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1.发明授权Conjugates of antioxidants with metal chelating ligands for use in diagnostic and therapeutic applications 失效抗氧化剂与金属螯合配体的结合物用于诊断和治疗应用公开(公告)号：US07582280B2
公开(公告)日：2009-09-01
申请号：US12169105
申请日：2008-07-08
IPC分类号： A61K51/00 , A61M36/14 , A61K49/00 , A61B5/055 , C07D225/02 , C07D225/00 , C07D225/04 , C07D267/22 , C07D487/00 , C07D245/00 , C07D255/02
CPC分类号： C07D405/12 , A61K51/12
摘要： The invention provides radiopharmaceuticals for diagnostic and therapeutic applications, conjugates of antioxidants with metal chelating ligands, intermediate compounds, methods of making such radiopharmaceuticals, ligands, and intermediate compounds, and kits for preparing the radiopharmaceutical complexes.
摘要翻译： 本发明提供用于诊断和治疗应用的放射性药物，抗氧化剂与金属螯合配体的缀合物，中间体化合物，制备这种放射性药物的方法，配体和中间体化合物，以及用于制备放射性药物复合物的试剂盒。
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2.发明申请公开(公告)号：US20080274048A1
公开(公告)日：2008-11-06
申请号：US12169105
申请日：2008-07-08
CPC分类号： C07D405/12 , A61K51/12
摘要： The invention provides radiopharmaceuticals for diagnostic and therapeutic applications, conjugates of antioxidants with metal chelating ligands, intermediate compounds, methods of making such radiopharmaceuticals, ligands, and intermediate compounds, and kits for preparing the radiopharmaceutical complexes.
摘要翻译： 本发明提供用于诊断和治疗应用的放射性药物，抗氧化剂与金属螯合配体的缀合物，中间体化合物，制备这种放射性药物的方法，配体和中间体化合物，以及用于制备放射性药物复合物的试剂盒。
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3.发明授权Conjugates of antioxidants with metal chelating ligands for use in diagnostic and therapeutic applications 失效抗氧化剂与金属螯合配体的结合物用于诊断和治疗应用公开(公告)号：US07407644B2
公开(公告)日：2008-08-05
申请号：US11561638
申请日：2006-11-20
CPC分类号： C07D405/12 , A61K51/12
摘要： The invention provides radiopharmaceuticals for diagnostic and therapeutic applications, conjugates of antioxidants with metal chelating ligands, intermediate compounds, methods of making such radiopharmaceuticals, ligands, and intermediate compounds, and kits for preparing the radiopharmaceutical complexes.
摘要翻译： 本发明提供用于诊断和治疗应用的放射性药物，抗氧化剂与金属螯合配体的缀合物，中间体化合物，制备这种放射性药物的方法，配体和中间体化合物，以及用于制备放射性药物复合物的试剂盒。
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公开(公告)号：US08420050B2
公开(公告)日：2013-04-16
申请号：US12137079
申请日：2008-06-11
申请人： Enrico Cappelletti , Luciano Lattuada , Karen E. Linder , Edmund R. Marinelli , Palaniappa Nanjappan , Adrian D. Nunn , Natarajan Raju , Kondareddiar Ramalingam , Rolf E. Swenson , Michael F. Tweedle , Mary Ellen Maddalena
发明人： Enrico Cappelletti , Luciano Lattuada , Karen E. Linder , Edmund R. Marinelli , Palaniappa Nanjappan , Adrian D. Nunn , Natarajan Raju , Kondareddiar Ramalingam , Rolf E. Swenson , Michael F. Tweedle , Mary Ellen Maddalena
CPC分类号： C07K14/57572 , A61K49/085 , A61K49/122 , A61K49/14 , A61K51/088
摘要： Novel methods of treating prostate tumors or of delaying the progression of prostate tumors are also provided, including, methods of treating bone or soft tissue metastases of prostate cancer methods for treating hormone sensitive and hormone refractory prostate cancer, methods for delaying the progression of hormone sensitive prostate cancer, for facilitating combination therapy in patients with hormone sensitive prostate cancer and for decreasing aberrant vascular permeability in patients with hormone sensitive prostate cancer, said methods comprising the step of administering to a subject a dose comprising an amount of radioactively labeled L70, N-[4-[[[[[4,7,10-Tris(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl]acetyl]amino]acetyl]amino]benzoyl]-L-glutaminyl-L-tryptophyl-L-alanyl-L-valyl-glycyl-L-histidyl-L-leucyl-L-methioninamide.
