公开(公告)号：US20230134844A1

公开(公告)日：2023-05-04

申请号：US17902374

申请日：2022-09-02

申请人： AGENEBIO, INC.

发明人： Belew Mekonnen ,  John A. Butera ,  Jianxing Huang ,  Hemantbhai Patel

IPC分类号： C07D487/14

摘要： This invention relates to benzodiazepine derivatives, compositions comprising therapeutically effective amounts of those benzodiazepine derivatives and methods of using those derivatives or compositions in treating cognitive impairment associated with central nervous system (CNS) disorders. In particular, it relates to the use of a α5-containing GABAA receptor agonist (e.g., a α5-containing GABAA receptor positive allosteric modulator) as described herein in treating cognitive impairment associated with central nervous system (CNS) disorders in a subject in need or at risk thereof, including, without limitation, subjects having or at risk for age-related cognitive impairment, Mild Cognitive Impairment (MCI), amnestic MCI (aMCI), Age-Associated Memory Impairment (AAMI), Age Related Cognitive Decline (ARCD), dementia, Alzheimer's Disease(AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cancer-therapy-related cognitive impairment, mental retardation, Parkinson's disease (PD), autism spectrum disorders, fragile X disorder, Rett syndrome, compulsive behavior, and substance addiction. It also relates to the use of a α5-containing GABAA receptor agonist (e.g., a α5-containing GABAA receptor positive allosteric modulator) as described herein in treating brain cancers (including brain tumors, e.g., medulloblastomas), and cognitive impairment associated therewith.

公开(公告)号：US20240132513A1

公开(公告)日：2024-04-25

申请号：US18235753

申请日：2023-08-18

申请人： AGENEBIO, INC.

发明人： Belew Mekonnen ,  John A. Butera ,  Jianxing Huang ,  Hemantbhai Patel

IPC分类号： C07D487/14 ,  A61K45/06 ,  A61P25/28 ,  C07D413/14 ,  C07D487/04 ,  C07D498/14 ,  C07D519/00

CPC分类号： C07D487/14 ,  A61K45/06 ,  A61P25/28 ,  C07D413/14 ,  C07D487/04 ,  C07D498/14 ,  C07D519/00

摘要： Benzazepine derivatives, compositions comprising therapeutically effective amounts of those benzazepine derivatives and methods of using those derivatives or compositions in treating cognitive impairment associated with central nervous system (CNS) disorders or associated with risk factors for cognitive impairment. In particular, it relates to the use of a α5-containing GABAA R agonist (e.g., a α5-containing GABAA R positive allosteric modulator) in treating cognitive impairment associated with central nervous system (CNS) disorders or having a risk factor associated with cognitive impairment in a subject in need or at risk thereof, including, without limitation, subjects having or at risk for age-related cognitive impairment, Mild Cognitive Impairment (MCI), amnestic MCI (aMCI), Age-Associated Memory Impairment (AAMI), Age Related Cognitive Decline (ARCD), dementia, Alzheimer's Disease (AD), prodromal AD, post-traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cancer-therapy-related cognitive impairment, mental retardation, Parkinson's disease (PD), autism spectrum disorders, fragile X disorder, Rett syndrome, compulsive behavior, and substance addiction. It also relates to the use of a α5-containing GABAA R agonist (e.g., a α5-containing GABAA R positive allosteric modulator) as described herein in treating brain cancers (including brain tumors, e.g., medulloblastomas), and cognitive impairment associated therewith.

公开(公告)号：US20230098667A1

公开(公告)日：2023-03-30

申请号：US17786175

申请日：2020-12-18

申请人： AGENEBIO, INC.

