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公开(公告)号:US20210395319A1
公开(公告)日:2021-12-23
申请号:US17461862
申请日:2021-08-30
申请人: OLIGOMERIX, INC.
发明人: James G. Moe , Eliot J. Davidowitz
摘要: Tau protein has a causative role in Alzheimer's disease and multiple other neurodegenerative disorders exhibiting tau histopathology collectively termed tauopathies. The primary function of tau protein is to facilitate assembly and maintenance of microtubules in neuronal axons. In the disease process tau protein becomes modified, loses its affinity to microtubules and accumulates in the cell body where it forms aggregates. The large neurofibrillary tangles formed from tau protein assembled into filaments were thought to be the pathological structure of tau. However, more recent work indicates that smaller, soluble oligomeric forms of tau are best associated with neuron loss and memory impairment. Here, novel compositions of tau oligomers and novel mechanisms for tau oligomer nucleation, extension and termination are taught. Methods for producing and purifying these structures for the development of small molecule and immunotherapeutics as well as antibodies for biomarkers of neurodegenerative diseases are taught.
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公开(公告)号:US20170015717A1
公开(公告)日:2017-01-19
申请号:US15285181
申请日:2016-10-04
申请人: OLIGOMERIX, INC.
发明人: JAMES G. MOE , Eliot J. Davidowitz
CPC分类号: C07K14/47 , A61K38/1709 , C12N9/6421
摘要: Tau protein has a causative role in Alzheimer's disease and multiple other neurodegenerative disorders exhibiting tau histopathology collectively termed tauopathies. The primary function of tau protein is to facilitate assembly and maintenance of microtubules in neuronal axons. In the disease process tau protein becomes modified, loses its affinity to microtubules and accumulates in the cell body where it forms aggregates. The large neurofibrillary tangles formed from tau protein assembled into filaments were thought to be the pathological structure of tau. However, more recent work indicates that smaller, soluble oligomeric forms of tau are best associated with neuron loss and memory impairment. Here, novel compositions of tau oligomers and novel mechanisms for tau oligomer nucleation, extension and termination are taught. Methods for producing and purifying these structures for the development of small molecule and immunotherapeutics as well as antibodies for biomarkers of neurodegenerative diseases are taught.
摘要翻译: Tau蛋白在阿尔茨海默病和多种其他神经退行性疾病中起着重要的作用,其表现为组织病理学统称为tau蛋白病。 tau蛋白的主要功能是促进神经元轴突中微管的组装和维持。 在疾病过程中,tau蛋白被修饰,丧失其对微管的亲和力,并在细胞体积聚,形成聚集体。 由tau蛋白形成的大的神经原纤维缠结组织成长丝被认为是tau的病理结构。 然而,最近的工作表明,较小的可溶性寡聚体形式的tau最好与神经元损失和记忆障碍有关。 在这里,教导了tau寡聚体的新型组合物和用于tau低聚物成核,延伸和终止的新机制。 制备和纯化用于开发小分子和免疫治疗剂的这些结构的方法以及用于神经变性疾病的生物标志物的抗体。
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3.
公开(公告)号:US20240158357A1
公开(公告)日:2024-05-16
申请号:US17967344
申请日:2022-10-17
申请人: OLIGOMERIX INC.
发明人: Eliot J. Davidowitz , James G. Moe , Allen B. Reitz , Haiyan Bian , Charles Gluchowski , James Hendrix , Albert S. Yehaskel , Mark E. McDonnell , H. Marie Loughran
IPC分类号: C07D239/91 , C07D401/04 , C07D401/14 , C07D471/04 , C07D495/04
CPC分类号: C07D239/91 , C07D401/04 , C07D401/14 , C07D471/04 , C07D495/04 , A61K45/06
摘要: Novel quinazolinones useful as inhibitors of tau oligomer formation, useful for the treatment of neurodegenerative diseases and related conditions are disclosed. The invention also relates to the pharmaceutically acceptable salts of said compounds, processes for the preparation of said compounds, intermediates used in the preparation of said compounds, and pharmaceutical compositions containing said compounds. The invention further relates to methods of use of said compounds, salts of said compounds, and said compositions in treating neurodegenerative diseases and related conditions.
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公开(公告)号:US11472776B2
公开(公告)日:2022-10-18
申请号:US16471363
申请日:2017-12-18
申请人: OLIGOMERIX INC.
发明人: Eliot J. Davidowitz , James G. Moe , Allen B. Reitz , Haiyan Bian , Charles Gluchowski , James Hendrix , Albert S. Yehaskel , Mark E. McDonnell , H. Marie Loughran
IPC分类号: C07D401/04 , C07D239/91 , C07D401/14 , C07D471/04 , C07D495/04 , A61K45/06
摘要: Novel quinazolinones useful as inhibitors of tau oligomer formation, useful for the treatment of neurodegenerative diseases and related conditions are disclosed. The invention also relates to the pharmaceutically acceptable salts of said compounds, processes for the preparation of said compounds, intermediates used in the preparation of said compounds, and pharmaceutical compositions containing said compounds. The invention further relates to methods of use of said compounds, salts of said compounds, and said compositions in treating neurodegenerative diseases and related conditions.
