IP Library Granted Patent US 10,752,653
Granted Patent B2
US 10,752,653 · App. 16/099,122 · Granted Aug 25, 2020

Oxysterols and methods of use thereof

Inventors: Gabriel Martinez Botella (Wayland, MA); Boyd L. Harrison (Princeton Junction, NJ); Albert Jean Robichaud (Boston, MA); Francesco G. Salituro (Marlborough, MA)
Assignee: Sage Therapeutics, Inc.
C07J9/00C07J9/005C07B2200/05
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Quick Facts
Patent No.
US 10,752,653
App. No.
16/099,122
Granted
Aug 25, 2020
Kind
B2
Abstract

Compounds are provided according to Formula (III) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R 2 , R 3 , R 5 , and n are as defined herein, and at least one hydrogen is replaced with a deuterium. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

Claims (26)

1. A compound of Formula (I):

or a pharmaceutically acceptable salt thereof, wherein:

R 1 is hydrogen or deuterium;

each of R 2 and R 3 is independently deuterium or —C 1-6 alkyl;

R 4 is hydrogen or deuterium;

R 5 is absent, hydrogen, or deuterium;

n is 1 or 2;

represents a single or double bond, wherein when one is a double bond, the other is a single bond and R 5 is absent; and

at least one of R 1 , R 2 , R 3 , R 4 , or R 5 is deuterium.

2. The compound of claim 1 , wherein R 1 is hydrogen.

3. The compound of claim 1 , wherein R 1 is deuterium.

4. The compound of claim 1 , wherein R 1 and R 2 are deuterium.

5. The compound of claim 1 , wherein one of R 2 and R 3 is deuterium and the other of R 2 and R 3 is C 1-6 alkyl.

6. The compound of claim 1 , wherein each of R 2 and R 3 is independently —C 1-6 alkyl.

7. The compound of claim 1 , wherein each of R 2 and R 3 is independently isopropyl, —CH 3 , or —CF 3 .

8. The compound of claim 1 , wherein R 4 is hydrogen.

9. The compound of claim 1 , wherein the compound of Formula (I) is a compound of Formula (I-A):

or a pharmaceutically acceptable salt thereof.

10. The compound of claim 1 , wherein the compound of Formula (I) is a compound of Formula (I-B):

or a pharmaceutically acceptable salt thereof.

11. The compound of claim 1 , wherein the compound of Formula (I) is a compound of Formula (I-C):

or a pharmaceutically acceptable salt thereof.

12. The compound of claim 1 , wherein the compound of Formula (I) is a compound of Formula (I-D):

or a pharmaceutically acceptable salt thereof.

13. The compound of claim 1 , wherein the compound of Formula (I) is selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

Assignments (2)
CHANGE OF NAME Recorded Mar 17, 2026
From: SAGE THERAPEUTICS, INC.
To: SAGE THERAPEUTICS, LLC
Reel/Frame 075171/0207 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 5, 2025
From: BOTELLA, GABRIEL MARTINEZ; ROBICHAUD, ALBERT JEAN; SALITURO, FRANCESCO G.; HARRISON, BOYD L.
To: SAGE THERAPEUTICS, INC.
Reel/Frame 071547/0662 →
Continuity (2)
Provisional Application 62332959 · May 6, 2016
Related Publication 20190359646A1 · Nov 28, 2019
Cited By (2)
US 12,448,409 US 12,540,157