US 11,851,457 B2
Oxysterols and methods of use thereof
Francesco G. Salituro, Marlborough, MA (US); Albert Jean Robichaud, Boston, MA (US); Gabriel Martinez Botella, Wayland, MA (US); Boyd L. Harrison, Princeton Junction, NJ (US); and Andrew Griffin, L'lle Bizard (CA)
Assigned to SAGE THERAPEUTICS, Cambridge, MA (US)
Filed by Sage Therapeutics, Inc., Cambridge, MA (US)
Filed on Aug. 5, 2021, as Appl. No. 17/395,155.
Application 17/395,155 is a division of application No. 16/343,235, granted, now 11,149,054, previously published as PCT/US2017/057277, filed on Oct. 18, 2017.
Claims priority of provisional application 62/409,767, filed on Oct. 18, 2016.
Claims priority of provisional application 62/409,761, filed on Oct. 18, 2016.
Claims priority of provisional application 62/409,774, filed on Oct. 18, 2016.
Claims priority of provisional application 62/409,764, filed on Oct. 18, 2016.
Claims priority of provisional application 62/409,772, filed on Oct. 18, 2016.
Prior Publication US 2021/0380631 A1, Dec. 9, 2021
Int. Cl. C07J 9/00 (2006.01); C07J 17/00 (2006.01); A61P 25/20 (2006.01); A61P 25/28 (2006.01); A61P 25/22 (2006.01); A61P 19/02 (2006.01); A61P 25/18 (2006.01); A61P 1/00 (2006.01); A61P 25/16 (2006.01); A61P 35/00 (2006.01); C07J 43/00 (2006.01)
CPC C07J 9/00 (2013.01) [A61P 1/00 (2018.01); A61P 19/02 (2018.01); A61P 25/16 (2018.01); A61P 25/18 (2018.01); A61P 25/20 (2018.01); A61P 25/22 (2018.01); A61P 25/28 (2018.01); A61P 35/00 (2018.01); C07J 17/00 (2013.01); C07J 43/003 (2013.01)] 18 Claims
 
1. A method for treating a CNS-related condition, comprising administering to a subject in need thereof an effective amount of a compound of Formula (I-66):

OG Complex Work Unit Chemistry
wherein:
R1 is substituted or unsubstituted C1-C6 alkyl;
R2 is substituted or unsubstituted aralkyl, substituted or unsubstituted heteroaralkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
R3 is hydrogen, substituted or unsubstituted C1-C6 alkyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
each of R4 and R5 is independently hydrogen, halo, or —ORC, wherein RC is hydrogen or unsubstituted or substituted C1-C3 alkyl, or
R4 and R5, together with the carbon atom to which they are attached form an oxo group;
R6 is absent or hydrogen; and
custom character represents a single or double bond, wherein when one of custom character is a double bond, the other custom character is a single bond; when both of custom character are single bonds, then R6 is hydrogen; and when one of custom character is a double bond, R6 is absent, or a pharmaceutically acceptable salt thereof; or a pharmaceutical composition comprising said compound of Formula (I-66), or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier;
wherein the CNS-related condition is selected from the group consisting of schizophrenia, an autism spectrum disorder, Huntington's disease, Parkinson's disease, a seizure disorder, a mood disorder, stroke, a traumatic brain injury, a substance-related disorder, and a cognitive disorder.