IP Library Granted Patent US 12,264,177
Granted Patent B2
US 12,264,177 · App. 18/616,762 · Granted Apr 1, 2025

Neuroactive steroids and their methods of use

Inventors: Maria Jesus Blanco-Pillado (Arlington, MA); Francesco G. Salituro (Marlborough, MA); Marshall Lee Morningstar (Framingham, MA)
Assignee: Sage Therapeutics, Inc.
C07J43/003C07J41/0044C07J41/0094
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Quick Facts
Patent No.
US 12,264,177
App. No.
18/616,762
Granted
Apr 1, 2025
Kind
B2
Abstract

Provided herein is a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R 19 , R 5 , R 3a , R 1a , R 1b , R 2a , R 2b , R 4a , R 4b , R 6a , R 6b , R 7a , R 7b , R 11a , R 11b , R 12a , R 12b , R 18 , R D , and q are defined herein. L is selected from the group consisting of: wherein A indicates the point of attachment at C17 and wherein X is selected from the group consisting of —C(O)N(R 55a )(R 55b ), —N(R 55a )(R 55b ), —N(R 55b )C(O)(R 55a ), and R 55C wherein R 55c is carbon-bound substituted or unsubstituted heteroaryl or substituted or unsubstituted aryl. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds, e.g., in the treatment of CNS-related disorders.

Claims (105)

1. A compound selected from

Ex-

ample

Structure

299

300

301

302

303

304

307

308

311

312

65

66

341

342

343

344

349

and

350

2. A compound selected from

Ex-

ample

Structure

299

301

303

307

311

65

341

343

and

349

3. A compound selected from

Ex-

ample

Structure

300

302

304

308

312

66

342

and

344

350

4. The compound of claim 1 , wherein the compound has the structural formula

5. The compound of claim 1 , wherein the compound has the structural formula

6. The compound of claim 1 , wherein the compound has the structural formula

7. The compound of claim 1 , wherein the compound has the structural formula

8. The compound of claim 1 , wherein the compound has the structural formula

9. The compound of claim 1 , wherein the compound has the structural formula

10. The compound of claim 1 , wherein the compound has the structural formula

11. The compound of claim 1 , wherein the compound has the structural formula

12. The compound of claim 1 , wherein the compound has the structural formula

13. The compound of claim 1 , wherein the compound has the structural formula

14. The compound of claim 1 , wherein the compound has the structural formula

15. The compound of claim 1 , wherein the compound has the structural formula

16. The compound of claim 1 , wherein the compound has the structural formula

17. The compound of claim 1 , wherein the compound has the structural formula

18. The compound of claim 1 , wherein the compound has the structural formula

19. The compound of claim 1 , wherein the compound has the structural formula

20. The compound of claim 1 , wherein the compound has the structural formula

21. The compound of claim 1 , wherein the compound has the structural formula

22. A pharmaceutical composition comprising a compound having the structural formula

and a pharmaceutically acceptable excipient.

23. A pharmaceutical composition comprising a compound having the structural formula

and a pharmaceutically acceptable excipient.

24. A pharmaceutical composition comprising a compound having the structural formula

and a pharmaceutically acceptable excipient.

25. A pharmaceutical composition comprising a compound having the structural formula

and a pharmaceutically acceptable excipient.

26. A pharmaceutical composition comprising a compound having the structural formula

and a pharmaceutically acceptable excipient.

27. A pharmaceutical composition comprising a compound having the structural formula

and a pharmaceutically acceptable excipient.

28. A pharmaceutical composition comprising a compound having the structural formula

and a pharmaceutically acceptable excipient.

29. A pharmaceutical composition comprising a compound having the structural formula

and a pharmaceutically acceptable excipient.

30. A pharmaceutical composition comprising a compound having the structural formula

and a pharmaceutically acceptable excipient.

31. A pharmaceutical composition comprising a compound having the structural formula

and a pharmaceutically acceptable excipient.

32. A pharmaceutical composition comprising a compound having the structural formula

and a pharmaceutically acceptable excipient.

33. A pharmaceutical composition comprising a compound having the structural formula

and a pharmaceutically acceptable excipient.

34. A pharmaceutical composition comprising a compound having the structural formula

and a pharmaceutically acceptable excipient.

35. A pharmaceutical composition comprising a compound having the structural formula

and a pharmaceutically acceptable excipient.

36. A pharmaceutical composition comprising a compound having the structural formula

and a pharmaceutically acceptable excipient.

37. A pharmaceutical composition comprising a compound having the structural formula

and a pharmaceutically acceptable excipient.

38. A pharmaceutical composition comprising a compound having the structural formula

and a pharmaceutically acceptable excipient.

39. A pharmaceutical composition comprising a compound having the structural formula

and a pharmaceutically acceptable excipient.

Assignments (2)
CHANGE OF NAME Recorded Apr 23, 2026
From: SAGE THERAPEUTICS, INC.
To: SAGE THERAPEUTICS, LLC
Reel/Frame 075472/0569 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 21, 2024
From: BLANCO-PILLADO, MARIA JESUS; SALITURO, FRANCESCO G.; MORNINGSTAR, MARSHALL LEE
To: SAGE THERAPEUTICS, INC.
Reel/Frame 067481/0001 →