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    RADIOMETAL-BINDING PEPTIDE ANALOGUES
    1.
    发明申请
    RADIOMETAL-BINDING PEPTIDE ANALOGUES 审中-公开
    放射性配体肽类似物

    公开(公告)号：WO1998002192A1

    公开(公告)日：1998-01-22

    申请号：PCT/US1997012084

    申请日：1997-07-11

    Applicant: IMMUNOMEDICS, INC. ,  McBRIDE, William, J. ,  GRIFFITHS, Gary, L.

    Inventor： IMMUNOMEDICS, INC.

    IPC: A61K51/08

    CPC classification number: A61K51/088 ,  A61K51/083 ,  A61K2123/00

    Abstract: Novel metal binding ligands are disclosed that may be coupled to peptides for use in methods of diagnosis and therapy. Peptides containing the ligands are produced using a method wherein ligand introduction or cyclization can be conducted at any point during the synthesis of the peptide. Such peptide derivatives are readily labeled with radiometals, such as isotopes of rhenium or technetium, while retaining their ability to tightly bind specific peptide receptors.

    Abstract translation: 公开了新颖的金属结合配体，其可以与肽偶联用于诊断和治疗方法。 使用其中配体引入或环化可以在肽合成期间的任何点进行的方法产生含有配体的肽。 这样的肽衍生物容易用放射性金属元素（如铼或锝的同位素）进行标记，同时保留其紧密结合特异性肽受体的能力。

    MASS SPECTROMETRY AND X-RAY CRYSTALLIZATION ANALYSIS OF BIOLOGICAL MATERIAL VIA SOLID PHASE SUPPORT
    2.
    发明申请
    MASS SPECTROMETRY AND X-RAY CRYSTALLIZATION ANALYSIS OF BIOLOGICAL MATERIAL VIA SOLID PHASE SUPPORT 审中-公开
    通过固体相支持的生物材料的质谱分析和X射线晶体结构分析

    公开(公告)号：WO1997040384A1

    公开(公告)日：1997-10-30

    申请号：PCT/US1997005839

    申请日：1997-04-22

    Applicant: IMMUNOMEDICS, INC. ,  McBRIDE, William, J.

    Inventor： IMMUNOMEDICS, INC.

    IPC: G01N33/543

    CPC classification number: H01J49/0418 ,  G01N23/20 ,  G01N33/54373

    Abstract: A support material is conjugated to an affinity material to produce an affinity matrix. The affinity matrix is contacted with a biological sample containing a receptor so that the receptor specifically binds to the affinity material portion of the affinity matrix. Unbound portions of the biological sample are removed, and the receptor specifically bound to the affinity matrix is analyzed by mass spectrometry, optionally with recovery of the receptor or receptor-affinity material complex for mass spectrometry analysis and recovery of the receptor for X-ray crystallographic analysis.

    Abstract translation: 支撑材料与亲和材料缀合以产生亲和基质。 亲和基质与含有受体的生物样品接触，使得受体特异性结合亲和基质的亲和材料部分。 去除生物样品的未结合部分，并通过质谱法分析特异性结合亲和基质的受体，任选地回收受体或受体亲和性材料配合物进行质谱分析并回收X射线晶体学受体 分析。

    METHODS FOR TECHNETIUM/RHENIUM LABELLING OF PROTEINS
    5.
    发明申请
    METHODS FOR TECHNETIUM/RHENIUM LABELLING OF PROTEINS 审中-公开
    蛋白质/旭硝子标记方法

    公开(公告)号：WO1990015626A1

    公开(公告)日：1990-12-27

    申请号：PCT/US1990003142

    申请日：1990-06-11

    Applicant: IMMUNOMEDICS, INC.

    Inventor： IMMUNOMEDICS, INC. ,  GRIFFITHS, Gary, L.

    IPC: A61K43/00

    CPC classification number: A61K51/1018 ,  A61K51/1048 ,  A61K2123/00 ,  Y10S435/975 ,  Y10S436/804

    Abstract: A method for radiolabelling a protein with a radioisotope of technetium or rhenium comprises the steps of contacting a solution of a protein comprising a plurality of adjacent free sulfhydryl groups, or in particular cases, intact protein containing at least one disulfide group, with stannous ions, and then with radiopertechnetate or radioperrhenate, the amount of stannous ion being sufficient to substantially completely reduce the radiopertechnetate or radioperrhenate, and recovering radiolabelled protein. Methods of imaging and methods of radiotherapy employing radiolabelled proteins produced by this method are also disclosed, as are kits for radiolabelling antibodies and antibody fragments.

    STABLE RADIOIODINE CONJUGATES AND METHODS FOR THEIR SYNTHESIS
    6.
    发明申请
    STABLE RADIOIODINE CONJUGATES AND METHODS FOR THEIR SYNTHESIS 审中-公开
    稳定的放射性素结合物及其合成方法

    公开(公告)号：WO1999011294A1

    公开(公告)日：1999-03-11

    申请号：PCT/US1997023711

    申请日：1997-12-19

    Applicant: IMMUNOMEDICS, INC. ,  GOVINDAN, Serengulam, V. ,  GRIFFITHS, Gary, L.

