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    Method of Rapid Methylation, Kit for Preparing PET Tracer and Method of Producing PET Tracer
    1.
    发明申请
    Method of Rapid Methylation, Kit for Preparing PET Tracer and Method of Producing PET Tracer 有权
    快速甲基化方法，制备PET示踪剂的试剂盒和生产PET示踪剂的方法

    公开(公告)号：US20100249477A1

    公开(公告)日：2010-09-30

    申请号：US12438711

    申请日：2007-08-24

    申请人： Masaaki Suzuki ,  Hisashi Doi ,  Hideo Tsukada

    发明人： Masaaki Suzuki ,  Hisashi Doi ,  Hideo Tsukada

    IPC分类号： C07C1/32 ,  C09K3/00

    CPC分类号： C07B59/001 ,  C07B37/04 ,  C07B59/00 ,  C07B2200/05 ,  C07C1/321 ,  C07C17/263 ,  C07C29/32 ,  C07C41/30 ,  C07C67/343 ,  C07C205/06 ,  C07C2531/24 ,  C07C2601/16 ,  C07C25/13 ,  C07C22/08 ,  C07C33/03 ,  C07C69/76 ,  C07C43/205

    摘要： It is intended to provide a method of rapid methylation of an aromatic compound or an alkenyl compound, which is capable of obtaining an aromatic compound or an alkenyl compound labeled with a methyl group or a fluoromethyl group under a mild condition rapidly in high yield using an organic boron compound whose toxicity is not so high as a substrate; a kit for preparing a PET tracer to be used in the same, and a method of producing a PET tracer using the same. In an aprotic polar solvent, methyl iodide or X—CH2F (wherein X is a functional group which can be easily released as an anion), an organic boron compound in which an aromatic ring or an alkenyl group is attached to boron are subjected to cross-coupling in the presence of a palladium(0) complex, a phosphine ligand, and a base.

    摘要翻译： 本发明旨在提供一种芳族化合物或烯基化合物的快速甲基化方法，其能够在温和条件下以高收率快速获得芳族化合物或用甲基或氟甲基标记的烯基化合物，使用 有机硼化合物的毒性不如底物高; 用于制备其中使用的PET示踪剂的试剂盒，以及使用其制备PET示踪剂的方法。 在非质子极性溶剂中，甲基碘或X-CH 2 F（其中X是可以容易地作为阴离子释放的官能团），其中芳环或烯基与硼连接的有机硼化合物经过十字 在钯（0）络合物，膦配体和碱的存在下偶联。

    Ligand for Vesicular Acetylcholine Transporter
    2.
    发明申请
    Ligand for Vesicular Acetylcholine Transporter 审中-公开
    水囊乙酰胆碱转运蛋白配体

    公开(公告)号：US20090163461A1

    公开(公告)日：2009-06-25

    申请号：US11887580

    申请日：2006-03-31

    申请人： Kazuhiro Shiba ,  Kiichi Ishiwata ,  Hideo Tsukada ,  Shingo Nishiyama

    发明人： Kazuhiro Shiba ,  Kiichi Ishiwata ,  Hideo Tsukada ,  Shingo Nishiyama

    IPC分类号： A61K31/555 ,  C07D211/22 ,  C07F15/00 ,  A61K31/445

    CPC分类号： C07D211/14 ,  A61K51/0457 ,  C07B59/002 ,  C07F7/2208

    摘要： The present invention provides a novel compound represented by the formula (I): wherein R1 and R2 are as defined in the specification, or a salt thereof, which is useful as a reagent (radiotracer) for VAChT mapping and the like, and can be used for positron emission tomography (PET), and a production method of the compound. Moreover, the present invention provides a diagnostic reagent for diagnosing cholinergic neurodegenerative disorders (e.g., Alzheimer's disease, memory disorder, learning disorder, schizophrenia, cognitive dysfunction, hyperactivity disorder, anxiety neurosis, depression, analgia, Parkinson's disease and the like) and the like, which contains the aforementioned compound.

    摘要翻译： 本发明提供由式（I）表示的新化合物：其中R1和R2如说明书中所定义，或其盐，其用作VAChT作图等的试剂（放射性示踪剂），并且可以是 用于正电子发射断层摄影（PET），以及该化合物的制备方法。 此外，本发明提供了用于诊断胆碱能神经变性疾病（例如阿尔茨海默病，记忆障碍，学习障碍，精神分裂症，认知功能障碍，多动障碍，焦虑性神经症，抑郁，肛门痛，帕金森病等）的诊断试剂， ，其含有上述化合物。

    Labeled compounds for measuring the function of the muscarinic acetylcholine nervous system
    5.
    发明授权
    Labeled compounds for measuring the function of the muscarinic acetylcholine nervous system 有权
    用于测量毒蕈碱性乙酰胆碱神经系统功能的标记化合物

    公开(公告)号：US06649142B2

    公开(公告)日：2003-11-18

    申请号：US10258061

    申请日：2002-10-18

    申请人： Hideo Tsukada ,  Kengo Sato ,  Shingo Nishiyama ,  Norihiro Harada

    发明人： Hideo Tsukada ,  Kengo Sato ,  Shingo Nishiyama ,  Norihiro Harada

    IPC分类号： A61K5100

    CPC分类号： C07D211/48 ,  A61K51/0455 ,  C07D211/42

    摘要： A muscarinic acetylcholine nervous system labeled compound for positron emission tomography measurement of the present invention has a structure represented by undermentioned general formula (I): [in the formula, W represents one selected from the group consisting of groups represented by undermentioned formulae (II) and (III): (in the formulae, R represents one selected from the group consisting of an 11C-labeled ethyl group and an 11C-labeled propyl group), and in the case that W is a group represented by above-mentioned formula (II), above-mentioned formula (I) is the (+)-isomer].

