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10 条记录 (耗时 0.012 秒)

    RADIOPHARMACEUTICAL COMPOSITIONS CAPABLE OF LOCALIZING AT SITES OF THROMBUS
    1.
    发明公开
    RADIOPHARMACEUTICAL COMPOSITIONS CAPABLE OF LOCALIZING AT SITES OF THROMBUS 失效
    RADIO注明化合物血栓IMAGING

    公开(公告)号：EP0910416A2

    公开(公告)日：1999-04-28

    申请号：EP97931012.0

    申请日：1997-06-05

    申请人： G.D. SEARLE & CO. ,  MALLINCKRODT MEDICAL, INC.

    发明人： FEIGEN, Larry, P. ,  FLYNN, Daniel, Lee ,  NEEDLEMAN, Philip ,  SRINIVASAN, Ananthachari ,  ZABLOCKI, Jeffery, Alan ,  SCHMIDT, Michelle A.

    IPC分类号： A61K38 ,  A61K51 ,  C07K5

    CPC分类号： C07K5/06113 ,  A61K51/088 ,  A61K2121/00 ,  A61K2123/00

    摘要： A radiopharmaceutical capable of localizing at a site of thrombus containing activated platelets within a mammalian body is provided wherein the radiopharmaceutical comprises a linear peptidomimetic containing ligand capable of specifically binding to the GPIIb/IIIa integrin receptor of platelets in the thrombus and a radionuclide covalently bound to the peptidomimetic containing ligand. The ligand compositions of the invention are provided complexed with a selected metal radionuclide to form a diagnostic or therapeutic radiopharmaceutical to image a site of thrombus or provide radiotherapy to the site of thrombus, respectively. Methods of imaging a site of thrombus in a mammalian body by administering a diagnostically effective amount of the radiopharmaceutical composition of this invention complexed with a selected diagnostic metal radionuclide and methods of providing therapy to a site of thrombus in a mammalian body by administering a therapeutically effective amount of the radiopharmaceutical composition of this invention complexed with a selected therapeutic metal radionuclide are also provided as well as kits for preparing such radiopharmaceutical compositions.

    A METHOD FOR PREPARING RADIOLABELED PEPTIDES
    2.
    发明公开
    A METHOD FOR PREPARING RADIOLABELED PEPTIDES 失效
    用于生产放射性标记肽

    公开(公告)号：EP0850072A1

    公开(公告)日：1998-07-01

    申请号：EP96919257.0

    申请日：1996-06-07

    申请人： MALLINCKRODT MEDICAL, INC.

    发明人： SRINIVASAN, Ananthachari

    IPC分类号： A61K51 ,  C07C227 ,  C07C229

    CPC分类号： A61K51/088 ,  A61K51/083 ,  C07C227/18 ,  Y02P20/55 ,  C07C229/16 ,  C07C229/24

    摘要： A method for radiolabelling peptides using polyaminocarboxylate ligands having suitable protecting groups such that they can be added to peptides by standard solid phase or solution phase peptide synthetic chemistry and can be deprotected using standard cleavage/deprotection reagents and produce the peptide/chelate conjugate as a high purity monoaddition product is provided. The cleaved and deprotected ligand-peptide molecules can then be labeled with lanthanide or actinide radionuclides. The protected polyaminocarboxylate ligands form mono-anhydrides or mono-active esters under solid phase or solution phase conditions and permit only the desired monoaddition chelate-peptide conjugate to be formed.

    LIGANDS FOR IMPROVING METAL CHELATE FORMATION KINETICS
    3.
    发明公开
    LIGANDS FOR IMPROVING METAL CHELATE FORMATION KINETICS 失效
    提高金属螯合物培养动力学的配基

    公开(公告)号：EP0630264A1

    公开(公告)日：1994-12-28

    申请号：EP93904905.0

    申请日：1993-02-05

    申请人： MALLINCKRODT MEDICAL, INC.

    发明人： SRINIVASAN, Ananthachari

    IPC分类号： C07D213 ,  A61K51 ,  C07B59 ,  C07C323 ,  C07F1 ,  C07F5 ,  C07F13 ,  C07F15 ,  C07K14

    CPC分类号： C07K14/815 ,  A61K51/0478 ,  A61K51/088 ,  A61K2121/00 ,  A61K2123/00 ,  C07B59/004 ,  C07D213/40 ,  C07D213/64 ,  C07D213/68 ,  C07F13/005 ,  C07K14/6555

    摘要： L'invention concerne des ligands d'amide-thiolate présentant une cinétique de formation d'agents chélateurs améliorée. Les ligands se composent d'une amine qui favorise la formation rapide d'un complexe intermédiaire amine-amide-thiolate, suivie du transfert du métal ou de la conversion du ligand en un complexe amide-thiolate thermodynamiquement stable. Dans un mode de réalisation, l'amine est une amine tertiaire ou l'équivalent qui est placée de manière stratégique afin de faciliter la formation du complexe. Dans un autre mode de réalisation, l'amine fait partie de la pyridine contenant un substituant alcoxyle inférieur en position 2 ou 4 dans le cycle. La désalcoylation-O se produit lors de la réaction de complexation qui entraîne la transformation de l'amine en amide vinylogue en tant que partie intégrante d'un complexe amide-thiolate thermodynamiquement stable. Les ligands d'amide-thiolate de ladite invention peuvent être utilisés pour le marquage postformé de substances biologiques à des fins diagnostiques et thérapeutiques.

