公开(公告)号：US20240270784A1

公开(公告)日：2024-08-15

申请号：US18535256

申请日：2023-12-11

Applicant: Sage Therapeutics, Inc.

Inventor： Albert Jean Robichaud ,  Francesco G. Salituro ,  Gabriel Martinez Botella ,  Boyd L. Harrison ,  John Gregory Reid

IPC: C07J9/00 ,  A61K31/57 ,  C07J17/00 ,  C07J43/00

CPC classification number: C07J9/00 ,  A61K31/57 ,  C07J17/00 ,  C07J43/003

Abstract: Compounds are provided according to Formula (I), and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein A, R1, and R5 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

公开(公告)号：US20240076310A1

公开(公告)日：2024-03-07

申请号：US18482079

申请日：2023-10-06

Applicant: Sage Therapeutics, Inc.

Inventor： Gabriel Martinez Botella ,  Boyd L. Harrison ,  Albert Jean Robichaud ,  Francesco G. Salituro ,  Richard Thomas Beresis

IPC: C07J43/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  C07J7/00

CPC classification number: C07J43/003 ,  A61P25/08 ,  A61P25/14 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  C07J7/0085 ,  C07J31/006

Abstract: Provided herein are 19-nor C3, 3-disubstituted steroids of Formula (I): and pharmaceutically acceptable salts thereof; wherein R1, R2, R3, and R4 are as defined herein, and A is a heteroaryl ring system comprising 3 or 4 nitrogens as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.

公开(公告)号：US11912737B2

公开(公告)日：2024-02-27

申请号：US17067093

申请日：2020-10-09

Applicant: Sage Therapeutics, Inc.

Inventor： Gabriel Martinez Botella ,  Boyd L. Harrison ,  Albert Jean Robichaud ,  Francesco G. Salituro ,  Richard Thomas Beresis

IPC: C07J21/00 ,  C07J43/00 ,  C07J1/00 ,  C07J7/00 ,  C07J13/00 ,  C07J31/00 ,  C07J71/00

CPC classification number: C07J43/003 ,  C07J1/007 ,  C07J1/0059 ,  C07J1/0074 ,  C07J7/002 ,  C07J7/007 ,  C07J7/0085 ,  C07J13/007 ,  C07J21/00 ,  C07J31/006 ,  C07J71/001

Abstract: Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I):




and pharmaceutical compositions thereof. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, tinnitus, status epilepticus.

公开(公告)号：US11878995B2

公开(公告)日：2024-01-23

申请号：US17860816

申请日：2022-07-08

Applicant: SAGE THERAPEUTICS, INC.

Inventor： Gabriel Martinez Botella ,  Boyd L Harrison ,  Albert Jean Robichaud ,  Francesco G. Salituro

IPC: C07J9/00

CPC classification number: C07J9/00 ,  C07J9/005 ,  C07B2200/05

Abstract: Compounds are provided according to Formula (III):




and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R2, R3, R5, and n are as defined herein, and at least one hydrogen is replaced with a deuterium. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

公开(公告)号：US11732000B2

公开(公告)日：2023-08-22

申请号：US17396034

申请日：2021-08-06

Applicant: Sage Therapeutics, Inc.

Inventor： Francesco G. Salituro ,  Albert Jean Robichaud ,  Gabriel Martinez Botella ,  Boyd L. Harrison

IPC: C07J9/00 ,  C07J7/00 ,  A61P23/00 ,  A61P25/20 ,  A61P3/00 ,  C07J17/00 ,  C07J31/00 ,  C07J13/00 ,  C07J41/00

CPC classification number: C07J9/00 ,  A61P3/00 ,  A61P23/00 ,  A61P25/20 ,  C07J17/00 ,  C07J7/002 ,  C07J9/005 ,  C07J13/005 ,  C07J13/007 ,  C07J31/006 ,  C07J41/0061

Abstract: Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R1, R2, and R3 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

公开(公告)号：US20230192756A1

公开(公告)日：2023-06-22

申请号：US17707303

申请日：2022-03-29

Applicant: SAGE THERAPEUTICS, INC.

