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41. 发明申请

US20110229409A1 LINKABLE LEWIS X ANALOGS 审中-公开
标题翻译：可链接的LEWIS X模拟
公开(公告)号：US20110229409A1
公开(公告)日：2011-09-22
申请号：US13116828
申请日：2011-05-26
申请人： Ramachandran Ranganathan , Kondareddiar Ramalingam , Radhakrishna Pillai , Edmund R. Marinelli , Rolf E. Swenson
发明人： Ramachandran Ranganathan , Kondareddiar Ramalingam , Radhakrishna Pillai , Edmund R. Marinelli , Rolf E. Swenson
IPC分类号： A61K51/00 , C07H15/26 , C07K9/00 , A61K31/7034 , A61K49/00 , A61K38/14 , A61P43/00 , A61P35/00 , A61P3/10 , A61P3/04 , A61P19/00 , A61P7/02 , A61P17/06
CPC分类号： C07H15/04 , A61K49/0002 , C07H7/02 , C07H15/00
摘要： Disclosed herein is a class of linkable tetrasaccharide compounds that includes the amino phenyl glycoside of sialyl Lewis X (SLeX) and related analogs. These compounds have conjugatable nucleophilic groups, making them useful in preparing multimeric SLeX compositions. In particular, the disclosed SLeX compounds can be used to prepare selectin binding ligand con-jugatcs by linking them to a reporter moiety, such as a contrast agent, a radiodiagnostic agent, or a cytotoxic or chemotherapeutic agent. The SLeX compounds and conjugates of the invention exhibit binding to selectin that is similar to native Sialyl LeX, and are, therefore, useful for diagnosing and treating selectin-mediated disorders and related conditions.
摘要翻译：本文公开了一类可连接的四糖化合物，其包括唾液酸基路易斯X（SLeX）的氨基苯基糖苷和相关类似物。这些化合物具有可共轭的亲核基团，使其可用于制备多聚体SLeX组合物。特别地，所公开的SLeX化合物可用于通过将选择蛋白结合配体结合物与报告物部分如造影剂，放射性诊断剂或细胞毒性或化学治疗剂连接来制备选择素结合配体。本发明的SLeX化合物和缀合物显示出与天然唾液酸LeX相似的选择蛋白结合，因此可用于诊断和治疗选择素介导的病症和相关病症。

42. 发明申请

US20080274048A1 CONJUGATES OF ANTIOXIDANTS WITH METAL CHELATING LIGANDS FOR USE IN DIAGNOSTIC AND THERAPEUTIC APPLICATIONS 失效
标题翻译：金属螯合剂用于诊断和治疗应用中的抗氧化剂结合
公开(公告)号：US20080274048A1
公开(公告)日：2008-11-06
申请号：US12169105
申请日：2008-07-08
申请人： Ramachandran S. Ranganathan , Hong (Helen) Fan , Michael F. Tweedle , Rolf E. Swenson
发明人： Ramachandran S. Ranganathan , Hong (Helen) Fan , Michael F. Tweedle , Rolf E. Swenson
IPC分类号： A61K51/04 , A61K51/10 , A61K51/08
CPC分类号： C07D405/12 , A61K51/12
摘要： The invention provides radiopharmaceuticals for diagnostic and therapeutic applications, conjugates of antioxidants with metal chelating ligands, intermediate compounds, methods of making such radiopharmaceuticals, ligands, and intermediate compounds, and kits for preparing the radiopharmaceutical complexes.
摘要翻译：本发明提供用于诊断和治疗应用的放射性药物，抗氧化剂与金属螯合配体的缀合物，中间体化合物，制备这种放射性药物的方法，配体和中间体化合物，以及用于制备放射性药物复合物的试剂盒。

43. 发明申请

US20080300220A1 Linkable Lewis X Analogs 审中-公开
标题翻译：可连接的Lewis X类似物
公开(公告)号：US20080300220A1
公开(公告)日：2008-12-04
申请号：US12190857
申请日：2008-08-13
申请人： Ramachandran Ranganathan , Kondareddiar Ramalingam , Radhakrishna Pillai , Edmund R. Marinelli , Rolf E. Swenson
发明人： Ramachandran Ranganathan , Kondareddiar Ramalingam , Radhakrishna Pillai , Edmund R. Marinelli , Rolf E. Swenson
IPC分类号： A61K31/715 , C07H15/22
CPC分类号： C07H15/04 , A61K49/0002 , C07H7/02 , C07H15/00
摘要： Disclosed herein is a class of linkable tetrasaccharide compounds that includes the amino phenyl glycoside of sialyl Lewis X (SLeX) and related analogs. These compounds have conjugatable nucleophilic groups, making them useful in preparing multimeric SLeX compositions. In particular, the disclosed SLeX compounds can be used to prepare selectin binding ligand conjugates by linking them to a reporter moiety, such as a contrast agent, a radiodiagnostic agent, or a cytotoxic or chemotherapeutic agent. The SLeX compounds and conjugates of the invention exhibit binding to selectin that is similar to native Sialyl LeX, and are, therefore, useful for diagnosing and treating selectin-mediated disorders and related conditions.
摘要翻译：本文公开了一类可连接的四糖化合物，其包括唾液酸基路易斯X（SLeX）的氨基苯基糖苷和相关类似物。这些化合物具有可共轭的亲核基团，使其可用于制备多聚体SLeX组合物。特别地，所公开的SLeX化合物可用于通过将选择蛋白结合配体缀合物连接到报告基因部分如造影剂，放射诊断剂或细胞毒性或化学治疗剂来制备。本发明的SLeX化合物和缀合物显示出与天然唾液酸LeX相似的选择蛋白结合，因此可用于诊断和治疗选择素介导的病症和相关病症。