发明人： Belew Mekonnen ,  John A. Butera ,  Jianxing Huang ,  Hemantbhai Patel ,  Qin Jiang ,  Robert Jason Herr ,  Emily Elizabeth Freeman ,  Nicholas James Mayhew

IPC分类号： A61K31/5517 ,  C07D487/14 ,  A61K31/496 ,  A61K31/5513 ,  A61K31/13 ,  A61K31/445 ,  A61K31/55 ,  A61K31/27 ,  A61P25/28

摘要： This invention relates to benzodiazepine derivatives, compositions comprising therapeutically effective amounts of those derivatives and methods of using those derivatives or compositions in treating cognitive impairment associated with CNS disorders. It also relates to the use of an α5-containing GABAA receptor agonist (e.g, an α5-containing GABAA receptor positive allosteric modulator) in treating cognitive impairment associated with CNS disorders in a subject in need or at risk thereof, including age-related cognitive impairment, Mild Cognitive Impairment (MCI), amnestic MCI, Age-Associated Memory Impairment, Age Related Cognitive Decline, dementia, Alzheimer's Disease (AD), prodromal AD, PTSD, schizophrenia, bipolar disorder, ALS, cancer-therapy-related cognitive impairment, mental retardation, Parkinson's disease, autism spectrum disorders, fragile X disorder, Rett syndrome, compulsive behavior, and substance addiction. It also relates to the use of an α5-containing GABAA receptor agonist (e.g., an α5-containing GABAA receptor positive allosteric modulator) in treating brain cancers (including brain tumors, e.g., medulloblastomas), and cognitive impairment associated therewith.

公开(公告)号：US20220274996A1

公开(公告)日：2022-09-01

申请号：US17592679

申请日：2022-02-04

申请人： AGENEBIO, INC.

发明人： Belew Mekonnen ,  John A. Butera ,  Jianxing Huang

IPC分类号： C07D487/14 ,  A61K45/06 ,  A61K31/13 ,  A61K31/551 ,  A61K31/496 ,  A61K31/445 ,  A61K31/55 ,  A61K31/27 ,  A61P25/00 ,  A61K31/5517

摘要： This invention relates to benzodiazepine derivatives, compositions comprising therapeutically effective amounts of those benzodiazepine derivatives and methods of using those derivatives or compositions in treating cognitive impairment associated with central nervous system (CNS) disorders. In particular, it relates to the use of α5-containing GABAA receptor agonist (e.g., a α5-containing GABAA receptor positive allosteric modulator) as described herein in treating cognitive impairment associated with central nervous system (CNS) disorders in a subject in need or at risk thereof, including, without limitation, subjects having or at risk for age-related cognitive impairment, Mild Cognitive Impairment (MCI), amnestic MCI (aMCI), Age-Associated Memory Impairment (AAMI), Age Related Cognitive Decline (ARCD), dementia, Alzheimer's Disease (AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cancer-therapy-related cognitive impairment, mental retardation, Parkinson's disease (PD), autism spectrum disorders, fragile X disorder, Rett syndrome, compulsive behavior, and substance addiction.

公开(公告)号：US11312721B2

公开(公告)日：2022-04-26

申请号：US17028917

申请日：2020-09-22

申请人： AGENEBIO, INC.

发明人： Belew Mekonnen ,  John A. Butera ,  Jianxing Huang

IPC分类号： C07D487/12 ,  C07D487/14 ,  A61K31/5513 ,  A61K45/06 ,  A61K31/13 ,  A61K31/551 ,  A61K31/496 ,  A61K31/445 ,  A61K31/55 ,  A61K31/27 ,  A61P25/00 ,  A61K31/5517

摘要： This invention relates to benzodiazepine derivatives, compositions comprising therapeutically effective amounts of those benzodiazepine derivatives and methods of using those derivatives or compositions in treating cognitive impairment associated with central nervous system (CNS) disorders. In particular, it relates to the use of a α5-containing GABAA receptor agonist (e.g., a α5-containing GABAA receptor positive allosteric modulator) as described herein in treating cognitive impairment associated with central nervous system (CNS) disorders in a subject in need or at risk thereof, including, without limitation, subjects having or at risk for age-related cognitive impairment, Mild Cognitive Impairment (MCI), amnestic MCI (aMCI), Age-Associated Memory Impairment (AAMI), Age Related Cognitive Decline (ARCD), dementia, Alzheimer's Disease (AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cancer-therapy-related cognitive impairment, mental retardation, Parkinson's disease (PD), autism spectrum disorders, fragile X disorder, Rett syndrome, compulsive behavior, and substance addiction.

