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(0)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.
Type:
Grant
Filed:
June 13, 2023
Date of Patent:
February 27, 2024
Assignee:
Sage Therapeutics, Inc.
Inventors:
Maria Jesus Blanco-Pillado, Francesco G. Salituro, Marshall Lee Morningstar
Abstract: 3beta, 17beta disubstituted steroidal compounds, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, are provided for the prevention and treatment of a variety of CNS-related conditions.
Type:
Grant
Filed:
July 21, 2021
Date of Patent:
February 20, 2024
Assignee:
SAGE THERAPEUTICS, INC.
Inventors:
Gabriel Martinez Botella, Boyd L Harrison, Albert Jean Robichaud, Francesco G. Salituro
Abstract: This invention relates to a crystalline 19-nor C3,3-disubstituted C21-pyrazolyl steroid of Formula (I), and compositions thereof. Also disclosed herein are methods of making the same and methods of using the same.
Type:
Grant
Filed:
August 6, 2021
Date of Patent:
January 30, 2024
Assignee:
Sage Therapeutics, Inc.
Inventors:
Paul Steven Watson, Bret Berner, John Gregory Reid, Jian Wang, James J. Doherty, Stephen Jay Kanes
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.
Type:
Grant
Filed:
April 28, 2021
Date of Patent:
January 30, 2024
Assignee:
Sage Therapeutics, Inc.
Inventors:
Albert Jean Robichaud, Francesco G. Salituro, Gabriel Martinez Botella, Boyd L. Harrison, John Gregory Reid
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.
Type:
Grant
Filed:
July 8, 2022
Date of Patent:
January 23, 2024
Assignee:
Sage Therapeutics, Inc.
Inventors:
Gabriel Martinez Botella, Boyd L Harrison, Albert Jean Robichaud, Francesco G. Salituro
Abstract: Described herein are steroids of Formula (I): and pharmaceutically acceptable salts thereof; wherein R1, R2a, R2b, R3, R4, R5a, R5b, R6, and Z are 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.
Type:
Grant
Filed:
September 13, 2021
Date of Patent:
October 10, 2023
Assignee:
Sage Therapeutics, Inc.
Inventors:
Boyd L. Harrison, Gabriel Martinez Botella, Albert Jean Robichaud, Francesco G. Salituro
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.
Type:
Grant
Filed:
August 6, 2021
Date of Patent:
August 22, 2023
Assignee:
Sage Therapeutics, Inc.
Inventors:
Francesco G. Salituro, Albert Jean Robichaud, Gabriel Martinez Botella, Boyd L. Harrison
Abstract: Provided herein is a compound of Formula (I-I), or a pharmaceutically acceptable salt thereof, wherein the variables 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.
Type:
Grant
Filed:
January 11, 2019
Date of Patent:
August 8, 2023
Assignee:
Sage Therapeutics, Inc.
Inventors:
Albert Jean Robichaud, Francesco G. Salituro, Maria Jesus Blanco-Pillado, Daniel La, Boyd L. Harrison
Abstract: Provided herein is a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R3a, R5, R6a, R6b, R17, R21a, R21b, Rm, Rn, R16a, R16b, R7a, R7b, R12a, R12b, R11a, R11b, R2a, R2b, R19, R4a, and R4b 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.
Type:
Grant
Filed:
December 8, 2021
Date of Patent:
June 6, 2023
Assignee:
Sage Therapeutics, Inc.
Inventors:
Francesco G. Salituro, Albert Jean Robichaud
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.
Type:
Grant
Filed:
May 29, 2020
Date of Patent:
May 9, 2023
Assignee:
Sage Therapeutics, Inc.
Inventors:
Francesco G. Salituro, Maria Jesus Blanco-Pillado, Marshall Lee Morningstar
Abstract: Provided herein is a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein n, R19, R5, R3a, R6a, R6b, R1, R2a, R2b, R4a, R4b, R7a, R7b, R11a, R11b, R12a, R12b, R17b, R15a, R15b, R16a and R16b 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.
