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    Polyamine-substituted ligands for use as contrast agents
    2.
    发明申请
    Polyamine-substituted ligands for use as contrast agents 审中-公开
    用作造影剂的多胺取代的配体

    公开(公告)号：US20070202047A1

    公开(公告)日：2007-08-30

    申请号：US11649503

    申请日：2007-01-04

    申请人： Markus Wolf ,  Ulrike Bauder-Wust ,  Uwe Haberkorn ,  Michael Eisenhut ,  Walter Mier

    发明人： Markus Wolf ,  Ulrike Bauder-Wust ,  Uwe Haberkorn ,  Michael Eisenhut ,  Walter Mier

    IPC分类号： A61K49/10 ,  C07F5/00 ,  C07D257/02

    CPC分类号： C07D257/02 ,  A61K49/103 ,  A61K49/106

    摘要： The present invention relates to a polyamine-substituted ligand for the preparation of a contrast agent derived from a chelating molecule selected from the group consisting of 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) and diethylentriamine-pentaacetic acid (DTPA), wherein at least one of the carboxylic groups of the chelating molecule is reacted with an amine of formula HNR1R2 to form an amide bond, wherein R1, R2 are independently selected from the group consisting of H; (CH2)n—NR3R4; and R5; R3, R4 are independently selected from the group consisting of H; (CH2)m—NR6R7; and (CH2)m-1—CH3; R6, R7 are independently selected from the group consisting of H; and (CH2)o-1—CH3; n, m, o are independently 2, 3, or 4; R5 is of formula and optionally at least one of the carboxylic groups of the chelating molecule is further reacted with a monoalkylamine having 1 to 18 carbon atoms to form an amide bond; provided that at least one of R1, R2 is other than H. Furthermore, the invention relates to contrast agents for magnetic resonance imaging (MRI) comprising said ligands and in-vivo diagnostic methods based on MRI using said contrast agents.

    摘要翻译： 本发明涉及用于制备衍生自螯合分子的造影剂的多胺取代配体，所述螯合分子选自1,4,7,10-四氮杂环十二烷-1,4,7,10-四乙酸（DOTA ）和二乙基三胺五乙酸（DTPA），其中螯合分子的至少一个羧基与式HNR 1 R 2的胺反应形成 酰胺键，其中R 1，R 2，R 2独立地选自H; （CH 2）n - NR 3 - 3 - - - - - - - 和R 5; R 3，R 4，R 4独立地选自H; （CH 2 CH 2）m -NR 6 R 6 R 7 R 7， 和（CH 2 CH 2）m-1 -CH 3 3; R 6，R 7，R 7独立地选自H; 和（CH 2）2 -O-1 -CH 3; n，m，o分别为2,3或4; R 5是下式，并且任选地，螯合分子的至少一个羧酸基团与具有1至18个碳原子的单烷基胺进一步反应以形成酰胺键; 条件是R 1，R 2和R 2中的至少一个不是H.此外，本发明涉及用于包含所述配体的磁共振成像（MRI）的造影剂，并且在 - 使用所述造影剂的基于MRI的体内诊断方法。

    Labelling compounds for the simple synthesis of 3'-[18F]fluoro-3'-deoxythymidine and a method for the production thereof
    7.
    发明授权
    Labelling compounds for the simple synthesis of 3'-[18F]fluoro-3'-deoxythymidine and a method for the production thereof 有权
    用于简单合成3' - [18 F]氟-3'-脱氧胸苷的化合物及其制备方法

    公开(公告)号：US06891033B2

    公开(公告)日：2005-05-10

    申请号：US10470817

    申请日：2002-01-28

    申请人： Stefan Johannes Martin ,  Joseph Antonius Maria Eisenbarth ,  Ulrike Wagner-Utermann ,  Michael Eisenhut ,  Walter Mier

    发明人： Stefan Johannes Martin ,  Joseph Antonius Maria Eisenbarth ,  Ulrike Wagner-Utermann ,  Michael Eisenhut ,  Walter Mier

    IPC分类号： C07H19/06 ,  A61K31/7072

    CPC分类号： C07H19/06

    摘要： The application relates to compounds that are suitable as labelable precursors for synthesis of 3′-[18F]fluoro-3′-deoxythymidine and that have formula (1), in which R denotes triphenylmethyl, triphenylmethyl substituted in the phenyl group, trialkylmethyl, triphenylsilyl, triphenylsilyl substituted in the phenyl group, or trialkylsilyl, R′ denotes R1—SO2, where R1 is an unsubstituted or substituted C1 to C5 alkyl or an unsubstituted or substituted phenyl, and R″ denotes C2 to C10 alkyloxycarbonyl, with the exception of 3-N-Boc-1-(3-O-nosyl-5-O-trityl-2-deoxy-β-D-lyxofuranosy The application also relates to a method for preparation of these compounds and to the use of the same for synthesis of 3′-[18F]fluoro-3′-deoxythymidine.

    摘要翻译： 本申请涉及适用于合成3' - [16 F]氟-3'-脱氧胸苷的可标记前体的化合物，其具有式（1），其中R表示三苯基甲基，三苯基甲基取代的 在苯基中，三烷基甲基，三苯基甲硅烷基，苯基取代的三苯基甲硅烷基或三烷基甲硅烷基，R'表示R 1 -SO 2 - ，其中R 1， SUP>是未取代或取代的C 1至C 5烷基或未取代或取代的苯基，R“表示C 2至C 除了3-N-Boc-1-（3-O-壬基-5-O-三苯甲基-2-脱氧-β-D-吡喃葡萄糖醛酸之外），除了3-N-Boc- 1-烷氧基羰基外，本申请还涉及 制备这些化合物的方法及其用于合成3' - [[18 F]氟-3'-脱氧胸苷的方法。