[¹²⁵I]IMPY

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: [¹²⁵I]IMPY
• 英文别名: [125I]6-Iodo-2-(4-dimethylamino)-phenyl-imidazo(1,2-a)pyridine；4-(6-(125I)iodanylimidazo[1,2-a]pyridin-2-yl)-N,N-dimethylaniline
• 化学式: C₁₅H₁₄IN₃
• 分子量: 361.296
• InChiKey: GUJHUHNUHJMRII-RFLHHMENSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  19
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.13
• 拓扑面积：
  20.5
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  4-(6-bromo-imidazo[1,2-a]pyridin-2-yl)-N,N-dimethylbenzenamine 在 钯 三乙胺 、 sodium iodide 、 双氧水 作用下， 以 1,4-二氧六环 、 氯仿 为溶剂， 生成 [¹²⁵I]IMPY
  参考文献：
  名称：

  Zhuang, Z. P.; Kung, M.-P.; Hou, C., Journal of labelled compounds and radiopharmaceuticals, 2001, vol. 44, p. S29 - S32

  摘要：

  DOI：

文献信息

• 2-ARYLBENZOTHIOPHENE DERIVATIVES OR PHARCEUTICALLY ACCEPTABLE SALTS THEREOF, PREPARATION METHOD THEREOF, AND PHARCEUTICAL COMPOSITION FOR THE DIAGNOSIS OR TREATMENT OF DEGENERATIVE BRAIN DISEASE CONTAINING THE SAME AS ACTIVE INGREDIENT
  申请人：Chi Dae Yoon

  公开号：US20100261727A1

  公开（公告）日：2010-10-14

  2-arylbenzothiophene derivatives or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition for the diagnosis or treatment of degenerative brain disease containing the same as an active ingredient. Since the 2-arylbenzothiophene derivatives of Formula 1 have a relatively high binding affinity for β-amyloid, they can be used as diagnostic reagents for diagnosing Alzheimer's disease at an early stage by non-invasive techniques when they are labeled with radioisotopes: wherein R 1 -R 4 , V, W, X, Y and Z are as defined in the Detailed Descript of the specification. Further, when the pharmaceutical composition containing the 2-arylbenzothiophene derivative binds with a low-molecular weight β-amyloid peptide binding compound, generation of malignant high-molecular weight β-amyloid deposits is minimized. Accordingly, the pharmaceutical composition can be used as a therapeutic agent of degenerative brain disease such as Alzheimer's disease.

  2-芳基苯并噻吩衍生物或其药用可接受盐，其制备方法，以及包含其作为活性成分的用于诊断或治疗退行性脑疾病的药物组合物。由于式1中的2-芳基苯并噻吩衍生物具有相对较高的β-淀粉样蛋白结合亲和力，因此当它们与放射性同位素标记时，它们可以作为诊断试剂用于通过非侵入性技术早期诊断阿尔茨海默病： 其中R1-R4，V，W，X，Y和Z如规范的详细描述中所定义。此外，当含有2-芳基苯并噻吩衍生物的药物组合物与低分子量β-淀粉样蛋白结合化合物结合时，最小化了恶性高分子量β-淀粉样蛋白沉积物的生成。因此，该药物组合物可用作治疗阿尔茨海默病等退行性脑疾病的治疗剂。
• 6-Methoxy-indanone derivatives as potential probes for β-amyloid plaques in Alzheimer's disease
  作者：Dou-Dou Nan、Chang-Sheng Gan、Chen-Wei Wang、Jin-Ping Qiao、Xin-Meng Wang、Jiang-Ning Zhou

  DOI：10.1016/j.ejmech.2016.07.069

  日期：2016.11

  A series of 6-methoxy indanone derivatives was synthesized and evaluated as potential probes for β-amyloid plaque imaging in Alzheimer's disease (AD). Two derivatives (5d and 5k) displayed significant binding abilities in fluorescent staining experiments using the brain sections of AD patients. Two derivatives showed high binding affinities to β-amyloid aggregates (5j, Ki = 5.82 ± 0.19 nM) and brain

