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    Systems and methods for high-resolution in vivo imaging of biochemical activity in a living organism
    1.
    发明授权
    Systems and methods for high-resolution in vivo imaging of biochemical activity in a living organism 失效
    生物体内生物化学活性高分辨率体内成像的系统和方法

    公开(公告)号：US07303741B2

    公开(公告)日：2007-12-04

    申请号：US10252311

    申请日：2002-09-23

    申请人： Ileana Hancu ,  Mohan Mark Amaratunga ,  Denyce Kramer Wicht ,  Paritosh Dhawale ,  Nadeem Ishaque ,  Faisal Ahmed Syud ,  Bruce Fletcher Johnson ,  Amy Casey Williams

    发明人： Ileana Hancu ,  Mohan Mark Amaratunga ,  Denyce Kramer Wicht ,  Paritosh Dhawale ,  Nadeem Ishaque ,  Faisal Ahmed Syud ,  Bruce Fletcher Johnson ,  Amy Casey Williams

    IPC分类号： A61B5/055

    CPC分类号： A61K49/0056 ,  A61K49/0002 ,  A61K49/0032 ,  A61K49/085 ,  A61K49/10 ,  A61K49/14

    摘要： This invention relates to bifunctional detection agents useful for providing high-resolution, in vivo imaging of biochemical activity in a living organism. Methods of using these bifunctional detection agents may comprise administering them into a living organism, and then estimating the localization of the detection agent using one modality (i.e., MRI), while concurrently estimating the level of biological activity using a second modality (i.e., optical imaging). One of the bifunctional detection agents comprises a magnetic resonance component and an optical imaging component. The magnetic resonance component comprises a contrast agent that is always activated or “on”. The optical imaging component comprises an activatable contrast agent or dye that is activated or turned “on” only in the presence of a particular event. For example, the optical imaging component may be activated by a certain wavelength of light and (1) by the presence of a particular biochemical marker, (2) by enzyme cleavage, or (3) by a change in the temperature or pH of the surrounding medium. These bifunctional detection agents allow both anatomical and functional/metabolic information to be obtained simultaneously.

    摘要翻译： 本发明涉及用于提供生物体内生化活性的高分辨率体内成像的双功能检测剂。 使用这些双功能检测剂的方法可以包括将它们施用于活生物体中，然后使用一种模态（即，MRI）估计检测剂的定位，同时使用第二模态估计生物活性的水平（即，光学 成像）。 双功能检测剂之一包括磁共振成分和光学成像成分。 磁共振成分包括始终被激活或“开启”的造影剂。 光学成像组件包括可激活的造影剂或染料，其仅在特定事件的存在下被激活或变为“开启”。 例如，光学成像组件可以被一定波长的光激活，并且（1）存在特定的生物化学标记，（2）通过酶切割，或（3）通过温度或pH的变化 周围介质。 这些双功能检测剂允许同时获得解剖学和功能性/代谢信息。

    ALPHA-FLUOROALKYL DIHYDROTETRABENAZINE IMAGING AGENTS AND PROBES
    4.
    发明申请
    ALPHA-FLUOROALKYL DIHYDROTETRABENAZINE IMAGING AGENTS AND PROBES 失效
    ALPHA-FLOOROALKYL DIHYDROTETRABENAZINE成像剂和探针

    公开(公告)号：US20090142276A1

    公开(公告)日：2009-06-04

    申请号：US12174167

    申请日：2008-07-16

    申请人： Michael James Rishel ,  Bruce Fletcher Johnson ,  Kande Kankanamalage Dayarathna Amarasinghe ,  Sean Richard Dinn

    发明人： Michael James Rishel ,  Bruce Fletcher Johnson ,  Kande Kankanamalage Dayarathna Amarasinghe ,  Sean Richard Dinn

    IPC分类号： C07D455/06 ,  A61K49/04

    CPC分类号： C07D471/04 ,  A61K51/0455 ,  C07B2200/05

    摘要： The present invention provides novel alpha-fluoroalkyl dihydrotetrabenazine compounds I wherein R1 is a C1-C10 fluorinated aliphatic radical; R2 is hydrogen or a C1-C10 aliphatic radical; R3 is hydrogen or a C1-C10 aliphatic radical; and R4 is a C1-C10 aliphatic radical, a C3-C10 cycloaliphatic radical, or a C3-C10 aromatic radical. The alpha-fluoroalkyl dihydrotetrabenazine compounds are provided in both racemic and enantiomerically enriched forms and may comprise either or both of fluorine-18 and fluorine 19. The alpha-fluoroalkyl dihydrotetrabenazine compounds are believed to possess high affinity for VMAT-2, a biomarker implicated in human diabetes. The alpha-fluoroalkyl dihydrotetrabenazine compounds comprising a fluorine-18 group are useful as PET imaging agents targeting the VMAT-2 biomarker. The non-radiolabled alpha-fluoroalkyl dihydrotetrabenazine compounds are useful as probes for the discovery of PET imaging agents.

