IP Library Granted Patent US 10,172,871
Granted Patent B2
US 10,172,871 · App. 15/297,845 · Granted Jan 8, 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
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Quick Facts
Patent No.
US 10,172,871
App. No.
15/297,845
Granted
Jan 8, 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 (13)

1. A method for positively modulating a GABA A receptor in a subject in need thereof, comprising administering to the subject an effective amount of a compound of the formula

2. The method of claim 1 , wherein the compound is administered orally, subcutaneously, intravenously, or intramuscularly.

3. The method of claim 1 , wherein the compound is administered chronically.

4. The method of claim 1 , wherein the subject has a CNS-related disorder.

5. The method of claim 2 , wherein the compound is administered orally.

6. The method of claim 2 , wherein the compound is administered intravenously.

7. A method for positively modulating a GABA A receptor in a subject in need thereof, comprising administering to the subject a pharmaceutical composition comprising an effective amount of a compound of the formula

and a pharmaceutically acceptable excipient.

8. The method of claim 7 , wherein the pharmaceutical composition is administered orally, subcutaneously, intravenously, or intramuscularly.

9. The method of claim 7 , wherein the compound is administered chronically.

10. The method of claim 7 , wherein the subject has a CNS-related disorder.

11. The method of claim 8 , wherein the pharmaceutical composition is administered orally.

12. The method of claim 8 , wherein the pharmaceutical composition is administered intravenously.

Assignments (4)
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 Jun 28, 2018
From: MARTINEZ BOTELLA, GABRIEL; HARRISON, BOYD L.; ROBICHAUD, ALBERT JEAN; SALITURO, FRANCESCO G.; BERESIS, RICHARD THOMAS
To: SAGE THERAPEUTICS, INC.
Reel/Frame 046229/0817 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 28, 2018
From: MARTINEZ BOTELLA, GABRIEL; HARRISON, BOYD L.; ROBICHAUD, ALBERT JEAN; SALITURO, FRANCESCO G.; BERESIS, RICHARD THOMAS
To: SAGE THERAPEUTICS, INC.
Reel/Frame 046231/0674 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 28, 2018
From: MARTINEZ BOTELLA, GABRIEL; HARRISON, BOYD L.; ROBICHAUD, ALBERT JEAN; SALITURO, FRANCESCO G.; BERESIS, RICHARD THOMAS
To: SAGE THERAPEUTICS, INC.
Reel/Frame 046231/0913 →
Priority Claims (1)
WO PCT/CN2013/074323 · Apr 17, 2013 · international
Continuity (2)
Division 14785171
Related Publication 20170246191A1 · Aug 31, 2017
Cited By (8)
US 12,201,640 US 12,358,942 US 12,421,275 US 12,473,327 US 12,534,495 US 12,552,829 US 12,655,175 US 12,673,970