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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。

    Five member ring sulfenate esters and thiosulfinate esters
    3.
    发明授权
    Five member ring sulfenate esters and thiosulfinate esters 有权
    五元环次硫酸酯和硫代亚磺酸酯

    公开(公告)号：US06242478B1

    公开(公告)日：2001-06-05

    申请号：US09459261

    申请日：1999-12-10

    申请人： Mark E. Welker ,  Suzy V. Torti ,  Frank M. Torti ,  Alan J. Townsend ,  Eva Pietsch ,  Allison L. Hurley

    发明人： Mark E. Welker ,  Suzy V. Torti ,  Frank M. Torti ,  Alan J. Townsend ,  Eva Pietsch ,  Allison L. Hurley

    IPC分类号： A61K31385

    CPC分类号： C07D327/04 ,  A61K31/385 ,  A61K31/39 ,  C07D339/04

    摘要： Disclosed are novel sulfenate esters and thiosulfinate esters that induce the expression of metabolic enzymes, particularly Phase II enzymes such as glutathione-s-transferase, DT-diaphorase and Ferritin H when administered to a subject. Also disclosed, such compounds are effective to displace a zinc ion from retroviral zinc finger nucleocapsid proteins effective to inhibit HIV replication. The present invention is further directed to novel methods of making these compounds, and any compounds produced by the process of making these novel compounds.

    摘要翻译： 公开了当施用于受试者时，诱导代谢酶，特别是II期酶如谷胱甘肽-S-转移酶，DT-心肌黄酶和铁蛋白H的新型次磺酸酯和硫代亚磺酸酯。 还公开了这样的化合物有效地置换有效抑制HIV复制的逆转录病毒锌指核衣壳蛋白的锌离子。 本发明还涉及制备这些化合物的新方法，以及通过制备这些新化合物的方法制备的任何化合物。