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US 11,396,525 B2Granted
C17, C20, and C21 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
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Abstract
Described herein are neuroactive steroids or a pharmaceutically acceptable salt thereof. 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.
Claims15
A compound of Formula (1-A):
- or a pharmaceutically acceptable salt thereof, wherein:
- a) the compound of Formula (1-A) is a compound of Formula (1-A-1)
- wherein each instance of RY4 is independently alkyl, cyano, or halo;
- and e is 0, 1, 2, 3, 4, or 5;
- or
- b) the compound of Formula (1-A) is a compound of Formula (1-A-3)
- wherein RY1 is hydrogen, —CH3, —CH2CH3, —CH(CH3)2, or cycloalkyl;
- RY2 is alkyl, cycloalkyl, heterocycyl, aryl, or heteroaryl;
- and b is 0, 1, 2, or 3;
- or
- c) the compound of Formula (1-A) is a compound of Formula (1-A-5)
- wherein each occurrence of RY3 is aryl or heteroaryl;
- two RY3 groups are joined together to form a 6-10 membered ring;
- c is 0, 1, 2, or 3;
- and d is 0, 1, 2, or 3,
- and wherein
- R3 is —CH3, —CF3, —CH2OCH3, —CH2OCH2CH3;
- each of RX and RY is independently hydrogen, aryl, or alkyl;
- or RX and RY are joined together to form a 3-10 membered heterocyclic ring;
- R19 is hydrogen or alkyl;
- R5 is absent or hydrogen;
- a is 0;
- and
- represents a single or double bond, wherein when one is a double bond, the other is a single bond and R5 is absent.
21 more elements
A compound selected from the group consisting of:
Dependencies are inferred from the claim text.