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

Patent metadata

Field	Value
Publication number	US-10172871-B2
Application number	US-201615297845-A
Country	US
Kind code	B2
Filing date	Oct 19, 2016
Priority date	Apr 17, 2013
Publication date	Jan 8, 2019
Grant date	Jan 8, 2019

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 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.

Assignees

• Sage Therapeutics Inc

Inventors

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

Classifications

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P27/16

  Otologicals · CPC title

• A61P25/30

  for treating abuse or dependence · CPC title

• A61P25/28

  for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia · CPC title

• A61P25/22

  Anxiolytics · CPC title