Type:
Grant
Filed:
October 11, 2019
Date of Patent:
April 25, 2023
Assignee:
Sage Therapeutics, Inc.
Inventors:
Maria Jesus Blanco-Pillado, Francesco G. Salituro, Marshall Lee Morningstar
Abstract: Compounds are provided according to Formula (A): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R1, R2, R3, R4, R5, R6, and RG are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.
Type:
Grant
Filed:
July 27, 2021
Date of Patent:
March 28, 2023
Assignee:
SAGE THERAPEUTICS, INC.
Inventors:
Francesco G. Salituro, Albert Jean Robichaud, Gabriel Martinez Botella, Boyd L. Harrison, Andrew Griffin
Abstract: Described herein are methods of treating a disorder, e.g., tremor, e.g., essential tremor; depression, e.g., postpostum depression; and anxiety disorder, the method comprising administering to a human subject suffering from a disorder, e.g., tremor, e.g., essential tremor; depression, e.g., postpostum depression, an anxiety disorder with a neuroactive steroid or a composition comprising a neuroactive steroid (e.g., pregnanolone, allopregnanolone, alphadalone, ganaxolone, or alphaxolone).
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.
Type:
Grant
Filed:
March 15, 2022
Date of Patent:
January 3, 2023
Assignee:
Sage Therapeutics, Inc.
Inventors:
Gabriel Martinez Botella, Francesco G. Salituro, Albert Jean Robichaud, Boyd L. Harrison
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.
Type:
Grant
Filed:
January 21, 2020
Date of Patent:
December 20, 2022
Assignee:
Sage Therapeutics, Inc.
Inventors:
Gabriel Martinez Botella, Francesco G. Salituro, Albert Jean Robichaud, Boyd L. Harrison
Abstract: Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein -------, R1, R2, R5, A and L 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.
Type:
Grant
Filed:
April 8, 2020
Date of Patent:
November 15, 2022
Assignee:
Sage Therapeutics, Inc.
Inventors:
Gabriel Martinez Botella, Boyd L. Harrison, Albert Jean Robichaud, Francesco G. Salituro, Robert Jason Herr, Robert Borbo Kargbo
Abstract: Formulations of comprising a neuroactive steroid, e.g., allopregnanolone; and optionally a cyclodextrin, e.g., a ?-cyclodextrin, e.g., a sulfo butyl ether ?-cyclodextrin, e.g., a ?-cyclodextrin, e.g., a sulfo butyl ether ?-cyclodextrin, e.g., CAPTISOL®; and methods of use in treating CNS disorders.
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.
Type:
Grant
Filed:
July 15, 2020
Date of Patent:
August 9, 2022
Assignee:
SAGE THERAPEUTICS, INC.
Inventors:
Gabriel Martinez Botella, Boyd L. Harrison, Albert Jean Robichaud, Francesco G. Salituro
Abstract: Described herein are neuroactive steroids or a pharmaceutically acceptable salt thereof. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. Also provided are pharmaceutical compositions comprising a compound described herein and methods of use and treatment, e.g., such as for inducing sedation and/or anesthesia.
Type:
Grant
Filed:
July 11, 2017
Date of Patent:
July 26, 2022
Assignee:
Sage Therapeutics, Inc.
Inventors:
Albert Jean Robichaud, Gabriel Martinez Botella, Boyd L. Harrison, Francesco G. Salituro, Andrew Griffin, Maria Jesus Blanco-Pillado
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.
Type:
Grant
Filed:
July 10, 2019
Date of Patent:
May 31, 2022
Assignee:
Sage Therapeutics, Inc.
Inventors:
Gabriel Martinez Botella, Boyd L. Harrison, Albert Jean Robichaud, Francesco G. Salituro, Richard Thomas Beresis