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：US11999765B2

公开(公告)日：2024-06-04

申请号：US18334189

申请日：2023-06-13

Applicant: SAGE THERAPEUTICS, INC.

Inventor： Maria Jesus Blanco-Pillado ,  Francesco G. Salituro ,  Marshall Lee Morningstar

IPC: C07J43/00 ,  C07J41/00

CPC classification number: C07J43/003 ,  C07J41/0044 ,  C07J41/0094

Abstract: Provided herein is a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R19, R5, R3a, R1a, R1b, R2a, R2b, R4a, R4b, R6a, R6b, R7a, R7b, R11a, R11b, R12a, R12b, R18, RD, 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(R55a)(R55b), —N(R55a)(R55b), —N(R55b)C(O)(R55a), and R55C wherein R55c 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.

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：US11643434B2

公开(公告)日：2023-05-09

申请号：US16887887

申请日：2020-05-29

Applicant: Sage Therapeutics, Inc.

Inventor： Francesco G. Salituro ,  Maria Jesus Blanco-Pillado ,  Marshall Lee Morningstar

IPC: C07J43/00

CPC classification number: C07J43/003

Abstract: Provided herein is a compound of Formula (I):




or a pharmaceutically acceptable salt thereof, wherein R1a, R1b, R2a, R2b, R3, R4a, R4b, R5, R6a, R6b, R7a, R7a, R11a, R11b, R12a, R12b, R16a, R16b, R19, R11a, R22, RX, RY and n are defined herein. 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.

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.