 1, 2, or 3;

T is CR 1 R 2 or O;

W is CR 4 R 5 or O;

U is CR 6 R 7 ;

X is CR 8 R 9 ;

V is CR 3 or N;

Y is NR 10 , O or absent;

Z is (CR 12 R 13 ) m ;

R is halogen or deuterium; and

p is 0, 1, 2, 3, or 4;

and further wherein:

m is 1, 2, 3, or 4;

R 1 , R 2 , R 4 , and R 5 are each, independently, selected from the group consisting of H, halogen, and deuterium;

or, alternatively, R 2 and R 5 together with the carbon atoms to which they are attached, form a single bond;

R 3 is selected from the group consisting of H, deuterium, halogen, hydroxyl, and cyano;

or, alternatively, R 3 and R 1 , together with the carbon atoms to which they are attached, form a C 3 -C 5 cycloalkyl;

or, alternatively, R 3 and R 4 , together with the carbon atoms to which they are attached, form a C 3 -C 5 cycloalkyl;

R 6 , R 7 , R 8 , R 9 , and R 11 are each, independently, selected from the group consisting of H, halogen, and deuterium;

R 10 is selected from the group consisting of H, unsubstituted C 1 -C 3 alkyl, and C 1 -C 3 alkyl substituted with one or more halogen atoms; and

each R 12 and R 13 is, independently, selected from the group consisting of H, halogen, deuterium, unsubstituted C 1 -C 3 alkyl, and C 1 -C 3 alkyl substituted with one or more halogen atoms.

2. The compound of claim 1 , wherein n is 1 or 2.

3. The compound of claim 1 , wherein ring A is phenyl.

4. The compound of claim 1 , wherein ring A is pyridinyl.

5. The compound of claim 1 , wherein Y is O.

6. The compound of claim 1 , wherein Y is absent.

7. The compound of claim 1 , wherein Tis CR 1 R 2 .

8. The compound of claim 1 , wherein Tis O.

9. The compound of claim 1 , wherein W is CR 4 R 5 .

10. The compound of claim 1 , wherein W is O.

11. The compound of claim 1 , wherein V is CR 3 .

12. The compound of claim 1 , wherein m is 1 or 2.

13. A pharmaceutical composition comprising a compound of claim 1 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

14. A method of treating narcolepsy in a subject in need thereof comprising administering to the subject a compound of claim 1 or a pharmaceutically acceptable salt thereof.

15. A method of treating cataplexy in a subject in need thereof comprising administering to the subject a compound of claim 1 or a pharmaceutically acceptable salt thereof.

16. The compound of claim 1 , wherein the compound is:

17. The compound of claim 1 , wherein the compound is:

18. The compound of claim 1 , wherein the compound is:

19. The compound of claim 1 , wherein the compound is:

20. The compound of claim 1 , wherein the compound is:

21. The compound of claim 1 , wherein the compound is:

22. The compound of claim 1 , wherein the compound is:

23. The compound of claim 1 , wherein the compound is:

24. The compound of claim 1 , wherein the compound is:

25. The compound of claim 1 , wherein the compound is:

26. The compound of claim 1 , wherein the compound is:

27. The compound of claim 1 , wherein the compound is:

28. The compound of claim 1 , wherein the compound is:

29. The compound of claim 1 , wherein the compound is:

30. The compound of claim 1 , wherein the compound is:

31. The compound of claim 1 , wherein the compound is:

32. The compound of claim 1 , wherein the compound is:

33. The compound of claim 1 , wherein the compound is:

34. The compound of claim 1 , wherein the compound is:

35. The compound of claim 1 , wherein the compound is:

36. The compound of claim 1 , wherein the compound is:

37. The compound of claim 1 , wherein the compound is:

38. The compound of claim 1 , wherein the compound is:

39. The compound of claim 1 , wherein the compound is:

40. The compound of claim 1 , wherein the compound is:

41. The compound of claim 1 , wherein the compound is:

42. The compound of claim 1 , wherein the compound is:

43. The compound of claim 1 , wherein the compound is:

44. The compound of claim 1 , wherein the compound is:

45. The compound of claim 1 , wherein the compound is:

46. The compound of claim 1 , wherein the compound is:

47. The compound of claim 1 , wherein the compound is:

48. The compound of claim 1 , wherein the compound is:

49. The compound of claim 1 , wherein the compound is:

50. The compound of claim 1 , wherein the compound is:

51. The compound of claim 1 , wherein the compound is:

Assignments (3)
SECURITY INTEREST Recorded Feb 13, 2026
From: ALKERMES, INC.
To: JPMORGAN CHASE BANK, N.A. AS ADMINISTRATIVE AGENT
Reel/Frame 073790/0950 →
RELEASE OF SECURITY INTEREST IN PATENTS PREVIOUSLY RECORDED AT REEL/FRAME (072656/0509) Recorded Feb 13, 2026
From: JPMORGAN CHASE BANK, N.A., AS ADMINISTRATIVE AGENT
To: ALKERMES, INC.
Reel/Frame 074858/0481 →
SECURITY INTEREST Recorded Oct 23, 2025
From: ALKERMES, INC.
To: JPMORGAN CHASE BANK, N.A. AS ADMINISTRATIVE AGENT
Reel/Frame 072656/0509 →