IP Library Granted Patent US 10,342,810
Granted Patent B2
US 10,342,810 · App. 16/020,641 · Granted Jul 9, 2019

19-nor C3, 3-disubstituted C21-N-pyrazolyl steroids and methods of use thereof

Inventors: Gabriel Martinez Botella (Wayland, MA); Boyd L. Harrison (Princeton Junction, NJ); Albert Jean Robichaud (Cambridge, MA); Francesco G. Salituro (Marlborough, MA); Richard Thomas Beresis (Shanghai, CN)
Assignee: Sage Therapeutics, Inc.
A61K31/58A61K9/0019A61K31/573C07J3/00C07J5/0053C07J7/00C07J15/00C07J43/003C07J1/007C07J1/0059C07J1/0074C07J5/0015C07J7/002C07J7/007C07J7/0085C07J13/007C07J21/00C07J31/006
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 10,342,810
App. No.
16/020,641
Granted
Jul 9, 2019
Kind
B2
Abstract

Provided herein are 19-nor C3,3-disubstituted C21-pyrazolyl steroids of Formula (I): and pharmaceutically acceptable salts thereof; wherein , R 1 , R 2 , R 3a , R 3b , R 4a , R 4b , R 5 , R 6 , and R 7 are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.

Claims (18)

1. A method of treating a sleep disorder or a mood disorder in a human subject in need thereof, comprising administering to the human subject a therapeutically effective amount of a compound of the formula

2. The method of claim 1 , wherein the method is a method of treating a sleep disorder.

3. The method of claim 2 , wherein the sleep disorder is insomnia.

4. The method of claim 1 , wherein the method is a method of treating a mood disorder.

5. The method of claim 4 , wherein the mood disorder is depression.

6. The method of claim 1 , wherein the compound is administered orally.

7. A method of treating a sleep disorder or a mood disorder in a human subject in need thereof, comprising administering to the human subject a pharmaceutical composition comprising a therapeutically effective amount of a compound of the formula

and a pharmaceutically acceptable excipient.

8. The method of claim 7 , wherein the method is a method of treating a sleep disorder.

9. The method of claim 8 , wherein the sleep disorder is insomnia.

10. The method of claim 7 , wherein the method is a method of treating a mood disorder.

11. The method of claim 10 , wherein the mood disorder is depression.

12. The method of claim 7 , wherein the pharmaceutical composition is administered orally.

13. A method of treating postnatal depression in a human subject in need thereof, comprising administering to the human subject a therapeutically effective amount of a compound of the formula.

14. The method of claim 13 , wherein the compound is administered orally.

15. A method of treating postnatal depression in a human subject in need thereof, comprising administering to the human subject a pharmaceutical composition comprising a therapeutically effective amount of a compound of the formula

and a pharmaceutically acceptable excipient.

16. The method of claim 15 , wherein the pharmaceutical composition is administered orally.

Assignments (2)
CHANGE OF NAME Recorded May 13, 2026
From: SAGE THERAPEUTICS, INC.
To: SAGE THERAPEUTICS, LLC
Reel/Frame 075610/0448 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 6, 2021
From: BOTELLA, GABRIEL MARTINEZ; HARRISON, BOYD L.; ROBICHAUD, ALBERT JEAN; SALITURO, FRANCESCO G.; BERESIS, RICHARD THOMAS
To: SAGE THERAPEUTICS, INC.
Reel/Frame 057102/0091 →
Priority Claims (1)
WO PCT/CN2013/074323 · Apr 17, 2013 · international
Continuity (3)
Division 15297845 · Oct 19, 2016
Division 14785171
Related Publication 20180311262A1 · Nov 1, 2018
Cited By (7)
US 12,201,640 US 12,358,942 US 12,473,327 US 12,534,495 US 12,552,829 US 12,655,175 US 12,673,970