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公开(公告)号：US07922998B2
公开(公告)日：2011-04-12
申请号：US11165721
申请日：2005-06-24
申请人： Enrico Cappelletti , Luciano Lattuada , Karen E. Linder , Edmund Marinelli , Palaniappa Nanjappan , Natarajan Raju , Kondareddiar Ramalingam , Rolf E. Swenson , Michael Tweedle
发明人： Enrico Cappelletti , Luciano Lattuada , Karen E. Linder , Edmund Marinelli , Palaniappa Nanjappan , Natarajan Raju , Kondareddiar Ramalingam , Rolf E. Swenson , Michael Tweedle
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.
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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公开(公告)号：US20110070165A1
公开(公告)日：2011-03-24
申请号：US12888736
申请日：2010-09-23
申请人： Christophe Arbogast , Philippe Bussat , Hong Fan , 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 , Aaron K. Sato , Sharon Michele Walker , Daniel T. Dransfield
发明人： Christophe Arbogast , Philippe Bussat , Hong Fan , 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 , Aaron K. Sato , Sharon Michele Walker , Daniel T. Dransfield
摘要： The invention provides compositions and methods for therapeutic and diagnostic applications.
摘要翻译： 本发明提供用于治疗和诊断应用的组合物和方法。
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公开(公告)号：US20100233090A1
公开(公告)日：2010-09-16
申请号：US12782783
申请日：2010-05-19
申请人： Philippe Bussat , Samir Cherkaoui , Hong (Helen) Fan , Bernard Lamy , Palaniappa Nanjappan , Radhakrishna Pillai , Sibylle Pochon , Bo Song , Rolf E. Swenson
发明人： Philippe Bussat , Samir Cherkaoui , Hong (Helen) Fan , Bernard Lamy , Palaniappa Nanjappan , Radhakrishna Pillai , Sibylle Pochon , Bo Song , Rolf E. Swenson
CPC分类号： A61K49/223 , A61K38/00 , A61K47/544 , A61K47/60 , A61K47/62 , A61K49/227 , C07K7/08 , C07K14/001 , C07K14/52 , C07K14/71 , C07K2319/00 , Y02A50/58
摘要： Peptide vectors having high KDR binding affinity and processes for making such vectors are provided. The peptide vectors may be conjugated to phospholipids and included in ultrasound contrast agent compositions. Such ultrasound contrast agents are particularly useful in therapeutic and diagnostic methods, such as in imaging KDR-containing tissue and in the evaluation and treatment of angiogenic processes associated with neoplastic conditions. The present invention also provides processes for the large scale production of highly pure dimeric and monomeric peptide phospholipid conjugates as well as precursor materials used to form the conjugates. The present invention further provides processes for the large scale production of highly pure peptide phospholipid conjugates which contain very low levels of TFA.
摘要翻译： 提供具有高KDR结合亲和力的肽载体和用于制备此类载体的方法。 肽载体可以与磷脂结合并包含在超声造影剂组合物中。 这样的超声造影剂在治疗和诊断方法中是特别有用的，例如在成像含KDR组织和评估和治疗与肿瘤病症相关的血管生成过程中。 本发明还提供大规模生产高纯度二聚体和单体肽磷脂共轭物以及用于形成缀合物的前体材料的方法。 本发明还提供了大规模生产含有非常低水平的TFA的高纯度肽磷脂缀合物的方法。
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74.发明申请FIBRIN BINDING PEPETIDE CONJUGATES FOR DIAGNOSTIC AND THERAPEUTIC APPLICATIONS 有权用于诊断和治疗应用的纤维蛋白结合胶原蛋白公开(公告)号：US20100202967A1
公开(公告)日：2010-08-12
申请号：US12448102
申请日：2007-12-11
申请人： Silvio Aime , Linda Chaabane , Luciano Lattuada , Vito Lorusso , Edmund R. Marinelli , Pierfrancesco Morosini , Kondareddiar Ramalingam , Bo Song , Rolf E. Swenson , Fulvio Uggeri
发明人： Silvio Aime , Linda Chaabane , Luciano Lattuada , Vito Lorusso , Edmund R. Marinelli , Pierfrancesco Morosini , Kondareddiar Ramalingam , Bo Song , Rolf E. Swenson , Fulvio Uggeri
IPC分类号： A61K49/00 , C07K7/08 , C07K7/50 , A61K38/10 , A61K38/16 , A61P35/00 , A61P35/04 , A61P29/00 , A61P7/02 , A61P9/00 , G01N33/50 , G01N33/567
CPC分类号： A61K49/14 , A61K49/0043 , A61K49/0056 , A61K49/085 , A61K49/124 , C07K7/06 , G01N33/532 , G01N33/574 , G01N33/86 , G01N2500/04
摘要： The present invention relates to a novel class of diagnostically or therapeutically effective compounds comprising novel peptides able to bind fibrin, to a process for their preparation and to compositions thereof for use in therapy and diagnostics. The compounds of the invention bind, in particular, to fibrin present in the extracellular matrix (EC) of tumor or connective tissue of stroma thus acting as targeting moieties able to bring and successfully bound an active moiety linked thereto to fibrin depositions inside solid tumors.
