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公开(公告)号：USRE49240E1
公开(公告)日：2022-10-11
申请号：US16815755
申请日：2020-03-11
IPC分类号： C07C237/40 , A61K31/167 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/455 , A61K31/4965 , A61K31/505 , A61K31/69 , A61K38/05 , A61K45/06 , C07C237/42 , C07D213/81 , C07D213/82 , C07D239/42 , C07D241/24
摘要： The present invention relates to compounds which inhibit histone deacetylase activity and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing these compounds. The present invention also relates to methods of treating and preventing hematological cell proliferative disorders, such as multiple myeloma, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
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公开(公告)号：US20210154184A1
公开(公告)日：2021-05-27
申请号：US16630294
申请日：2018-07-12
申请人： Dana-Farber Cancer Institute, Inc. , The General Hospital Corporation D/B/A Massachusetts General Hospital
发明人： Nathanael S. Gray , Stephen J. Haggarty , Quan Cai , Tinghu Zhang , Maria Catarina Telo Baptista Lima da Silva , Fleur M. Ferguson
IPC分类号： A61K31/4545 , A61K31/437 , A61K51/04 , A61P25/28 , G01N33/68 , G01N33/534 , C07D471/04 , A61K38/05 , C07K5/062
摘要： Provided herein are bifunctional compounds that bind tau protein and/or promote targeted ubiquitination for the degradation of tau protein. In particular, provided are compounds that can bind tau protein, a protein whose aggregation is implicated in a variety of neurodegenerative disease (e.g., tauopathies), and can promote its degradation by recruiting an E3 ubiquitin ligase (e.g., Cereblon), which can ubiquitinate tau protein, marking it for proteasomal degradation. Also provided are radiolabeled forms of the bifunctional compounds, pharmaceutical compositions comprising the bifunctional compounds, methods of detecting and/or diagnosing neurological disorders, methods of detecting and/or diagnosing pathological aggregation of tau protein (e.g., in the central nervous system), methods of treating and/or preventing neurological disorders, and methods of promoting the degradation of tau protein by E3 ubiquitin ligase activity in a subject by administering a compound or composition described herein.
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公开(公告)号：US09988343B2
公开(公告)日：2018-06-05
申请号：US15034276
申请日：2014-11-05
IPC分类号： A61K31/4406 , A61K31/167 , A61K31/69 , C07C237/40 , C07D213/82 , C07D241/24 , A61K38/05 , A61K45/06 , A61K31/4402 , A61K31/4409 , A61K31/455 , A61K31/4965 , A61K31/505 , C07D213/81 , C07D239/42 , C07C237/42
CPC分类号： C07C237/40 , A61K31/167 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/455 , A61K31/4965 , A61K31/505 , A61K31/69 , A61K38/05 , A61K45/06 , C07C237/42 , C07D213/81 , C07D213/82 , C07D239/42 , C07D241/24 , A61K2300/00
摘要： The present invention relates to compounds which inhibit histone deacetylase activity and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing these compounds. The present invention also relates to methods of treating and preventing hematological cell proliferative disorders, such as multiple myeloma, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
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公开(公告)号：US20240091213A1
公开(公告)日：2024-03-21
申请号：US18200950
申请日：2023-05-23
申请人： DANA-FARBER CANCER INSTITUTE, INC. , THE GENERAL HOSPITAL CORPORATION d/b/a MASSACHUSETTS GENERAL HOSPITAL
发明人： Nathanael S. Gray , Stephen J. Haggarty , Quan Cai , Tinghu Zhang , Maria Catarina Telo Baptista Lima da Silva , Fleur M. Ferguson
IPC分类号： A61K31/4545 , A61P25/28 , A61K31/437 , A61K38/05 , A61K51/04 , C07D471/04 , C07K5/062 , G01N33/534 , G01N33/68
CPC分类号： A61K31/4545 , A61P25/28 , A61K31/437 , A61K38/05 , A61K51/0455 , C07D471/04 , C07K5/06034 , G01N33/534 , G01N33/6896
摘要： Provided herein are bifunctional compounds that bind tau protein and/or promote targeted ubiquitination for the degradation of tau protein. In particular, provided are compounds that can bind tau protein, a protein whose aggregation is implicated in a variety of neurodegenerative disease (e.g., tauopathies), and can promote its degradation by recruiting an E3 ubiquitin ligase (e.g., Cereblon), which can ubiquitinate tau protein, marking it for proteasomal degradation. Also provided are radiolabeled forms of the bifunctional compounds, pharmaceutical compositions comprising the bifunctional compounds, methods of detecting and/or diagnosing neurological disorders, methods of detecting and/or diagnosing pathological aggregation of tau protein (e.g., in the central nervous system), methods of treating and/or preventing neurological disorders, and methods of promoting the degradation of tau protein by E3 ubiquitin ligase activity in a subject by administering a compound or composition described herein.
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公开(公告)号：US20230133538A1
公开(公告)日：2023-05-04
申请号：US17912272
申请日：2021-03-17
发明人： Fleur M. Ferguson , Nathanael S. Gray , Stephen J. Haggarty , Maria Catarina Telo Baptista Lima Da Silva
IPC分类号： C07D417/06 , C07D413/06 , C07D401/04 , C07D403/04 , C07D417/14 , C07D487/04
摘要： Disclosed are bispecific compounds (degraders) that target tau protein for degradation. Also disclosed are pharmaceutical compositions containing the degraders and methods of using the compounds to treat neurodegenerative and neuropsychiatric diseases associated with aberrant tau.
