Neuroactive steroids and their methods of use

Patent metadata

Field	Value
Publication number	US-12252509-B2
Application number	US-202418616903-A
Country	US
Kind code	B2
Filing date	Mar 26, 2024
Priority date	Dec 5, 2018
Publication date	Mar 18, 2025
Grant date	Mar 18, 2025

Abstract

Provided herein is a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R 19 , R 5 , R 3a , R 1a , R 1b , R 2a , R 2b , R 4a , R 4b , R 6a , R 6b , R 7a , R 7b , R 11a , R 11b , R 12a , R 12b , R 18 , R D , and q are defined herein. L is selected from the group consisting of: wherein A indicates the point of attachment at C17 and wherein X is selected from the group consisting of —C(O)N(R 55a )(R 55b ), —N(R 55a )(R 55b ), —N(R 55b )C(O)(R 55a ), and R 55C wherein R 55c is carbon-bound substituted or unsubstituted heteroaryl or substituted or unsubstituted aryl. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds, e.g., in the treatment of CNS-related disorders.

First claim

What is claimed:

1. A compound selected from

Example
Structure

435

436

437

438

439

440

441

and

442

2. A compound selected from

Example
Structure

435

437

439

441

3. A compound selected from

Example
Structure

436

438

440

442

.

4. The compound of claim 1 , wherein the compound has the structural formula

5. The compound of claim 1 , wherein the compound has the structural formula

6. The compound of claim 1 , wherein the compound has the structural formula

7. The compound of claim 1 , wherein the compound has the structural formula

8. The compound of claim 1 , wherein the compound has the structural formula

9. The compound of claim 1 , wherein the compound has the structural formula

Assignees

• Sage Therapeutics Inc

Inventors

• Blanco-Pillado Maria Jesus
• Salituro Francesco G
• Morningstar Marshall Lee

Classifications

• C07J41/0094

  containing nitrile radicals, including thiocyanide radicals · CPC title

• C07J41/0044

  with an estrane or gonane skeleton, including 18-substituted derivatives and derivatives where position 17-beta is substituted by a carbon atom not directly bonded to another carbon atom and not being part of an amide group · CPC title

• A61P25/00

  Drugs for disorders of the nervous system · CPC title

• A61K31/58

  containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin (digitoxin {A61K31/7048}) · CPC title

• C07J41/0055

  the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives · CPC title