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    • 37. 发明公开
    • CONTRAST AGENTS
    • 对比剂
    • EP2245003A2
    • 2010-11-03
    • EP09715655.8
    • 2009-02-26
    • GE Healthcare ASPriebe, Hanno
    • PRIEBE, Hanno
    • C07C235/66C07C235/84C07D309/10C07C233/09A61K49/04
    • A61K49/04A61K49/0438B22D11/1287B23K9/048B23K35/02B23K35/0261B23K35/30B23K35/3086B23K2201/04B23K2203/04C07C235/66C07C235/84C07D309/10C22C38/18C22C38/26
    • The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds. More specifically the iodine containing compounds are chemical compounds containing two linked iodinated phenyl groups of the general formula R-N(CO-CH
      3 ) — X— N(CO-CH
      3 )- R and salts or optical active isomers thereof, wherein X denotes a divalent linking moiety with 5 to 10 bridge elements of carbon, oxygen, sulphur and nitrogen separating the acetylated nitrogen atoms, and which may be further substituted by hydroxyl groups, by C
      1 to C
      4 alkyl moieties optionally substituted by hydroxyl groups, by C
      1 to C
      4 alkoxy groups, by amino groups and by C
      1 to C
      4 alkylamino groups, and wherein 2 or 3 carbon bridge elements together with alkyl or alkoxy groups form a cyclopentane, cyclohexane, pentahydropyran or tetrahydrofuran entity which may be alkyl- or hydroxyalkyl- substituted and each R denotes a triiodinated phenyl residue further substituted by hydrophilic moieties. The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging and in particular in X-ray imaging, and to contrast media containing such compounds.
    • 本发明涉及一类化合物和含有这些化合物的诊断组合物,其中化合物是含碘化合物。 更具体地说,含碘化合物是含有两个通式为RN(CO-CH 3)-X-N(CO-CH 3)-R的连接碘化苯基的化合物及其盐或光学活性异构体,其中X表示 二价连接部分与碳原子,氧原子,硫原子和氮原子的5至10个桥联元素分隔乙酰化的氮原子,并且可以被羟基进一步取代,被C 1至C 4烷基部分任选地被羟基取代,被C 1 至C 4烷氧基,氨基和C 1至C 4烷基氨基,并且其中2或3个碳桥基与烷基或烷氧基一起形成环戊烷,环己烷,五氢吡喃或四氢呋喃实体,其可以是烷基或羟烷基 - 取代的并且每个R表示进一步被亲水部分取代的三碘代苯基残基。 本发明还涉及这种诊断组合物作为造影剂在诊断成像中,特别是在X射线成像中的用途,以及含有这种化合物的造影剂。
    • 39. 发明公开
    • Method of magnetic resonance investigation with hyperpolarised contrast agents
    • Verfahren zur Herstellung eines hyperpolarisierten Kontrastmittels
    • EP2119457A1
    • 2009-11-18
    • EP09009608.2
    • 1998-12-23
    • GE Healthcare AS
    • Ardenkjaer-Larsen, Jan HenrikAxelsson, OskarGolman, KlaesHansson, GeorgLeunbach, IbPetersson, StefanWistrand, Lars-Göran
    • A61K49/06A61K49/08G01R33/28G01R33/62
    • G01R33/5601A61K49/08A61K49/10A61K49/18A61K49/1815G01R33/282G01R33/62
    • This invention provides a method of magnetic resonance investigation of a sample, preferably of a human or non-human animal body, said method comprising:
      (i) producing a hyperpolarised solution of a high T 1 agent by dissolving in a physiologically tolerable solvent a hyperpolarised solid sample of said high T 1 agent;
      (ii) where the hyperpolarisation of the solid sample of said high T 1 agent in step (i) is effected by means of a polarising agent, optionally separating the whole, substantially the whole, or a portion of said polarising agent from said high T 1 agent;
      (iii) administering said hyperpolarised solution to said sample;
      (iv) exposing said sample to a second radiation of a frequency selected to excite nuclear spin transitions in selected nuclei eg the MR imaging nuclei of the high T 1 agent;
      (v) detecting magnetic resonance signals from said sample; and
      (vi) optionally, generating an image, dynamic flow data, diffusion data, perfusion data, physiological data (eg. pH, pO 2 , pCO 2 , temperature or ionic concentrations) or metabolic data from said detected signals,

      wherein said high T 1 agent in said hyperpolarised solution has a T 1 value (at a field strength in the range 0.01-5T and a temperature in the range 20-40°C) of at least 5 seconds.
    • 本发明提供了一种样品,优选人或非人动物体的磁共振研究方法,所述方法包括:(i)通过将高T 1试剂溶解在生理上可耐受的溶剂中制成超极化溶液 所述高T 1试剂的固体样品; (ii)其中步骤(i)中所述高T 1试剂的固体样品的超极化是通过偏振剂进行的,任选地从所述高T分离整个,基本上全部或部分所述偏振剂 1代理; (iii)将所述超极化溶液施用于所述样品; (iv)将所述样品暴露于所选频率的第二辐射,以激发所选择的核中的核自旋跃迁,例如高T 1试剂的MR成像核; (v)检测来自所述样品的磁共振信号; 和(vi)可选地,从所述检测到的信号生成图像,动态流动数据,扩散数据,灌注数据,生理数据(例如pH,pO 2,pCO 2,温度或离子浓度)或代谢数据,其中所述高T 所述超极化溶液中的一种试剂具有至少5秒的T 1值(在0.011-5T的范围内的场强和20-40℃的温度)。