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

Patent metadata

Field	Value
Publication number	US-11241446-B2
Application number	US-201916428386-A
Country	US
Kind code	B2
Filing date	May 31, 2019
Priority date	Apr 17, 2013
Publication date	Feb 8, 2022
Grant date	Feb 8, 2022

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

The invention claimed is:

1. A method for treating tremor in a subject in need thereof comprising administering to the subject 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 2 , wherein the compound is administered orally.

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

6. A method for treating tremor in a subject in need thereof comprising administering to the subject a pharmaceutically acceptable salt of a compound of the formula:

7. The method of claim 6 , wherein the compound is administered orally, subcutaneously, intravenously, or intramuscularly.

8. The method of claim 6 , wherein the compound is administered chronically.

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

10. The method of claim 7 , wherein the compound is administered intravenously.

11. A method for treating tremor 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.

12. The method of claim 11 , wherein the pharmaceutical composition is administered orally, subcutaneously, intravenously, or intramuscularly.

13. The method of claim 11 , wherein the pharmaceutical composition is administered chronically.

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

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

Assignees

• Sage Therapeutics Inc

Inventors

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

Classifications

• C07J43/003 Primary

  not condensed · CPC title

• C07J7/00

  Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms (C07J5/00 takes precedence) · CPC title

• A61P25/00

  Drugs for disorders of the nervous system · CPC title

• C07J1/0059

  substituted in position 17 by a keto group · CPC title

• C07J1/007

  the substituent being an OH group free esterified or etherified · CPC title