    摘要翻译： 本发明涉及具有改进的螯合剂形成动力学的酰胺 - 硫醇盐配体。 配体由促进胺 - 酰胺 - 硫醇盐中间体配合物快速形成的胺组成，随后转移金属或将配体转化为热力学稳定的酰胺 - 硫醇盐配合物。 在一个实施方案中，胺是叔胺或等同物，其策略性地放置以促进复合物的形成。 在另一个实施方案中，所述胺是在环中2-或4-位含有低级烷氧基取代基的吡啶的一部分。 O-脱烷基化发生在络合反应过程中，导致胺转化成乙烯基乙酰胺，作为热力学稳定的酰胺 - 硫醇盐配合物的组成部分。 为了诊断和治疗目的，本发明的酰胺 - 硫醇盐配体可以用于生物物质的后形式标记。

    METAL CHELATES AS SPACER COMPOUNDS IN BIOLOGICALLY ACTIVE PEPTIDES
    4.
    发明公开
    METAL CHELATES AS SPACER COMPOUNDS IN BIOLOGICALLY ACTIVE PEPTIDES 失效
    金属络合物作为持有人生物活性肽

    公开(公告)号：EP0705105A1

    公开(公告)日：1996-04-10

    申请号：EP94916780.0

    申请日：1994-05-13

    申请人： MALLINCKRODT MEDICAL, INC.

    发明人： DUNN, T. Jeffrey ,  SRINIVASAN, Ananthachari ,  LYLE, Leon R. ,  RAJAGOPALAN, Raghavan

    IPC分类号： A61K51 ,  A61K49 ,  C07K1 ,  C07K5 ,  C07K7 ,  C07K14

    CPC分类号： A61K49/14 ,  C07K1/04 ,  C07K14/815

    摘要： Ligands that are capable of forming metal complexes are incorporated directly into peptides at nonbiologically active locations. The metal complex serves as a bifunctional agent and as a spacer molecule. In one aspect of the invention, the ligands are prepared by replacing a nonbiologically active peptide spacer sequence with either Cys-Gly-Gly-Glu(η-)CO- (SEQ ID NO:1) or Cys-Gly-Gly-Lys(ε-)NH-CO(CH2)2-CO- (SEQ ID NO:2). In these examples, unnatural peptide bonds are used to attach the ligand to the terminal end of the peptide. Peptides incorporating such ligands are also disclosed. Other spacer ligands which may be incorporated into peptides include the following natural peptide sequences: -Cys-Gly-His-, -Asp-Gly-Cys-, -Glu-Gly-Cys-, -Gly-Asp-Cys-, and -Gly-Glu-Cys-. Unnatural tripeptides which function as spacer ligands include: -Cys-Gly-(imidazolyl glycyl)-, -isoCys-Gly-(imidazolyl glycyl)-, and -isoCys-Gly-His-. When the above peptide sequences are present in a nonbiologically active peptide spacer, they are able to form metal complexes with desired metal ions, and the resulting complexes serve as bifunctional agents and as spacer molecules in the peptide.

    RADIOLABELED PEPTIDE COMPOSITIONS FOR SITE-SPECIFIC TARGETING
    7.
    发明公开
    RADIOLABELED PEPTIDE COMPOSITIONS FOR SITE-SPECIFIC TARGETING 失效
    资源的基于放射性标记肽对于特殊地方行政

    公开(公告)号：EP0831938A1

    公开(公告)日：1998-04-01

    申请号：EP96922403.0

    申请日：1996-06-06

    申请人： MALLINCKRODT MEDICAL, INC.

    发明人： SRINIVASAN, Ananthachari ,  DYSZLEWSKI, Mary, Marmion ,  BUGAJ, Joseph, E.

    IPC分类号： A61K51 ,  A61P35 ,  C07K14

    CPC分类号： C07K14/6555 ,  A61K51/083 ,  A61K51/088

    摘要： This invention relates to radiolabeled peptide compositions for radiopharmaceutical use and, more specifically, to radiolabeled peptides for diagnostic or therapeutic use having an unmodified carboxy terminal amino acid. The radiopharmaceutical composition may be used for targeting a selected biological site. The radiolabeled peptide is characterized by having its carboxy terminal amino acid in its carboxylic acid form and the peptide is coupled to a diagnostic or therapeutic radionuclide by a chelating agent. The radiopharmaceutical composition preferably comprises a radiolabeled peptide selected from the group consisting of somatostatin, an analog of somatostatin, a derivative of somatostatin and peptides capable of binding to the somatostatin receptor, where the peptide is coupled to a diagnostic or therapeutic radionuclide by a chelating agent has its carboxy terminal amino acid in its carboxylic acid form.