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    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.

    AZANORADAMANTANES
    10.
    发明公开
    AZANORADAMANTANES 失效

    公开(公告)号：EP0674639A1

    公开(公告)日：1995-10-04

    申请号：EP94902349.0

    申请日：1993-11-26

    申请人： G.D. SEARLE & CO.

    发明人： FLYNN, Daniel, Lee ,  MOORMAN, Alan, Edward

    IPC分类号： A61K31 ,  A61P1 ,  A61P43 ,  C07D471

    CPC分类号： C07D471/18

    摘要： This invention relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof wherein Z is selected from the group consisting of (a) and (b); R1 is alkoxy of one to six carbon atoms; R2, R3, R4 and R5 are the same or different and are selected from the group consisting of hydrogen, halogen, CF3, hydroxy, alkoxy of one to six carbon atoms, acyl of two to seven carbon atoms, amino, amino substituted by one or two alkyl groups of one to six carbon atoms, C2-C7 acylamino, aminocarbonyl, aminosulfone optionally substituted by one or two alkyl groups of one to six carbon atoms, C1-C6 alkylsulfone and nitro; n is 0, 1 or 2; m is 0 or 1; X is O or NR7; and R7 is hydrogen or alkyl of 1 to 6 carbon atoms, which act as 5-HT4 agonists or antagonists and/or 5-HT3 antagonists in mammals.

    摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，其中Z选自（a）和（b）; R 1是1-6个碳原子的烷氧基; R2，R3，R4和R5相同或不同，选自氢，卤素，CF3，羟基，1-6个碳原子的烷氧基，2-7个碳原子的酰基，氨基，被一个 或一个至六个碳原子的两个烷基，C 2 -C 7酰氨基，氨基羰基，任选被一个或两个1至6个碳原子的烷基取代的氨基砜，C 1 -C 6烷基砜和硝基; n是0,1或2; m是0或1; X是O或NR7; 并且R 7是氢或1至6个碳原子的烷基，其在哺乳动物中充当5-HT 4激动剂或拮抗剂和/或5-HT 3拮抗剂。