IP Library Granted Patent US 11,542,297
Granted Patent B2
US 11,542,297 · App. 17/695,033 · Granted Jan 3, 2023

Compositions and methods for treating CNS disorders

Inventors: Gabriel Martinez Botella (Wayland, MA); Francesco G. Salituro (Marlborough, MA); Albert Jean Robichaud (Boston, MA); Boyd L. Harrison (Princeton Junction, NJ)
Assignee: Sage Therapeutics, Inc.
C07J43/003A61K31/575A61K31/58A61K45/06C07J9/00C07J1/0011C07J1/0022C07J3/005C07J5/0053C07J7/002C07J7/007C07J7/008C07J11/00C07J13/007C07J21/00C07J31/006C07J41/0066C07J51/00C07J71/001
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Quick Facts
Patent No.
US 11,542,297
App. No.
17/695,033
Granted
Jan 3, 2023
Kind
B2
Abstract

Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof, wherein , A, R 1 , R 2 , R 3a , R 4a , R 4b , R 5 , R 7a , and R 7b are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia.

Claims (30)

1. A method of treating a movement disorder in a human subject, comprising administering to the human subject a therapeutically effective amount of a compound having a structure:

or a pharmaceutically acceptable salt thereof.

2. The method according to claim 1 , wherein the movement disorder is tremor.

3. The method according to claim 2 , wherein the tremor is cerebellar tremor, dystonic tremor, essential tremor, orthostatic tremor, Parkinsonian tremor, physiological tremor, psychogenic tremor, or rubral tremor.

4. The method according to claim 3 , wherein the tremor is essential tremor.

5. The method according to claim 1 , wherein the compound or pharmaceutically acceptable salt thereof is a citrate salt of the compound

6. The method of claim 1 , wherein the compound or pharmaceutically acceptable salt thereof is administered orally.

7. The method of claim 6 , wherein the compound or pharmaceutically acceptable salt thereof is administered as a tablet.

8. The method of claim 7 , wherein the tablet comprises from about 0.1% to about 50% of the compound or pharmaceutically acceptable salt thereof by weight of the tablet.

9. The method of claim 1 , wherein the compound or pharmaceutically acceptable salt thereof is administered one to five times per day.

10. The method of claim 1 , wherein the compound or pharmaceutically acceptable salt thereof is administered chronically.

11. The method of claim 10 , wherein the compound or pharmaceutically acceptable salt thereof is administered for a period of at least 3 months.

12. The method of claim 5 , wherein the citrate salt of the compound is administered orally.

13. The method of claim 12 , wherein the citrate salt of the compound is administered as a tablet.

14. The method of claim 13 , wherein the tablet comprises from about 0.1% to about 50% of the citrate salt of the compound by weight of the tablet.

15. The method of claim 5 , wherein the citrate salt of the compound is administered one to five times per day.

16. The method of claim 5 , wherein the citrate salt of the compound is administered chronically.

17. The method of claim 16 , wherein the citrate salt is administered for a period of at least 3 months.

18. A method of treating a movement disorder in a human subject, comprising administering to the human subject a therapeutically effective amount of a pharmaceutical composition comprising compound having a structure:

or a pharmaceutically acceptable salt thereof.

19. The method of claim 18 , wherein the movement disorder is tremor selected from the group consisting of cerebellar tremor, dystonic tremor, essential tremor, orthostatic tremor, Parkinsonian tremor, physiological tremor, psychogenic tremor, and rubral tremor.

20. The method of claim 18 , wherein the compound or pharmaceutically acceptable salt of the compound is a citrate salt of the compound

21. The method of claim 18 , wherein the pharmaceutical composition is administered orally.

22. The method of claim 21 , wherein the pharmaceutical composition is a tablet.

23. The method of claim 22 , wherein the tablet comprises from about 0.1% to about 50% of the compound or pharmaceutically acceptable salt thereof by weight of the tablet.

24. The method of claim 18 , wherein the pharmaceutical composition is administered one to five times per day.

25. The method of claim 20 , wherein the pharmaceutical composition is administered orally.

26. The method of claim 25 , wherein the pharmaceutical composition is a tablet.

27. The method of claim 26 , wherein the tablet comprises from about 0.1% to about 50% of the citrate salt of the compound by weight of the tablet.

28. The method of claim 20 , wherein the pharmaceutical composition is administered one to five times per day.

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 26, 2022
From: MARTINEZ BOTELLA, GABRIEL; SALITURO, FRANCESCO G.; ROBICHAUD, ALBERT JEAN; HARRISON, BOYD L.
To: SAGE THERAPEUTICS, INC.
Reel/Frame 060022/0364 →
Cited By (3)
US 12,473,327 US 12,534,495 US 12,655,175