Method of determining the activity of a central nervous system drug on striatal dopamine transporter populations
    71.
    发明申请
    Method of determining the activity of a central nervous system drug on striatal dopamine transporter populations 审中-公开
    确定中枢神经系统药物对纹状体多巴胺转运体群体的活性的方法

    公开(公告)号:US20030130336A1

    公开(公告)日:2003-07-10

    申请号:US10334239

    申请日:2002-12-31

    申请人: Pfizer Inc.

    IPC分类号: A61K051/00 A61K031/405

    CPC分类号: A61K51/0476

    摘要: This invention relates to a method of predicting the activity of a CNS drug on striatal dopamine transporter populations. The method uses SPECT brain imaging to predict the activity of antidepressants or anxiolytic agents on striatal dopamine transporter populations. The method uses the increase in dopamine transporter populations as a marker for predicting sexual dysfunction side effects, as well as to determine proper dosing for antidepressants or anxiolytics agents in order to avoid the sexual dysfunction side effects.

    摘要翻译: 本发明涉及一种预测CNS药物对纹状体多巴胺转运体群体的活性的方法。 该方法使用SPECT脑成像来预测抗抑郁药或抗焦虑剂对纹状体多巴胺转运体群体的活性。 该方法使用多巴胺转运蛋白群体的增加作为预测性功能障碍副作用的标志物,以及确定抗抑郁药或抗焦虑剂的适当给药以避免性功能障碍的副作用。

    Formulation of Tc and Re carbonyl complexes using stannous ion as the reductant for pertechnetate and perrhenate
    72.
    发明申请
    Formulation of Tc and Re carbonyl complexes using stannous ion as the reductant for pertechnetate and perrhenate 审中-公开
    使用亚锡离子作为高铼酸盐和高铼酸盐的还原剂制备Tc和Re羰基络合物

    公开(公告)号:US20020147316A1

    公开(公告)日:2002-10-10

    申请号:US10053612

    申请日:2002-01-24

    申请人: Mallinckrodt Inc.

    IPC分类号: C07F013/00

    摘要: The invention relates to novel aminocarboxylate ligands that are suitable for completing with a radionuclide, and are useful as therapeutic agents and as imaging agents for diagnostic purposes. In accordance with the present invention, a method of preparing a compound of formulafac-nullM(CO)3(OH2)3nullnullnullnull(I)wherein M is Mn, 99mTc, 186Re or 188Re, involves reacting a metal in permetallate form with carbon monoxide and stannous ion. The compound of formula (I) can be reacted with a ligand Lx to form a compound of the formulai fac-nullM(CO)3Lxnullnnullnull(II)wherein M is as defined above, Lx is a monodentate or multidentate ligand or a mixture of these ligands, and n is a charge of the ligand Lx increased with onenullcharge. The invention also is directed to novel compounds, and kits for carrying out the disclosed methods.

    摘要翻译: 本发明涉及适用于用放射性核素完成的新的氨基羧酸盐配体,并且可用作诊断目的的治疗剂和成像剂。 根据本发明,制备式(I-1)化合物的方法,即式(Ⅰ)化合物 线配方>其中M是Mn,99mTc,186Re或188Re,包括使多金属盐形式的金属与一氧化碳和亚锡离子反应。 式(I)化合物可以与配体Lx反应形成下式的化合物:其中,式(I) 其中M如上所定义,Lx是单齿或多齿配体或这些配体的混合物,n是配体L x的电荷随着+电荷而增加。 本发明还涉及用于实施所公开的方法的新化合物和试剂盒。

    Formulation of Tc and Re carbonyl complexes using stannous ion as the reductant for pertechnetate and perrhenate
    73.
    发明授权
    Formulation of Tc and Re carbonyl complexes using stannous ion as the reductant for pertechnetate and perrhenate 失效
    使用亚锡离子作为高铼酸盐和高铼酸盐的还原剂制备Tc和Re羰基络合物

