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    Cytotoxic metal chelators and methods for making and using same
    2.
    发明授权
    Cytotoxic metal chelators and methods for making and using same 有权
    细胞毒性金属螯合剂及其制备和使用方法

    公开(公告)号：US06589966B1

    公开(公告)日：2003-07-08

    申请号：US09646428

    申请日：2000-09-18

    申请人： Suzy V. Torti ,  Frank M. Torti ,  Roy P. Planalp ,  Martin W. Brechbiel

    发明人： Suzy V. Torti ,  Frank M. Torti ,  Roy P. Planalp ,  Martin W. Brechbiel

    IPC分类号： A61K3144

    CPC分类号： C07D213/53 ,  C07C211/36 ,  C07C2601/14 ,  C07D213/38 ,  C07D215/12 ,  C07D233/64

    摘要： A family of hexadentate Fe(II) chelators having marked antiproliferative activity against tumor cells is disclosed. The cytotoxic metal chelators and complexes of the present invention are represented by the general formula below: wherein: X1, X3, and X5 are N, O or S, wherein the X1, X3, and X5 atoms are at the 1, 3, and 5 positions of a cyclohexyl group and are in a cis, cis disposition; B, B′, and B″ are aliphatic, branched aliphatic, or aryl groups, or any combination thereof, wherein the number of atoms between X and Y is about 2 to about 4; Y, Y′ and Y″ contain N, O, or S atoms that originate from either aliphatic, branched aliphatic, aryl, or heterocyclic groups, or any combination thereof, and/or Y, Y′ and Y″ are NH2 or NHR, OH, or SH, CO2H, P(O)(OH)2, RP(O)OH, ROP(O)OH groups or a combination thereof, and R is H, aliphatic, branched aliphatic, or aryl groups, or any combination thereof that may or may not be identical in Y, Y′ and Y″; s, s′, and s″ are 0 to about 2; and t, t′, and t″ are 0 to about 2. Application of the metal chelators of the present invention as chemotherapeutic agents is also disclosed.

    摘要翻译： 公开了一种对肿瘤细胞具有显着的抗增殖活性的六价铁（II）螯合剂族。 本发明的细胞毒性金属螯合剂和络合物由以下通式表示：其中：X 1，X 3和X 5为N，O或S，其中X 1，X 3和X 5原子为1,3和 环己基的5个位置为顺式，顺式配置; B，B'和B“为脂族，支链脂族或芳基，或其任何组合，其中X和Y之间的原子数约为 2至约4; Y，Y'和Y“含有源自脂族，支链脂族，芳基或杂环基团的N，O或S原子，或其任何组合，和/或Y，Y'和Y NH 2或NHR，OH或SH，CO 2 H，P（O）（OH）2，RP（O）OH，ROP（O）OH基团或其组合，R为H，脂族，支链脂族， 或芳基，或它们在Y，Y'和Y“中可以相同也可以不相同的任何组合; s，s'和s”为0至约2; andt，t'和t“为0至约2.本发明的金属螯合剂作为化学治疗剂的应用也被公开。

    Methods for functional kidney imaging using small dendrimer contrast agents
    4.
    发明授权
    Methods for functional kidney imaging using small dendrimer contrast agents 失效
    使用小树状大分子造影剂的功能性肾脏成像方法

    公开(公告)号：US06852842B2

    公开(公告)日：2005-02-08

    申请号：US10229316

    申请日：2002-08-26

    申请人： Martin W. Brechbiel ,  Robert A. Star ,  Hisataka Kobayashi

    发明人： Martin W. Brechbiel ,  Robert A. Star ,  Hisataka Kobayashi

    IPC分类号： A61K49/08 ,  A61K49/12 ,  A61K49/18 ,  A61K51/12 ,  C07F5/00

    CPC分类号： A61K49/124 ,  A61K51/065 ,  B82Y5/00

    摘要： Small dendrimer-based MRI contrast agents are disclosed to accumulate in renal tubules. The accumulation enables visualization of renal structure and function, permitting assessment of structural and functional damage to the kidneys. In a disclosed embodiment, six, small dendrimer-based MRI contrast agents were synthesized, and their pharmacokinetics, whole body retention, and renal MRI images were evaluated in mice. Surprisingly, despite having unequal renal clearance properties, all of the dendrimer agents clearly visualized the renal anatomy and proximal straight tubules of the mice better than Gd-[DTPA]-dimeglumine. Dendrimer conjugate contrast agents prepared from PAMAM-G2D, DAB-G3D, and DAB-G2D dendrimers were excreted rapidly and may be acceptable for use in clinical applications.

