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    COMPOUNDS AND THEIR SYNTHESIS
    51.
    发明公开
    COMPOUNDS AND THEIR SYNTHESIS 审中-公开
    VERBINDUNGEN UND DEREN SYNTHESE

    公开(公告)号：EP2906548A1

    公开(公告)日：2015-08-19

    申请号：EP13783361.2

    申请日：2013-10-14

    申请人： UCL Business Plc.

    发明人： ARSTAD, Erik ,  SANDER, Kerstin ,  GENDRON, Thibault

    IPC分类号： C07D333/74 ,  C07D333/76 ,  C07D401/06 ,  C07C381/12 ,  C07D207/46 ,  C07D211/22 ,  C07D211/70 ,  C07D213/70 ,  A61K51/04 ,  A61K51/06 ,  A61K51/08

    CPC分类号： C07C381/12 ,  B01D15/08 ,  B01J20/22 ,  C07B59/001 ,  C07B59/002 ,  C07C17/361 ,  C07C25/13 ,  C07C45/65 ,  C07C47/55 ,  C07C49/807 ,  C07C67/317 ,  C07C69/78 ,  C07D207/46 ,  C07D211/20 ,  C07D211/22 ,  C07D211/32 ,  C07D211/70 ,  C07D213/61 ,  C07D213/70 ,  C07D333/74 ,  C07D333/76 ,  C07D401/06 ,  C07D403/06

    摘要： The present invention relates to sulfonium salts of formula (I): (I), their preparation, and utility as precursors for preparing functionalised organic compounds, wherein R1 and R2 are the same or different and each is independently selected from an optionally substituted aryl group, an optionally substituted alkynyl group, an optionally substituted alkenyl group, an optionally substituted alkyl group, an optionally substituted cycloalkyl group, an optionally substituted cycloalkenyl group, an optionally substituted aralkyl group, an optionally substituted arylalkenyl group, an optionally substituted heteroaryl group, an optionally substituted heterocyclyl group, an optionally substituted amine, an optionally substituted alkoxy group, an optionally substituted thioether group, an optionally substituted phosphine group, an optionally substituted boron species, an optionally substituted carbene, an organometallic moiety, and a halide, or R1 and R2 are joined together to form an optionally substituted sulfur-containing ring; W is a bond, an optionally substituted alkynylene group, an optionally substituted alkenylene group, and optionally substituted alkylene group, an optionally substituted heterocyclyl group, an optionally substituted aryl group or an optionally substituted heteroaryl group; R3 is a moiety comprising at least one basic group, provided that when R3 does not contain any carbon atoms, W is not a bond; X is an anionic species; and n is an integer selected from 1 to 5.

    摘要翻译： 本发明涉及式（I）的锍盐：（I），其制备和用作制备官能化有机化合物的前体，其中R 1和R 2相同或不同，并且各自独立地选自任选取代的芳基 ，任选取代的炔基，任选取代的烯基，任选取代的烷基，任选取代的环烷基，任选取代的环烯基，任选取代的芳烷基，任选取代的芳基烯基，任选取代的杂芳基， 任选取代的杂环基，任选取代的胺，任选取代的烷氧基，任选取代的硫醚基，任选取代的膦基，任选取代的硼种，任选取代的卡宾，有机金属部分和卤化物，或R 1和 R2连接在一起形成一个选项 取代的含硫环; W是键，任选取代的亚炔基，任选取代的亚烯基和任选取代的亚烷基，任选取代的杂环基，任选取代的芳基或任选取代的杂芳基; R3是包含至少一个碱性基团的部分，条件是当R3不含任何碳原子时，W不是键; X是阴离子物种; n为1〜5的整数。

    PET/SPECT AGENTS FOR APPLICATIONS IN BIOMEDICAL IMAGING
    57.
    发明公开
    PET/SPECT AGENTS FOR APPLICATIONS IN BIOMEDICAL IMAGING 有权
    PET / SPECT-MITTELFÜRANWENDUNGEN IN DER BIOMEDIZINISCHEN BILDGEBUNG

    公开(公告)号：EP2673257A4

    公开(公告)日：2014-11-12

    申请号：EP12744282

    申请日：2012-02-10

    申请人： UNIV WASHINGTON

    发明人： SHARMA VIJAY ,  SIVAPACKIAM JOTHILINGAM ,  PIWNICA-WORMS DAVID

    IPC分类号： C07C211/49 ,  C05D9/00 ,  C07F5/00

    CPC分类号： A61K51/0478 ,  C05D9/02 ,  C07B59/001 ,  C07B59/002 ,  C07C251/24 ,  C07F5/003

    摘要： Tracers that can be used for PET or SPECT imaging of the distribution of Pgp are disclosed. The tracers are metalloprobes that can comprise a radioactive metal ion such as 67Ga or 68Ga. Methods of synthesizing the tracers, and methods of imaging heart and other tissues are also disclosed. The tracers can be used to obtain high signal-to-background ratios for imaging tissues in vivo such as heart or tumor tissue. In various embodiments, disclosed tracers can exhibit, a) enhanced first pass extraction into heart tissue compared to presently available probes, b) linearity with true blood flow, c) enhanced detection of myocardial viability compared to presently available probes, d) reduced liver retention compared to presently available probes, and e) more efficient clearance from non-cardiac and adjoining tissues compared to presently available probes.

    摘要翻译： 公开了可用于Pgp分布的PET或SPECT成像的示踪剂。 示踪剂是可以包含放射性金属离子如67Ga或68Ga的金属杂酚。 还公开了合成示踪剂的方法，以及心脏和其他组织成像方法。 示踪剂可用于获得体内成像组织（例如心脏或肿瘤组织）的高信噪比。 在各种实施方案中，所公开的示踪剂可以显示a）与目前可用的探针相比，增强的第一次通过提取到心脏组织中，b）具有真实血流的线性，c）与目前可用的探针相比增强了心肌存活力的检测，d） 与目前可用的探针相比，和e）与目前可用的探针相比，非心脏和邻近组织的更有效的清除。

    RADIOLABELLED GLUTAMINYL CYCLASE INHIBITORS
    59.
    发明公开
    RADIOLABELLED GLUTAMINYL CYCLASE INHIBITORS 审中-公开
    放射性标记的谷氨酰胺环化酶抑制剂

    公开(公告)号：EP2714098A1

    公开(公告)日：2014-04-09

    申请号：EP12723476.3

    申请日：2012-05-24

    申请人： Probiodrug AG

    发明人： HEISER, Ulrich ,  RAMSBECK, Daniel ,  DEMUTH, Hans-Ulrich

    IPC分类号： A61K51/04 ,  A61K101/00

    CPC分类号： A61K51/0453 ,  C07B59/002

    摘要： Radiolabeled glutaminylcyclase (QC) inhibitors as imaging agents, in particular, but not exclusively, as medical imaging agents for the detection of neurological disorders; and pharmaceutical compositions, methods and kits for detecting neurological disorders, using the radiolabeled inhibitors.

    摘要翻译： 本发明涉及放射性标记的谷氨酰胺酰基环化酶（QC）抑制剂作为成像剂的用途，特别是但不仅限于用于检测神经疾病的医学成像剂。 本发明还涉及包含所述放射性标记的抑制剂的药物组合物以及用于检测神经障碍的方法和试剂盒。