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    CYCLOOXYGENASE-2 SELECTIVE AGENTS USEFUL AS IMAGING PROBES AND RELATED METHODS
    1.
    发明申请
    CYCLOOXYGENASE-2 SELECTIVE AGENTS USEFUL AS IMAGING PROBES AND RELATED METHODS 失效
    CYCLOOXYGENASE-2选择性试剂有用的成像探针和相关方法

    公开(公告)号：US20070286801A1

    公开(公告)日：2007-12-13

    申请号：US10341316

    申请日：2003-01-10

    申请人： Tatsushi Toyokuni ,  Nagichettiar Satyamurthy ,  Harvey Herschman ,  Michael Phelps ,  Jorge Barrio

    发明人： Tatsushi Toyokuni ,  Nagichettiar Satyamurthy ,  Harvey Herschman ,  Michael Phelps ,  Jorge Barrio

    IPC分类号： A61K51/00 ,  A61K31/42 ,  C07D261/06

    CPC分类号： A61K49/10 ,  A61K51/0453

    摘要： This invention provides novel cyclooxygenase-2 selective agents that are particularly useful as imaging probes in non-invasive imaging techniques, such as PET and SPECT. Preferred cyclooxygenase-2 selective agents inhibit cyclooxygenase-2 activity with greater potency and specificity than conventional cyclooxygenase-2 inhibitors. Other aspects of the invention include pharmaceutical compositions including the cyclooxygenase-2 selective agents as well as methods for detecting and/or inhibiting cyclooxygenase-2. These methods are particularly useful for diagnosing and treating disorders, such as inflammation, which is characterized by elevated cyclooxygenase-2 levels.

    摘要翻译： 本发明提供了新的环加氧酶-2选择剂，其特别可用作非侵入性成像技术如PET和SPECT中的成像探针。 优选的环氧合酶-2选择剂以比常规环加氧酶-2抑制剂更强的效力和特异性抑制环氧合酶-2活性。 本发明的其它方面包括包含环氧合酶-2选择剂的药物组合物以及用于检测和/或抑制环氧合酶-2的方法。 这些方法对于诊断和治疗诸如炎症的疾病特别有用，其特征在于环氧合酶-2水平升高。

    Cyclooxygenase-2 selective agents useful as imaging probes and related methods
    2.
    发明授权
    Cyclooxygenase-2 selective agents useful as imaging probes and related methods 失效
    可用作成像探针和相关方法的环氧合酶-2选择剂

    公开(公告)号：US07329401B2

    公开(公告)日：2008-02-12

    申请号：US10341316

    申请日：2003-01-10

    申请人： Tatsushi Toyokuni ,  Nagichettiar Satyamurthy ,  Harvey R. Herschman ,  Michael E. Phelps ,  Jorge R. Barrio

    发明人： Tatsushi Toyokuni ,  Nagichettiar Satyamurthy ,  Harvey R. Herschman ,  Michael E. Phelps ,  Jorge R. Barrio

    IPC分类号： A61K51/00 ,  A61M36/14

    CPC分类号： A61K49/10 ,  A61K51/0453

    摘要： This invention provides novel cyclooxygenase-2 selective agents that are particularly useful as imaging probes in non-invasive imaging techniques, such as PET and SPECT. Preferred cyclooxygenase-2 selective agents inhibit cyclooxygenase-2 activity with greater potency and specificity than conventional cyclooxygenase-2 inhibitors. Other aspects of the invention include pharmaceutical compositions including the cyclooxygenase-2 selective agents as well as methods for detecting and/or inhibiting cyclooxygenase-2. These methods are particularly useful for diagnosing and treating disorders, such as inflammation, which is characterized by elevated cyclooxygenase-2 levels.

