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US 10,329,320 B2Granted
Neuroactive steroids, compositions, and uses thereof
AssigneeSage Therapeutics, Inc.
InventorsAlbert J. Robichaud, Francesco G. Salituro, Boyd L. Harrison, Gabriel Martinez Botella
Life of this patent
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Abstract
Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein R1, R2, Ra, G, X, Y, Z, and n 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 for inducing sedation and/or anesthesia.
Claims25
A compound of the Formula (I):
- or a pharmaceutically acceptable salt thereof, wherein:
- each X, Y, and Z is independently CH or N;
- G is —C(R3a)(R3b)(OR1);
- R1 is C1-C6 alkyl, C1-C6 alkenyl, C1-C6 alkynyl, carbocyclyl, heterocyclyl, aryl, or heteroaryl;
- R2 is C1-C6 alkyl, or C1-C6 alkoxy;
- each of R3a and R3b is independently H, D, or C1-C6 alkyl;
- Ra is cyano, halogen, nitro, C1-C6 alkyl, C1-C6 alkoxy, S(O)mRb, NRcRd, C(O)Re, or C(O)ORf;
- Rb is C1-C6 alkyl, NRcRd, or ORf;
- each of Rc and Rd is independently H, C1-C6 alkyl, C(O)Re, or C(O)ORf;
- Re is C1-C6 alkyl or NRgRh;
- Rf is H or C1-C6 alkyl;
- each of Rg and Rh is independently H or C1-C6 alkyl;
- m is 0, 1, or 2;
- n is 0, 1, 2, 3, or 4;
- and
- the compound is not selected from a compound selected from:
13 more elements
A compound selected from:
- and a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.