    公开(公告)号:US06359119B1

    公开(公告)日:2002-03-19

    申请号:US09576960

    申请日:2000-05-24

    IPC分类号: C07F1300

    摘要: The invention relates to novel aminocarboxylate ligands that are suitable for complexing with a radionuclide, and are useful as therapeutic agents and as imaging agents for diagnostic purposes. In accordance with the present invention, a method of preparing a compound of formula fac-[M(CO)3(OH2)3]+  (I) wherein M is Mn, 99mTc, 186Re or 188Re, involves reacting a metal in permetallate form with carbon monoxide and stannous ion. The compound of formula (I) can be reacted with a ligand Lx to form a compound of the formula fac-[M(CO)3Lx]n  (II) wherein M is as defined above, Lx is a monodentate or multidentate ligand or a mixture of these ligands, and n is a charge of the ligand Lx increased with one + charge. The invention also is directed to novel compounds, and kits for carrying out the disclosed methods.

    摘要翻译: 本发明涉及适用于与放射性核素络合的新型氨基羧酸酯配体,并且可用作诊断目的的治疗剂和成像剂。 根据本发明,制备M肟化合物的方法是Mn,99mTc,186Re或188Re,包括使金属以多金属盐形式与一氧化碳和亚锡离子反应。 式(I)化合物可以与配体Lx反应形成如下定义的糠醛的化合物:Lx是单齿或多齿配体或这些配体的混合物,n是配体Lx的电荷 增加一个+电荷。 本发明还涉及用于实施所公开的方法的新化合物和试剂盒。

    Radioactive transition metal nitride heterocomplex
    74.
    发明授权
    Radioactive transition metal nitride heterocomplex 有权
    放射性过渡金属氮化物杂复合物

    公开(公告)号:US06270745B1

    公开(公告)日:2001-08-07

    申请号:US09331237

    申请日:1999-06-17

    IPC分类号: A61K5100

    摘要: The present invention provides a single radioactive transition metal nitride heterocomplex which permits labeling of a physiologically active substance such as a peptide, hormone or the like without impairing the activity of the substance. The radioactive transition metal nitride heterocomplex of the present invention is represented by the following formula (I): (M≡N)XY  (I) wherein a radioactive transition metal M is radioactive technetium or radioactive rhenium, N is a nitrogen atom, X is a diphosphine compound or a diarsine compound, and Y is a bindentate ligand having a combination of electron-donating atoms.

    摘要翻译: 本发明提供了一种单一的放射性过渡金属氮化物异复合体,其允许在不损害物质活性的情况下标记生理活性物质如肽,激素等。 本发明的放射性过渡金属氮化物异构复合体由下式(I)表示:其中放射性过渡金属M为放射性锝或放射性铼,N为氮原子,X为二膦化合物或胂系化合物, Y是具有给电子原子的组合的结合配体。

    Ternary radiopharmaceutical complexes
    75.
    发明授权
    Ternary radiopharmaceutical complexes 失效
    三元放射性药物复合物

    公开(公告)号:US6010679A

    公开(公告)日:2000-01-04

    申请号:US13320

    申请日:1998-01-26

    摘要: This invention provides novel radiopharmaceuticals which are useful as imaging agents for the diagnosis of cardiovascular disorders, infectious disease and cancer. The radiopharmaceuticals are comprised of phosphine or arsine ligated technetium-99m labeled hydrazino or diazino modified biologically active molecules that selectively localize at sites of disease and thus allow an image to be obtained of the loci using gamma scintigraphy. This invention also provides methods for using the radiopharmaceuticals and kits comprising radiopharmaceutical precursors. The radiopharmaceuticals of this invention have the structure:[(Q).sub.d 'L.sub.n -C.sub.h '].sub.x -M.sub.t (A.sub.L1).sub.y (A.sub.L2)z;wherein the variables are as defined herein.