Inventor： Ravindra B. Upasani ,  Boyd L. Harrison ,  Benny C. Askew ,  Jean-Cosme Dodart ,  Francesco G. Salituro ,  Albert Jean Robichaud

IPC: C07J41/00 ,  C07J9/00 ,  C07J1/00 ,  C07J3/00 ,  C07J7/00 ,  C07J31/00 ,  C07J43/00 ,  C07J75/00

CPC classification number: C07J41/00 ,  C07J9/00 ,  C07J1/0029 ,  C07J3/00 ,  C07J7/007 ,  C07J9/005 ,  C07J31/003 ,  C07J31/006 ,  C07J41/0005 ,  C07J41/0011 ,  C07J41/0055 ,  C07J43/003 ,  C07J75/00 ,  C07J1/00

Abstract: Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, wherein Z is a group of the formula (i), (ii), (iii), (iv), or (v), and wherein L1, L2, L3, X1, X2, Y, Rz4, Rz5, Rz6, n, R1, R2, R3a, R3b, R4a, R4b, R6a, R6b, R7a, R7b, R11a, R11b, R14, R17, R19, R20, R23a, R23b, and R24 are as defined herein, and pharmaceutical compositions thereof. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions in mammals.

公开(公告)号：US20230190770A1

公开(公告)日：2023-06-22

申请号：US18107965

申请日：2023-02-09

Applicant: Washington University ,  Sage Therapeutics, Inc.

Inventor： Douglas Covey ,  Albert Jean Robichaud

IPC: A61K31/58 ,  C07J1/00 ,  C07J5/00 ,  C07J7/00 ,  C07J21/00 ,  C07J41/00 ,  C07J9/00 ,  C07J13/00 ,  A61K31/56 ,  A61K31/565 ,  A61K31/566 ,  A61K31/573

CPC classification number: A61K31/58 ,  C07J1/0011 ,  C07J1/0018 ,  C07J1/0029 ,  C07J5/0015 ,  C07J7/002 ,  C07J21/00 ,  C07J41/0005 ,  C07J41/0094 ,  C07J9/005 ,  C07J13/007 ,  A61K31/56 ,  A61K31/565 ,  A61K31/566 ,  A61K31/573 ,  C07J21/006 ,  C07J21/008 ,  C07J51/00

Abstract: The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.

公开(公告)号：US20230047157A1

公开(公告)日：2023-02-16

申请号：US17749976

申请日：2022-05-20

Applicant: SAGE THERAPEUTICS, INC.

Inventor： Francesco G. Salituro ,  Albert Jean Robichaud ,  Gabriel Martinez Botella

IPC: C07J9/00 ,  C07J31/00 ,  C07J41/00 ,  C07J51/00 ,  A61P1/00 ,  A61P25/00

Abstract: Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R1, R2, R3, R4, R5, and R8 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

公开(公告)号：US11530237B2

公开(公告)日：2022-12-20

申请号：US16748117

申请日：2020-01-21

Applicant: Sage Therapeutics, Inc.

Inventor： Gabriel Martinez Botella ,  Francesco G. Salituro ,  Albert Jean Robichaud ,  Boyd L. Harrison

IPC: C07J43/00 ,  C07J1/00 ,  C07J7/00 ,  A61K31/58 ,  A61K31/575 ,  A61P23/00 ,  A61P25/00 ,  A61P25/06 ,  A61P25/08 ,  A61P25/14 ,  A61P25/18 ,  A61P25/20 ,  A61K45/06 ,  C07J9/00 ,  C07J3/00 ,  C07J5/00 ,  C07J11/00 ,  C07J13/00 ,  C07J21/00 ,  C07J31/00 ,  C07J41/00 ,  C07J51/00 ,  C07J71/00

Abstract: Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein , A, R1, R2, R3a, R4a, R4b, R5, R7a, and R7b 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.

公开(公告)号：US20220315621A1

公开(公告)日：2022-10-06

申请号：US16955736

申请日：2018-12-21

Applicant: Sage Therapeutics, Inc.

Inventor： Albert Jean Robichaud ,  Francesco G. Salituro ,  Maria Jesus Blanco-Pillado ,  Daniel La ,  Boyd L. Harrison

IPC: C07J63/00 ,  C07J61/00

Abstract: Provided herein is a compound of Formula (I-I) or a pharmaceutically acceptable salt thereof, wherein t, R7, R3, R9, R6a, R6b, R11a, R11b, R15a, R15b, R16a, R16b, R17a, R17b, R18a, R18b, R19a, R19b, R5a, R5b, R8 and R13 are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I-I) and methods of using the compounds, e.g., in the treatment of CNS-related disorders.