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公开(公告)号：US08444954B2
公开(公告)日：2013-05-21
申请号：US12958572
申请日：2010-12-02
申请人： Enrico Cappelletti , Luciano Lattuada , Karen E. Linder , Edmund Marinelli , Palaniappa Nanjappan , Adrian Nunn , Natarajan Raju , Kondareddiar Ramalingam , Rolf E. Swenson , Michael Tweedle
发明人： Enrico Cappelletti , Luciano Lattuada , Karen E. Linder , Edmund Marinelli , Palaniappa Nanjappan , Adrian Nunn , Natarajan Raju , Kondareddiar Ramalingam , Rolf E. Swenson , Michael Tweedle
CPC分类号： C07K14/57572 , A61K49/085 , A61K49/122 , A61K49/14 , A61K51/088
摘要： New and improved compounds for use in diagnostic imaging or therapy having the formula M-N—O—P-G, wherein M is a metal chelator having the structure: wherein R1-R5 and FG are as defined herein (in the form complexed with a metal radionuclide or not), N—O—P is the linker containing at least one non-alpha amino acid with a cyclic group, at least one substituted bile acid or at least one non-alpha amino acid, and G is the GRP receptor targeting peptide. In the preferred embodiment, M is an Aazta metal chelator or a derivative thereof. Methods for imaging a patient and/or providing radiotherapy or phototherapy to a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound is further provided. Methods and kits for preparing a radiotherapeutic agent are further provided.
摘要翻译： 用于具有式MNOPG的诊断成像或治疗的新的和改进的化合物，其中M是具有以下结构的金属螯合剂：其中R1-R5和FG如本文所定义（以与金属放射性核素复合的形式），NOP 是含有至少一个具有环状基团，至少一个取代的胆汁酸或至少一个非α氨基酸的非α氨基酸的接头，G是GRP受体靶向肽。 在优选的实施方案中，M是Aazta金属螯合剂或其衍生物。 还提供了使用本发明的化合物对患者成像和/或向患者提供放射治疗或光疗的方法。 还提供了用于从该化合物制备诊断显像剂的方法和试剂盒。 还提供了用于制备放射治疗剂的方法和试剂盒。
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公开(公告)号：US08420053B2
公开(公告)日：2013-04-16
申请号：US12551394
申请日：2009-08-31
申请人： Enrico Cappelletti , Luciano Lattuada , Karen E. Linder , Edmund Marinelli , Palaniappa Nanjappan , Natarajan Raju , Kondareddiar Ramalingam , Rolf E. Swenson , Michael Tweedle
发明人： Enrico Cappelletti , Luciano Lattuada , Karen E. Linder , Edmund Marinelli , Palaniappa Nanjappan , Natarajan Raju , Kondareddiar Ramalingam , Rolf E. Swenson , Michael Tweedle
IPC分类号： A61K49/00
CPC分类号： C07K7/086 , A61K51/088
摘要： Improved compounds for use in diagnostic imaging or therapy having the formula M-N-O-P-G, wherein M is an optical label or a metal chelator (in the form complexed with a metal radionuclide or not), N-O-P is the linker, and G is the GRP receptor targeting peptide. Methods for imaging a patient and/or providing radiotherapy or phototherapy to a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound are further provided. Methods and kits for preparing a radiotherapeutic agent are further provided.