公开(公告)号：US20210253588A1

公开(公告)日：2021-08-19

申请号：US16471237

申请日：2017-12-20

申请人： AGENEBIO, INC.

发明人： Belew Mekonnen ,  John A. Butera ,  Jianxing Huang

IPC分类号： C07D487/14

摘要： This invention relates to benzodiazepine derivatives, compositions comprising therapeutically effective amounts of those benzodiazepine derivatives and methods of using those derivatives or compositions in treating cognitive impairment associated with central nervous system (CNS) disorders. In particular, it relates to the use of a α5-containing GABAA receptor agonist (e.g., a α5-C containing GABAA receptor positive allosteric modulator) as described herein in treating cognitive impairment associated with central nervous system (CNS) disorders in a subject in need or at risk thereof, including, without limitation, subjects having or at risk for age-related cognitive impairment, Mild Cognitive Impairment (MCI), amnestic MCI (aMCI), Age-Associated Memory Impairment (AAMI), Age Related Cognitive Decline (ARCD), dementia, Alzheimer's Disease (AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cancer-therapy-related cognitive impairment, mental retardation, Parkinson's disease (PD), autism spectrum disorders, fragile X disorder, Rett syndrome, compulsive behavior, and substance addiction. It also relates to the use of a α5-containing GABAA receptor agonist (e.g., a α5-containing GABAA receptor positive allosteric modulator) as described herein in treating brain cancers (including brain tumors, e.g., medulloblastomas), and cognitive impairment associated therewith.

公开(公告)号：US20200048268A1

公开(公告)日：2020-02-13

申请号：US16445854

申请日：2019-06-19

申请人： AGENEBIO, INC.

发明人： Belew Mekonnen ,  John A. Butera ,  Jianxing Huang ,  Hemantbhai Patel ,  Qin Jiang ,  Robert Jason Herr ,  Emily Elizabeth Freeman ,  Nicholas James Mayhew

IPC分类号： C07D487/14 ,  A61P25/16 ,  A61P25/28 ,  A61P25/18

摘要： This invention relates to benzodiazepine derivatives, compositions comprising therapeutically effective amounts of those derivatives and methods of using those derivatives or compositions in treating cognitive impairment associated with CNS disorders. It also relates to the use of an α5-containing GABAA receptor agonist (e.g., an α5-containing GABAA receptor positive allosteric modulator) in treating cognitive impairment associated with CNS disorders in a subject in need or at risk thereof, including age-related cognitive impairment, Mild Cognitive Impairment (MCI), amnestic MCI, Age-Associated Memory Impairment, Age Related Cognitive Decline, dementia, Alzheimer's Disease (AD), prodromal AD, PTSD, schizophrenia, bipolar disorder, ALS, cancer-therapy-related cognitive impairment, mental retardation, Parkinson's disease, autism spectrum disorders, fragile X disorder, Rett syndrome, compulsive behavior, and substance addiction. It also relates to the use of an α5-containing GABAA receptor agonist (e.g., an α5-containing GABAA receptor positive allosteric modulator) in treating brain cancers (including brain tumors, e.g., medulloblastomas), and cognitive impairment associated therewith.

公开(公告)号：US20190284196A1

公开(公告)日：2019-09-19

申请号：US16428394

申请日：2019-05-31

申请人： AGENEBIO, INC.

