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1. 发明申请

US20110206606A1 STABLE RADIOPHARMACEUTICAL COMPOSITIONS AND METHODS FOR PREPARATION 审中-公开
标题翻译：稳定的放射性物质组合物和制备方法
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
IPC分类号： A61K51/08 , A61K51/00 , A61K51/04 , A61K47/42
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）。

2. 发明申请

US20120065365A1 Stable Radiopharmaceutical Compositions and Methods for Their Preparation 审中-公开
标题翻译：稳定的放射性药物组合物及其制备方法
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）。

3. 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。

4. 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。

5. 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。

6. 发明申请

US20120315220A1 Compounds for Targeting Endothelial Cells, Compositions Containing the Same and Methods for Their Use 审中-公开
标题翻译：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。

7. 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。

8. 发明授权

US07820621B2 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：US07820621B2
公开(公告)日：2010-10-26
申请号：US11381884
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 , A61K38/04
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。

9. 发明授权

US08642010B2 KDR and VEGF/KDR binding peptides and their use in diagnosis and therapy 有权
标题翻译： KDR和VEGF / KDR结合肽及其在诊断和治疗中的应用
公开(公告)号：US08642010B2
公开(公告)日：2014-02-04
申请号：US12480578
申请日：2009-06-08
申请人： Aaron K. Sato , Daniel J. Sexton , Daniel T. Dransfield , Robert C. Ladner , Christophe Arbogast , Philippe Bussat , Hong Fan , Sudha Khurana , Karen E. Linder , Edmund R. Marinelli , Palaniappa Nanjappan , Adrian D. Nunn , Radhakrishna K. Pillai , Sibylle Pochon , Feng Yan , Kondareddiar Ramalingam , Ajay Shrivastava , Bo Song , Rolf E. Swenson , Mathew A. Von Wronski
发明人： Aaron K. Sato , Daniel J. Sexton , Daniel T. Dransfield , Robert C. Ladner , Christophe Arbogast , Philippe Bussat , Hong Fan , Sudha Khurana , Karen E. Linder , Edmund R. Marinelli , Palaniappa Nanjappan , Adrian D. Nunn , Radhakrishna K. Pillai , Sibylle Pochon , Feng Yan , Kondareddiar Ramalingam , Ajay Shrivastava , Bo Song , Rolf E. Swenson , Mathew A. Von Wronski
IPC分类号： A61K49/00 , A61B8/00
CPC分类号： A61K49/221 , A61K38/00 , A61K47/62 , A61K49/223 , A61K51/088 , C07K7/08 , C07K14/001 , C07K14/52 , C07K14/71 , C07K2319/00 , Y02A50/411 , Y02A50/58
摘要： The present invention provides polypeptides, peptide dimer, and multimeric complexes comprising at least one binding moiety for KDR or VEGF/KDR complex, which have a variety of uses wherever treating, detecting, isolating or localizing angiogenesis is advantageous. Particularly disclosed are synthetic, isolated polypeptides capable of binding KDR or VEGF/KDR complex with high affinity (e.g., having a KD
摘要翻译：本发明提供了包含用于KDR或VEGF / KDR复合物的至少一个结合部分的多肽，肽二聚体和多聚体复合物，其具有各种用途，无论何处治疗，检测，分离或定位血管发生都是有利的。特别公开的是能够以高亲和力（例如具有KD <1μM）结合KDR或VEGF / KDR复合物的合成，分离的多肽，以及包含这些多肽的二聚体和多聚体构建体。

10. 发明申请

US20110097275A1 KDR AND VEGF/KDR BINDING PEPTIDES AND THEIR USE IN DIAGNOSIS AND THERAPY 有权
标题翻译： KDR和VEGF / KDR结合肽及其在诊断和治疗中的应用
公开(公告)号：US20110097275A1
公开(公告)日：2011-04-28
申请号：US12898119
申请日：2010-10-05
申请人： Christophe Arbogast , Philippe Bussat , Hong Fan , Sudha Khurana , Karen E. Linder , Edmund R. Marinelli , Palaniappa Nanjappan , Adrian D. Nunn , Radhakrishna K. Pillai , Sibylle Pochon , Kondareddiar Ramalingam , Ajay Shrivastava , Bo Song , Rolf E. Swenson , Mathew A. Von Wronski , Feng Yan
发明人： Christophe Arbogast , Philippe Bussat , Hong Fan , Sudha Khurana , Karen E. Linder , Edmund R. Marinelli , Palaniappa Nanjappan , Adrian D. Nunn , Radhakrishna K. Pillai , Sibylle Pochon , Kondareddiar Ramalingam , Ajay Shrivastava , Bo Song , Rolf E. Swenson , Mathew A. Von Wronski , Feng Yan
IPC分类号： A61K49/22 , A61P35/00
CPC分类号： A61K49/221 , A61K38/00 , A61K49/223 , A61K51/088 , C07K7/08 , C07K14/001 , C07K14/52 , C07K14/71 , C07K2319/00 , Y02A50/58
摘要： The present invention provides polypeptides, peptide dimers, and multimeric complexes comprising at least one binding moiety for KDR or VEGF/KDR complex, which have a variety of uses wherever treating, detecting, isolating or localizing angiogenesis is advantageous. Particularly disclosed are synthetic, isolated polypeptides capable of binding KDR or VEGF/KDR complex with high affinity (e.g., having a KD
摘要翻译：本发明提供了包含用于KDR或VEGF / KDR复合物的至少一个结合部分的多肽，肽二聚体和多聚体复合物，其具有各种用途，无论何处治疗，检测，分离或定位血管发生都是有利的。特别公开的是能够以高亲和力（例如具有KD <1μM）结合KDR或VEGF / KDR复合物的合成，分离的多肽，以及包含这些多肽，特别是造影剂的二聚体和多聚体构建体。还提供了使用本发明的造影剂监测和评估与血管生成或内皮细胞过度增殖相关的疾病（例如癌症）的治疗方案的治疗有效性的方法。

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