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公开(公告)号：US10781178B2
公开(公告)日：2020-09-22
申请号：US15751778
申请日：2016-02-09
发明人： Neil Vasdev , Huan Steven Liang
IPC分类号： C07D215/28 , C07D401/12 , A61K31/4709 , C07D215/26 , A61K45/06 , A61P25/28 , A61P35/00 , A61K51/04 , C07B59/00
摘要： The present application provides compounds useful in methods of treating neurological disorders such as Alzheimer's disease, and cancer such as prostate cancer. Also provided herein are radiolabeled compounds useful for imaging techniques, and techniques for diagnosis and monitoring of treatment of neurological disorders and cancer. An exemplary radiolabeled compound provided herein is useful as a radiotracer for positron emission tomography or single-photon emission computed tomography. Methods for preparing radiolabeled compounds and methods for preparing unlabeled compounds are also provided.
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公开(公告)号：US11434203B2
公开(公告)日：2022-09-06
申请号：US16997501
申请日：2020-08-19
发明人： Neil Vasdev , Huan Steven Liang
IPC分类号： C07D215/28 , C07D401/12 , A61P35/00 , A61K51/04 , C07D215/26 , A61K45/06 , A61P25/28 , C07B59/00
摘要： The present application provides compounds useful in methods of treating neurological disorders such as Alzheimer's disease, and cancer such as prostate cancer. Also provided herein are radiolabeled compounds useful for imaging techniques, and techniques for diagnosis and monitoring of treatment of neurological disorders and cancer. An exemplary radiolabeled compound provided herein is useful as a radiotracer for positron emission tomography or single-photon emission computed tomography. Methods for preparing radiolabeled compounds and methods for preparing unlabeled compounds are also provided.
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公开(公告)号：US20180280551A1
公开(公告)日：2018-10-04
申请号：US15764087
申请日：2016-10-01
申请人： Whitehead Institute for Biomedical Research , The General Hospital Corporation d/b/a Massachusetts General Hospital
摘要： Provided herein are methods for producing site specific PEG modifications to single domain antibodies (e.g., VHHs). Methods for producing site-specific ally conjugated bivalent single domain antibodies (e.g., VHHs) are also provided. Methods for labeling (e.g., with a fluorophore or radionuclide) site-specifically PEGylated single domain antibodies and site-specifically conjugated bivalent single domain antibodies are also provided.
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公开(公告)号：US09957231B2
公开(公告)日：2018-05-01
申请号：US15231470
申请日：2016-08-08
IPC分类号： C07D213/57 , C07D239/553 , C07D319/06 , C07D319/08 , C07D405/12 , C07J17/00 , C07J1/00 , C07J51/00 , C07B59/00
CPC分类号： C07D213/57 , C07B59/00 , C07B59/002 , C07B2200/05 , C07D239/553 , C07D319/06 , C07D319/08 , C07D405/12 , C07J1/0059 , C07J17/00 , C07J51/00
摘要： A process for fluorination of aromatic compounds employing iodonium ylides and applicable to radiofluorination using 18F is described. Processes, intermediates, reagents and radiolabelled compounds are described.
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公开(公告)号：US10259800B2
公开(公告)日：2019-04-16
申请号：US15166063
申请日：2016-05-26
IPC分类号： C07D319/08 , C07D319/06 , C07D413/12 , C07D405/12
摘要： A process for fluorination of aromatic compounds employing iodonium ylides and applicable to radiofluorination using 18F is described. Processes, intermediates, reagents and radiolabelled compounds are described.
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公开(公告)号：US20180327362A1
公开(公告)日：2018-11-15
申请号：US15751778
申请日：2016-02-09
发明人： Neil Vasdev , Huan Steven Liang
IPC分类号： C07D215/28 , C07D401/12 , C07B59/00 , A61K51/04 , A61P35/00 , A61P25/28
CPC分类号： C07D215/28 , A61K45/06 , A61K51/0455 , A61K2123/00 , A61P25/28 , A61P35/00 , C07B59/002 , C07D215/26 , C07D401/12
摘要： The present application provides compounds useful in methods of treating neurological disorders such as Alzheimer's disease, and cancer such as prostate cancer. Also provided herein are radiolabeled compounds useful for imaging techniques, and techniques for diagnosis and monitoring of treatment of neurological disorders and cancer. An exemplary radiolabeled compound provided herein is useful as a radiotracer for positron emission tomography or single-photon emission computed tomography. Methods for preparing radiolabeled compounds and methods for preparing unlabeled compounds are also provided.
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公开(公告)号：US09434699B2
公开(公告)日：2016-09-06
申请号：US14641094
申请日：2015-03-06
IPC分类号： C07D239/553 , C07D319/06 , C07D319/08 , C07D405/12 , C07J17/00 , C07J1/00 , C07J51/00 , C07B59/00
CPC分类号： C07D213/57 , C07B59/00 , C07B59/002 , C07B2200/05 , C07D239/553 , C07D319/06 , C07D319/08 , C07D405/12 , C07J1/0059 , C07J17/00 , C07J51/00
摘要： A process for fluorination of aromatic compounds employing iodonium ylides and applicable to radiofluorination using 18F is described. Processes, intermediates, reagents and radiolabelled compounds are described.
摘要翻译： 描述了使用碘鎓叶立德氟化芳族化合物并适用于使用18F的放射性氟化的方法。 描述了方法，中间体，试剂和放射性标记的化合物。
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公开(公告)号：US10280152B2
公开(公告)日：2019-05-07
申请号：US15563022
申请日：2016-03-30
发明人： Neil Vasdev , Huan Steven Liang
IPC分类号： A61K51/04 , C07D401/14 , C07D413/12 , C07D417/14
摘要： Provided herein are radiolabelled compounds useful for imaging GSK-3 kinase. An exemplary radiolabelled compound provided herein is useful as a radiotracer for imaging GSK-3 kinase using PET imaging. Methods for preparing the radiolabelled compounds and diagnostic methods using the radiolabelled compounds are also provided.
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公开(公告)号：US20170121300A1
公开(公告)日：2017-05-04
申请号：US15166063
申请日：2016-05-26
IPC分类号： C07D319/08 , C07D413/12 , C07D405/12 , C07D319/06
CPC分类号： C07D319/08 , C07D319/06 , C07D405/12 , C07D413/12
摘要： A process for fluorination of aromatic compounds employing iodonium ylides and applicable to radiofluorination using 18F is described. Processes, intermediates, reagents and radiolabelled compounds are described.
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公开(公告)号：US09546167B2
公开(公告)日：2017-01-17
申请号：US15087681
申请日：2016-03-31
发明人： Neil Vasdev , Timothy M. Shoup
IPC分类号： C07D471/04 , C07B59/00
CPC分类号： C07D471/04 , C07B59/002
摘要： This disclosure relates to a one-step method for preparing the tau radiopharmaceutical, [18F]T807, using an unprotected or protected precursor (e.g., tert-butyl 7-(6-nitropyridin-3-yl)-5H-pyrido[4,3-b]indole-5-carboxylate).
摘要翻译： 本公开涉及使用未保护或被保护的前体（例如，7-（6-硝基吡啶-3-基）-5H-吡啶并[4,3-d]吡啶）的制备tau放射性药物[18 F] T807的一步法， 3-b]吲哚-5-羧酸乙酯）。
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