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    Cocaine receptor binding ligands
    1.
    发明授权
    Cocaine receptor binding ligands 失效
    可卡因受体结合配体

    公开(公告)号：US5380848A

    公开(公告)日：1995-01-10

    申请号：US233723

    申请日：1994-04-26

    申请人： Michael J. Kuhar ,  John W. Boja ,  Frank I. Carroll ,  Anita H. Lewin ,  Philip Abraham

    发明人： Michael J. Kuhar ,  John W. Boja ,  Frank I. Carroll ,  Anita H. Lewin ,  Philip Abraham

    IPC分类号： A61K51/04 ,  C07D451/02 ,  C07F7/22

    CPC分类号： C07F7/2212 ,  A61K51/0448 ,  C07D451/02 ,  A61K2123/00

    摘要： Novel compounds show high affinity for specific cocaine receptors in the brain, particularly dopamine transporter sites, and have the formula ##STR1## Wherein Y=CH.sub.2 R.sub.3, CO.sub.2 R.sub.2 or ##STR2## R.sub.1 =hydrogen, C.sub.1-5 alkyl, R.sub.2 =hydrogen, C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.1-4 alkoxy, C.sub.1-6 alkynyl, halogen or amine,R.sub.3 =OH, hydrogen, C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.1-4 alkoxy, Cl Br, I, CN, NH.sub.2, NHC.sub.1-6 alkyl, NC.sub.1-6 alkyl, OCOC.sub.1-6 alkyl, OCOC.sub.1-3 alkylaryl,A=S, 0 or NHX=H, C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.1-4 alkoxy, C.sub.1-6 alkynyl, halogen, amino, acylamido, andZ=H, I, Br, Cl, F, CN, CF.sub.3 NO.sub.2, N.sub.3, OR.sub.1, CO.sub.2 NH.sub.2, CO.sub.2 R.sub.1, C.sub.1-6 alkyl , NR.sub.4 R.sub.5, NHCOR.sub.5, NHCO.sub.2 R.sub.6,wherein R.sub.4 -R.sub.6 are each C.sub.1-6 alkyl.

    摘要翻译： 新型化合物对脑中特定的可卡因受体，特别是多巴胺转运蛋白位点表现出高亲和力，并且具有下式：其中Y = CH 2 R 3，CO 2 R 2或R 1 =氢，C 1-5烷基，R 2 =氢， C6烷基，C3-8环烷基，C1-4烷氧基，C1-6炔基，卤素或胺，R3 = OH，氢，C1-6烷基，C3-8环烷基，C1-4烷氧基，C1 Br，I，CN， NH 2，NHC 1-6烷基，NC 1-6烷基，OCOC 1-6烷基，OCOC 1-3烷基芳基，A = S，O或NH X = H，C 1-6烷基，C 3-8环烷基，C 1-4烷氧基， 6炔基，卤素，氨基，酰氨基和Z = H，I，Br，Cl，F，CN，CF 3 NO 2，N 3，OR 1，CO 2 NH 2，CO 2 R 1，C 1-6烷基，NR 4 R 5，NHCOR 5，NHCO 2 R 6， 各自为C 1-6烷基。

    Cocaine receptor binding ligands
    2.
    发明授权
    Cocaine receptor binding ligands 失效
    可卡因受体结合配体

    公开(公告)号：US5413779A

    公开(公告)日：1995-05-09

    申请号：US972472

    申请日：1993-03-23

    申请人： Michael J. Kuhar ,  Frank I. Carroll ,  John W. Boja ,  Anita H. Lewin ,  Philip Abraham

    发明人： Michael J. Kuhar ,  Frank I. Carroll ,  John W. Boja ,  Anita H. Lewin ,  Philip Abraham

    IPC分类号： A61K51/00 ,  C07D451/02 ,  C07F7/22 ,  G01N33/50

    CPC分类号： C07D451/02 ,  C07F7/2212

    摘要： 3.beta.-[4-iodophenyl]-tropan-2.beta.-carboxylic acid methyl ester tartrate is a high affinity binding ligand for cocaine receptors in mammalian brains. It and its congeners may be employed for imaging and other brain scanning techniques that allow the determination of the presence of cocaine receptors, such as dopamine and serotonin transporters and the like.

