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1.发明授权Methods for the in vivo measurement of the concentration of NMR-detectable xenobiotic compounds 失效用于体内测量可NMR检测的异生物化合物的浓度的方法
公开(公告)号：US5603917A
公开(公告)日：1997-02-18
申请号：US365013
申请日：1994-12-28
CPC分类号： A61K49/06 , G01R33/448 , G01R33/465 , Y10S514/836 , Y10T436/24
摘要： Methods wherein the concentration of NMR-detectable xenobiotic compounds may be determined in living subjects by in vivo measurement of one or more magnetic resonance signals. In preferred embodiments, the present invention provides a method for evaluating, in vivo, the clearance rate of a xenobiotic compound from a living subject, thereby providing a noninvasive method for determining the status of the excretory organs of the subject, and a method for determining the proper dosing regimen of a pharmacologically active compound to be administered to the subject.
摘要翻译： 可以通过一个或多个磁共振信号的体内测量在活体受体中测定可检测NMR的异生物化合物的浓度的方法。 在优选的实施方案中，本发明提供了一种用于在体内评价来自活体的异生素化合物的清除率的方法，从而提供了用于确定受试者的排泄器官状态的非侵入性方法，以及用于确定 给予受试者的药理活性化合物的适当给药方案。
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2.发明授权Methods for the in vivo measurement of the concentration of non-imaging nmr-detectable xenobiotic compounds 失效用于体内测量非成像nmr可检测异种生物化合物浓度的方法
公开(公告)号：US5468467A
公开(公告)日：1995-11-21
申请号：US52959
申请日：1993-04-23
CPC分类号： A61K49/06 , G01R33/448 , G01R33/465 , Y10S514/836 , Y10T436/24
摘要： Methods wherein the concentration of NMR-detectable xenobiotic compounds may be determined in living subjects by in vivo measurement of one or more magnetic resonance signals. In preferred embodiments, the present invention provides a method for evaluating, in vivo, the clearance rate of a xenobiotic compound from a living subject, thereby providing a noninvasive method for determining the status of the excretory organs of the subject, and a method for determining the proper dosing regimen of a pharmacologically active compound to be administered to the subject.
摘要翻译： 可以通过一个或多个磁共振信号的体内测量在活体受体中测定可检测NMR的异生物化合物的浓度的方法。 在优选的实施方案中，本发明提供了一种用于在体内评价来自活体的异生素化合物的清除率的方法，从而提供了用于确定受试者的排泄器官状态的非侵入性方法，以及用于确定 给予受试者的药理活性化合物的适当给药方案。
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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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5.发明申请COMPOUNDS FOR TARGETING ENDOTHELIAL CELLS, COMPOSITIONS CONTAINING THE SAME AND METHODS FOR THEIR USE 审中-公开用于靶向内皮细胞的化合物，包含其的组合物及其使用方法公开(公告)号：US20110262366A1
公开(公告)日：2011-10-27
申请号：US12969327
申请日：2010-12-15
申请人： Mathew A. Von Wronski , Edmund R. Marinelli , Adrian D. Nunn , Radhakrishna K. Pillai , Kondareddiar Ramalingam , Michael F. Tweedle , Karen E. Linder , Palaniappa Nanjappan , Natarajan Raju , Feng Yan , Michel Schneider
发明人： Mathew A. Von Wronski , Edmund R. Marinelli , Adrian D. Nunn , Radhakrishna K. Pillai , Kondareddiar Ramalingam , Michael F. Tweedle , Karen E. Linder , Palaniappa Nanjappan , Natarajan Raju , Feng Yan , Michel Schneider
IPC分类号： A61K49/22 , C07K7/08 , C07K14/00 , C12N9/96 , A61P43/00 , C07K1/107 , A61K38/08 , A61K9/14 , A61K38/10 , A61K38/16 , C07K7/06 , C07K19/00
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：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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7.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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8.发明授权Metal complexes derivatized with folate for use in diagnostic and therapeutic applications 失效用叶酸衍生的金属络合物用于诊断和治疗应用公开(公告)号：US07399460B2
公开(公告)日：2008-07-15
申请号：US11534919
申请日：2006-09-25
申请人： Paul W. Wedeking , Ruth E. Wager , Thangavel Arunachalam , Kondareddiar Ramalingam , Karen E. Linder , Ramachandran S. Ranganathan , Adrian D. Nunn , Nataranjan Raju , Michael F. Tweedle
发明人： Paul W. Wedeking , Ruth E. Wager , Thangavel Arunachalam , Kondareddiar Ramalingam , Karen E. Linder , Ramachandran S. Ranganathan , Adrian D. Nunn , Nataranjan Raju , Michael F. Tweedle
CPC分类号： A61K49/10 , A61K49/085 , A61K49/122 , A61K49/124 , A61K49/146 , A61K51/0459 , A61K51/0497
摘要： Diagnostic and therapeutic compositions in the form of complexes for enhancing transmembrane transport of a diagnostic or therapeutic agent and methods for their use. The complexes contain the α, γ, or bis isomers of folate receptor-binding analogs of folate, a metal chelated by a ligand, and in one embodiment, a chemotherapeutic agent.
摘要翻译： 用于增强诊断或治疗剂的跨膜转运的复合物形式的诊断和治疗组合物及其使用方法。 复合物含有叶酸的叶酸受体结合类似物的α，γ或双异构体，被配体螯合的金属，在一个实施方案中，化学治疗剂。
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9.发明申请Compounds for Targeting Endothelial Cells, Compositions Containing the Same and Methods for Their Use 审中-公开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：US20120315220A1
公开(公告)日：2012-12-13
申请号：US13445434
申请日：2012-04-12
申请人： Mathew A. Von Wronski , Edmund R. Marinelli , Adrian D. Nunn , Radhakrishna Pillai , Kondareddiar Ramalingam , Michael F. Tweedle , Karen E. Linder , Palaniappa Nanjappan , Natarajan Raju
发明人： Mathew A. Von Wronski , Edmund R. Marinelli , Adrian D. Nunn , Radhakrishna Pillai , Kondareddiar Ramalingam , Michael F. Tweedle , Karen E. Linder , Palaniappa Nanjappan , Natarajan Raju
IPC分类号： A61K38/08 , G01N33/566 , A61P35/00 , C07K7/06 , A61K49/00
CPC分类号： A61K49/0067 , A61K38/00 , A61K47/6923 , A61K47/6929 , A61K49/0056 , A61K49/14 , A61K49/223 , A61K51/088 , 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：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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