2-(4-Fluorophenyl)-1-benzofuran-5-amine | 461387-95-1

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 2-芳基苯并呋喃类黄酮
• 英文名称: 2-(4-Fluorophenyl)-1-benzofuran-5-amine
• CAS: 461387-95-1
• 化学式: C₁₄H₁₀FNO
• 分子量: 227.238
• InChiKey: AUXLFEABWDOVFO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  17
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  39.2
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• Isotopically-Labeled Benzofuran Compounds as Imaging Agents for Amyloidogenic Proteins
  申请人：Klunk William E.

  公开号：US20080274058A1

  公开（公告）日：2008-11-06

  Benzofuran compounds which contain at least one detectable label selected from the group consisting of 131 I, 123 I, 124 I, 125 I, 76 Br, 75 Br, 18 F, 19 F, 11 C, 13 C, 14 C and 3 H are provided as amyloid imaging agents for detecting brain amyloid deposits as well as other amyloidogenic peptides associated with systemic or localized amyloidosis. Additionally, the compounds are useful for determining if patients, presenting with clinically confusing cases of dementia or presenting with mild cognitive impairment, have Alzheimer's disease. The compounds are additionally useful as surrogate markers for monitoring the efficacy of anti-amyloidosis therapies.

  提供了含有至少一种可检测标记的苯并呋喃类化合物，所述可检测标记选自131I、123I、124I、125I、76Br、75Br、18F、19F、11C、13C、14C和3H，作为淀粉样蛋白成像剂，用于检测脑淀粉样沉积物以及与全身或局部淀粉样变性相关的其他淀粉样肽。此外，这些化合物可用于确定患有临床混淆的痴呆症状或轻度认知障碍的患者是否患有阿尔茨海默病。这些化合物还可用作监测抗淀粉样变性治疗疗效的代用标记。
• ISOTOPICALLY-LABELED BENZOFURAN COMPOUNDS AS IMAGING AGENTS FOR AMYLOIDOGENIC PROTEINS
  申请人：KLUNK William E.

  公开号：US20120148494A1

  公开（公告）日：2012-06-14

  Benzofuran compounds which contain at least one detectable label selected from the group consisting of 131 I, 123 I, 124 I, 76 Br, 75 Br, 18 F, 19 F, 11 C, 13 C, 14 C and 3 H are provided as amyloid imaging agents for detecting brain amyloid deposits as well as other amyloidogenic peptides associated with systemic or localized amyloidosis. Additionally, the compounds are useful for determining if patients, presenting with clinically confusing cases of dementia or presenting with mild cognitive impairment, have Alzheimer's disease. The compounds are additionally useful as surrogate markers for monitoring the efficacy of anti-amyloidosis therapies.

  提供至少含有以下可检测标记中的一个的苯并呋喃化合物，所述标记包括131I、123I、124I、76Br、75Br、18F、19F、11C、13C、14C和3H，作为用于检测脑淀粉样沉积物以及与系统性或局部淀粉样病变相关的其他淀粉样肽的淀粉样成像剂。此外，这些化合物可用于确定患有阿尔茨海默病的患者，这些患者表现出临床上令人困惑的痴呆症状或轻度认知障碍。这些化合物还可用作监测抗淀粉样病治疗的有效性的替代标志物。
• ISOTOPICALLY-LABELED BENZOFURAN COMPOUNDS AS IMAGINGAGENTS FOR AMYLOIDOGENIC PROTEINS
  申请人：University of Pittsburgh - Of the Commonwealth System of Higher Education

  公开号：EP1945622B1

  公开（公告）日：2011-12-28
• US8138360B2
  申请人：——

  公开号：US8138360B2

  公开（公告）日：2012-03-20
• [EN] ISOTOPICALLY-LABELED BENZOFURAN COMPOUNDS AS IMAGINGAGENTS FORAMYLOIDOGENIC PROTEINS<br/>[FR] COMPOSES DE BENZOFURANNE MARQUES PAR DES ISOTOPES EN TANT QU'AGENTS D'IMAGERIE POUR DES PROTEINES AMYLOIDOGENES
  申请人：UNIV PITTSBURGH

  公开号：WO2007047204A1

  公开（公告）日：2007-04-26

  [EN] Benzofuran compounds which contain at least one detectable label selected from the group consisting of ¹³¹I, ¹²³I, ¹²⁴I^{, 125}I, ⁷⁶Br, ⁷⁵Br, ¹⁸F, ¹⁹F, ¹¹C, ¹³C, ¹⁴C and ³H are provided as amyloid imaging agents for detecting brain amyloid deposits as well as other amyloidogenic peptides associated with systemic or localized amyloidosis. Additionally, the compounds are useful for determining if patients, presenting with clinically confusing cases of dementia or presenting with mild cognitive impairment, have Alzheimer's disease. The compounds are additionally useful as surrogate markers for monitoring the efficacy of anti-amyloidosis therapies.
  [FR] La présente invention concerne des composés de benzofuranne contenant au moins un marqueur détectable, choisi dans le groupe comprenant les ¹³¹I, ¹²³I,¹²⁴I^{, 125}I, ⁷⁶Br, ⁷⁵Br, ¹⁸F, ¹⁹F, ¹¹C, ¹³C, ¹⁴C et ³H, et servant d'agents d'imagerie des amyloïdes permettant de détecter les dépôts amyloïdes dans le cerveau ainsi que d'autres peptides amyloïdogènes associés à une amyloïdose systémique ou localisée. En outre, les composés peuvent être utilisés pour déterminer la présence éventuelle de la maladie d'Alzheimer chez des patients présentant des cas de démence mal définis sur le plan clinique ou des troubles cognitifs bénins. Les composés peuvent également être utilisés en tant que marqueurs de remplacement pour surveiller l'efficacité des traitements anti-amyloïdose.