摘要翻译： 本发明涉及一类新的诊断或治疗有效化合物，其包含能够结合纤维蛋白的新肽，其制备方法及其组合物用于治疗和诊断。 本发明的化合物特别结合存在于基质的肿瘤或结缔组织的细胞外基质（EC）中的纤维蛋白，因此作为能够使与其连接的活性部分与实质瘤内的纤维蛋白沉积成功结合的靶向部分。
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75.发明申请TARGETING AND THERAPEUTIC COMPOUNDS AND GAS-FILLED MICROVESICLES COMPRISING SAID COMPOUNDS 有权靶向和治疗化合物和包含化合物的气体填充微量元素公开(公告)号：US20100008863A1
公开(公告)日：2010-01-14
申请号：US12448401
申请日：2007-12-19
CPC分类号： A61K49/223
摘要： New targeting or therapeutic compounds which can be incorporated into a composition of gas-filled microvesicles. The invention further relates to gas-filled microvesicles for diagnostic and/or therapeutic use comprising said compounds and to their method of use. The new compounds are compounds of formula M-S-T, wherein: M represents a component capable of associating with an envelope of a gas-filled microvesicle; T represents a component comprising a targeting ligand or a therapeutic agent; and S represents a component comprising at least two bissulfone groups.
摘要翻译： 可以掺入气体填充微泡组合物中的新靶向或治疗化合物。 本发明还涉及用于诊断和/或治疗用途的充气微泡，其包含所述化合物及其使用方法。 新化合物是式M-S-T的化合物，其中：M表示能与气体填充的微泡的包膜缔合的成分; T表示包含靶向配体或治疗剂的组分; S表示包含至少两个双砜基团的组分。
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76.发明申请KDR AND VEGF/KDR BINDING PEPTIDES AND THEIR USE IN DIAGNOSIS AND THERAPY 有权KDR和VEGF / KDR结合肽及其在诊断和治疗中的应用公开(公告)号：US20100003195A1
公开(公告)日：2010-01-07
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 Pillai , Sibylle Pochon , 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 Pillai , Sibylle Pochon , Kondareddiar Ramalingam , Ajay Shrivastava , Bo Song , Rolf E. Swenson , Mathew A. Von Wronski
IPC分类号： A61K49/22
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。
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公开(公告)号：US07611692B2
公开(公告)日：2009-11-03
申请号：US10828925
申请日：2004-04-20
申请人： Enrico Cappelletti , Luciano Lattuada , Karen E. Linder , Edmund Marinelli , Palaniappa Nanjappan , Natarajan Raju , Kondareddiar Ramalingam , Rolf E. Swenson , Michael Tweedle
发明人： Enrico Cappelletti , Luciano Lattuada , Karen E. Linder , Edmund Marinelli , Palaniappa Nanjappan , Natarajan Raju , Kondareddiar Ramalingam , Rolf E. Swenson , Michael Tweedle
IPC分类号： A61K49/00
CPC分类号： C07K7/086 , 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 an optical label or a 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 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MNOPG的诊断成像或治疗的新的和改进的化合物，其中M是光学标记或金属螯合剂（以与金属放射性核素复合的形式），NOP是接头，G是GRP受体 靶向肽。 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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公开(公告)号：US07211240B2
公开(公告)日：2007-05-01
申请号：US10379287
申请日：2003-03-03