发明人： Belew Mekonnen ,  John A. Butera ,  Jianxing Huang

IPC分类号： C07D487/14 ,  A61K45/06 ,  A61K31/551 ,  A61K31/5517

摘要： This invention relates to benzodiazepine derivatives, compositions comprising therapeutically effective amounts of those benzodiazepine derivatives and methods of using those derivatives or compositions in treating cognitive impairment associated with central nervous system (CNS) disorders. In particular, it relates to the use of a a5-containing GABAA receptor agonist (e.g., a α5-containing GABAA receptor positive allosteric modulator) as described herein in treating cognitive impairment associated with central nervous system (CNS) disorders in a subject in need or at risk thereof, including, without limitation, subjects having or at risk for age-related cognitive impairment, Mild Cognitive Impairment (MCI), amnestic MCI (aMCI), Age-Associated Memory Impairment (AAMI), Age Related Cognitive Decline (ARCD), dementia, Alzheimer's Disease (AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cancer-therapy-related cognitive impairment, mental retardation, Parkinson's disease (PD), autism spectrum disorders, fragile X disorder, Rett syndrome, compulsive behavior, and substance addiction.

公开(公告)号：US20190055258A1

公开(公告)日：2019-02-21

申请号：US15736697

申请日：2016-06-17

申请人： AgeneBio, Inc.

发明人： Belew Mekonnen ,  John A. Butera ,  Jianxing Huang

IPC分类号： C07D487/14 ,  A61K31/551 ,  A61K31/5517 ,  A61K45/06 ,  A61K31/13 ,  A61P25/00

CPC分类号： C07D487/14 ,  A61K31/13 ,  A61K31/27 ,  A61K31/445 ,  A61K31/496 ,  A61K31/55 ,  A61K31/551 ,  A61K31/5517 ,  A61K45/06 ,  A61P25/00 ,  A61K2300/00

摘要： This invention relates to benzodiazepine derivatives, compositions comprising therapeutically effective amounts of those benzodiazepine derivatives and methods of using those derivatives or compositions in treating cognitive impairment associated with central nervous system (CNS) disorders. In particular, it relates to the use of a α5-containing GABAA receptor agonist (e.g., a α5-containing GABAA receptor positive allosteric modulator) as described herein in treating cognitive impairment associated with central nervous system (CNS) disorders in a subject in need or at risk thereof, including, without limitation, subjects having or at risk for age-related cognitive impairment, Mild Cognitive Impairment (MCI), amnestic MCI (aMCI), Age-Associated Memory Impairment (AAMI), Age Related Cognitive Decline (ARCD), dementia, Alzheimer's Disease (AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cancer-therapy-related cognitive impairment, mental retardation, Parkinson's disease (PD), autism spectrum disorders, fragile X disorder, Rett syndrome, compulsive behavior, and substance addiction.

公开(公告)号：US11414425B2

公开(公告)日：2022-08-16

申请号：US16445854

申请日：2019-06-19

申请人： AGENEBIO, INC.

发明人： Belew Mekonnen ,  John A. Butera ,  Jianxing Huang ,  Hemantbhai Patel ,  Qin Jiang ,  Robert Jason Herr ,  Emily Elizabeth Freeman ,  Nicholas James Mayhew

IPC分类号： A61K31/551 ,  A61K31/5517 ,  A61K45/06 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28 ,  C07D487/12 ,  C07D487/14

摘要： This invention relates to benzodiazepine derivatives, compositions comprising therapeutically effective amounts of those derivatives and methods of using those derivatives or compositions in treating cognitive impairment associated with CNS disorders. It also relates to the use of an α5-containing GABAA receptor agonist (e.g., an α5-containing GABAA receptor positive allosteric modulator) in treating cognitive impairment associated with CNS disorders in a subject in need or at risk thereof, including age-related cognitive impairment, Mild Cognitive Impairment (MCI), amnestic MCI, Age-Associated Memory Impairment, Age Related Cognitive Decline, dementia, Alzheimer's Disease (AD), prodromal AD, PTSD, schizophrenia, bipolar disorder, ALS, cancer-therapy-related cognitive impairment, mental retardation, Parkinson's disease, autism spectrum disorders, fragile X disorder, Rett syndrome, compulsive behavior, and substance addiction. It also relates to the use of an α5-containing GABAA receptor agonist (e.g., an α5-containing GABAA receptor positive allosteric modulator) in treating brain cancers (including brain tumors, e.g., medulloblastomas), and cognitive impairment associated therewith.