[11C]4-N-methylamino-4-hydroxystilbene

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二苯乙烯类
• 英文名称: [11C]4-N-methylamino-4-hydroxystilbene
• 英文别名: 4-[(E)-2-[4-((111C)methylamino)phenyl]ethenyl]phenol
• 化学式: C15H15NO
• 分子量: 224.29
• InChiKey: ZWIARAQZLULYPG-CKRIYKSPSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  32.3
• 氢给体数：
  2
• 氢受体数：
  2

文献信息

• (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
  申请人：Chi Dae-Yoon

  公开号：US20120214994A1

  公开（公告）日：2012-08-23

  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.

  本发明涉及（3-氟-2-羟基）丙基官能化芳基衍生物或其药用可接受的盐，以及制备该衍生物的方法，以及含有该衍生物作为活性成分的药物组合物，用于诊断或治疗神经退行性脑疾病。本发明的芳基衍生物经（3-氟-2-羟基）丙基官能化以增加其极性，因此含有该芳基衍生物的药物可以轻松渗透到脑血管膜中，从而增加药物的有效性。由于本发明的芳基衍生物与β-淀粉样蛋白结合强，因此当该芳基衍生物标记放射性同位素时，可用作无创诊断早期阿尔茨海默病的诊断剂。此外，本发明的芳基衍生物与低分子量β-淀粉样肽结合以抑制恶性高分子量β-淀粉样斑块的生成，因此可以有效用作治疗阿尔茨海默病等神经退行性脑疾病的治疗剂。
• AMYLOID BINDING AGENTS
  申请人：Yang Jerry

  公开号：US20120302603A1

  公开（公告）日：2012-11-29

  There are provided compounds and methods for the detection and treatment of amyloid deposits and diseases and disorders characterized by amyloid deposits including Alzheimer's disease and related amyloid-based neurodegenerative disorders.