摘要翻译： 还提供了治疗前列腺肿瘤或延缓前列腺肿瘤进展的新方法，包括治疗前列腺癌的治疗激素敏感性和激素难治性前列腺癌的骨或软组织转移的方法，延迟激素敏感性进展的方法 前列腺癌，用于促进激素敏感性前列腺癌患者的联合治疗，并减少激素敏感性前列腺癌患者的异常血管通透性，所述方法包括向受试者施用包含一定量的放射性标记的L70，N- [4 - [[[[[[4,7,10-三（羧甲基）-1,4,7,10-四氮杂环十二烷-1-基]乙酰基]氨基]乙酰基]氨基]苯甲酰基] -L-谷氨酰胺基-L- 色氨酰-L-丙氨酰-L-缬氨酰 - 甘氨酰-L-组氨酰-L-亮氨酰-L-甲硫氨酰胺。
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公开(公告)号：US20120009122A1
公开(公告)日：2012-01-12
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 D. Nunn , Natarajan Raju , Kondareddiar Ramalingam , Rolf E. Swenson , Michael F. Tweedle
发明人： Enrico Cappelletti , Luciano Lattuada , Karen E. Linder , Edmund Marinelli , Palaniappa Nanjappan , Adrian D. Nunn , Natarajan Raju , Kondareddiar Ramalingam , Rolf E. Swenson , Michael F. 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：US20090175786A1
公开(公告)日：2009-07-09
申请号：US12137079
申请日：2008-06-11
申请人： Enrico Cappelletti , Luciano Lattuada , Karen E. Linder , Edmund R. Marinelli , Palaniappa Nanjappan , Adrian D. Nunn , Natarajan Raju , Kondareddiar Ramalingam , Rolf E. Swenson , Michael F. Tweedle , Mary Ellen Maddalena
发明人： Enrico Cappelletti , Luciano Lattuada , Karen E. Linder , Edmund R. Marinelli , Palaniappa Nanjappan , Adrian D. Nunn , Natarajan Raju , Kondareddiar Ramalingam , Rolf E. Swenson , Michael F. Tweedle , Mary Ellen Maddalena
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.Novel methods of treating prostate tumors or of delaying the progression of prostate tumors are also provided, including, methods of treating bone or soft tissue metastases of prostate cancer, methods for treating hormone sensitive and hormone refractory prostate cancer, methods for delaying the progression of hormone sensitive prostate cancer, for facilitating combination therapy in patients with hormone sensitive prostate cancer and for decreasing aberrant vascular permeability in patients with hormone sensitive prostate cancer.
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。 还提供了治疗前列腺肿瘤或延缓前列腺肿瘤进展的新方法，包括治疗前列腺癌骨或软组织转移的方法，治疗激素敏感性和激素难治性前列腺癌的方法，延迟激素进展的方法 敏感前列腺癌，用于促进激素敏感性前列腺癌患者的联合治疗，并减少激素敏感性前列腺癌患者异常血管通透性。
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公开(公告)号：US07850947B2
公开(公告)日：2010-12-14
申请号：US11352156
申请日：2006-02-10
申请人： Enrico Cappelletti , Luciano Lattuada , Karen E. Linder , Edmund Marinelli , Palaniappa Nanjappan , Adrian D. Nunn , Natarajan Raju , Kondareddiar Ramalingam , Rolf E. Swenson , Michael F. Tweedle
发明人： Enrico Cappelletti , Luciano Lattuada , Karen E. Linder , Edmund Marinelli , Palaniappa Nanjappan , Adrian D. Nunn , Natarajan Raju , Kondareddiar Ramalingam , Rolf E. Swenson , Michael F. 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 define 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在本文中定义（以与金属放射性核素复合的形式 ），N-O-P是含有至少一个具有环状基团的非α氨基酸，至少一个取代的胆汁酸或至少一个非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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8.发明申请公开(公告)号：US20120065365A1
公开(公告)日：2012-03-15
申请号：US13280485
申请日：2011-10-25
申请人： Jianqing Chen , Karen E. Linder , Edmund R. Marinelli , Edmund Metcalfe , Adrian D. Nunn , Rolf E. Swenson , Michael F. Tweedle
发明人： Jianqing Chen , Karen E. Linder , Edmund R. Marinelli , Edmund Metcalfe , Adrian D. Nunn , Rolf E. Swenson , Michael F. Tweedle
IPC分类号： C07K7/06 , C07K14/655 , C07K7/18 , C07K14/595 , C07K7/23 , C07K14/68 , C07K7/16 , C07K14/62 , C07K14/545
CPC分类号： A61K51/12 , A61K51/088
摘要： Stabilized radiopharmaceutical formulations are disclosed. Methods of making and using stabilized radiopharmaceutical formulations are also disclosed. The invention relates to stabilizers that improve the radiostability of radiotherapeutic and radiodiagnostic compounds and formulations containing them. In particular, it relates to stabilizers useful in the preparation and stabilization of targeted radiodiagnostic and radiotherapeutic compounds, and, in a preferred embodiment, to the preparation and stabilization of radiodiagnostic and radiotherapeutic compounds that are targeted to the Gastrin Releasing Peptide Receptor (GRP-Receptor).
