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    Bifunctional chelating agent for the design and development of site specific radiopharmaceuticals and biomolecule conjugation strategy
    1.
    发明授权
    Bifunctional chelating agent for the design and development of site specific radiopharmaceuticals and biomolecule conjugation strategy 失效
    双功能螯合剂用于设计和开发位点特异性放射性药物和生物分子共轭策略

    公开(公告)号：US06635235B1

    公开(公告)日：2003-10-21

    申请号：US09602487

    申请日：2000-06-23

    申请人： Kattesh V. Katti ,  Kandikere R. Prabhu ,  Hariprasad Gali ,  Nagavara Kishore Pillarsetty ,  Wynn A. Volkert

    发明人： Kattesh V. Katti ,  Kandikere R. Prabhu ,  Hariprasad Gali ,  Nagavara Kishore Pillarsetty ,  Wynn A. Volkert

    IPC分类号： A61K5100

    CPC分类号： A61K49/0002 ,  A61K51/0478

    摘要： There is provided a method of labeling a biomolecule with a transition metal or radiometal in a site specific manner to produce a diagnostic or therapeutic pharmaceutical compound by synthesizing a P2N2-bifunctional chelating agent intermediate, complexing the intermediate with a radio metal or a transition metal, and covalently linking the resulting metal-complexed bifunctional chelating agent with a biomolecule in a site specific manner. Also provided is a method of synthesizing the —PR2 containing biomolecules by synthesizing a P2N2-bifunctional chelating agent intermediate, complexing the intermediate with a radiometal or a transition metal, and covalently linking the resulting radio metal-complexed bifunctional chelating agent with a biomolecule in a site specific manner. There is provided a therapeutic or diagnostic agent comprising a —PR2 containing biomolecule.

    摘要翻译： 提供了以特异性方式用过渡金属或放射性金属标记生物分子的方法，以通过合成P2N2-双功能螯合剂中间体，将中间体与放射性金属或过渡金属络合来制备诊断或治疗药物化合物， 并以特异性方式将所得的金属络合的双功能螯合剂与生物分子共价连接。 还提供了通过合成P2N2-双功能螯合剂中间体，使中间体与放射性金属或过渡金属络合，并将所得的放射性金属络合的双功能螯合剂与生物分子共价连接的方法来合成含有-PPR的生物分子的方法 现场具体方式。 提供包含含有-PR2的生物分子的治疗或诊断剂。

    Gold-containing chemotherapeutic agents
    2.
    发明授权
    Gold-containing chemotherapeutic agents 失效
    含金化学治疗剂

    公开(公告)号：US06989158B1

    公开(公告)日：2006-01-24

    申请号：US10019192

    申请日：2000-06-23

    申请人： Kattesh V. Katti ,  Wynn A. Volkert ,  Timothy Hoffman

    发明人： Kattesh V. Katti ,  Wynn A. Volkert ,  Timothy Hoffman

    IPC分类号： A61K31/28 ,  A61K33/24

    CPC分类号： A61K31/28

    摘要： There is provided a complex for use as a therapeutic pharmaceutical, the complex has a ligand containing at least one hydroxyalkyl phosphine donor group bound to a gold atom to form a stable gold-ligand complex. Also provided is a method of treating cancer by administering an effective amount of a complex having a ligand of at least one hydroxyalkyl phosphine group bound to a gold atom to form a stable gold-ligand complex. Also provided is a method of preventing the metastasis of cancer and arresting cell growth by administering an effective amount of a complex having a ligand of at least one hydroxyalkyl phosphine group bound to a gold atom to form a stable gold-ligand complex.

    摘要翻译： 提供了用作治疗药物的复合物，该配合物具有含有至少一个与金原子结合的羟烷基膦供体基团以形成稳定的金 - 配体络合物的配体。 还提供了通过施用有效量的具有与金原子结合的至少一个羟基烷基膦基团的配体的络合物以形成稳定的金 - 配体络合物来治疗癌症的方法。 还提供了通过施用有效量的具有与金原子结合的至少一个羟烷基膦基配体的配合物以形成稳定的金 - 配体络合物的方法来防止癌症转移和阻止细胞生长的方法。

    Method for treating liquid wastes
    7.
    发明授权
    Method for treating liquid wastes 失效
    液体废物处理方法

