IP Library Granted Patent US 12,410,210
Granted Patent B2
US 12,410,210 · App. 18/616,995 · Granted Sep 9, 2025

Neuroactive steroids and their methods of use

Inventors: Maria Jesus Blanco-Pillado (Arlington, MA); Francesco G. Salituro (Marlborough, MA); Marshall Lee Morningstar (Framingham, MA)
Assignee: Sage Therapeutics, Inc.
C07J43/003C07J41/0044C07J41/0094
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 12,410,210
App. No.
18/616,995
Granted
Sep 9, 2025
Kind
B2
Abstract

Provided herein is a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R 19 , R 5 , R 3a , R 1a , R 1b , R 2a , R 2b , R 4a , R 4b , R 6a , R 6b , R 7a , R 7b , R 11a , R 11b , R 12a , R 12b , R 18 , R D , and q are defined herein. L is selected from the group consisting of: wherein A indicates the point of attachment at C17 and wherein X is selected from the group consisting of —C(O)N(R 55a )(R 55b ), —N(R 55a )(R 55b ), —N(R 55b )C(O)(R 55a ), and R 55C wherein R 55c is carbon-bound substituted or unsubstituted heteroaryl or substituted or unsubstituted aryl. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds, e.g., in the treatment of CNS-related disorders.

Claims (62)

1. A compound selected from

Exa-

Structure

mple

305

306

317

318

325

326

 51

 52

355

and

356

2. A compound selected from

Example

Structure

305

317

325

 51

and

355

3. A compound selected from

Example

Structure

306

318

326

 52

356

4. The compound of claim 1 , wherein the compound has the structural formula

5. The compound of claim 1 , wherein the compound has the structural formula

6. The compound of claim 1 , wherein the compound has the structural formula

7. The compound of claim 1 , wherein the compound has the structural formula

8. The compound of claim 1 , wherein the compound has the structural formula

9. The compound of claim 1 , wherein the compound has the structural formula

10. The compound of claim 1 , wherein the compound has the structural formula

11. The compound of claim 1 , wherein the compound has the structural formula

12. The compound of claim 1 , wherein the compound has the structural formula

13. The compound of claim 1 , wherein the compound has the structural formula

14. A pharmaceutical composition comprising a compound having the structural formula

and a pharmaceutically acceptable excipient.

15. A pharmaceutical composition comprising a compound having the structural formula

and a pharmaceutically acceptable excipient.

16. A pharmaceutical composition comprising a compound having the structural formula

and a pharmaceutically acceptable excipient.

17. A pharmaceutical composition comprising a compound having the structural formula

and a pharmaceutically acceptable excipient.

18. A pharmaceutical composition comprising a compound having the structural formula

and a pharmaceutically acceptable excipient.

19. A pharmaceutical composition comprising a compound having the structural formula

and a pharmaceutically acceptable excipient.

20. A pharmaceutical composition comprising a compound having the structural formula

and a pharmaceutically acceptable excipient.

21. A pharmaceutical composition comprising a compound having the structural formula

and a pharmaceutically acceptable excipient.

22. A pharmaceutical composition comprising a compound having the structural formula

and a pharmaceutically acceptable excipient.

23. A pharmaceutical composition comprising a compound having the structural formula

and a pharmaceutically acceptable excipient.

Assignments (2)
CHANGE OF NAME Recorded Apr 23, 2026
From: SAGE THERAPEUTICS, INC.
To: SAGE THERAPEUTICS, LLC
Reel/Frame 075472/0569 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 21, 2024
From: BLANCO-PILLADO, MARIA JESUS; SALITURO, FRANCESCO G.; MORNINGSTAR, MARSHALL LEE
To: SAGE THERAPEUTICS, INC.
Reel/Frame 067481/0402 →
Continuity (4)
Continuation 18334124 · Jun 13, 2023
Continuation 17311056
Provisional Application 62775470 · Dec 5, 2018
Related Publication 20240343756A1 · Oct 17, 2024
References Cited (36)
US 5939545A · Upasani et al. · 1999 [cited by applicant]
US 8569275B2 · Frincke · 2013 [cited by applicant]
US 9512165B2 · Martinez Botella et al. · 2016 [cited by applicant]
US 11236121B2 · Watson et al. · 2022 [cited by applicant]
US 11643434B2 · Salituro et al. · 2023 [cited by applicant]
US 20200384003A1 · Zheng et al. · 2020 [cited by applicant]
US 20210139530A1 · Su et al. · 2021 [cited by applicant]
US 20220226350A1 · Macconell et al. · 2022 [cited by applicant]
US 20220396597A1 · Covey et al. · 2022 [cited by applicant]
US 20230287037A1 · Upasani et al. · 2023 [cited by applicant]
CN 108727453 · 2018 [cited by applicant]
FR 2969M · 1904 [cited by applicant]
GB 1494097 · 1977 [cited by applicant]
GB 1521235 · 1978 [cited by applicant]
GB 1538869 · 1979 [cited by applicant]
GB 1570394 · 1980 [cited by applicant]
GB 1581234 · 1980 [cited by applicant]
WO 9616076A1 · 1996 [cited by applicant]
WO 9805337A1 · 1998 [cited by applicant]
WO 2016061527A1 · 2016 [cited by applicant]
WO 2017049044A1 · 2017 [cited by applicant]
WO 2017187343A2 · 2017 [cited by applicant]
WO 2019126761A1 · 2019 [cited by applicant]
WO 2020061332A1 · 2020 [cited by applicant]
WO 2020210116A1 · 2020 [cited by applicant]
WO 2020210117A1 · 2020 [cited by applicant]
WO 2020264512A1 · 2020 [cited by applicant]
Chisari et al., “The Influence of Neuroactive Steroid Lipophilicity on GABAA Receptor Modulation: Evidence for a Low-Affinity Interaction”, Journal of Neurophysiology, vol. 102, No. 2, Jun. 24, 2009, pp. 1254-1264. [cited by applicant]
Dansey et al., “Synthesis and GABA receptor activity of A-homo analogues of neuroactive steroids”, European Journal of Medicinal Chemistry, vol. 45, n. 7, Mar. 26, 2021, pp. 3063-3069. [cited by applicant]
G. Akk et al. “Neurosteroid Access to the GABAA Receptor”, The Journal of Neuroscience, vol. 25, No. 50, Dec. 14, 2005, pp. 11605-11613. [cited by applicant]
Phillipps G.H. et al., “Water-Soluble Steroidal Anasthetics”, Journal of Steroid Biochemisty, vol. 11, No. 1, Jul. 1, 1979, pp. 79-86. [cited by applicant]
Search Report and Written Opinion for PCT/US2019/064692. [cited by applicant]
Search Report and Written Opinion for PCT/US2020/040164. [cited by applicant]
H.J. Shu et al., “Photodynamic Effects of Steroid-Conjugated Fluorophores on GABAA Receptors”, Molecular Pharmacology, vol. 76, No. 4, Oct. 1, 2009, pp. 754-765. [cited by applicant]
Sunol, Cristina et al., “Activity of B-Nor analogues of Neurosteroids on the GABAA receptor in Primary Neuronal Cultures”, Journal of Medicinal Chemistry, vol. 49, No. 11, Jun. 1, 2006 pp. 3225-3234. [cited by applicant]
U.S. Appl. No. 18/473,702, filed Sep. 25, 2023, Maria Jesus Blanco-Pillado et al., Pending. [cited by applicant]