申请人： Christophe Arbogast , Philippe Bussat , Hong Fan , Karen E. Linder , Edmund R. Marinelli , Palaniappa Nanjappan , Adrian Nunn , Radhakrishna Pillai , Sybille Pochon , Kondareddiar Ramalingam , Ajay Shrivastava , Bo Song , Rolf E. Swenson , Mathew A. Von Wronski , Aaron Sato , Sharon Michele Walker , Daniel T. Dransfield
发明人： Christophe Arbogast , Philippe Bussat , Hong Fan , Karen E. Linder , Edmund R. Marinelli , Palaniappa Nanjappan , Adrian Nunn , Radhakrishna Pillai , Sybille Pochon , Kondareddiar Ramalingam , Ajay Shrivastava , Bo Song , Rolf E. Swenson , Mathew A. Von Wronski , Aaron Sato , Sharon Michele Walker , Daniel T. Dransfield
IPC分类号： A61K49/00
摘要： The invention provides compositions and methods for therapeutic and diagnostic applications.
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公开(公告)号：US5616759A
公开(公告)日：1997-04-01
申请号：US441966
申请日：1995-05-16
IPC分类号： A61K31/59 , A61P35/00 , C07C35/14 , C07C35/17 , C07C43/115 , C07C49/497 , C07C67/343 , C07C69/732 , C07C69/734 , C07C69/74 , C07C317/18 , C07C401/00 , C07D307/20 , C07D309/12 , C07F7/08 , C07F7/18 , C07F9/40 , C07F9/53 , C07F7/04 , C07F9/02
CPC分类号： C07F7/1856 , C07C401/00 , C07F9/532 , Y02P20/55
摘要： Cyclohexylidene compounds of the structure: ##STR1## where X.sup.1 and X.sup.2, which may be the same or different, is hydrogen or a hydroxy-protecting group, and Y is --POPh.sub.2, or --PO (OAlkyl).sub.2, or --SO.sub.2 Ar, or --Si(Alkyl).sub.3. The compounds are used as intermediates in the preparation of 19-nor-vitamin D compounds.
摘要翻译： 结构的环亚己基化合物：其中X1和X2可以相同或不同，是氢或羟基保护基，Y是-POPh2或-PO（O烷基）2或-SO2Ar，或 -Si（烷基）3。 该化合物用作制备19-维生素D化合物的中间体。
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公开(公告)号：US5597932A
公开(公告)日：1997-01-28
申请号：US442508
申请日：1995-05-16
IPC分类号： A61K31/59 , A61P35/00 , C07C35/14 , C07C35/17 , C07C43/115 , C07C49/497 , C07C67/343 , C07C69/732 , C07C69/734 , C07C69/74 , C07C317/18 , C07C401/00 , C07D307/20 , C07D309/12 , C07F7/08 , C07F7/18 , C07F9/40 , C07F9/53 , C07D309/00 , C07C47/28
CPC分类号： C07F7/1856 , C07C401/00 , C07F9/532 , Y02P20/55
摘要： The invention is drawn to a compound having the following formula ##STR1## in which X.sup.1 and X.sup.2, which may be the same or different, represent hydrogen or a hydroxy-protecting group, X.sup.4 is hydrogen, A is selected from --COOAlkyl and CH.sub.2 OH, and B is a hydroxy group, or A and B, when taken together, represent an oxo group. These compounds are useful as intermediates in the production of 19-nor vitamin D derivatives.
摘要翻译： 本发明涉及具有下式的化合物，其中X 1和X 2可以相同或不同，表示氢或羟基保护基，X 4是氢，A选自-COOA烷基和CH 2 OH， 并且B是羟基，或者A和B一起表示氧基。 这些化合物可用作生产19-维生素D衍生物的中间体。
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