摘要翻译： 公开了稳定的放射性药物制剂。 还公开了制备和使用稳定的放射性药物制剂的方法。 本发明涉及改善放射治疗和放射性诊断化合物和含有它们的制剂的无线电稳定性的稳定剂。 特别地，本发明涉及可用于靶向放射性诊断和放射治疗化合物的制备和稳定化的稳定剂，并且在优选的实施方案中涉及靶向胃泌素释放肽受体（GRP-受体）的放射性诊断和放射治疗化合物的制备和稳定 ）。
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公开(公告)号：US20110206606A1
公开(公告)日：2011-08-25
申请号：US12975087
申请日：2010-12-21
申请人： Jianqing Chen , Karen E. Linder , Edmund R. Marinelli , Edmund Metcalfe , Adrian D. Nunn , Rolf E. Swenson , Michael F. Tweedle
发明人： Jianqing Chen , Karen E. Linder , Edmund R. Marinelli , Edmund Metcalfe , Adrian D. Nunn , Rolf E. Swenson , Michael F. Tweedle
CPC分类号： A61K51/12 , A61K51/088
摘要： Stabilized radiopharmaceutical formulations are disclosed. Methods of making and using stabilized radiopharmaceutical formulations are also disclosed. The invention relates to stabilizers that improve the radiostability of radiotherapeutic and radiodiagnostic compounds, and formulations containing them. In particular, it relates to stabilizers useful in the preparation and stabilization of targeted radiodiagnostic and radiotherapeutic compounds, and, in a preferred embodiment, to the preparation and stabilization of radiodiagnostic and radiotherapeutic compounds that are targeted to the Gastrin Releasing Peptide Receptor (GRP-Receptor).
摘要翻译： 公开了稳定的放射性药物制剂。 还公开了制备和使用稳定的放射性药物制剂的方法。 本发明涉及改善放射治疗和放射性诊断化合物的放射稳定性的稳定剂，以及含有它们的制剂。 特别地，本发明涉及可用于靶向放射性诊断和放射治疗化合物的制备和稳定化的稳定剂，并且在优选的实施方案中涉及靶向胃泌素释放肽受体（GRP-受体）的放射性诊断和放射治疗化合物的制备和稳定 ）。
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公开(公告)号：US20080124270A1
公开(公告)日：2008-05-29
申请号：US10584430
申请日：2004-12-20
IPC分类号： A61K51/00 , C07D255/02 , A61P43/00 , A61B5/055
CPC分类号： C07D257/02 , A61K51/0482
摘要： New compounds are provided that may be used to chelute a metal. The compound comprise polyazamacrocyclic compound with at least one phosphonic group substituted on at least one of the aza groups of the polyazamacrocyclic compound. Methods for preparing the compounds are also provided. Methods for preparing a diagnostic imaging agent using the compounds and methods for diagnostic imaging are further provided. Methods for preparing a therapeutic agent using the compounds and methods for therapy are further provided.
摘要翻译： 提供了可用于螯合金属的新化合物。 该化合物包括在多氮杂环辛基化合物的至少一个氮杂基团上被至少一个膦酸基取代的多氮杂环化合物。 还提供了制备化合物的方法。 还提供了使用该化合物的诊断成像剂的制备方法和诊断成像方法。 还提供了使用该化合物制备治疗剂的方法和治疗方法。
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