    摘要翻译: 本发明提供了可用作诊断心血管疾病,感染性疾病和癌症的成像剂的新型放射性药物。 放射性药物由磷化氢或胂连接的锝-99m标记的肼或二氮嗪修饰的生物活性分子组成,其选择性地定位在疾病部位,从而允许使用γ闪烁扫描获得基因座的图像。 本发明还提供了使用放射性药物和包含放射性药物前体的试剂盒的方法。 本发明的放射性药物具有以下结构:[(Q)d'Ln-Ch'] x-Mt(AL1)y(AL2)z;其中变量如本文所定义。

    Nuclear medicine techniques for detecting carcinoma in the dense breast
    76.
    发明授权
    Nuclear medicine techniques for detecting carcinoma in the dense breast 失效
    用于检测致密乳腺癌的核医学技术

    公开(公告)号:US5895640A

    公开(公告)日:1999-04-20

    申请号:US740639

    申请日:1996-10-31

    申请人: Iraj Khalkhali

    发明人: Iraj Khalkhali

    IPC分类号: A61B10/00 A61K51/04 A61B5/05

    CPC分类号: A61K51/0476 A61B10/0041

    摘要: A nuclear medicine technique for detecting and localizing carcinomas in the breasts of patients with dense breast. In the method, a patient with dense breast is administering a dose of Technetium-99m Sestamibi, or another nuclear medicine substance which selectively accumulates in breast carcinomas. The breast is then imaged with a nuclear medicine detector to image the carcinomas with the accumulated nuclear medicine agent and localize the carcinomas in real time and in three dimensions. The imaging can be done in a first plane with the detector perpendicular to a lateral side of the breast and also in a second plane parallel to the patient's chest wall.

    摘要翻译: 用于检测和定位乳腺癌患者乳腺癌的核医学技术。 在该方法中,具有致密乳房的患者正在施用一定剂量的锝-99m Sestamibi或选择性积累在乳腺癌中的另一核药物质。 然后用核医学检测器对乳房进行成像,用积累的核药物对癌症进行成像,并实时和三维地定位癌。 成像可以在第一平面中进行,其中检测器垂直于乳房的侧面,并且在平行于患者的胸壁的第二平面中。

    Cores for technetium radiopharmaceuticals
    78.
    发明授权
    Cores for technetium radiopharmaceuticals 失效
    锝放射性药物的核心

    公开(公告)号:US5589576A

    公开(公告)日:1996-12-31

    申请号:US289654

    申请日:1994-08-12

    IPC分类号: A61K51/04 C07F13/00

    摘要: Novel complexes of technetium (.sup.99 Tc or .sup.99m Tc) which contain the moiety Tc.dbd.NR, Tc--N.dbd.NY or Tc(--N.dbd.NY).sub.2, and a ligand which confers biological target-seeking properties on the complex, wherein R represents an aryl group, a substituted or unsubstituted alkyl group, or the grouping .dbd.NR.sup.1 R.sup.2 ; Y represents an aryl group or a substituted or unsubstituted alkyl group; and R.sup.1 and R.sup.2 are hydrogen, aryl groups or substituted or unsubstituted aliphatic or cyclic alkyl groups, and may be both the same or different, provided that both are not hydrogen. The complexes are suitable for use in radiopharmaceuticals for a variety of clinical applications. Methods for the preparation of these technetium complexes are also described.

    摘要翻译: 含有部分Tc = NR,Tc-N = NY或Tc(-N = NY)2的锝(99Tc或99mTc)的新型络合物和赋予复合物生物靶寻求性质的配体,其中R表示 芳基,取代或未取代的烷基,或基团= NR 1 R 2; Y表示芳基或取代或未取代的烷基; 并且R 1和R 2是氢,芳基或取代或未取代的脂族或环状烷基,并且可以相同或不同,条件是两者都不是氢。 该配合物适用于各种临床应用的放射性药物。 还描述了制备这些锝络合物的方法。