IP Library Granted Patent US 11,643,434
Granted Patent B2
US 11,643,434 · App. 16/887,887 · Granted May 9, 2023

Neuroactive steroids and compositions thereof

Inventors: Francesco G. Salituro (Marlborough, MA); Maria Jesus Blanco-Pillado (Arlington, MA); Marshall Lee Morningstar (Framingham, MA)
Assignee: Sage Therapeutics, Inc.
C07J43/003
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Quick Facts
Patent No.
US 11,643,434
App. No.
16/887,887
Granted
May 9, 2023
Kind
B2
Abstract

Provided herein is a compound of Formula (I): or a pharmaceutically acceptable salt thereof, wherein R 1a , R 1b , R 2a , R 2b , R 3 , R 4a , R 4b , R 5 , R 6a , R 6b , R 7a , R 7a , R 11a , R 11b , R 12a , R 12b , R 16a , R 16b , R 19 , R 11a , R 22 , R X , R Y and n are defined herein. 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 (63)

1. A compound of Formula (I-e6):

or a pharmaceutically acceptable salt thereof;

wherein:

each of R 2a , R 2b , R 15a ,and R 15b is hydrogen;

R 3 is unsubstituted C 1-3 alkyl, —CH 2 OCH 3 , or —CH 2 OCH 2 CH 3 ;

R 19 is hydrogen, methyl, or ethyl;

R X is —OH;

R Y is methyl; and

R 22 is —CN.

2. The compound or pharmaceutically acceptable salt of claim 1 , wherein R 3 is methyl, ethyl, or propyl.

3. The compound or pharmaceutically acceptable salt of claim 2 , wherein R 3 is methyl.

4. The compound or pharmaceutically acceptable salt of claim 2 , wherein R 3 is ethyl.

5. The compound or pharmaceutically acceptable salt of claim 2 , wherein R 3 is propyl.

6. The compound or pharmaceutically acceptable salt of claim 1 , wherein R 3 is —CH 2 OCH 3 .

7. The compound or pharmaceutically acceptable salt of claim 1 , wherein R 3 is —CH 2 OCH 2 CH 3 .

8. The compound or pharmaceutically acceptable salt of claim 1 , wherein R 19 is hydrogen.

9. The compound or pharmaceutically acceptable salt of claim 1 , wherein R 19 is methyl.

10. The compound or pharmaceutically acceptable salt of claim 1 , wherein R 19 is ethyl.

11. A compound selected from

Com-

pound

No.

Structure

2

3

7

11

15

24

26

or a pharmaceutically acceptable salt thereof.

12. A compound selected from

Com-

pound

No.

Structure

29

42

44

or a pharmaceutically acceptable salt thereof.

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

14. A pharmaceutical composition comprising a compound or pharmaceutically acceptable salt of claim 11 and a pharmaceutically acceptable excipient.

15. A pharmaceutical composition comprising a compound or pharmaceutically acceptable salt of claim 12 and a pharmaceutically acceptable excipient.

16. A compound of the formula

or a pharmaceutically acceptable salt thereof.

17. A compound of the formula

or a pharmaceutically acceptable salt thereof.

18. A compound of the formula

or a pharmaceutically acceptable salt thereof.

19. A compound of the formula

or a pharmaceutically acceptable salt thereof.

20. A compound of the formula

or a pharmaceutically acceptable salt thereof.

21. A compound of the formula

or a pharmaceutically acceptable salt thereof.

22. A compound of the formula

or a pharmaceutically acceptable salt thereof.

23. A compound of the formula

or a pharmaceutically acceptable salt thereof.

24. A compound of the formula

or a pharmaceutically acceptable salt thereof.

25. A compound of the formula

or a pharmaceutically acceptable salt thereof.

Assignments (3)
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 Sep 30, 2021
From: SALITURO, FRANCESCO G.; BLANCO-PILLADO, MARIA JESUS; MORNINGSTAR, MARSHALL LEE
To: SAGE THERAPEUTICS, INC.
Reel/Frame 057655/0004 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 15, 2020
From: SALITURO, FRANCESCO G.; BLANCO-PILLADO, MARIA JESUS; MORNINGSTAR, MARSHALL LEE
To: SAGE THERAPEUTICS, INC.
Reel/Frame 053209/0375 →
Cited By (3)
US 12,552,829 US 12,617,789 US 12,673,970