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：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：US11344563B2

公开(公告)日：2022-05-31

申请号：US16507214

申请日：2019-07-10

Applicant: Sage Therapeutics, Inc.

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

IPC: A61K31/58 ,  C07J7/00 ,  C07J3/00 ,  C07J9/00 ,  C07J17/00 ,  C07J33/00 ,  C07J15/00 ,  C07J43/00 ,  A61K31/573 ,  C07J1/00 ,  C07J13/00 ,  C07J21/00 ,  C07J41/00 ,  C07J5/00 ,  C07J31/00

Abstract: Provided herein are 19-nor C3,3-disubstituted steroids of Formula (I): and pharmaceutically acceptable salts thereof; wherein , R1, R2, R3a, R3b, R4a, and R4b are as defined herein, and A is a carbon bound substituted or unsubstituted 5- to 6-membered heteroaryl ring 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：US20210380631A1

公开(公告)日：2021-12-09

申请号：US17395155

申请日：2021-08-05

Applicant: Sage Therapeutics, Inc.

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

IPC: C07J9/00 ,  C07J17/00 ,  A61P25/20 ,  A61P25/28 ,  A61P25/22 ,  A61P19/02 ,  A61P25/18 ,  A61P1/00 ,  A61P25/16 ,  A61P35/00 ,  C07J43/00

Abstract: Compounds are provided according to Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R2, R3, R4, R5, and R6 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：US11147877B2

公开(公告)日：2021-10-19

申请号：US16545727

申请日：2019-08-20

Applicant: Sage Therapeutics, Inc.

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

IPC: C07J3/00 ,  C07J7/00 ,  A61K31/00 ,  A61K45/06 ,  C07J13/00 ,  C07J41/00 ,  C07J43/00 ,  C07J51/00 ,  C07J9/00 ,  A61K45/00

Abstract: Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein , A, R1, R2, and R3 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, e.g., for treating a subject suffering from a disease or disorder described herein.