# US 10,765,685 B2 · Oxysterols and methods of use thereof

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- Number: US 10,765,685 B2
- Document ID: US10765685B2
- Status: Granted
- Kind: B2
- Application number: 16/227,099
- Filed: 2018-12-20
- Published: 2019-05-02
- Granted: 2020-09-08
- Earliest claimed: 2015-07-06
- Assignees: Sage Therapeutics, Inc.
- Applicants: Sage Therapeutics, Inc.
- Inventors: Francesco G. Salituro; Albert Jean Robichaud; Gabriel Martinez Botella
- Web page: https://patentgrep.com/patent/US10765685B2

## CPC

- A61K 31/575: substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/20: Hypnotics; Sedatives
- A61P 35/00: Antineoplastic agents
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07J 9/00: Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
- C07J 7/002: {not substituted in position 16}
- C07J 9/005: {containing a carboxylic function directly attached or attached by a chain containing only carbon atoms to the cyclopenta[a]hydrophenanthrene skeleton}
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07J: STEROIDS (seco-steroids C07C)

## Abstract

Compounds are provided according to Formula (I): Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, wherein R1, R2, R3, R6, R7, R8, and n are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

## Claims

### Claim 1

A compound of Formula (III-A):
or a pharmaceutically acceptable salt thereof, wherein:
R1 is C1-6 alkyl; and
R2 and R3 are each independently substituted or unsubstituted methyl, substituted or unsubstituted ethyl, propyl, isopropyl, cyclopropyl, or butyl.

### Claim 2 (depends on 1)

The compound of claim 1, wherein R1 is methyl, substituted C1-6 alkyl selected from the group consisting of —CHF2, —CF3, —CH2OCH3, and —CH2OCH2CH3, ethyl, or isopropyl.

### Claim 3 (depends on 2)

The compound of claim 2, wherein R1 is methyl or ethyl.

### Claim 4 (depends on 1)

The compound of claim 1, wherein the compound is
or a pharmaceutically acceptable salt thereof.

### Claim 5 (depends on 1)

A pharmaceutical composition comprising a compound of claim 1, or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

### Claim 6 (depends on 1)

A method for modulating an NMDA receptor in a subject in need thereof, comprising administering to the subject in need thereof an effective amount of a compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein the subject has a CNS-related condition.

### Claim 7 (depends on 6)

The method according to claim 6, wherein the CNS-related condition is an obsessive-compulsive disorder, posttraumatic stress disorder, social phobia, cognitive disorder (including Alzheimer's disease and other forms of dementia), eating disorder, schizophrenia, autism spectrum disorders, pain, anti-NMDA receptor encephalitis, Huntington's disease, or Parkinson's disease.