    摘要翻译： 本发明提供了新的环加氧酶-2选择剂，其特别可用作非侵入性成像技术如PET和SPECT中的成像探针。 优选的环氧合酶-2选择剂以比常规环加氧酶-2抑制剂更强的效力和特异性抑制环氧合酶-2活性。 本发明的其它方面包括包含环加氧酶-2选择剂的药物组合物以及用于检测和/或抑制环氧合酶-2的方法。 这些方法对于诊断和治疗诸如炎症的疾病特别有用，其特征在于环氧合酶-2水平升高。

    MODULAR RADIOCHEMISTRY SYNTHESIS SYSTEM
    5.
    发明申请
    MODULAR RADIOCHEMISTRY SYNTHESIS SYSTEM 有权
    模块化放射化学合成系统

    公开(公告)号：US20120107175A1

    公开(公告)日：2012-05-03

    申请号：US13058526

    申请日：2009-08-19

    申请人： Nagichettiar Satyamurthy ,  Jorge R. Barrio ,  Bernard Amarasekera ,  R. Michael Van Dam ,  Sebastian Olma ,  Dirk Williams ,  Mark A. Eddings ,  Clifton Kwang-Fu Shen

    发明人： Nagichettiar Satyamurthy ,  Jorge R. Barrio ,  Bernard Amarasekera ,  R. Michael Van Dam ,  Sebastian Olma ,  Dirk Williams ,  Mark A. Eddings ,  Clifton Kwang-Fu Shen

    IPC分类号： G01N31/00 ,  G05B1/00

    CPC分类号： C07H19/16 ,  B01J19/004 ,  B01J19/126 ,  B01J2219/00049 ,  B01J2219/24 ,  C07B59/001 ,  C07B59/002 ,  C07B59/005 ,  C07B2200/05 ,  C07C201/06 ,  C07D207/46 ,  C07H5/02 ,  C07H19/06 ,  Y10T436/115831 ,  Y10T436/12

    摘要： A modular chemical production system includes multiple modules for performing a chemical reaction, particularly of radiochemical compounds, from a remote location. One embodiment comprises a reaction vessel including a moveable heat source with the position thereof relative to the reaction vessel being controllable from a remote position. Alternatively the heat source may be fixed in location and the reaction vial is moveable into and out of the heat source. The reaction vessel has one or more sealing plugs, the positioning of which in relationship to the reaction vessel is controllable from a remote position. Also the one or more reaction vessel sealing plugs can include one or more conduits there through for delivery of reactants, gases at atmospheric or an elevated pressure, inert gases, drawing a vacuum and removal of reaction end products to and from the reaction vial, the reaction vial with sealing plug in position being operable at elevated pressures. The modular chemical production system is assembled from modules which can each include operating condition sensors and controllers configured for monitoring and controlling the individual modules and the assembled system from a remote position. Other modules include, but are not limited to a Reagent Storage and Delivery Module, a Cartridge Purification Module, a Microwave Reaction Module, an External QC/Analysis/Purification Interface Module, an Aliquotting Module, an F-18 Drying Module, a Concentration Module, a Radiation Counting Module, and a Capillary Reactor Module.

    摘要翻译： 模块化化学生产系统包括从远程位置进行化学反应，特别是放射化学化合物的多个模块。 一个实施例包括一个包括可移动热源的反应容器，其相对于反应容器的位置可从远程位置控制。 或者，热源可以固定在位置，并且反应小瓶可移动进入和离开热源。 反应容器具有一个或多个密封塞，其与反应容器相关的定位可从远程位置控制。 此外，一个或多个反应容器密封塞可以包括一个或多个导管，用于输送反应物，大气压或高压气体，惰性气体，抽真空和从反应小瓶中除去反应终产物， 具有密封塞位置的反应小瓶可在升高的压力下操作。 模块化化学生产系统由模块组装，每个模块可以包括操作状态传感器和配置成用于从远程位置监控和控制各个模块和组装系统的控制器。 其他模块包括但不限于试剂储存和输送模块，滤芯净化模块，微波反应模块，外部QC /分析/纯化界面模块，等分模块，F-18干燥模块，浓缩模块 ，辐射计数模块和毛细管反应堆模块。

    Compositions for labeling β-amyloid plaques and neurofibrillary tangles
    7.
    发明授权
    Compositions for labeling β-amyloid plaques and neurofibrillary tangles 有权

