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公开(公告)号：US06958141B2
公开(公告)日：2005-10-25
申请号：US10742348
申请日：2003-12-19
申请人： Karen Linder , Adrian D. Nunn , David P. Nowotnik , Kondareddiar Ramalingam , Richard J. DiRocco , William L. Rumsey , John P. Pirro
发明人： Karen Linder , Adrian D. Nunn , David P. Nowotnik , Kondareddiar Ramalingam , Richard J. DiRocco , William L. Rumsey , John P. Pirro
IPC分类号： A61K51/04 , C07C251/38 , A61K49/00
CPC分类号： C07C251/38 , A61K51/0478 , A61K51/0497 , A61K2123/00
摘要： Novel methods, processes and metal complexes attached to a hypoxia-localizing moiety comprisinga metal, preferably radionuclide of rhenium or technetium;a hypoxia-localizing moiety; and,a complexing ligand, wherein said ligand and said radionuclide combined have cell membrane permeabilities greater than that of sucrose, are disclosed.
摘要翻译： 附着于低氧定位部分的新型方法，方法和金属络合物，其包含金属，优选铼或锝的放射性核素; 缺氧定位部分; 并且公开了其中所述配体和所述放射性核素组合的络合配体具有大于蔗糖的细胞膜渗透性。
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62.发明申请CHELATION OF METALS TO THIOL GROUPS USING IN SITU REDUCTION OF DISULFIDE-CONTAINING COMPOUNDS BY PHOSPHINES 审中-公开通过磷酸盐还原含有崩解剂的化合物将金属螯合到硫醇组合公开(公告)号：US20120178906A1
公开(公告)日：2012-07-12
申请号：US13423751
申请日：2012-03-19
IPC分类号： C07K2/00
CPC分类号： A61K51/088
摘要： A method is disclosed for the syntheses of thiol-containing radiopharmaceuticals without the need for purification starting from chelators containing disulfide bonds. This is done by providing a method that reduces disulfide bonds on a precursor molecule or a precursor compound in the presence of phosphine compounds, thus freeing thiols for metal complexation.
摘要翻译： 公开了用于合成含硫醇的放射性药物的方法，而不需要从含有二硫键的螯合剂开始纯化。 这通过提供在膦化合物存在下还原前体分子或前体化合物上的二硫键的方法来实现，从而释放硫醇以进行金属络合。
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63.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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64.发明授权Methods of synthesizing heteroatom-bearing ligands and intermediate used thereof 失效合成含杂原子的配体的方法及其使用的中间体公开(公告)号：US06384232B1
公开(公告)日：2002-05-07
申请号：US09818301
申请日：2001-03-27
IPC分类号： C07D23391
CPC分类号： C07D403/14 , C07D233/91
摘要： The invention provides improved and simplified methods of synthesizing ligands containing a heteroatom-bearing bridge using a novel intermediate compound. The ligands may be used to form metal complexes that are useful in diagnostic and therapeutic applications.
摘要翻译： 本发明提供了使用新型中间体化合物合成含有带杂原子的桥的配体的改进和简化的方法。 配体可用于形成可用于诊断和治疗应用的金属络合物。
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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。
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66.发明申请Multidentate AZA Ligands Able to Complex Metal Ions And The Use Thereof In Diagnostics And Therapy 有权多齿AZA配体能够复杂的金属离子及其在诊断和治疗中的应用公开(公告)号：US20100069628A1
公开(公告)日：2010-03-18
申请号：US12553421
申请日：2009-09-03
IPC分类号： C07D243/08
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; andR′ 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, 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，113In ，90°，97Ru，62Cu，64Cu，52Fe，52mM，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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67.发明申请CHELATION OF METALS TO THIOL GROUPS USING IN SITU REDUCTION OF DISULFIDE-CONTAINING COMPOUNDS BY PHOSPHINES 审中-公开通过磷酸盐还原含有崩解剂的化合物将金属螯合到硫醇组合公开(公告)号：US20090062509A1
公开(公告)日：2009-03-05
申请号：US12282766
申请日：2007-03-14
CPC分类号： A61K51/088
摘要： A method is disclosed for the syntheses of thiol-containing radiopharmaceuticals without the need for purification starting from chelators containing disulfide bonds. This is done by providing a method that reduces disulfide bonds on a precursor molecule or a precursor compound in the presence of phosphine compounds, thus freeing thiols for metal complexation.
摘要翻译： 公开了用于合成含硫醇的放射性药物的方法，而不需要从含有二硫键的螯合剂开始纯化。 这通过提供在膦化合物存在下还原前体分子或前体化合物上的二硫键的方法来实现，从而释放硫醇以进行金属络合。
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68.发明授权Boronic acid adducts of metal dioxime complexes useful in labelling proteins and other amine-containing compounds 失效金属二氧化钛复合物的标记蛋白和其他含氨化合物有用的硼酸添加剂
公开(公告)号：US5183653A
公开(公告)日：1993-02-02
申请号：US508433
申请日：1990-04-13
CPC分类号： C07F13/005 , A61K47/48707 , A61K51/0478 , A61K51/1093 , A61K2121/00 , A61K2123/00
摘要： Boronic acid adducts of metal dioxime complexes are useful as reagents for labeling proteins and other amine-containing compounds.
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公开(公告)号：US07422733B2
公开(公告)日：2008-09-09
申请号：US10432914
申请日：2001-11-29
申请人： Ramachandran Ranganathan , Kondareddiar Ramalingam , Radhakrishua Pillai , Edmund E. Marinelli , Rolf E. Swenson
发明人： Ramachandran Ranganathan , Kondareddiar Ramalingam , Radhakrishua Pillai , Edmund E. Marinelli , Rolf E. Swenson
IPC分类号： A61B8/00 , A61B8/13 , A61K31/702 , A61K9/127
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： 本文公开的是一类可连接的四糖化合物，其包括唾液酸基路易斯X（SLE）X的氨基苯基糖苷和相关的类似物。 这些化合物具有可共轭的亲核基团，使得它们可用于制备多聚体SLeX组合物。 特别地，所公开的SLex X化合物可用于通过将选择素结合配体缀合物连接到报道部分如造影剂，放射性诊断剂或细胞毒性或化学治疗剂来制备选择素结合配体缀合物。 本发明的SLe <！ - SIPO
- >化合物和缀合物显示出与天然唾液酸酯类似的选择蛋白结合，因此可用于诊断和治疗选择素介导的病症 和相关条件。 -
70.发明授权Targeting and therapeutic compounds and gas-filled microvesicles comprising said compounds 有权靶向和治疗化合物和包含所述化合物的充气微泡公开(公告)号：US08293214B2
公开(公告)日：2012-10-23
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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