    摘要翻译： PCT No.PCT / US91 / 05553。 371日期1993年3月23日 102（e）1993年3月23日PCT PCT 1991年8月9日PCT公布。 出版物WO92 / 02260 日期：1992年2月20日.β-[4-碘苯基] - 丙酰基-2β-羧酸甲酯酒石酸盐是哺乳动物脑中可卡因受体的高亲合力结合配体。 它和其同源物可用于成像和其它脑扫描技术，其允许测定可卡因受体（例如多巴胺和5-羟色胺转运蛋白）等的存在。

    Dopamine transporter imaging ligand
    3.
    发明授权
    Dopamine transporter imaging ligand 失效
    多巴胺转运蛋白成像配体

    公开(公告)号：US06358492B1

    公开(公告)日：2002-03-19

    申请号：US08946007

    申请日：1997-10-07

    申请人： Michael J. Kuhar ,  Frank I. Carroll ,  John W. Boja ,  Anita H. Lewin ,  Philip Abraham

    发明人： Michael J. Kuhar ,  Frank I. Carroll ,  John W. Boja ,  Anita H. Lewin ,  Philip Abraham

    IPC分类号： C07D45102

    CPC分类号： A61K51/0448 ,  C07D451/02

    摘要： The 3&agr; isomer of RTI-55, RTI-352, is an effective in vivo binding ligand that reflects greater selectivity for the dopamine transporter than is observed with RTI-55. In addition, there is also a more rapid achievement of apparent equilibrium in the striatal-to-cerebellar ratio (compared to RTI-55) as the ratio peaks at about 30 min and is maintained for about 20 min thereafter. Such apparent equilibrium is useful in developing an approach to measuring the number of dopamine transporters present in tissues. Moreover, these results indicate that the utilization of 3&agr; isomers of a variety of 3&bgr;-(substituted phenyl)tropanes will result in greater selectivity for dopamine transporters and a more rapid of achievement of apparent equilibrium.

    摘要翻译： RTI-55，RTI-352的3α异构体是一种有效的体内结合配体，其反映了对多巴胺转运蛋白的选择性高于用RTI-55观察到的选择性。 另外，纹状体与小脑的比例（与RTI-55相比）的表观平衡也更快，因为在30分钟左右的比例达到峰值，此后保持约20分钟。 这种表观平衡在开发测量组织中存在的多巴胺转运蛋白数量的方法中是有用的。 此外，这些结果表明，使用各种3'-巯基（取代苯基）托烷的3α异构体将导致对多巴胺转运蛋白的更高选择性和更快速地达到表观平衡。

    Methods for controlling invertebrate pests using cocaine receptor binding ligands
    4.
    发明授权
    Methods for controlling invertebrate pests using cocaine receptor binding ligands 失效
    用可卡因受体结合配体控制无脊椎动物害虫的方法

    公开(公告)号：US5935953A

    公开(公告)日：1999-08-10

    申请号：US823563

    申请日：1997-03-25

    申请人： Michael J. Kuhar ,  Frank I. Carroll ,  John W. Boja ,  Anita H. Lewin ,  Philip Abraham

    发明人： Michael J. Kuhar ,  Frank I. Carroll ,  John W. Boja ,  Anita H. Lewin ,  Philip Abraham

    IPC分类号： A61K31/46 ,  A61P25/00 ,  A61P25/24 ,  A61P25/30 ,  A61P43/00 ,  C07D451/02 ,  C07F7/22 ,  A61K31/535 ,  A61K31/44 ,  A01N43/42

    CPC分类号： C07D451/02 ,  C07F7/2212

    摘要： The invention relates to a method of controlling an invertebrate pest, comprising contacting the pest with a pest-controlling amount of an agent having substantial inhibitory activity toward a phenylethanolamine reuptake transporter as determined by radioactive octopamine reuptake inhibition assay is disclosed. Compositions comprising compounds capable of inhibiting the octopamine reuptake transporter include cocaine analogs. A process for inhibiting the feeding of an invertebrate pest comprising contacting said pest with a pest-controlling amount of an agent having substantial inhibitory activity toward a phenylethanolamine reuptake transporter as determined by radioactive octopamine reuptake inhibition assay, with the proviso that said agent is not cocaine. A process for delaying the maturation of a juvenile invertebrate by contacting it with an inhibitory amount of a phenylethanolamine reuptake transporter blocker is also disclosed. A radioactive phenylethanolamine reuptake inhibition assay for determining whether a given compound is an inhibitor of octopamine neuronal transport is also disclosed.

