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US 2022/0064207 A1Published application
Neuroactive steroids and methods of use thereof
AssigneeSage Therapeutics, Inc.
InventorsGabriel Martinez Botella, Boyd L. Harrison, Albert Jean Robichaud, Francesco G. Salituro
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Abstract
3beta, 17beta disubstituted steroidal compounds, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, are provided for the prevention and treatment of a variety of CNS-related conditions.
Claims21
A compound of Formula (I):
- or a pharmaceutically acceptable salt thereof,
- wherein:
- R1 is substituted or unsubstituted aliphatic;
- R2 is hydrogen, halogen, substituted or unsubstituted C1-6alkyl, substituted or unsubstituted cyclopropyl, or —ORA2, wherein RA2 is hydrogen or substituted or unsubstituted alkyl;
- R3a is hydrogen or —ORA3, wherein RA3 is hydrogen or substituted or unsubstituted alkyl, and R3b is hydrogen;
- or R3a and R3b are joined to form an oxo (═O) group;
- R4 is hydrogen, substituted or unsubstituted alkyl, or halogen;
- X is —C(RX)2— or —O—, wherein RX is hydrogen or fluorine, or one RX group and R5b are joined to form a double bond;
- each instance of R5a and R5b is independently hydrogen or fluorine;
- R6a is a non-hydrogen group selected from the group consisting of substituted and unsubstituted alkyl, substituted and unsubstituted alkenyl, substituted and unsubstituted alkynyl, substituted and unsubstituted carbocyclyl, substituted and unsubstituted heterocyclyl, substituted and unsubstituted aryl, and substituted and unsubstituted heteroaryl group, wherein the non-hydrogen group is optionally substituted with fluorine;
- and
- R6b is hydrogen or a substituted or unsubstituted alkyl group optionally substituted with fluorine;
- represents a single or double bond, provided if a single bond is present, then the hydrogen at C5 is in the alpha configuration;
- and further provided that:
- (1) at least one of RX, R5a, and R5b is fluorine;
- or
- (2) at least one of R6a and R6b is a non-hydrogen group substituted with a fluorine;
- or
- (3) R6a is a non-hydrogen group comprising between two and ten carbon atoms.
16 more elements
-41. (canceled)
Dependencies are inferred from the claim text.