    摘要翻译： 公开了基于树枝状大分子的MRI造影剂以积累在肾小管中。 累积能够显示肾结构和功能，允许评估肾脏的结构和功能损伤。 在公开的实施方案中，合成了6种基于小树枝状大分子的MRI造影剂，并在小鼠中评估了它们的药代动力学，全身保留和肾脏MRI图像。 令人惊讶的是，尽管具有不均匀的肾清除性质，但是所有的树枝状大分子试剂比Gd- [DTPA] - 葡甲胺清楚地显现了小鼠的肾解剖结构和近端直管。 从PAMAM-G2D，DAB-G3D和DAB-G2D树枝状大分子制备的树枝状共聚物造影剂被快速排泄，并且可用于临床应用。

    METHOD OF PREPARING MACROMOLECULAR CONTRAST AGENTS AND USES THEREOF
    7.
    发明申请
    METHOD OF PREPARING MACROMOLECULAR CONTRAST AGENTS AND USES THEREOF 有权
    制备大分子对比剂的方法及其用途

    公开(公告)号：US20100056776A1

    公开(公告)日：2010-03-04

    申请号：US12513813

    申请日：2007-11-06

    申请人： Martin W. Brechbiel ,  Heng Xu

    发明人： Martin W. Brechbiel ,  Heng Xu

    IPC分类号： C07D403/12 ,  C07C229/00 ,  C07D207/46 ,  C07D207/40 ,  C07D257/02

    CPC分类号： A61K51/065 ,  A61K47/59 ,  A61K47/595 ,  A61K49/085 ,  A61K49/124

    摘要： Disclosed are methods of preparing a macromolecular conjugated ligand and a metal complex thereof. The metal complex is targeted for use as a contrast agent, for example, in MRI. The method of preparing a macromolecular conjugated ligand comprises: (a) providing a compound of formula (I) wherein R, A, and Pg are as defined herein, (b) reacting the compound of formula (I) with a macromolecular compound (e.g., dendrimer) in an organic solvent medium which is substantially free of water to obtain a macromolecular conjugated compound, and (c) removing the carboxyl-protecting groups to obtain a carboxyl-deprotected macromolecular conjugated compound. The metal complex can be prepared by reacting the carboxyl-deprotected macromolecular conjugated compound with an ion (e.g., Gd(III)). Also disclosed are two carboxyl-protected 1B4M-DTPA intermediate compounds.

    摘要翻译： 公开了制备大分子共轭配体及其金属络合物的方法。 金属络合物被靶向用作造影剂，例如在MRI中。 制备大分子缀合配体的方法包括：（a）提供其中R，A和Pg如本文所定义的式（I）化合物，（b）使式（I）化合物与高分子化合物 树枝状大分子）在基本上不含水的有机溶剂介质中，得到高分子共轭化合物，（c）除去羧基保护基，得到羧基脱保护的高分子共轭化合物。 金属络合物可以通过羧基脱保护的大分子共轭化合物与离子（例如Gd（III））反应来制备。 还公开了两种羧基保护的1B4M-DTPA中间体化合物。

    Method of preparing macromolecular contrast agents and uses thereof
    10.
    发明授权
    Method of preparing macromolecular contrast agents and uses thereof 有权
    制备大分子造影剂的方法及其应用

    公开(公告)号：US08288530B2

    公开(公告)日：2012-10-16

    申请号：US12513813

    申请日：2007-11-06

    申请人： Martin W. Brechbiel ,  Heng Xu

    发明人： Martin W. Brechbiel ,  Heng Xu

    IPC分类号： C07D403/12 ,  C07D207/46 ,  C07D207/40 ,  C07D257/02 ,  C07C229/00

    CPC分类号： A61K51/065 ,  A61K47/59 ,  A61K47/595 ,  A61K49/085 ,  A61K49/124

    摘要： Disclosed are methods of preparing a macromolecular conjugated ligand and a metal complex thereof. The metal complex is targeted for use as a contrast agent, for example, in MRI. The method of preparing a macromolecular conjugated ligand comprises: (a) providing a compound of formula (I) wherein R, A, and Pg are as defined herein, (b) reacting the compound of formula (I) with a macromolecular compound (e.g., dendrimer) in an organic solvent medium which is substantially free of water to obtain a macromolecular conjugated compound, and (c) removing the carboxyl-protecting groups to obtain a carboxyl-deprotected macromolecular conjugated compound. The metal complex can be prepared by reacting the carboxyl-deprotected macromolecular conjugated compound with an ion (e.g., Gd(III)). Also disclosed are two carboxyl-protected 1B4M-DTPA intermediate compounds.

    摘要翻译： 公开了制备大分子共轭配体及其金属络合物的方法。 金属络合物被靶向用作造影剂，例如在MRI中。 制备大分子缀合配体的方法包括：（a）提供其中R，A和Pg如本文所定义的式（I）化合物，（b）使式（I）化合物与高分子化合物 树枝状大分子）在基本上不含水的有机溶剂介质中，得到高分子共轭化合物，（c）除去羧基保护基，得到羧基脱保护的高分子共轭化合物。 金属络合物可以通过羧基脱保护的大分子共轭化合物与离子（例如Gd（III））反应来制备。 还公开了两种羧基保护的1B4M-DTPA中间体化合物。