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：US09145372B2

公开(公告)日：2015-09-29

申请号：US13885569

申请日：2011-11-15

申请人： John A. Lowe, III

发明人： John A. Lowe, III

IPC分类号： C07D403/00 ,  C07D405/00 ,  C07D409/00 ,  C07D401/00 ,  C07D251/00 ,  A61K31/50 ,  C07D237/24 ,  C07D413/04 ,  C07D401/04 ,  C07D403/04 ,  C07D413/14

CPC分类号： A61K31/501 ,  A61K31/50 ,  C07D237/24 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04 ,  C07D413/14

摘要： This invention relates to pyridazine derivatives, compositions comprising therapeutically effective amounts of those pyridazine derivatives and methods of using those derivatives or compositions in treating central nervous system (CNS) disorders with cognitive impairment that are responsive to agonists of α5 subunit containing GABAA receptor, e.g., age-related cognitive impairment, Mild Cognitive Impairment (MCI), dementia, Alzheimer's Disease (AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia and cancer-therapy-related cognitive impairment.

摘要翻译： 本发明涉及哒嗪衍生物，包含治疗有效量的那些哒嗪衍生物的组合物和使用这些衍生物或组合物治疗对具有含有GABA A受体的α5亚基的激动剂有反应的认知障碍的中枢神经系统（CNS）障碍的方法， 年龄相关的认知障碍，轻度认知障碍（MCI），痴呆，阿尔茨海默病（AD），前驱性AD，创伤后应激障碍（PTSD），精神分裂症和癌症治疗相关的认知障碍。

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.

公开(公告)号：US20220062296A1

公开(公告)日：2022-03-03

申请号：US17372405

申请日：2021-07-09

申请人： AGENEBIO, INC.

发明人： Michela Gallagher ,  Sharon Rosenzweig-Lipson

IPC分类号： A61K31/5517 ,  A61K45/06

摘要： This disclosure relates to methods, uses, combinations, pharmaceutical compositions, combinations for use, and pharmaceutical compositions for use useful for treating cognitive impairment associated with central nervous system (CNS) disorders. In particular, it relates to the use of inhibitors of synaptic vesicle glycoprotein 2A (SV2A), in combination with GABAA α5 receptor agonists, 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, cancer-therapy-related cognitive impairment, mental retardation, Parkinson's disease, autism, compulsive behavior, and substance addiction. Further, the disclosure relates to methods, uses, combinations, pharmaceutical compositions, combinations for use, and pharmaceutical compositions for use useful for treating cognitive impairment associated with brain cancer or for treating brain cancer itself in a subject in need thereof. Additionally, the disclosure relates to methods, uses, combinations, pharmaceutical compositions, combinations for use, and pharmaceutical compositions for use useful for treating Parkinson's disease psychosis in a subject in need thereof.

公开(公告)号：US10815242B2

公开(公告)日：2020-10-27

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： C07D487/12 ,  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 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：US09801879B2

公开(公告)日：2017-10-31

申请号：US14858959

申请日：2015-09-18

申请人： AGENEBIO, INC.

发明人： John A. Lowe, III

IPC分类号： A61K31/50 ,  A61K31/501 ,  C07D237/24 ,  C07D413/04 ,  C07D401/04 ,  C07D403/04 ,  C07D413/14

CPC分类号： A61K31/501 ,  A61K31/50 ,  C07D237/24 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04 ,  C07D413/14

摘要： This invention relates to pyridazine derivatives, compositions comprising therapeutically effective amounts of those pyridazine derivatives and methods of using those derivatives or compositions in treating central nervous system (CNS) disorders with cognitive impairment that are responsive to agonists of α5 subunit containing GABAA receptor, e.g., age-related cognitive impairment, Mild Cognitive Impairment (MCI), dementia, Alzheimer's Disease (AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia and cancer-therapy-related cognitive impairment.

公开(公告)号：US20230270753A1

公开(公告)日：2023-08-31

申请号：US18015439

申请日：2021-07-09

申请人： AGENEBIO, INC.

发明人： Michela Gallagher ,  Sharon Rosenzweig-Lipson

IPC分类号： A61K31/5517 ,  A61P25/28 ,  A61K9/00 ,  A61K31/4015

CPC分类号： A61K31/5517 ,  A61P25/28 ,  A61K9/0053 ,  A61K31/4015 ,  C07B2200/13

摘要： This disclosure relates to methods, uses, combinations, pharmaceutical compositions, combinations for use, and pharmaceutical compositions for use useful for treating cognitive impairment associated with central nervous system (CNS) disorders. In particular, it relates to the use of inhibitors of synaptic vesicle glycoprotein 2A (SV2A), in combination with GABAA α5 receptor agonists, 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, cancer-therapy-related cognitive impairment, mental retardation, Parkinson's disease, autism, compulsive behavior, and substance addiction. Further, the disclosure relates to methods, uses, combinations, pharmaceutical compositions, combinations for use, and pharmaceutical compositions for use useful for treating cognitive impairment associated with brain cancer or for treating brain cancer itself in a subject in need thereof. Additionally, the disclosure relates to methods, uses, combinations, pharmaceutical compositions, combinations for use, and pharmaceutical compositions for use useful for treating Parkinson's disease psychosis in a subject in need thereof.

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：US11160785B2

公开(公告)日：2021-11-02

申请号：US14776378

申请日：2014-03-14

申请人： AgeneBio, Inc.

发明人： Gardiner Smith

IPC分类号： A61K31/4015 ,  A61K31/445 ,  A61K31/27 ,  A61K31/662 ,  A61K31/55

摘要： The invention relates to compositions comprising a synaptic vesicle glycoprotein 2A (SV2A) inhibitor in an extended release and an acetylcholinesterase inhibitor (AChEIs). The invention also relates to using such compositions in treating cognitive impairment associated with central nervous system 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), 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, compulsive behavior, and substance addiction.