    摘要翻译： 本发明提供新的α-氟烷基二氢丁苯那嗪化合物I，其中R1是C1-C10氟化脂族基; R2是氢或C1-C10脂族基; R3是氢或C1-C10脂族基; 并且R 4是C 1 -C 10脂族基团，C 3 -C 10脂环族基团或C 3 -C 10芳族基团。 α-氟烷基二氢丁苯那嗪化合物以外消旋和对映异构体富集的形式提供，并且可以包含氟-18和氟19中的任一种或两者。认为α-氟烷基二氢丁苯那嗪化合物对VMAT-2具有高亲和力，VMAT-2是涉及 人类糖尿病 包含氟-18基团的α-氟烷基二氢丁苯那嗪化合物可用作靶向VMAT-2生物标志物的PET显像剂。 非放射性α-氟烷基二氢丁苯那嗪化合物可用作发现PET成像剂的探针。

    FLUORINATED DIHYDROTETRABENAZINE ETHER IMAGING AGENTS AND PROBES
    5.
    发明申请
    FLUORINATED DIHYDROTETRABENAZINE ETHER IMAGING AGENTS AND PROBES 有权
    氟化二氢异喹啉醚成像剂和探针

    公开(公告)号：US20090110636A1

    公开(公告)日：2009-04-30

    申请号：US11923926

    申请日：2007-10-25

    申请人： Kande Kankanamalage Dayarathna Amarasinghe ,  Michael James Rishel ,  Sean Richard Dinn ,  Bruce Fletcher Johnson

    发明人： Kande Kankanamalage Dayarathna Amarasinghe ,  Michael James Rishel ,  Sean Richard Dinn ,  Bruce Fletcher Johnson

    IPC分类号： A61K51/04 ,  C07D455/06

    CPC分类号： C07D455/06 ,  A61K51/0455

    摘要： The present invention provides novel fluorinated ether compounds having structure I wherein R1 is a C2-C10 fluorinated aliphatic radical; R2 is a C1-C10 aliphatic radical, or a C3-C10 cycloaliphatic radical; R3 is hydrogen or a C1-C10 aliphatic radical; and R4 is hydrogen or a C1-C10 aliphatic radical. The fluorinated ether compounds are provided in both racemic and enantiomerically enriched forms and may comprise either or both of fluorine-18 and fluorine 19. The fluorinated ether compounds are shown to possess high affinity for VMAT-2, a biomarker implicated in human diabetes. The fluorinated ether compounds comprising a fluorine-18 group are useful as PET imaging agents targeting the VMAT-2 biomarker. The non-radiolabeled fluorinated ether compounds are useful as probes for the discovery of PET imaging agents.

    摘要翻译： 本发明提供具有结构I的新型氟化醚化合物，其中R 1是C 2 -C 10氟化脂族基; R2是C1-C10脂族基团，或C3-C10脂环族基团; R3是氢或C1-C10脂族基; 并且R 4是氢或C 1 -C 10脂族基。 氟化醚化合物以外消旋和对映异构体富集的形式提供，并且可以包含氟-18和氟19中的任一种或两者。显示氟化醚化合物对于涉及人类糖尿病的生物标志物VMAT-2具有高亲和力。 包含氟-18基团的氟化醚化合物可用作靶向VMAT-2生物标志物的PET显像剂。 非放射性标记的氟化醚化合物可用作发现PET成像剂的探针。

    Method and catalyst system for producing aromatic carbonates
    9.
    发明授权
    Method and catalyst system for producing aromatic carbonates 失效
    用于生产芳族碳酸酯的方法和催化剂体系

    公开(公告)号：US06372683B2

    公开(公告)日：2002-04-16

    申请号：US09757247

    申请日：2001-01-10

    申请人： Kirill Vladimirovich Shalyaev ,  Grigorii Lev Soloveichik ,  Bruce Fletcher Johnson ,  Donald Wayne Whisenhunt, Jr.

    发明人： Kirill Vladimirovich Shalyaev ,  Grigorii Lev Soloveichik ,  Bruce Fletcher Johnson ,  Donald Wayne Whisenhunt, Jr.

    IPC分类号： B01J3100

    CPC分类号： C07C68/005 ,  C07C69/96

    摘要： A method and catalyst system for producing aromatic carbonates from aromatic hydroxy compounds. In one embodiment, the method includes the step of contacting at least one aromatic hydroxy compound with oxygen and carbon monoxide in the presence of a carbonylation catalyst system having catalytic amounts of the following components: a Group VIII B metal source; a combination of inorganic co-catalysts including a copper source and at least one of a titanium source or a zirconium source; an onium chloride composition; and a base. Alternative embodiments include inorganic co-catalyst combinations of a lead source and at least one of a titanium source or a manganese source.

    摘要翻译： 用于由芳族羟基化合物制备芳族碳酸酯的方法和催化剂体系。 在一个实施方案中，该方法包括在具有催化量的以下组分的羰基化催化剂体系的存在下使至少一种芳族羟基化合物与氧和一氧化碳接触的步骤：VIIIB族金属源; 包括铜源和至少一种钛源或锆源的无机助催化剂的组合; 氯化铟组合物; 和一个基地。 替代实施方案包括铅源和钛源或锰源中的至少一种的无机助催化剂组合。