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公开(公告)号：US20110256067A1
公开(公告)日：2011-10-20
申请号：US11630600
申请日：2005-06-28
申请人： Silvio Aime , Matteo Galli , Luciano Lattuada , Pierfrancesco Morosini , Fulvio Uggeri , Kondareddiar Ramalingam
发明人： Silvio Aime , Matteo Galli , Luciano Lattuada , Pierfrancesco Morosini , Fulvio Uggeri , Kondareddiar Ramalingam
IPC分类号： A61K49/10 , C07F5/00 , C07D243/10 , C07H15/26 , C07D243/08
CPC分类号： C07H15/26 , A61K49/085 , A61K49/124 , C07C237/08 , C07D243/08 , C07D243/10 , C07F9/3808 , C07F9/4006 , C07F9/5728 , C07H17/02
摘要： The present invention relates to a novel class of paramagnetic ion-based contrast agents of formula (I), wherein a chelating backbone moiety is highly functionalized by the presence of one or more polyhydroxylated chain, that show a pharmacokinetic profile analogous to that of the commonly used T1-general extravascular agents (NSA) but are further characterized by a higher relaxivity.
摘要翻译： 本发明涉及式（I）的新型顺磁离子型造影剂，其中螯合骨架部分通过存在一个或多个多羟基化链而被高度官能化，其显示类似于常规的药代动力学特征 使用T1一般血管外药物（NSA），但其进一步的特征是较高的松弛度。
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公开(公告)号：US20060239914A1
公开(公告)日：2006-10-26
申请号：US11352156
申请日：2006-02-10
申请人： Enrico Cappelletti , Luciano Lattuada , Karen Linder , Edmund Marinelli , Palaniappa Nanjappan , Adrian Nunn , Natarajan Raju , Kondareddiar Ramalingam , Rolf Swenson , Michael Tweedle
发明人： Enrico Cappelletti , Luciano Lattuada , Karen Linder , Edmund Marinelli , Palaniappa Nanjappan , Adrian Nunn , Natarajan Raju , Kondareddiar Ramalingam , Rolf Swenson , Michael Tweedle
IPC分类号： A61K51/00 , A61K49/00 , C07K14/775
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.
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33.发明授权Multidentate AZA ligands able to complex metal ions and the use thereof in diagnostics and therapy 有权能够复合金属离子的多齿AZA配体及其在诊断和治疗中的应用公开(公告)号：US08105567B2
公开(公告)日：2012-01-31
申请号：US12553421
申请日：2009-09-03
CPC分类号： C07C209/62 , A61K49/0002 , A61K49/085 , A61K49/106 , A61K49/122 , A61K49/14 , A61K51/088 , C07D243/08 , C07D243/14 , C07F9/301 , C07F9/3808 , C07F9/4816 , C07F9/645 , C07C211/50
摘要： Compounds of the formula: Wherein R is selected from the group consisting of H, NH2, and NHBoc; and R′ is selected from the group consisting of H, CH2Ph and tBu, optionally de-protected. Such compounds may be conjugated with a suitable molecule able to interact with physiological systems; and their chelates with bi-trivalent ions of the metal elements having atomic number ranging between 20 and 31, 39, 42, 43, 44, 49, and between 57 and 83, and radioisotopes chosen among 203Pb, 67Ga, 68Ga, 72As, 111In, 113In, 90Y, 97Ru, 62Cu, 64Cu, 52Fe, 52mMn, 140La, 175Yb, 153Sm, 166Ho, 149Pm, 177Lu, 142Pr, 159Gd, 212Bi, 47Sc, 149Pm, 67Cu, 111Ag, 199Au, 161Tb, 51Cr, 167Tm, 141Ce, 168Yb, 88Y, 165Dy, 166Dy, 97Ru, 103Ru, 186Re, 188Re, 99mTc, 211Bi, 212Bi, 213Bi, 214Bi, 105Rh, 109Pd, 117mSn, 177Sn and 199Au, as well as the salts thereof with physiologically compatible bases or acids.
摘要翻译： 下式的化合物：其中R选自H，NH 2和NHBoc; 并且R'选自H，CH 2 Ph和tBu，任选地被去保护。 这样的化合物可以与能够与生理系统相互作用的合适分子缀合; 其螯合物与金属元素的二价离子的原子序数范围在20,31,39,42,43,44,49和57和83之间，并且放射性同位素选自203Pb，67Ga，68Ga，72As，111In ，113In，90Y，97Ru，62Cu，64Cu，52Fe，52mMn，140La，175Yb，153Sm，166Ho，149Pm，177Lu，142Pr，159Gd，212Bi，47Sc，149Pm，67Cu，111Ag，199Au，161Tb，51Cr，167Tm，141Ce ，168Yb，88Y，165Dy，166Dy，97Ru，103Ru，186Re，188Re，99mTc，211Bi，212Bi，213Bi，214Bi，105Rh，109Pd，117mSn，177Sn和199Au，以及其与生理上相容的碱或酸的盐。
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34.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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35.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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36.发明授权Compounds for targeting endothelial cells, compositions containing the same and methods for their use 失效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：US08263739B2
公开(公告)日：2012-09-11
申请号：US11342050
申请日：2006-01-27
申请人： Mathew A. Von Wronski , Edmund R. Marinelli , Adrian 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 Nunn , Radhakrishna Pillai , Kondareddiar Ramalingam , Michael F. Tweedle , Karen E. Linder , Palaniappa Nanjappan , Natarajan Raju
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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37.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：US07186397B2
公开(公告)日：2007-03-06
申请号：US09752867
申请日：2000-12-30
申请人： Paul W. Wedeking , Ruth E. Wager , Thangavel Arunachalam , Kondareddiar Ramalingam , Karen E. Linder , Ramachandran S. Ranganathan , Adrian D. Nunn , Natarajan 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 , Natarajan 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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38.发明授权Compounds for targeting endothelial cells, compositions containing the same and methods for their use 有权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
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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39.发明授权Compounds for targeting endothelial cells, compositions containing the same and methods for their use 有权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
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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40.发明授权公开(公告)号：US07109167B2
公开(公告)日：2006-09-19
申请号：US09871974
申请日：2001-06-04
申请人： Mathew A. Von Wronski , Edmund R. Marinelli , Adrian D. Nunn , Radhakrishna Pillai , Kondareddiar Ramalingam , Michael F. Tweedle , Karen 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 Linder , Palaniappa Nanjappan , Natarajan Raju
IPC分类号： A61K38/00
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.
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