# US 10,870,677 B2 · Compositions and methods for treating CNS disorders

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- Number: US 10,870,677 B2
- Document ID: US10870677B2
- Status: Granted
- Kind: B2
- Application number: 16/365,123
- Filed: 2019-03-26
- Published: 2020-01-23
- Granted: 2020-12-22
- Earliest claimed: 2014-10-16
- Assignees: Sage Therapeutics, Inc.
- Applicants: Sage Therapeutics, Inc.
- Inventors: Gabriel Martinez Botella; Francesco G. Salituro; Albert Jean Robichaud; Boyd L. Harrison
- Web page: https://patentgrep.com/patent/US10870677B2

## CPC

- C07J 43/003: {not condensed}
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 31/58: containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin (digitoxin {A61K31/7048})
- A61P 25/00: Drugs for disorders of the nervous system
- C07D 231/14: with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D 249/04: 1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
- C07D 249/18: Benzotriazoles
- C07D 295/033: with the ring nitrogen atoms directly attached to carbocyclic rings
- C07J 9/00: Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
- C07J 13/007: {with double bond in position 17 (20)}
- C07J 75/00: Processes for the preparation of steroids in general
- C07J: STEROIDS (seco-steroids C07C)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable said thereof; wherein, R1, R2a, R2b, R3 and A 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.

## Claims

### Claim 1

A process for preparing a compound of Formula (A14):
the process comprising, treating a compound of Formula (A13):
with trimethyl(trifluoromethyl)silane and tetra-n-butylammonium fluoride, wherein the process is performed in tetrahydrofuran at room temperature.