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

Patent metadata

Field	Value
Publication number	US-12201640-B2
Application number	US-202117560732-A
Country	US
Kind code	B2
Filing date	Dec 23, 2021
Priority date	Apr 17, 2013
Publication date	Jan 21, 2025
Grant date	Jan 21, 2025

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.

First claim

We claim:

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.

Assignees

• Sage Therapeutics Inc

Inventors

• Martinez Botella Gabriel
• Harrison Boyd L
• Robichaud Albert Jean
• Salituro Francesco G
• Beresis Richard Thomas

Classifications

• A61K31/573

  substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone · CPC title

• C07J5/0053

  not substituted in position 16 · CPC title

• A61K9/0019

  Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00) · CPC title

• C07J43/003 Primary

  not condensed · CPC title

• C07J31/006

  not covered by C07J31/003 · CPC title