    摘要翻译： 本发明涉及一种控制无脊椎害虫的方法，其包括使害虫与害虫控制量的对苯基乙醇胺再摄取转运蛋白具有显着抑制活性的药剂接触，所述药物通过放射性的八聚胺再摄取抑制测定法测定。 包含能够抑制章鱼胺再摄取转运蛋白的化合物的组合物包括可卡因类似物。 一种抑制无脊椎害虫进食的方法，包括使所述有害生物与害虫控制量的苯基乙醇胺再吸收转运蛋白具有显着的抑制活性的药剂接触，所述方法是通过放射性章鱼胺再摄取抑制测定法确定的，条件是所述药剂不可卡因 。 还公开了一种通过使少年无脊椎动物与抑制量的苯乙醇胺再摄取转运蛋白阻断剂接触来延迟成熟的方法。 还公开了用于确定给定化合物是否是章鱼胺神经元转运抑制剂的放射性苯乙醇胺再摄取抑制测定。

    Cocaine receptor binding ligands
    5.
    发明授权
    Cocaine receptor binding ligands 失效

    公开(公告)号：US07189737B2

    公开(公告)日：2007-03-13

    申请号：US10279851

    申请日：2002-10-25

    申请人： Michael J. Kuhar ,  Frank I. Carroll ,  John W. Boja ,  Anita H. Lewin ,  Philip Abraham

    发明人： Michael J. Kuhar ,  Frank I. Carroll ,  John W. Boja ,  Anita H. Lewin ,  Philip Abraham

    IPC分类号： A61K31/44

    CPC分类号： C07D451/02 ,  A61K31/439

    摘要： A class of binding ligands for cocaine receptors and other receptors in the brain. Specifically, a novel family of compounds shows high binding specificity and activity, and, in a radiolabeled form, can be used to bind to these receptors, for biochemical assays and imaging techniques. Such imaging is useful for determining effective doses of new drug candidates in human populations. In addition, the high specificity, slow onset and long duration of the action of these compounds at the receptors makes them particularly well suited for therapeutic uses, for example as substitute medication for psychostimulant abuse. Some of these compounds may be useful in treating Parkinson's Disease or depression, by virtue of their inhibitory properties at monoamine transporters.

    Cocaine receptor binding ligands
    7.
    发明授权
    Cocaine receptor binding ligands 失效
    可卡因受体结合配体

    公开(公告)号：US07291737B2

    公开(公告)日：2007-11-06

    申请号：US10986352

    申请日：2004-11-12

    申请人： Michael J. Kuhar ,  Frank I. Carroll ,  John W. Boja ,  Anita H. Lewin ,  Philip Abraham

    发明人： Michael J. Kuhar ,  Frank I. Carroll ,  John W. Boja ,  Anita H. Lewin ,  Philip Abraham

    IPC分类号： C07D451/02

    CPC分类号： C07D451/02 ,  A61K31/439

    摘要： A class of binding ligands for cocaine receptors and other receptors in the brain. Specifically, a novel family of compounds shows high binding specificity and activity, and, in a radiolabeled form, can be used to bind to these receptors, for biochemical assays and imaging techniques. Such imaging is useful for determining effective doses of new drug candidates in human populations. In addition, the high specificity, slow onset and long duration of the action of these compounds at the receptors makes them particularly well suited for therapeutic uses, for example as substitute medication for psychostimulant abuse. Some of these compounds may be useful in treating Parkinson's Disease or depression, by virtue of their inhibitory properties at monoamine transporters.

    摘要翻译： 一类可卡因受体和脑中其他受体的结合配体。 具体来说，新型化合物家族显示出高结合特异性和活性，并且以放射性标记的形式可用于结合这些受体，用于生物化学测定和成像技术。 这种成像可用于确定人群中新的候选药物的有效剂量。 此外，这些化合物在受体的高度特异性，缓慢发作和长时间的作用使得它们特别适用于治疗用途，例如作为精神兴奋剂滥用的替代药物。 这些化合物中的一些可能由于其在单胺转运蛋白上的抑制性质而可用于治疗帕金森病或抑郁症。