Neuroactive steroids, compositions, and uses thereof
AssigneeSage Therapeutics, Inc.
InventorsGabriel Martinez Botella, Boyd L. Harrison, Albert Jean Robichaud, Francesco G. Salituro, Robert Jason Herr, Robert Borbo Kargbo
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Abstract
Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein -------, R1, R2, R3, A and L are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia.
Claims33
A compound of the Formula (Ib):
- or a pharmaceutically acceptable salt thereof,
- wherein:
- A is an optionally substituted nitrogen-containing bicyclic heteroaryl or bicyclic heterocyclyl;
- L is —C(R3)(R3)—, —O—, —S—, or —NR3—;
- R1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, carbocyclyl, or heterocyclyl;
- R2 is C1-C6 alkyl or C1-C6 alkoxy;
- each R3 is independently hydrogen;
- R5 is absent or hydrogen;
- and
- is a single or double bond, wherein when one of is a double bond, the other is a single bond;
- and when one of the is a double bond, R5 is absent.
A compound selected from
- or a pharmaceutically acceptable salt thereof.
A compound of Formula (Ia):
- or a pharmaceutically acceptable salt thereof;
- wherein:
- Ring A is an optionally substituted 5-membered or 6-membered monocyclic heterocyclyl or an optionally substituted 5-membered or 6-membered monocyclic heteroaryl, wherein the heterocyclyl or heteroaryl of ring A comprises 1, 2, 3, or 4 nitrogen atoms and wherein the heterocyclyl or heteroaryl of ring A is linked through a nitrogen atom;
- L is —C(R3)(R3)—, —O—, —S—, or —NR3—;
- R1 is unsubstituted C1-C6 alkyl;
- each R3 is hydrogen;
- R5 is absent or hydrogen;
- and
- is a single or double bond, wherein when one of is a double bond, the other is a single bond;
- and when one of the is a double bond, R5 is absent.
A compound selected from
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.