44. 发明授权

US07407644B2 Conjugates of antioxidants with metal chelating ligands for use in diagnostic and therapeutic applications 失效
标题翻译：抗氧化剂与金属螯合配体的结合物用于诊断和治疗应用
公开(公告)号：US07407644B2
公开(公告)日：2008-08-05
申请号：US11561638
申请日：2006-11-20
申请人： Ramachandran S. Ranganathan , Hong (Helen) Fan , Michael F. Tweedle , Rolf E. Swenson
发明人： Ramachandran S. Ranganathan , Hong (Helen) Fan , Michael F. Tweedle , Rolf E. Swenson
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： C07D405/12 , A61K51/12
摘要： The invention provides radiopharmaceuticals for diagnostic and therapeutic applications, conjugates of antioxidants with metal chelating ligands, intermediate compounds, methods of making such radiopharmaceuticals, ligands, and intermediate compounds, and kits for preparing the radiopharmaceutical complexes.
摘要翻译：本发明提供用于诊断和治疗应用的放射性药物，抗氧化剂与金属螯合配体的缀合物，中间体化合物，制备这种放射性药物的方法，配体和中间体化合物，以及用于制备放射性药物复合物的试剂盒。

45. 发明授权

US09333272B2 Fibrin binding peptide conjugates for diagnostic and therapeutic applications 有权
标题翻译：用于诊断和治疗应用的纤维蛋白结合肽缀合物
公开(公告)号：US09333272B2
公开(公告)日：2016-05-10
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： A61K38/36 , A61K49/14 , A61K49/00 , A61K49/08 , A61K49/12 , C07K7/06 , G01N33/532 , G01N33/574 , G01N33/86
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。

46. 发明申请

US20100202967A1 FIBRIN BINDING PEPETIDE CONJUGATES FOR DIAGNOSTIC AND THERAPEUTIC APPLICATIONS 有权
标题翻译：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。

47. 发明授权

US08105567B2 Multidentate AZA ligands able to complex metal ions and the use thereof in diagnostics and therapy 有权
标题翻译：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
申请人： Kondareddiar Ramalingam , Rolf E. Swenson
发明人： Kondareddiar Ramalingam , Rolf E. Swenson
IPC分类号： A61K51/00 , A61M36/14
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。

48. 发明申请

US20110280802A1 Linkers For Radiopharmaceutical Compounds 审中-公开
标题翻译：放射性药物化合物的接头
公开(公告)号：US20110280802A1
公开(公告)日：2011-11-17
申请号：US13179035
申请日：2011-07-08
申请人： Christoph De Haen , Adrian D. Nunn , Rolf E. Swenson
发明人： Christoph De Haen , Adrian D. Nunn , Rolf E. Swenson
IPC分类号： A61K51/00 , C07K14/62 , C07K7/06 , C07D207/46 , C07D257/02 , C12N9/96 , C07K14/00
CPC分类号： A61K51/0493 , A61K47/64 , A61K51/088 , C07J41/00 , C07K7/23 , C07K14/62
摘要： A new and improved method for extending the half life of pharmaceutical compounds for use in diagnostic imaging or therapy uses a novel linker to attach a diagnostic or therapeutic moiety to a targeting peptide or another diagnostic or therapeutic moiety. The resulting compound may have the general formula M-N—O—P-Q, wherein M is the diagnostic or therapeutic moiety, N—O—P is the linker of the present invention, and Q is the targeting peptide. In another embodiment the compounds may have the formula M-N—O—P-M, wherein M is independently a diagnostic or therapeutic moiety and N—O—P is the linker of the invention. Methods for imaging or treating a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound are further provided. Methods for radiotherapy of a patient using the compounds are further provided, as are methods for preparing a radiotherapeutic agent from the compounds.
摘要翻译：用于延长用于诊断成像或治疗的药物化合物的半衰期的新的和改进的方法使用新的接头将诊断或治疗部分附着于靶向肽或另一诊断或治疗部分。所得化合物可具有通式M-N-O-P-Q，其中M为诊断或治疗部分，N-O-P为本发明的接头，Q为靶向肽。在另一个实施方案中，化合物可以具有式M-N-O-P-M，其中M独立地是诊断或治疗性部分，N-O-P是本发明的接头。还提供了使用本发明化合物对患者进行成像或治疗的方法。还提供了用于从化合物制备诊断显像剂的方法和试剂盒。还提供了使用该化合物的患者放射治疗的方法，以及从化合物制备放射治疗剂的方法。