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公开(公告)号:US10597649B2
公开(公告)日:2020-03-24
申请号:US15358984
申请日:2016-11-22
申请人: Oligomerix, Inc.
IPC分类号: C12N9/64 , C12Q1/37 , G01N33/68 , A61K38/48 , A61K39/395 , C07K16/40 , G01N33/573 , A61K38/00
摘要: Disclosed are mammalian tau proteases, as well as proteolytically-active fragments, variants, and mutants thereof. Also disclosed are polynucleotides and recombinant expression vectors that encode these polypeptides, as well as methods for producing such proteins in selected recombinant host cells, and for using the compositions in a variety of diagnostic and analytical assays.
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公开(公告)号:US12060591B2
公开(公告)日:2024-08-13
申请号:US16822906
申请日:2020-03-18
申请人: Oligomerix, Inc.
IPC分类号: C12N9/64 , A61K38/00 , A61K38/48 , A61K39/395 , C07K16/40 , C12Q1/37 , G01N33/573 , G01N33/68
CPC分类号: C12N9/6424 , A61K38/482 , A61K39/3955 , C07K16/40 , C12Q1/37 , G01N33/573 , G01N33/6896 , A61K38/00 , G01N2800/2821
摘要: Disclosed are mammalian tau proteases, as well as proteolytically-active fragments, variants, and mutants thereof. Also disclosed are polynucleotides and recombinant expression vectors that encode these polypeptides, as well as methods for producing such proteins in selected recombinant host cells, and for using the compositions in a variety of diagnostic and analytical assays.
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7.
公开(公告)号:US20240158379A1
公开(公告)日:2024-05-16
申请号:US17721178
申请日:2022-04-14
申请人: OLIGOMERIX INC.
发明人: Eliot J. Davidowitz , James G. Moe , Allen B. Reitz , Haiyan Bian , Charles Gluchowski , James Hendrix , Albert S. Yehaskel , Mark E. McDonnell , H. Marie Loughran
IPC分类号: C07D409/14 , C07D307/80 , C07D405/14
CPC分类号: C07D409/14 , C07D307/80 , C07D405/14
摘要: Novel benzofurans, benzothiophenes and indoles useful as inhibitors of tau oligomer formation, useful for the treatment of neurodegenerative diseases and related conditions are disclosed. The invention also relates to the pharmaceutically acceptable salts of said compounds, processes for the preparation of said compounds, intermediates used in the preparation of said compounds, and pharmaceutical compositions containing said compounds. The invention further relates to methods of use of said compounds, salts of said compounds, and said compositions in treating neurodegenerative diseases and related conditions.
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公开(公告)号:US20210130335A1
公开(公告)日:2021-05-06
申请号:US16471424
申请日:2017-12-18
申请人: OLIGOMERIX INC.
发明人: Eliot J. Davidowitz , James G. Moe , Allen B. Reitz , Haiyan Bian , Charles Gluchowski , James Hendrix , Albert S. Yehaskel , Mark E. McDonnell , Marie H. Loughran
IPC分类号: C07D409/14 , C07D307/80 , C07D405/14
摘要: Novel benzofurans, benzothiophenes and indoles useful as inhibitors of tau oligomer formation, useful for the treatment of neurodegenerative diseases and related conditions are disclosed. The invention also relates to the pharmaceutically acceptable salts of said compounds, processes for the preparation of said compounds, intermediates used in the preparation of said compounds, and pharmaceutical compositions containing said compounds. The invention further relates to methods of use of said compounds, salts of said compounds, and said compositions in treating neurodegenerative diseases and related conditions.
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公开(公告)号:US10465001B2
公开(公告)日:2019-11-05
申请号:US15424444
申请日:2017-02-03
申请人: Oligomerix, Inc.
发明人: James G. Moe , Eliot J. Davidowitz
摘要: The invention relates to antibodies, antibody fragments and binding agents that specifically recognize oligomeric tau but do not bind to monomelic tau, fibrillar tau or non-disease associated forms of tau.
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公开(公告)号:US11306075B2
公开(公告)日:2022-04-19
申请号:US16471424
申请日:2017-12-18
申请人: OLIGOMERIX INC.
发明人: Eliot J. Davidowitz , James G. Moe , Allen B. Reitz , Haiyan Bian , Charles Gluchowski , James Hendrix , Albert S. Yehaskel , Mark E. McDonnell , H. Marie Loughran
IPC分类号: C07D409/14 , C07D307/80 , C07D405/14
摘要: Novel benzofurans, benzothiophenes and indoles useful as inhibitors of tau oligomer formation, useful for the treatment of neurodegenerative diseases and related conditions are disclosed. The invention also relates to the pharmaceutically acceptable salts of said compounds, processes for the preparation of said compounds, intermediates used in the preparation of said compounds, and pharmaceutical compositions containing said compounds. The invention further relates to methods of use of said compounds, salts of said compounds, and said compositions in treating neurodegenerative diseases and related conditions.
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