Granted Patent
B2
US 12,201,640 · App. 17/560,732 · Granted Jan 21, 2025
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 (Boston, MA); Francesco G. Salituro (Marlborough, MA); Richard Thomas Beresis (Shanghai, CN)
Assignee:
Sage Therapeutics, Inc.
A61K31/58A61K9/0019A61K31/573C07J3/00C07J5/0053C07J7/00C07J15/00C07J43/003C07J1/0059C07J1/007C07J1/0074C07J5/0015C07J7/002C07J7/007C07J7/0085C07J13/007C07J21/00C07J31/006
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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 (25)
1. A method for treating a CNS-related disorder in a subject in need thereof comprising administering to the subject a compound of the formula:
wherein the CNS-related disorder is a bipolar disorder, an anxiety disorder, or tinnitus.
2. The method of claim 1 , wherein the CNS-related disorder is the bipolar disorder.
3. The method of claim 2 , wherein the bipolar disorder is bipolar I or bipolar II.
4. The method of claim 1 , wherein the CNS-related disorder is the anxiety disorder.
5. The method of claim 4 , wherein the anxiety disorder is generalized anxiety disorder.
6. The method of claim 1 , wherein the CNS-related disorder is tinnitus.
7. The method of claim 1 , wherein the compound is administered orally.
8. A method for treating a CNS-related disorder in a subject in need thereof comprising administering to the subject a pharmaceutically acceptable salt of a compound of the formula:
wherein the CNS-related disorder is a bipolar disorder, an anxiety disorder, or tinnitus.
9. The method of claim 8 , wherein the CNS-related disorder is the bipolar disorder.
10. The method of claim 9 , wherein the bipolar disorder is bipolar I or bipolar II.
11. The method of claim 8 , wherein the CNS-related disorder is the anxiety disorder.
12. The method of claim 11 , wherein the anxiety disorder is generalized anxiety disorder.
13. The method of claim 8 , wherein the CNS-related disorder is tinnitus.
14. The method of claim 8 , wherein the compound is administered orally.
15. A method for treating a CNS-related disorder in a subject in need thereof comprising administering to the subject a pharmaceutical composition comprising a compound of the formula:
and a pharmaceutically acceptable excipient,
wherein the CNS-related disorder is a bipolar disorder, an anxiety disorder, or tinnitus.
16. The method of claim 15 , wherein the CNS-related disorder is the bipolar disorder.
17. The method of claim 16 , wherein the bipolar disorder is bipolar I or bipolar II.
18. The method of claim 15 , wherein the CNS-related disorder is the anxiety disorder.
19. The method of claim 18 , wherein the anxiety disorder is generalized anxiety disorder.
20. The method of claim 15 , wherein the CNS-related disorder is tinnitus.
21. The method of claim 15 , wherein the compound is administered orally.
Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST
Recorded Aug 16, 2023
From: BOTELLA, GABRIEL MARTINEZ; HARRISON, BOYD L.; ROBICHAUD, ALBERT JEAN; SALITURO, FRANCESCO G.; BERESIS, RICHARD THOMAS
To: SAGE THERAPEUTICS, INC.
Reel/Frame 064614/0886 →
Priority Claims (1)
WO PCT/CN2013/074323
· Apr 17, 2013
· international
Continuity (5)
Division
14785171
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