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US 12,129,276 B2Granted
Oxysterols and methods of use thereof
AssigneeSage Therapeutics, Inc.
InventorsBoyd L. Harrison, Gabriel Martinez Botella, Albert Jean Robichaud, Francesco G. Salituro
Life of this patent
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Abstract
Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, wherein X, Y, R1, R2a, R2b, R4a, R4b, R5a, R5b, R6a, R6b, R7, and R8 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.
Claims20
A compound of Formula (I):
- or a pharmaceutically acceptable salt thereof;
- wherein:
- R1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, carbocyclyl, or heterocyclyl;
- each of R2a and R2b is independently hydrogen, C1-C6 alkyl, halo, cyano,—ORA, or —NRBRC, or
- R2a and R2b together with the carbon atom to which they are attached form a 3-7 membered ring;
- each of R4a and R4b is independently absent, hydrogen, C1-C6 alkyl, or halo;
- X is —C(RX)2— or —O—, wherein RX is independently hydrogen, halo, or one RX group and R5b are joined to form a double bond;
- Y is —ORY, wherein RY is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, —C(O)RA, —C(O)ORA, —C(O)NRBRC, or —S(O)2RD;
- each instance of R5a and R5b is independently hydrogen, halo, or C1-C6 alkyl;
- each of R6a and R6b is independently hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, carbocyclyl, heterocyclyl, aryl, or heteroaryl, or
- R6a and R6b, taken together with the carbon atom to which they are attached, form a 3-6 membered ring;
- or
- R5a and R6a, together with the carbon atoms to which they are attached, form a 3-6-membered ring;
- and
- R7 is absent or hydrogen in the alpha configuration;
- R8 is hydrogen, halo, C1-6alkyl, carbocyclyl, or —ORA;
- represents a single or double bond, wherein when one is a double bond, the other is a single bond;
- wherein when the between —CR7 and —CR4aR4b is a double bond, then one of R4a or R4b is absent;
- and
- when one of the is a double bond, R7 is absent;
- RA is hydrogen, C1-C6 alkyl, carbocyclyl, heterocyclyl, aryl, or heteroaryl;
- each of RB and RC is independently hydrogen, C1-C6 alkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, or taken together with the atom to which they are attached form a 3-7-membered ring;
- and
- RD is hydrogen, C1-C6 alkyl, carbocyclyl, heterocyclyl, aryl, or heteroaryl.
21 more elements
Dependencies are inferred from the claim text.