IP Library Granted Patent US 11,149,056
Granted Patent B2
US 11,149,056 · App. 16/338,315 · Granted Oct 19, 2021

C7 substituted oxysterols and methods of use thereof

Inventors: Francesco G. Salituro (Marlborough, MA); Albert Jean Robichaud (Boston, MA); Gabriel Martinez Botella (Wayland, MA); Andrew Griffin (L'lle Bizard, CA); Boyd L. Harrison (Princeton Junction, NJ); Daniel La (Chestnut Hill, MA)
Assignee: SAGE THERAPEUTICS, INC.
C07J31/006C07J9/005
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Quick Facts
Patent No.
US 11,149,056
App. No.
16/338,315
Granted
Oct 19, 2021
Kind
B2
Abstract

Compounds are provided according to Formula (A): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R 1A , R 1b , n, R 2A , R 2b , R 3 , and R 4 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

Claims (18)

1. A compound of Formula (B):

or a pharmaceutically acceptable salt thereof, wherein:

each of R 1A and R 1B is independently hydrogen, substituted or unsubstituted alkyl, carbocyclyl, heterocyclyl, aryl, or heteroaryl, or R 1A and R 1B , together with the carbon atom to which they are attached form a 3-8 membered ring;

n is 1 or 2;

each of R 2A and R 2B is independently hydrogen, halo, —OR C , substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein R C is hydrogen or alkyl, or R 2A and R 2B , together with the carbon atom to which they are attached form an oxo group, wherein R 2A and R 2B are not both simultaneously hydrogen;

R 3 is substituted or unsubstituted alkyl, alkenyl, or alkynyl, or —OR A , wherein R A is alkyl;

R 4 is absent or hydrogen; and

represents a single or double bond, wherein when one of is a double bond, the other is a single bond; when both of are single bonds, then R 4 is hydrogen; and when one of the is a double bond, R 4 is absent.

2. The compound of claim 1 , where n is 1.

3. The compound of claim 1 , where n is 2.

4. The compound of claim 1 , wherein each of R 1A and R 1B is independently unsubstituted or substituted alkyl.

5. The compound of claim 4 , wherein each of R 1A and R 1B is independently selected from the group consisting of haloalkyl, alkoxyalkyl, —CH 3 , —CH 2 CH 3 , —CH(CH 3 ) 2 , —CF 3 and —CH 2 OCH 3 .

6. The compound of claim 1 , wherein R 1A and R 1B , together with the carbon atom to which they are attached form a 3-8 membered ring.

7. The compound of claim 1 , wherein R 1A is hydrogen and R 1B is alkyl, carbocyclyl, heterocyclyl, aryl, or heteroaryl.

8. The compound of claim 1 , wherein each of R 2A and R 2B is independently substituted or unsubstituted alkyl.

9. The compound of claim 1 , wherein R 3 is substituted or unsubstituted alkyl.

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

11. The compound of claim 1 , wherein the compounds is selected from the group consisting of

Continuity (3)
Provisional Application 62402789 · Sep 30, 2016
Provisional Application 62402797 · Sep 30, 2016
Related Publication 20200024300A1 · Jan 23, 2020
Cited By (3)
US 12,331,070 US 12,448,409 US 12,540,157