IP Library › Granted Patent US 11,149,054
Granted Patent B2
US 11,149,054 · App. 16/343,235 · Granted Oct 19, 2021

Oxysterols and methods of use thereof

Inventors: Francesco G. Salituro (Marlborough, MA); Albert Jean Robichaud (Boston, MA); Gabriel Martinez Botella (Wayland, MA); Boyd L. Harrison (Princeton Junction, NJ); Andrew Griffin (L'Ile Bizard, CA)
Assignee: SAGE THERAPEUTICS, INC.
C07J9/00A61P1/00A61P19/02A61P25/16A61P25/18A61P25/20A61P25/22A61P25/28A61P35/00C07J17/00C07J43/003
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Quick Facts
Patent No.
US 11,149,054
App. No.
16/343,235
Granted
Oct 19, 2021
Kind
B2
Abstract

Compounds are provided according to Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R 2 , R 3 , R 4 , R 5 , and and R 6 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

Claims (16)

1. A compound of Formula (I-66):

or a pharmaceutically acceptable salt thereof, wherein:

R 1 is substituted or unsubstituted C 1 -C 6 alkyl;

R 2 is substituted or unsubstituted aralkyl, substituted or unsubstituted heteroaralkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;

R 3 is hydrogen, substituted or unsubstituted C 1 -C 6 alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;

each of R 4 and R 5 is independently hydrogen, halo, or —OR C , wherein R C is hydrogen or unsubstituted or substituted C 1 -C 3 alkyl, or

R 4 and R 5 , together with the carbon atom to which they are attached, form an oxo group;

R 6 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; wherein when both of are single bonds, R 6 is hydrogen; and wherein when one of is a double bond, R 6 is absent.

2. The compound of claim 1 , or the pharmaceutically acceptable salt thereof, wherein R 2 is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or substituted or unsubstituted aralkyl.

3. A compound, or a pharmaceutically acceptable salt thereof, selected from the group consisting of:

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

5. The compound of claim 2 , or the pharmaceutically acceptable salt thereof, wherein R 2 is substituted or unsubstituted phenyl, substituted or unsubstituted benzyl, or substituted or unsubstituted pyridyl.

6. The compound of claim 5 , or the pharmaceutically acceptable salt thereof, wherein R 2 is unsubstituted phenyl, unsubstituted benzyl, or unsubstituted pyridyl.

7. The compound of claim 3 , wherein the compound is selected from the group consisting of:

8. The pharmaceutically acceptable salt of claim 3 , wherein the compound is selected from the group consisting of:

Continuity (6)
Provisional Application 62409761 · Oct 18, 2016
Provisional Application 62409772 · Oct 18, 2016
Provisional Application 62409767 · Oct 18, 2016
Provisional Application 62409764 · Oct 18, 2016
Provisional Application 62409774 · Oct 18, 2016
Related Publication 20190248829A1 · Aug 15, 2019
Cited By (5)
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