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

IPC分类号： A61K51/08 ,  A61P35/00

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。

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

IPC分类号： A61K51/08 ,  A61P35/04

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。

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

IPC分类号： A61K51/08 ,  C07K2/00 ,  C07K1/00

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。

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。

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

IPC分类号： A61K51/00 ,  C07F5/00

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.

公开(公告)号：US20050008573A1

公开(公告)日：2005-01-13

申请号：US10485847

申请日：2002-07-26

申请人： Silvio Aime ,  Eliana Gianolio ,  Giancarlo Morelli ,  Carlo Pedone ,  Diego Tesauro ,  Luciano Lattuada ,  Massimo Visigalli ,  Pier Anelli

发明人： Silvio Aime ,  Eliana Gianolio ,  Giancarlo Morelli ,  Carlo Pedone ,  Diego Tesauro ,  Luciano Lattuada ,  Massimo Visigalli ,  Pier Anelli

IPC分类号： A61K38/04 ,  A61B5/055 ,  A61K49/00 ,  A61K49/08 ,  A61P35/00 ,  C07K14/00 ,  C07K14/595 ,  C07K14/655 ,  C07K7/64

CPC分类号： A61K49/14 ,  A61K49/085 ,  C07K14/595 ,  C07K14/655

摘要： The present invention relates to a novel class of contrast agents for use in nuclear magnetic resonance (MRI), to identify and locate primary human tumours and their metastases which over-express type CCK A and/or type B cholecystokinin receptors, and/or type SSTR 1-5 somatostatin receptors.

摘要翻译： 本发明涉及一种用于核磁共振（MRI）的新型造影剂，用于鉴定和定位过表达CCK A和/或B型胆囊收缩素受体的原发性人类肿瘤及其转移，和/或类型 SSTR 1-5生长抑素受体。