    公开(公告)号：US5478474A

    公开(公告)日：1995-12-26

    申请号：US165373

    申请日：1993-12-10

    申请人： Kattesh V. Katti ,  Wynn A. Volkert ,  Prahlad Singh ,  Alan R. Ketring

    发明人： Kattesh V. Katti ,  Wynn A. Volkert ,  Prahlad Singh ,  Alan R. Ketring

    IPC分类号： B01D15/08 ,  C22B3/20 ,  G21C19/46 ,  G21F9/12

    CPC分类号： G21F9/12 ,  C22B3/205 ,  C22B3/42 ,  G21C19/46 ,  Y02P10/234 ,  Y02W30/883

    摘要： The method of treating liquid waste in a media is accomplished by exposing the media to phosphinimines and sequestering .sup.99 Tc from the media by the phosphinimine (PN) functionalities. The system for treating the liquid waste in the media includes extraction of .sup.99 TcO.sub.4.sup.- from aqueous solutions into organic solvents or mixed organic/polar media, extraction of .sup.99 Tc from solutions on a solid matrix by using a container containing PN functionalities on solid matrices including an inlet and outlet for allowing flow of media through an immobilized phosphinimine ligand system contained within the container. Also, insoluble suspensions of phosphinimine functionalities on solid matrices in liquid solutions or present on supported liquid membranes (SLM) can be used to sequester .sup.99 Tc from those liquids.

    摘要翻译： 通过将介质暴露于次膦酰亚胺并通过膦亚胺（PN）官能团从介质中螯合99Tc来实现处理介质中废液的方法。 用于处理介质中的液体废物的系统包括将99TcO4-从水溶液中萃取到有机溶剂或混合有机/极性介质中，通过使用在包括入口的固体基质上含有PN官能团的容器从固体基质上的溶液中提取99Tc 和用于允许介质流过包含在容器内的固定化膦酰亚胺配体系统的出口。 此外，膦酰亚胺功能性在液体溶液中固体基质上的不溶性悬浮液或存在于载体液膜（SLM）上的不溶性悬浮液可用于从这些液体中螯合99Tc。

    Biomolecule conjugation strategy using novel water-soluble phosphine-based chelating agents
    10.
    发明授权
    Biomolecule conjugation strategy using novel water-soluble phosphine-based chelating agents 失效
    使用新型水溶性膦类螯合剂的生物分子结合策略

    公开(公告)号：US06780397B2

    公开(公告)日：2004-08-24

    申请号：US09386657

    申请日：1999-08-31

    申请人： Kattesh V. Katti ,  Hariprasad Gali ,  Wynn A. Volkert

    发明人： Kattesh V. Katti ,  Hariprasad Gali ,  Wynn A. Volkert

    IPC分类号： A61K4900

    CPC分类号： A61K51/0497 ,  A61K49/0002 ,  A61K51/0478 ,  A61K51/0489

    摘要： This invention describes a novel strategy to produce phosphine-functionalized biomolecules (e.g. peptides or proteins) for potential use in the design and development of site-specific radiopharmaceuticals for diagnosis or therapy of specific cancers. Hydrophilic alkyl phosphines, in general, tend to be oxidatively unstable. Therefore, incorporation of such phosphine functionalities on peptide (and other biomolecule) backbones, without oxidizing the PIII centers, is difficult. In this context this discovery reports on a new technology by which phosphines, in the form of bifunctional chelating agents, can be directly incorporated on biomolecular backbones using manual synthetic or solid phase peptide synthesis methodologies. The superior ligating abilities of phosphine ligands, with various diagnostically (e.g. TC-99m) or therapeutically (e.g. Re186/188, Rh-105, Au-199) useful radiometals, coupled with the findings that the resulting complexes demonstrate high in vivo stability makes this approach useful in the development of radiolabeled biomolecules for applications in the design of tumor-specific radiopharmaceuticals.

    摘要翻译： 本发明描述了一种新颖的制备磷酸化官能化生物分子（例如肽或蛋白质）的策略，用于设计和开发用于诊断或治疗特定癌症的位点特异性放射性药物。 亲水性烷基膦通常趋于氧化不稳定。 因此，难以在肽（和其他生物分子）骨架上引入磷化氢功能而不氧化P III族中心。 在这方面，这一发现报道了一种新技术，通过这种新技术，双功能螯合剂形式的膦可以使用手工合成或固相肽合成方法直接掺入到生物分子骨架上。 膦配体的各种诊断（例如TC-99m）或治疗性（例如Re186 / 188，Rh-105，Au-199）有用的放射性金属的优异的结合能力与所得复合物表现出高的体内稳定性的发现相结合 这种方法在开发用于设计肿瘤特异性放射性药物的放射性标记的生物分子中是有用的。