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11. 发明授权

US5573752A Aromatic amide compounds and metal chelates thereof 失效
标题翻译：芳族酰胺化合物及其金属螯合物
公开(公告)号：US5573752A
公开(公告)日：1996-11-12
申请号：US585290
申请日：1996-01-11
申请人： Ramachandran S. Ranganathan , Edmund R. Marinelli , Radhakrishna Pillai , Michael F. Tweedle
发明人： Ramachandran S. Ranganathan , Edmund R. Marinelli , Radhakrishna Pillai , Michael F. Tweedle
IPC分类号： A61K49/00 , A61K49/06 , A61K49/08 , C07C237/04 , C07D257/02 , A61B5/055
CPC分类号： A61K49/122 , A61K49/085 , A61K49/106 , C07D257/02 , Y10S436/806 , Y10S514/836 , Y10T436/24
摘要： Novel aromatic amide compounds comprising a ligand nucleus containing at least one aminocarboxylate, aminophosphonate and/or aminohydroxamate chelating group, substituted with a substituted aromatic amide group of the formula ##STR1## wherein R is ##STR2## or --[(CH.sub.2).sub.2 --Y]--R.sub.13, salts and/or multimers thereof, and metal chelates, particularly useful for MRI of the hepatobiliary system.
摘要翻译：包含被包含至少一个氨基羧酸盐，氨基膦酸盐和/或氨基羟肟酸盐螯合基团的配体核心的新型芳香族酰胺化合物，被取代的芳基酰胺基团，其中R是其特征，和金属螯合物，特别可用于肝胆系统

12. 发明授权

US5358704A Hepatobiliary tetraazamacrocyclic magnetic resonance contrast agents 失效
标题翻译：肝胆四氮胞质磁共振造影剂
公开(公告)号：US5358704A
公开(公告)日：1994-10-25
申请号：US129870
申请日：1993-09-30
申请人： Jean F. Desreux , Michael F. Tweedle , Peter C. Ratsep , Thomas R. Wagler , Edmund R. Marinelli
发明人： Jean F. Desreux , Michael F. Tweedle , Peter C. Ratsep , Thomas R. Wagler , Edmund R. Marinelli
IPC分类号： A61K49/00 , C07D257/02 , C07D257/10 , C07F5/00 , A61B5/055 , C07D245/00
CPC分类号： C07D257/02 , Y10S514/836 , Y10T436/24
摘要： Novel compounds of the formula ##STR1## and metal chelates of the compounds are useful particularly for MRI of the hepatobiliary system.
摘要翻译：新型化合物“IMAGE”和化合物的金属螯合物特别适用于肝胆系统的MRI。

13. 发明授权

US08420050B2 Gastrin releasing peptide compounds 失效
标题翻译：胃泌素释放肽化合物
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
IPC分类号： A61K51/00 , A61M36/14
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。

14. 发明申请

US20120009122A1 GASTRIN RELEASING PEPTIDE COMPOUNDS 失效
标题翻译： GASTRIN释放肽化合物
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。

15. 发明申请

US20110262366A1 COMPOUNDS FOR TARGETING ENDOTHELIAL CELLS, COMPOSITIONS CONTAINING THE SAME AND METHODS FOR THEIR USE 审中-公开
标题翻译：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。

16. 发明申请

US20090175786A1 Gastrin Releasing Peptide Compounds 失效
标题翻译：胃泌素释放肽化合物
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。

17. 发明授权

US06264916B1 N,N-dimethyldiatrizoic acid and its conjugates as hepatobiliary agents for x-ray CT imaging 失效
标题翻译： N，N-二甲基二异辛酸及其共轭物作为X线CT成像的肝胆药
公开(公告)号：US06264916B1
公开(公告)日：2001-07-24
申请号：US09484840
申请日：2000-01-18
申请人： Rama S. Ranganathan , Thangavel Arunachalam , Michael F. Tweedle
发明人： Rama S. Ranganathan , Thangavel Arunachalam , Michael F. Tweedle
IPC分类号： A61K4904
CPC分类号： A61K49/0447 , A61K49/0438
摘要： Compounds having formulae I, II or/III, or pharmaceutically acceptable salts thereof, R1, R2, R3, R4, R5, R6, R7 and R8 are the same or different and are hydrogen, alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aralkyl, substituted or unsubstituted aryl, haloalkyl, hydroxyalkyl, alkoxyalkyl, carboxyalkyl or carboxamido alkyl with the proviso that in formula I R2 and R3 cannot be methyl; and m, n and p are the same or different and are 0-24 with the proviso that m+n≦24, are useful as contrast agents in x-ray imaging compositions and methods.
摘要翻译：具有式I，II或/ III的化合物或其药学上可接受的盐，R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8相同或不同，为氢，烷基，取代或未取代的环烷基，取代或未取代的芳烷基，取代或未取代的芳基，卤代烷基，羟基烷基，烷氧基烷基，羧基烷基或甲酰氨基烷基，条件是式I中R 2和R 3不能为甲基; andm，n和p相同或不同，并且0-24，条件是m + n <= 24，可用作x射线成像组合物和方法中的造影剂。

18. 发明授权

US4455291A Accelerators for forming cationic technetium complexes useful as radiodiagnostic agents 失效
标题翻译：用于形成阳离子锝络合物的促进剂可用作放射诊断剂
公开(公告)号：US4455291A
公开(公告)日：1984-06-19
申请号：US341553
申请日：1982-01-22
申请人： Michael F. Tweedle
发明人： Michael F. Tweedle
IPC分类号： A61K51/00 , A61K51/04 , C07F9/70 , C07F13/00 , A61K43/00 , A61K49/00 , C07F9/66 , C07F9/90
CPC分类号： A61K51/0497 , C07F13/005 , C07F9/703 , A61K2123/00
摘要： A composition for preparing cationic lipophilic technetium complexes is described. The composition comprises an admixture of (a) an accelerator compound selected from the group of water-soluble organic bidentate ligands that are capable of coordinating with technetium to form a 4 to 6 member ring and (b) a target-seeking ligand, or aqueous salt thereof, having the structure indicated in formulas I, II or III. The accelerator compound has a weaker coordinating bond with technetium than the target-seeking ligand has with technetium.
摘要翻译：描述了用于制备阳离子亲脂锝络合物的组合物。所述组合物包含（a）选自能与锝配位以形成4-6元环的水溶性有机二齿配体的促进剂化合物和（b）寻靶配体，或水性其盐，具有式I，II或III所示的结构。加速剂化合物与锝的配位键与目标寻找配体与锝有较弱的配位键。

19. 发明授权

US07884183B2 Compounds for targeting endothelial cells, compositions containing the same and methods for their use 有权
标题翻译：用于靶向内皮细胞的化合物，含有其的组合物及其使用方法
公开(公告)号：US07884183B2
公开(公告)日：2011-02-08
申请号：US11381908
申请日：2006-05-05
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： A61K38/00 , A61K51/00
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。

20. 发明授权

US07850947B2 Gastrin releasing peptide compounds 失效
标题翻译：胃泌素释放肽化合物
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
IPC分类号： A61K51/00 , A61M36/14
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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