  合成了一系列6-甲氧基茚满酮衍生物，并将其评估为阿尔茨海默氏病（AD）中β-淀粉样蛋白斑成像的潜在探针。在使用AD患者大脑切片的荧光染色实验中，两种衍生物（5d和5k）显示出显着的结合能力。在体外结合试验 中，两种衍生物显示出对β-淀粉样蛋白聚集体的高结合亲和力（5j，K i  = 5.82±0.19 nM）和AD患者的脑匀浆（5j，K i = 18.96±0.28 nM）。log P值为3.45，[ 125 I] 5k表现出出色的初始大脑摄取（5.29％ID g -1，静脉注射后2分钟），并在正常小鼠的生物分布实验中快速清除了大脑。在放射自显影中，[ 125 I] 5k在AD患者（体外）和APP / PS1转基因小鼠（体外和离体）的脑部中表现出明显的与β淀粉样蛋白斑块的结合能力和相对较低的非特异性结合。结果表明5k是体内检测β-淀粉样蛋白斑的潜在探针。
• (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。
• Alzheimer's Disease Imaging Agents
  申请人：Goodman Mark M.

  公开号：US20080219922A1

  公开（公告）日：2008-09-11

  This invention provides compounds and methods of imaging amyloid deposits using radiolabeled compounds. This invention also provides a method of inhibiting the aggregation of amyloid proteins to form amyloid plaques or deposits, a method of determining a therapeutic compound's ability to inhibit aggregation of amyloid protein, and a method of delivering a therapeutic agent to amyloid deposits.

  本发明提供了使用放射性标记化合物成像淀粉样沉积物的化合物和方法。本发明还提供了一种抑制淀粉样蛋白聚集形成淀粉样斑块或沉积物的方法，一种确定治疗化合物抑制淀粉样蛋白聚集能力的方法，以及将治疗剂递送到淀粉样沉积物的方法。
• COMPOUNDS AND AMYLOID PROBES THEREOF FOR THERAPEUTIC AND IMAGING USES
  申请人：Tamagnan Gilles D.

  公开号：US20100143251A1

  公开（公告）日：2010-06-10

  The present invention provides compounds and amyloid probes thereof that allow for an antemortem method of diagnosing AD and quantitating the extent or progression of amyloid deposits (plaques) by in vivo imaging of amyloid and/or amyloid deposits in the regions of the brain. Preferably, an amyloid probe of the invention can cross the blood-brain barrier and distinguish AD brain from normal brain. An amyloid probe can be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits. Amyloid probes of the invention can also be used to detect and quantitate amyloid deposits in diseases including, without limitation, Down's syndrome, familial AD and homozygotes for the apolipoprotein E4 allele. In one aspect, the compounds may be used in the treatment or prophylaxis of diseases that include, without limitation, AD and type 2 diabetes mellitus. The compounds and amyloid probes of the invention include analogs, salts, pharmaceutical compositions, derivatives, prodrugs, racemic mixtures or tautomeric forms thereof.

  本发明提供了化合物及其淀粉样探针，可通过体内成像淀粉样和/或脑部区域的淀粉样沉积物，从而实现诊断AD和量化淀粉样沉积物（斑块）的程度或进展的生前方法。优选地，本发明的淀粉样探针可以穿过血脑屏障，区分AD脑和正常脑。可以向患者施用本发明的淀粉样探针，以适量成像淀粉样沉积物。本发明的淀粉样探针还可用于检测和量化包括但不限于唐氏综合症、家族性AD和载脂蛋白E4等位基因纯合子在内的疾病中的淀粉样沉积物。在一方面，这些化合物可以用于治疗或预防包括但不限于AD和2型糖尿病的疾病。本发明的化合物和淀粉样探针包括其类似物、盐、制药组合物、衍生物、前药、外消旋混合物或其互变异构体。