C7, C12, and C16 substituted neuroactive steroids and their methods of use
AssigneeSage Therapeutics, Inc.
InventorsAlbert Jean Robichaud, Gabriel Martinez Botella, Boyd L. Harrison, Francesco G. Salituro, Andrew Griffin, Maria Jesus Blanco-Pillado
Life of this patent
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Abstract
Described herein are neuroactive steroids of Formula (I), Formula (V), or Formula (IX) or a pharmaceutically acceptable salt thereof; wherein each instance of R2, R3, R4, R5, R6, R7, R11a, R11b, R12, R16, R17, R19, and are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. Also provided are pharmaceutical compositions comprising a compound described herein and methods of use and treatment, e.g., such as for inducing sedation and/or anesthesia.
Claims39
A compound of Formula (IX):
- or a pharmaceutically acceptable salt thereof, wherein represents a single or double bond as valency permits;
- each of R2, R4, R6, R11a and R11b is independently hydrogen;
- R3 is C1-C6 alkyl;
- R5 is absent or hydrogen;
- and represents a single or double bond, wherein when one of a double bond, the other is a single bond;
- when both of are single bonds, then R5 is hydrogen;
- and when one of the is a double bond, R5 is absent;
- R17 is alkoxy, cyano, nitro, aryl, heteroaryl, —C(O)RB1, —C(O)CH2RB1, or —C(O)CH2CH2RB1, wherein RB1 is hydrogen, —OH, —N(RA1)2, alkoxy, aryl, or heteroaryl, and each RA1 is independently hydrogen, C1-C6 alkyl, carbocyclyl, aryl, or heteroaryl;
- R19 is hydrogen or alkyl;
- and
- R16 or ORA1.
A compound selected from the group consisting of:
A pharmaceutically acceptable salt of a compound selected from the group consisting of:
Dependencies are inferred from the claim text.