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发明授权
US09133143B2 (3-fluoro-2-hydroxy)propyl-functionalized aryl derivatives or pharmaceutically acceptable salts thereof, method for preparing same, and pharmaceutical composition containing same as active ingredient for the diagnosis or treatment of neurodegenerative brain diseases 有权
（3-氟-2-羟基）丙基官能化的芳基衍生物或其药学上可接受的盐，其制备方法和含有作为神经变性性脑病诊断或治疗的活性成分的药物组合物

(3-fluoro-2-hydroxy)propyl-functionalized aryl derivatives or pharmaceutically acceptable salts thereof, method for preparing same, and pharmaceutical composition containing same as active ingredient for the diagnosis or treatment of neurodegenerative brain diseases
摘要：
The present invention relates to (3-fluoro-2-hydroxy)propyl-functionalized aryl derivatives or to the pharmaceutically acceptable salt thereof, to a method for preparing same, and to a pharmaceutical composition containing same as active ingredients for the diagnosis or treatment of neurodegenerative brain diseases. The aryl derivatives of the present invention are (3-fluoro-2-hydroxy)propyl-functionalized to increase the polarity thereof, and therefore the drugs containing the aryl derivatives can easily permeate into the cerebrovascular membrane, thus increasing the effectiveness of the drugs. As the aryl derivatives of the present invention strongly bind to β-amyloid, the aryl derivatives, when labeled with radioisotope, can be used as a diagnostic agent for non-invasively diagnosing early Alzheimer's disease. Further, the aryl derivatives of the present invention bind to low molecular β-amyloid peptide conjugates to inhibit the generation of malignant high molecular β-amyloid plaque, and thus can be effectively used as a therapeutic agent for neurodegenerative brain diseases such as Alzheimer's disease.
摘要（中）：

本发明涉及（3-氟-2-羟基）丙基官能化的芳基衍生物或其药学上可接受的盐，涉及其制备方法，以及含有其作为诊断或治疗的有效成分的药物组合物 神经退行性脑疾病 本发明的芳基衍生物是（3-氟-2-羟基）丙基官能化以提高其极性，因此含有芳基衍生物的药物可以容易地渗入脑血管膜，从而提高药物的有效性。 由于本发明的芳基衍生物与β-淀粉样蛋白强烈结合，当用放射性同位素标记时，芳基衍生物可用作非侵入性诊断早期阿尔茨海默氏病的诊断剂。 此外，本发明的芳基衍生物结合低分子量淀粉样蛋白肽缀合物以抑制恶性高分子量淀粉样斑块的产生，因此可以有效地用作神经变性脑疾病如阿尔茨海默氏症的治疗剂 疾病。

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