    Inventor： IMMUNOMEDICS, INC.

    IPC: A61K51/04

    CPC classification number: A61K51/0491 ,  A61K51/088 ,  A61K51/10 ,  A61K51/1093 ,  C07H3/04 ,  C07K1/1077 ,  G01N33/543

    Abstract: Methods are described for conjugating radioiodinated peptides or carbohydrate structures to proteins with improved yields and qualities of conjugates. In one method, specially designed radioiodinated bifunctional peptides containing nonmetabolizable bonds such as amide bonds are coupled to cell targeting protein. In a second method, radioiodinated nonmetabolizable bifunctional peptides, which also contain aminopolycarboxylates, are coupled to protein. In a third method, radioiodinated bifunctional aminopolycarboxylates are coupled to protein. In a fourth method, a hydrazide-appended protein is coupled to a radioiodinated carbohydrate or a thiolated protein is coupled to a hydrazide-appended and radioiodinated carbohydrate. In a fifth method a monoderivatized cyanuric chloride is used to conjugate thiolated protein. Radioiodinated residualizing protein conjugates made by these methods are particularly stable in vivo and are suitable for radioimmunodetection and radioimmunotherapy.

    Abstract translation: 描述了将放射性碘化肽或碳水化合物结构与缀合物的产率和质量提高的蛋白质缀合的方法。 在一种方法中，特异设计的含有非代谢性键如酰胺键的放射性碘化双功能肽与细胞靶向蛋白偶联。 在第二种方法中，也含有氨基多羧酸盐的放射性碘化的不可代谢的双功能肽与蛋白质偶联。 在第三种方法中，放射性碘化双官能氨基多羧酸盐与蛋白质偶联。 在第四种方法中，酰肼附着的蛋白质与放射性碘化碳水化合物偶联，或硫醇化蛋白质与酰肼附着和放射性碘化碳水化合物偶联。 在第五种方法中，使用monoderivatized氰尿酰氯来缀合硫醇化蛋白质。 通过这些方法制备的放射性碘化残留蛋白质缀合物在体内特别稳定，适用于放射免疫检测和放射免疫治疗。

    IMPROVED DELIVERY OF DIAGNOSTIC AND THERAPEUTIC AGENTS TO A TARGET SITE
    8.
    发明申请
    IMPROVED DELIVERY OF DIAGNOSTIC AND THERAPEUTIC AGENTS TO A TARGET SITE 审中-公开
    改进诊断和治疗药物到目标网站

    公开(公告)号：WO1996040245A1

    公开(公告)日：1996-12-19

    申请号：PCT/US1996008696

    申请日：1996-06-07

    Applicant: IMMUNOMEDICS, INC.

    Inventor： IMMUNOMEDICS, INC. ,  GRIFFITHS, Gary, L. ,  HANSEN, Hans, J. ,  GOVINDAN, Serengulam

    IPC: A61K39/395

    CPC classification number: B82Y5/00 ,  A61K41/0095 ,  A61K47/665 ,  A61K47/6893 ,  A61K47/6897 ,  A61K47/6898 ,  A61K49/0017 ,  A61K51/1078 ,  A61K51/1093 ,  A61K2121/00 ,  A61K2123/00 ,  G01N33/531 ,  G01N33/534 ,  G01N33/574 ,  G01N33/686 ,  Y10S424/90

    Abstract: An in vivo method for delivering a diagnostic or therapeutic agent to a target site in a mammal, wherein a targeting species including a targeting moiety and a diagnostic or therapeutic agent or a binding site for a subsequently administered diagnostic or therapeutic agent conjugate, the targeting moiety having a primary binding site whereby it specifically binds to the target, is administered and allowed to accrete at the target site, is improved by injecting into the circulatory system of the mammal a clearing agent that binds to the primary binding site of the targeting species, whereby non-localized primary targeting species is cleared from circulation. The method is especially useful in pretargeting methods because the clearing agent does not remove the primary targeting species or block secondary binding sites of the primary targeting species.

    Abstract translation: 用于将诊断或治疗剂递送至哺乳动物的靶位点的体内方法，其中包括靶向部分和诊断或治疗剂的靶向物质或用于随后施用的诊断或治疗剂缀合物的结合位点靶向部分 通过向哺乳动物的循环系统注射与靶向物种的主要结合位点结合的结合剂，改善其具有与靶标特异性结合的主要结合位点，并且允许其在目标位点被吸收， 从而非局部化的主要靶向物质从循环中清除。 该方法在预靶向方法中特别有用，因为清除剂不除去主要靶向物种的主要靶向物种或阻断二级结合位点。

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