    公开(公告)号：US07341709B2

    公开(公告)日：2008-03-11

    申请号：US10680818

    申请日：2003-10-07

    申请人： Jorge R. Barrio ,  Andrej Petric ,  Nagichettiar Satyamurthy ,  Gary W. Small ,  Gregory M. Cole ,  Sung-Cheng Huang

    发明人： Jorge R. Barrio ,  Andrej Petric ,  Nagichettiar Satyamurthy ,  Gary W. Small ,  Gregory M. Cole ,  Sung-Cheng Huang

    IPC分类号： A61K51/00

    CPC分类号： A61K51/0406 ,  A61K51/0455 ,  A61K51/0459

    摘要： Compositions useful for labeling β-amyloid plaques and neurofibrillary tangles are provided. The compositions comprises compounds of formula (I): wherein R1 is selected from the group consisting of —C(O)-alkyl, —C(O)-alkylenyl-R4, —C(O)O-alkyl, —C(O)O-alkylenyl-R4, —C═C(CN)2-alkyl, —C═C(CN)2-alkylenyl-R4, wherein R4 is a radical selected from the group consisting of alkyl, substituted alkyl, aryl and substituted aryl; R5 is a radical selected from the group consisting of —NH2, —OH, —SH, —NH-alkyl, —NHR4, —NH-alkylenyl-R4, —O-alkyl, —O-alkylenyl-R4, —S-alkyl, and —S-alkylenyl-R4; R6 is a radical selected from the group consisting of —CN, —COOH, —C(O)O-alkyl, —C(O)O-alkylenyl-R4, —C(O)-alkyl, —C(O)-alkylenyl-R4, —C(O)-halogen, —C(O)NH-alkyl, —C(O)NH-alkylenyl-R4 and —C(O)NH2; R7 is a radical selected from the group consisting of O, NH, and S; and R8 is N, O or S; and R2 is selected from the group consisting of alkyl and alkylenyl-R10 and R3 is alkylenyl-R10, wherein R10 is selected from the group consisting of —OH, —OTs, halogen, spiperone, spiperone ketal, and spiperone-3-yl, or R2 and R3 together form a heterocyclic ring, optionally substituted with at least one radical selected from the group consisting of alkyl, alkoxy, OH, OTs, halogen, alkyl-R10, carbonyl, spiperone, spiperone ketal and spiperone-3-yl, and further wherein one or more of the hydrogen, halogen or carbon atoms are optionally replaced with a radiolabel.

    8-fluoropurine compounds
    8.
    发明授权
    8-fluoropurine compounds 有权
    8-氟嘌呤化合物

    公开(公告)号：US06262254B1

    公开(公告)日：2001-07-17

    申请号：US09199975

    申请日：1998-11-25

    申请人： Jorge R. Barrio ,  Nagichettiar Satyamurthy ,  Mohammad Namavari ,  Michael E. Phelps

    发明人： Jorge R. Barrio ,  Nagichettiar Satyamurthy ,  Mohammad Namavari ,  Michael E. Phelps

    IPC分类号： C07H19167

    CPC分类号： C07D473/00

    摘要： An efficient, regiocontrolled approach to the synthesis of 8-fluoropurines by direct fluorination of purines with dilute elemental fluorine, or acetyl hypofluorite, is provided. In a preferred embodiment, a purine compound is dissolved in a polar solvent and reacted with a dilute mixture of F2 in He or other inert gas.

    摘要翻译： 提供了通过用稀释的元素氟或乙酰基次氟酸直接氟化嘌呤来合成8-氟嘌呤的有效的区域控制方法。 在一个优选的实施方案中，将嘌呤化合物溶解在极性溶剂中并与F 2在He或其它惰性气体中的稀混合物反应。

    Methods for labeling &bgr;-amyloid plaques and neurofibrillary tangles
    10.
    发明授权
    Methods for labeling &bgr;-amyloid plaques and neurofibrillary tangles 有权
    β-淀粉样蛋白斑和神经原纤维缠结的标记方法