摘要翻译： 用于具有式MNOPG的诊断成像或治疗的改进的化合物，其中M是光学标记或金属螯合剂（以与金属放射性核素复合的形式），NOP是接头，G是GRP受体靶向肽 。 还提供了使用本发明的化合物对患者成像和/或向患者提供放射治疗或光疗的方法。 还提供了用于从化合物制备诊断显像剂的方法和试剂盒。 还提供了用于制备放射治疗剂的方法和试剂盒。
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3.发明申请Compounds for Targeting Endothelial Cells, Compositions Containing the Same and Methods for Their Use 有权靶向内皮细胞的化合物，含有它们的组合物及其使用方法公开(公告)号：US20060263303A1
公开(公告)日：2006-11-23
申请号：US11381908
申请日：2006-05-05
申请人： Mathew Von Wronski , Edmund Marinelli , Adrian Nunn , Radhakrishna Pillai , Kondareddiar Ramalingam , Michael Tweedle , Karen Linder , Palaniappa Nanjappan , Natarajan Raju
发明人： Mathew Von Wronski , Edmund Marinelli , Adrian Nunn , Radhakrishna Pillai , Kondareddiar Ramalingam , Michael Tweedle , Karen Linder , Palaniappa Nanjappan , Natarajan Raju
CPC分类号： A61K51/088 , A61K47/64 , A61K47/6925 , A61K49/006 , A61K49/0091 , A61K49/223 , A61K49/225 , A61K49/227 , B82Y5/00 , B82Y10/00 , B82Y30/00 , C07K7/06
摘要： The present invention provides compounds for targeting endothelial cells, tumor cells or other cells that express the NP-1 receptor, compositions containing the same and methods for their use. Additionally, the present invention includes diagnostic, therapeutic and radiotherapeutic compositions useful for visualization, therapy or radiotherapy.
摘要翻译： 本发明提供用于靶向表达NP-1受体的内皮细胞，肿瘤细胞或其他细胞的化合物，其含有该组合物的组合物及其使用方法。 另外，本发明包括可用于可视化，治疗或放射治疗的诊断，治疗和放射治疗组合物。
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公开(公告)号：US08414864B2
公开(公告)日：2013-04-09
申请号：US11467301
申请日：2006-08-25
申请人： Enrico Cappelletti , Luciano Lattuada , Karen E. Linder , Edmund R. Marinelli , Palaniappa Nanjappan , Natarajan Raju , Rolf E. Swenson , Michael Tweedle
发明人： Enrico Cappelletti , Luciano Lattuada , Karen E. Linder , Edmund R. Marinelli , Palaniappa Nanjappan , Natarajan Raju , Rolf E. Swenson , Michael Tweedle
CPC分类号： A61K51/088 , C07K7/086
摘要： New and improved compounds for use in radiodiagnostic imaging or radiotherapy having the formula M-N—O—P-G, wherein M is the metal chelator (in the form complexed with a metal radionuclide or not), N—O—P is the linker, and G is the GRP receptor targeting peptide. Methods for imaging a patient and/or providing radiotherapy to a patient using the compounds of the invention are also provided. A method for preparing a diagnostic imaging agent from the compound is further provided. A method for preparing a radiotherapeutic agent is further provided.
摘要翻译： 用于放射诊断成像或放射治疗的具有式MN-O-PG的新的和改进的化合物，其中M是金属螯合剂（以与金属放射性核素复合的形式），N-O-P为连接体，G 是GRP受体靶向肽。 还提供了使用本发明的化合物使患者成像和/或向患者提供放射疗法的方法。 还提供了用于从化合物制备诊断显像剂的方法。 还提供了一种制备放射治疗剂的方法。
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公开(公告)号：US20080247946A1
公开(公告)日：2008-10-09
申请号：US11467301
申请日：2006-08-25
申请人： Enrico Cappelletti , Luciano Lattuada , Karen E. Linder , Edmund R. Marinelli , Palaniappa Nanjappan , Natarajan Raju , Rolf E. Swenson , Michael Tweedle
发明人： Enrico Cappelletti , Luciano Lattuada , Karen E. Linder , Edmund R. Marinelli , Palaniappa Nanjappan , Natarajan Raju , Rolf E. Swenson , Michael Tweedle
CPC分类号： A61K51/088 , C07K7/086
摘要： New and improved compounds for use in radiodiagnostic imaging or radiotherapy having the formula M-N—O—P-G, wherein M is the metal chelator (in the form complexed with a metal radionuclide or not), N—O—P is the linker, and G is the GRP receptor targeting peptide. Methods for imaging a patient and/or providing radiotherapy to a patient using the compounds of the invention are also provided. A method for preparing a diagnostic imaging agent from the compound is further provided. A method for preparing a radiotherapeutic agent is further provided.