49. 发明申请

US20100312039A1 INFUSION SYSTEM CONFIGURATIONS 有权
标题翻译：灌注系统配置
公开(公告)号：US20100312039A1
公开(公告)日：2010-12-09
申请号：US12865924
申请日：2009-06-11
申请人： Charles R. Quirico , Ernest Balestracci , Rolf E. Swenson , Daniel D. Darst , Eric J. Krause , Vishal N. Lokhande , Jacob S. Childs
发明人： Charles R. Quirico , Ernest Balestracci , Rolf E. Swenson , Daniel D. Darst , Eric J. Krause , Vishal N. Lokhande , Jacob S. Childs
IPC分类号： A61M36/00
CPC分类号： A61M5/007 , A61B6/037 , A61B6/107 , A61B6/481 , A61B6/507 , A61B50/13 , A61B90/39 , A61B2050/105 , A61B2090/392 , A61K51/00 , A61M5/14 , A61M5/1409 , A61M5/142 , A61M5/1452 , A61M5/158 , A61M5/16854 , A61M5/16881 , A61M5/365 , A61M2005/1403 , A61M2205/18 , A61M2205/276 , A61M2205/3375 , A61M2205/50 , A61M2205/505 , A61M2205/52 , A61M2205/584 , A61M2205/587 , A61M2205/6009 , A61M2205/6054 , A61M2205/6072 , A61M2205/70 , A61M2205/75 , A61M2209/084 , A61N5/1001 , A61N5/1007 , A61N5/1075 , A61N2005/1021 , A61N2005/1022 , A61N2005/1074 , A61N2005/1094 , B62B3/005 , G06F19/00 , G06F19/3468 , G06F21/31 , G21F3/00 , G21F7/00 , G21G1/0005 , G21G1/001 , G21G4/08 , G21G2001/0031
摘要： Infusion system configurations and assemblies facilitate routing of infusion circuit tubing lines. Tubing lines are routed into and out from compartments of a shielding assembly for the infusion system, at locations which prevent kinking and/or crushing of the lines, and/or provide for ease in assembling the circuit. A plurality of the lines may be held together by a support frame to form a disposable infusion circuit subassembly, that can further facilitate routing of the lines.
摘要翻译：输液系统配置和组件便于输注电路管线的布线。在防止线路扭结和/或破碎的位置处和/或为组装电路提供便利的位置，将管道线路输入和输出用于输注系统的屏蔽组件的隔间。多个线可以由支撑框架保持在一起以形成一次性输注电路子组件，其可以进一步促进线路的布线。

50. 发明授权

US06355490B1 Attached tags for use in combinatorial chemistry synthesis 失效
标题翻译：用于组合化学合成的附加标签
公开(公告)号：US06355490B1
公开(公告)日：2002-03-12
申请号：US08923206
申请日：1997-09-04
申请人： Jill Edie Hochlowski , Thomas J. Sowin , Daniel W. Norbeck , Anne-Laure Marie Grillot , Rolf E. Swenson
发明人： Jill Edie Hochlowski , Thomas J. Sowin , Daniel W. Norbeck , Anne-Laure Marie Grillot , Rolf E. Swenson
IPC分类号： G01N33543
CPC分类号： C40B50/16 , B01J2219/005 , B01J2219/00572 , B01J2219/0059 , B01J2219/00592 , B01J2219/00596 , B01J2219/0072 , C07B2200/11 , C40B70/00 , Y10T436/13
摘要： The present invention relates to a process of coding and identifying individual members of a chemical combinatorial library synthesized on a plurality of solid supports which undergo mix and split synthesis. The process provides for tagging the solid supports with a coding identifier that is attached to the solid support and which can be decoded by infrared or raman spectroscopy when directly attached to the support.
摘要翻译：本发明涉及编码和鉴定在经历混合和分裂合成的多个固体支持物上合成的化学组合文库的各个成员的方法。该过程提供了用固定支持物附接的编码标识符来标记固体支持物，并且当直接连接到支持物时可以通过红外或拉曼光谱进行解码。

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