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2. 发明申请

WO2013062751A1 FLUORINE-18 LABELED HYDROGEN ION PROBES 审中-公开
标题翻译：氟代-18标记氢离子探针
公开(公告)号：WO2013062751A1
公开(公告)日：2013-05-02
申请号：PCT/US2012/059322
申请日：2012-10-09
申请人： THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
发明人： KACHUR, Alexander, Victor , POPOV, Anatoliy, V. , DELIKATNY, Edward, James , KARP, Joel, S.
IPC分类号： A61Q5/10
CPC分类号： A61K51/04 , A61K51/0438 , C07B59/001 , C09B11/06 , C09B11/08
摘要： Fluorine-containing molecules include fluorine-18 labeled hydrogen ion indicator molecules and methods of making and using the same. Fluorine atoms incorporated into the indicator molecules provides novel structural modifications to the precursor molecules, shifting the absorbance maxima relative to their non-fluorinated precursor / cogeners. These molecules are useful for non-invasive in vivo measurement of blood volume, blood flow and pH in biological objects. Compounds are functionalized by a radioisotopically enriched fluorine-18 label and indicator molecule with structure derived from triarylmethane derived indicators, such as phenol red, cresol red, cresol purple, thymol blue, bromophenol red, naphthol blue, phenolphthalein, cresolphthalein, thymolphthalein, naphtholphthalein, gentian violet (methyl violet 10B), methyl violet 2B, methyl violet 6B, leucomalachite green (malachite green), brilliant green, pararosaniline, fuchsines, or salts thereof. During its radioactive decay, fluorine-18 produces high-energy positrons, which can be detected by positron emission tomography (PET) or single photon emission computer tomography (SPECT).
摘要翻译：含氟分子包括氟-18标记的氢离子指示剂分子及其制备和使用方法。结合到指示剂分子中的氟原子为前体分子提供新的结构修饰，相对于它们的非氟化前体/同族物移动吸光度最大值。这些分子可用于非侵入性体内测量生物体内血容量，血流量和pH值。化合物通过放射性同位素富集的氟-18标记和指示剂分子进行官能化，其具有衍生自三芳基甲烷衍生指标的结构，例如酚红，甲酚红，甲酚紫，百里酚蓝，溴酚红，萘酚蓝，酚酞，甲酚酞，百里酚酞，萘酚酞，龙胆紫（甲基紫10B），甲基紫2B，甲基紫6B，白蛋白绿（孔雀石绿），亮绿色，对苯二胺，紫红色或其盐。在其放射性衰变期间，氟-18产生高能正电子，其可以通过正电子发射断层扫描（PET）或单光子发射计算机断层摄影（SPECT）检测。

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