    公开(公告)号：US06274119B1

    公开(公告)日：2001-08-14

    申请号：US09378662

    申请日：1999-08-20

    申请人： Jorge R. Barrio ,  Andrej Petric ,  Nagichettiar Satyamurthy ,  Gary W. Small ,  Gregory M. Cole ,  Sung-Cheng Huang

    发明人： Jorge R. Barrio ,  Andrej Petric ,  Nagichettiar Satyamurthy ,  Gary W. Small ,  Gregory M. Cole ,  Sung-Cheng Huang

    IPC分类号： A61K5100

    CPC分类号： A61K51/0406 ,  A61K51/0455 ,  A61K51/0459

    摘要： A method for labeling &bgr;-amyloid plaques and neurofibrillary tangles in vivo and in vitro, comprises contacting a compound of formula (I): with mammalian tissue. In formula (I), R1 is selected from the group consisting of —C(O)-alkyl, —C(O)-alkylenyl-R4, —C(O)O-alkyl, —C(O)O-alkylenyl-R4, —C═C(CN)2-alkyl, —C═C(CN)2-alkylenyl-R4 , R4 is a radical selected from the group consisting of alkyl, substituted alkyl, aryl and substituted aryl; R5, is a radical selected from the group consisting of —NH2, —OH, —SH, —NH-alkyl, —NHR4, —NH-alkylenyl-R4, —O-alkyl, —O-alkylenyl-R4, —S-alkyl, and —S-alkylenyl-R4; R6 is a radical selected from the group consisting of —CN, —COOH, —C(O)O-alkyl, —C(O)O-alkylenyl-R4, —C(O)-alkyl, —C(O)-alkylenyl-R4, —C(O)-halogen, —C(O)NH , —C(O)NH-alkyl, —C(O)NH-alkylenyl-R4; R7 is a radical selected from the group consisting of O, NH, and S; and R8 is N, O or S. R2 and R3 are each independently selected from the group consisting of alkyl and alkylenyl-R10, wherein R10 is selected from the group consisting of —OH, —OTs, halogen, spiperone, spiperone ketal and spiperone-3-yl. Alternatively, R2 and R3 together form a heterocyclic ring, optionally substituted with at least one radical selected from the group consisting of alkyl, alkoxy, OH, OTs, halogen, alkylenyl-R10, carbonyl, spiperone, spiperone ketal and spiperone-3-yl. In the compounds of formula (I), one or more of the hydrogen, halogen or carbon atoms can, optionally, be replaced with a radiolabel.

    摘要翻译： 一种用于在体内和体外标记β-淀粉样蛋白斑和神经原纤维缠结的方法，包括使式（I）化合物与哺乳动物组织接触。 在式（I）中，R 1选自-C（O） - 烷基，-C（O） - 亚烷基基-R 4，-C（O）O-烷基，-C（O）O-亚烷基 - R4，-C = C（CN）2-烷基，-C = C（CN）2 - 亚烷基-R4，R4为选自烷基，取代烷基，芳基和取代芳基的基团; R5是选自-NH 2，-OH，-SH，-NH-烷基，-NHR 4，-NH-亚烷基-R 4，-O-烷基，-O-亚烷基基-R 4，-S- 烷基和-S-亚烷基基-R4; R6是选自-CN，-COOH，-C（O）O-烷基，-C（O）O-亚烷基-R4，-C（O） - 烷基，-C（O） - 亚烷基-R4，-C（O） - 卤素，-C（O）NH，-C（O）NH-烷基，-C（O）NH-亚烷基基-R4; R7是选自O，NH和S的基团; 并且R 8是N，O或S.R 2和R 3各自独立地选自烷基和亚烷基-R 10，其中R 10选自-OH，-OT，卤素，螺哌
    酮，螺哌酮缩酮和螺哌隆 -3-基。 或者，R2和R3一起形成杂环，任选被至少一个选自烷基，烷氧基，OH，OT，卤素，亚烷基-R 10，羰基，螺哌
    酮，螺哌酮缩酮和螺哌酮-3-基 。 在式（I）的化合物中，氢，卤素或碳原子中的一个或多个可以任选地被放射性标记代替。