    摘要翻译： 本发明的用于正电子发射断层摄影测定的毒蕈碱性乙酰胆碱神经系统标记化合物具有下述通式（I）所示的结构：[式中，W表示选自下述式（II）表示的基团的一种， 和（III）:(式中，R表示选自由11 C标记的乙基和11 C标记的丙基组成的组中的一个），在W表示为 通过上述式（II），上述式（I）是（+） - 异构体]。

    Method of rapid methylation, kit for preparing PET tracer and method of producing PET tracer
    8.
    发明授权
    Method of rapid methylation, kit for preparing PET tracer and method of producing PET tracer 有权
    快速甲基化方法，制备PET示踪剂的试剂盒和生产PET示踪剂的方法

    公开(公告)号：US08288604B2

    公开(公告)日：2012-10-16

    申请号：US12438711

    申请日：2007-08-24

    申请人： Masaaki Suzuki ,  Hisashi Doi ,  Hideo Tsukada

    发明人： Masaaki Suzuki ,  Hisashi Doi ,  Hideo Tsukada

    IPC分类号： C07C2/60 ,  C07C2/68

    CPC分类号： C07B59/001 ,  C07B37/04 ,  C07B59/00 ,  C07B2200/05 ,  C07C1/321 ,  C07C17/263 ,  C07C29/32 ,  C07C41/30 ,  C07C67/343 ,  C07C205/06 ,  C07C2531/24 ,  C07C2601/16 ,  C07C25/13 ,  C07C22/08 ,  C07C33/03 ,  C07C69/76 ,  C07C43/205

    摘要： A method of rapid methylation of an aromatic compound or an alkenyl compound, which is capable of obtaining an aromatic compound or an alkenyl compound labeled with a methyl group or a fluoromethyl group under a mild condition rapidly in high yield using an organic boron compound whose toxicity is not so high as a substrate. A kit for preparing a PET tracer and a method of producing a PET tracer can be practiced using the rapid methylation method. In an aprotic polar solvent, methyl iodide or X—CH2F (wherein X is a functional group which can be easily released as an anion), and an organic boron compound in which an aromatic ring or an alkenyl group is attached to boron are subjected to cross-coupling in the presence of a palladium(0) complex, a phosphine ligand, and a base.

    摘要翻译： 芳族化合物或链烯基化合物的快速甲基化方法，其能够使用有机硼化合物以高收率快速地获得芳香族化合物或用甲基或氟甲基标记的烯基化合物，所述有机硼化合物的毒性 不如底物那么高。 用于制备PET示踪剂的试剂盒和生产PET示踪剂的方法可以使用快速甲基化方法来实施。 在非质子极性溶剂中，甲基碘或X-CH 2 F（其中X是可以容易地作为阴离子释放的官能团）和其中将芳环或烯基连接到硼上的有机硼化合物进行 在钯（0）络合物，膦配体和碱的存在下交联。

    Positron emission tomograph apparatus
    10.
    发明授权
    Positron emission tomograph apparatus 有权
    正电子发射断层摄影仪

    公开(公告)号：US07191109B2

    公开(公告)日：2007-03-13

    申请号：US10203161

    申请日：2001-01-29

    申请人： Hiroyuki Ohba ,  Hideo Tsukada

    发明人： Hiroyuki Ohba ,  Hideo Tsukada

    IPC分类号： G06G7/48 ,  G06G7/58 ,  A61K49/04

    CPC分类号： G01T1/2985 ,  A61B6/037

    摘要： In a PET apparatus 1, in a calculation processing unit 50, for each frame, radiation data for a region of interest K of a measurement-subjected part H is extracted, and then the optimum administration rate of a labeled substance T is calculated based on the radiation data such that the radiation concentration for the region of interest K will be steady regardless of the physiological state (blood flow rate etc.) of the subject S. In an administration rate control unit 60, feedback control of the administration rate of the labeled substance into the subject S is carried out based on the calculated optimum administration condition. As a result, the change in the amount accumulated of the labeled substance T in the region of interest K between before and after administration of a drug being tested Y can be obtained easily and precisely in real time as the amount of change in the radiation concentration, and it becomes possible to grasp the measurement results rapidly and easily.

    摘要翻译： 在PET装置1中，在计算处理单元50中，对于每帧，提取测量对象部分H的感兴趣区域K的辐射数据，然后基于 辐射数据，使得感兴趣区域K的辐射浓度将与受试者S的生理状态（血液流量等）无关。在给药率控制单元60中，反馈控制 基于计算的最佳给药条件进行标记物质进入受试者S. 结果，可以容易且精确地实时地获得在被测试药物Y给药前后的感兴趣区域K中的标记物质T的积累量的变化，因为辐射浓度的变化量 ，能够快速，容易地掌握测定结果。