Radiopharmaceutical compositions capable of localizing at sites of
thrombus
    1.
    发明授权
    Radiopharmaceutical compositions capable of localizing at sites of thrombus 失效
    可以在血栓位置定位的放射性药物组合物

    公开(公告)号:US6132697A

    公开(公告)日:2000-10-17

    申请号:US870042

    申请日:1997-06-05

    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.

    摘要翻译: 提供了能够在哺乳动物体内含有活化血小板的血栓位点定位的放射性药物,其中放射性药物包含能够特异性结合血栓中血小板的GPIIb / IIIa整联蛋白受体的线性拟肽含量配体和共价结合的放射性核素 含有拟肽的配体。 提供本发明的配体组合物与所选择的金属放射性核素复合以形成诊断或治疗性放射性药物,以分别对血栓位点成像或向血栓部位提供放射治疗。 通过施用诊断上有效量的本发明的放射性药物组合物与选定的诊断性金属放射性核素复合而在哺乳动物体内成像血栓位点的方法和通过施用治疗有效的方法向哺乳动物体内的血栓位点提供治疗 还提供了与选定的治疗性金属放射性核素复合的本发明的放射性药物组合物的量以及用于制备这种放射性药物组合物的试剂盒。

    4-aminomethyl-1-azaadamantane derived benzamides
    4.
    发明授权
    4-aminomethyl-1-azaadamantane derived benzamides 失效
    4-氨基甲基-1-氮杂金刚烷衍生的苯甲酰胺

    公开(公告)号:US5840903A

    公开(公告)日:1998-11-24

    申请号:US919679

    申请日:1992-07-27

    CPC分类号: C07D471/18

    摘要: This invention relates to compounds of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein Z is selected from the group consisting of ##STR2## R.sub.1 is alkoxy of one to six carbon atoms; R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are the same or different and are selected from the group consisting of hydrogen, halogen, CF.sub.3, 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, C.sub.2 -C.sub.7 acylamino, aminocarbonyl, aminosulfone optionally substituted by one or two alkyl groups of one to six carbon atoms, C.sub.1 -C.sub.6 alkylsulfone and nitro; m is 1 or 2; X is O or NR.sub.7 ; and R.sub.7 is hydrogen or alkyl of 1 to 6 carbon atoms.

    摘要翻译: 本发明涉及下式的化合物或其药学上可接受的盐,其中Z选自由下列组成的组:R1是1-6个碳原子的烷氧基; R 2,R 3,R 4和R 5相同或不同,并且选自氢,卤素,CF 3,羟基,1至6个碳原子的烷氧基,2至7个碳原子的酰基,氨基,被1个 或两个1-6个碳原子的烷基,任选被1至6个碳原子的一个或两个烷基取代的C 2 -C 7酰基氨基,氨基羰基,氨基砜,C 1 -C 6烷基砜和硝基; m为1或2; X为O或NR7; 且R 7为氢或1至6个碳原子的烷基。