摘要翻译： 用于具有式M-N-O-P-G的放射诊断成像或放射治疗的新的和改进的化合物，其中M是金属螯合剂（以与金属放射性核素复合的形式），N-O-P是接头，G是GRP受体靶向肽。 还提供了使用本发明的化合物使患者成像和/或向患者提供放射疗法的方法。 还提供了从化合物制备诊断显像剂的方法。 还提供了一种制备放射治疗剂的方法。
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公开(公告)号：US20070231257A1
公开(公告)日：2007-10-04
申请号：US11467237
申请日：2006-08-25
申请人： Enrico Cappelletti , Luciano Lattuada , Karen Linder , Edmund Marinelli , Palaniappa Nanjappan , Natarajan Raju , Rolf Swenson , Michael Tweedle
发明人： Enrico Cappelletti , Luciano Lattuada , Karen Linder , Edmund Marinelli , Palaniappa Nanjappan , Natarajan Raju , Rolf Swenson , Michael Tweedle
IPC分类号： A61K51/08 , C07K14/595
CPC分类号： A61K51/088 , C07K7/086
摘要： New and improved compounds for use in radiodiagnostic imaging or radiotherapy having the formula M-N—O—P-G, wherein M is the metal chelator (in the form complexed with a metal radionuclide or not), N—O—P is the linker, and G is the GRP receptor targeting peptide. Methods for imaging a patient and/or providing radiotherapy to a patient using the compounds of the invention are also provided. A method for preparing a diagnostic imaging agent from the compound is further provided. A method for preparing a radiotherapeutic agent is further provided.
摘要翻译： 用于具有式M-N-O-P-G的放射诊断成像或放射治疗的新的和改进的化合物，其中M是金属螯合剂（以与金属放射性核素复合的形式），N-O-P是接头，G是GRP受体靶向肽。 还提供了使用本发明的化合物使患者成像和/或向患者提供放射疗法的方法。 还提供了从化合物制备诊断显像剂的方法。 还提供了一种制备放射治疗剂的方法。
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公开(公告)号：US20060018830A1
公开(公告)日：2006-01-26
申请号：US11165721
申请日：2005-06-24
申请人： Enrico Cappelletti , Luciano Lattuada , Karen Linder , Edmund Marinelli , Palaniappa Nanjappan , Natarajan Raju , Kondareddiar Ramalingam , Rolf Swenson , Michael Tweedle
发明人： Enrico Cappelletti , Luciano Lattuada , Karen Linder , Edmund Marinelli , Palaniappa Nanjappan , Natarajan Raju , Kondareddiar Ramalingam , Rolf Swenson , Michael Tweedle
CPC分类号： A61K51/088 , A61K49/0002 , C07C269/04 , C07D257/00 , C07J41/0005 , C07J41/0011 , C07J43/003 , C07K14/57572 , C07C271/22
摘要： New and improved compounds for use in diagnostic imaging or therapy having the formula M-N—O—P-G, wherein M is a metal chelator having the structure: wherein R1-R5 and FG are as defined herein (in the form complexed with a metal radionuclide or not), N—O—P is the linker containing at least one non-alpha amino acid with a cyclic group, at least one substituted bile acid or at least one non-alpha amino acid, and G is the GRP receptor targeting peptide. In the preferred embodiment, M is an Aazta metal chelator or a derivative thereof. Methods for imaging a patient and/or providing radiotherapy or phototherapy to a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound is further provided. Methods and kits for preparing a radiotherapeutic agent are further provided.
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公开(公告)号：US20050090689A1
公开(公告)日：2005-04-28
申请号：US10963708
申请日：2004-10-13
申请人： Radhakrishna Pillai , Sang Kang , Edmund Marinelli , Ramachandran Ranganathan , Michael Tweedle
发明人： Radhakrishna Pillai , Sang Kang , Edmund Marinelli , Ramachandran Ranganathan , Michael Tweedle
IPC分类号： A61K49/06 , A61K51/04 , C07C211/00
CPC分类号： A61K49/06 , A61K51/0478 , A61K51/0482 , A61K2123/00
摘要： Novel metal-chelate complexes comprising aminocarboxylate ligands including substituted aromatic amide moieties, such as those having the formula wherein R13, A1, R1 and R2 are as defined herein, are disclosed.