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公开(公告)号：US11052080B2
公开(公告)日：2021-07-06
申请号：US16198589
申请日：2018-11-21
申请人： The Broad Institute, Inc. , Dana-Farber Cancer Institute, Inc. , The General Hospital Corporation
发明人： Florence Fevrier Wagner , Jennifer Q. Pan , Sivaraman Dandapani , Andrew Germain , Edward Holson , Benito Munoz , Partha P. Nag , Michael C. Lewis , Stephen J. Haggarty , Joshua A. Bishop , Kimberly Stegmaier , Michel Weiwer , Versha Banerji
IPC分类号： C07D471/04 , C07D471/10 , A61K31/4745 , A61K31/4747
摘要： The present invention provides compounds of formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting kinase (e.g., GSK3 (e.g., GSK3α or GSK3β) or CK1) activity. The present invention further provides methods of using the compounds described herein for treating kinase-mediated disorders, such as neurological diseases, psychiatric disorders, metabolic disorders, and cancer.
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公开(公告)号：US20160272579A1
公开(公告)日：2016-09-22
申请号：US15034276
申请日：2014-11-05
IPC分类号： C07C237/40 , A61K31/69 , C07D213/82 , A61K31/4406 , A61K31/167 , C07D239/42 , A61K31/505 , C07D241/24 , A61K31/4965 , A61K45/06 , C07D213/81
CPC分类号： C07C237/40 , A61K31/167 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/455 , A61K31/4965 , A61K31/505 , A61K31/69 , A61K38/05 , A61K45/06 , C07C237/42 , C07D213/81 , C07D213/82 , C07D239/42 , C07D241/24 , A61K2300/00
摘要： The present invention relates to compounds which inhibit histone deacetylase activity and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing these compounds. The present invention also relates to methods of treating and preventing hematological cell proliferative disorders, such as multiple myeloma, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
摘要翻译： 本发明涉及抑制组蛋白脱乙酰酶活性的化合物和合成这些化合物的方法。 本发明还涉及含有这些化合物的药物组合物。 本发明还涉及通过将这些化合物和药物组合物给予有需要的受试者来治疗和预防血液细胞增殖性疾病如多发性骨髓瘤的方法。
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公开(公告)号：US20220160702A1
公开(公告)日：2022-05-26
申请号：US17344830
申请日：2021-06-10
申请人： The Broad Institute, Inc. , Dana-Farber Cancer Institute, Inc. , The General Hospital Corporation d/b/a Massachusetts General Hospital
发明人： Florence Fevrier Wagner , Jennifer Q. Pan , Sivaraman Dandapani , Andrew Germain , Edward Holson , Benito Munoz , Partha P. Nag , Michael C. Lewis , Stephen J. Haggarty , Joshua A. Bishop , Kimberly Stegmaier , Michel Weiwer , Versha Banerji
IPC分类号： A61K31/4745 , C07D471/04 , C07D471/10 , A61K31/4747
摘要： The present invention provides compounds of formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting kinase (e.g., GSK3 (e.g., GSK3α or GSK3β) or CK1) activity. The present invention further provides methods of using the compounds described herein for treating kinase-mediated disorders, such as neurological diseases, psychiatric disorders, metabolic disorders, and cancer.
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公开(公告)号：US20190175584A1
公开(公告)日：2019-06-13
申请号：US16198589
申请日：2018-11-21
申请人： The Broad Institute, Inc. , Dana-Farber Cancer Institute, Inc. , The General Hospital Corporation d/b/a Massachusetts General Hospital
发明人： Florence Fevrier Wagner , Jennifer Q. Pan , Sivaraman Dandapani , Andrew Germain , Edward Holson , Benito Munoz , Partha P. Nag , Michael C. Lewis , Stephen J. Haggarty , Joshua A. Bishop , Kimberly Stegmaier , Michel Weiwer , Versha Banerji
IPC分类号： A61K31/4745 , C07D471/04 , A61K31/4747 , C07D471/10
摘要： The present invention provides compounds of formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting kinase (e.g., GSK3 (e.g., GSK3α or GSK3β) or CK1) activity. The present invention further provides methods of using the compounds described herein for treating kinase-mediated disorders, such as neurological diseases, psychriatic disorders, metabolic disorders, and cancer.
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公开(公告)号：US10137122B2
公开(公告)日：2018-11-27
申请号：US14799281
申请日：2015-07-14
申请人： The Broad Institute, Inc. , Dana-Farber Cancer Institute, Inc. , The General Hospital Corporation
发明人： Florence Fevrier Wagner , Jennifer Q. Pan , Sivaraman Dandapani , Andrew Germain , Edward Holson , Benito Munoz , Partha P. Nag , Michael C. Lewis , Stephen J. Haggarty , Joshua A. Bishop , Kimberly Stegmaier , Michel Weiwer , Versha Banerji
IPC分类号： A61K31/4745 , C07D471/04 , A61K31/4747 , C07D471/10
摘要： The present invention provides compounds of formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting kinase (e.g., GSK3 (e.g., GSK3α or GSK3β) or CK1) activity. The present invention further provides methods of using the compounds described herein for treating kinase-mediated disorders, such as neurological diseases, psychiatric disorders, metabolic disorders, and cancer.
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