摘要翻译： 包含氨基羧酸酯配体（包括取代的芳族酰胺部分）的新型金属螯合络合物，例如具有下式的那些：其中R 13，A 1，R 1， 和R 2 2如本文所定义。
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公开(公告)号：US07922998B2
公开(公告)日：2011-04-12
申请号：US11165721
申请日：2005-06-24
申请人： Enrico Cappelletti , Luciano Lattuada , Karen E. Linder , Edmund Marinelli , Palaniappa Nanjappan , Natarajan Raju , Kondareddiar Ramalingam , Rolf E. Swenson , Michael Tweedle
发明人： Enrico Cappelletti , Luciano Lattuada , Karen E. Linder , Edmund Marinelli , Palaniappa Nanjappan , Natarajan Raju , Kondareddiar Ramalingam , Rolf E. Swenson , Michael Tweedle
CPC分类号： A61K51/088 , A61K49/0002 , C07C269/04 , C07D257/00 , C07J41/0005 , C07J41/0011 , C07J43/003 , C07K14/57572 , C07C271/22
摘要： New and improved compounds for use in diagnostic imaging or therapy having the formula M-N—O—P-G, wherein M is a metal chelator having the structure: wherein R1-R5 and FG are as defined herein (in the form complexed with a metal radionuclide or not), N—O—P is the linker containing at least one non-alpha amino acid with a cyclic group, at least one substituted bile acid or at least one non-alpha amino acid, and G is the GRP receptor targeting peptide. In the preferred embodiment, M is an Aazta metal chelator or a derivative thereof. Methods for imaging a patient and/or providing radiotherapy or phototherapy to a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound is further provided. Methods and kits for preparing a radiotherapeutic agent are further provided.
摘要翻译： 用于具有式MN-O-PG的诊断成像或治疗的新的和改进的化合物，其中M是具有以下结构的金属螯合剂：其中R1-R5和FG如本文所定义（以与金属放射性核素复合的形式或 不是），N-O-P是含有至少一个具有环状基团，至少一个取代的胆汁酸或至少一个非α氨基酸的非α氨基酸的接头，G是GRP受体靶向肽。 在优选的实施方案中，M是Aazta金属螯合剂或其衍生物。 还提供了使用本发明的化合物对患者成像和/或向患者提供放射治疗或光疗的方法。 还提供了用于从该化合物制备诊断显像剂的方法和试剂盒。 还提供了用于制备放射治疗剂的方法和试剂盒。
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公开(公告)号：US07611692B2
公开(公告)日：2009-11-03
申请号：US10828925
申请日：2004-04-20
申请人： Enrico Cappelletti , Luciano Lattuada , Karen E. Linder , Edmund Marinelli , Palaniappa Nanjappan , Natarajan Raju , Kondareddiar Ramalingam , Rolf E. Swenson , Michael Tweedle
发明人： Enrico Cappelletti , Luciano Lattuada , Karen E. Linder , Edmund Marinelli , Palaniappa Nanjappan , Natarajan Raju , Kondareddiar Ramalingam , Rolf E. Swenson , Michael Tweedle
IPC分类号： A61K49/00
CPC分类号： C07K7/086 , A61K51/088
摘要： New and improved compounds for use in diagnostic imaging or therapy having the formula M—N—O—P—G, wherein M is an optical label or a metal chelator (in the form complexed with a metal radionuclide or not), N—O—P is the linker, and G is the GRP receptor targeting peptide. Methods for imaging a patient and/or providing radiotherapy or phototherapy to a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound is further provided. Methods and kits for preparing a radiotherapeutic agent are further provided.
摘要翻译： 用于具有式MNOPG的诊断成像或治疗的新的和改进的化合物，其中M是光学标记或金属螯合剂（以与金属放射性核素复合的形式），NOP是接头，G是GRP受体 靶向肽。 还提供了使用本发明的化合物对患者成像和/或向患者提供放射治疗或光疗的方法。 还提供了用于从该化合物制备诊断显像剂的方法和试剂盒。 还提供了用于制备放射治疗剂的方法和试剂盒。
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