7-fluoro-fluoren-2-ylamine | 363-16-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 芴
• 英文名称: 7-fluoro-fluoren-2-ylamine
• 英文别名: 7-Fluor-fluoren-2-ylamin；2-amino-7-fluorofluorene；7-Fluor-fluoren-amin-(2)；2-Amino-7-fluor-fluoren；2-Fluor-7-amino-fluoren；7-Fluoro-9h-fluoren-2-amine
• CAS: 363-16-6
• 化学式: C₁₃H₁₀FN
• 分子量: 199.228
• InChiKey: AEJHTUJROGXNNH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  15
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  26
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  7-fluoro-fluoren-2-ylamine 生成 2-Fluor-7-cyan-fluoren
  参考文献：
  名称：

  Berkovic,S., Israel Journal of Chemistry, 1963, vol. 1, p. 1 - 11

  摘要：

  DOI：
• 作为产物：
  描述：

  (4'-Fluoro-4-nitro-biphenyl-2-yl)-methanol 在 platinum(IV) oxide PPA 、 氢气 作用下， 以 四氢呋喃 、 甲醇 为溶剂， 生成 7-fluoro-fluoren-2-ylamine
  参考文献：
  名称：

  Synthesis and biological activities of aryl-ether-, biaryl-, and fluorene-aspartic acid and diaminopropionic acid analogs as potent inhibitors of the high-affinity glutamate transporter EAAT-2

  摘要：

  Excitatory amino acid transporters (EAATs) play a pivotal role in maintaining glutamate homeostasis in the mammalian central nervous system, with the EAAT-2 subtype thought to be responsible for the bulk of the glutamate uptake in forebrain regions. A complete elucidation of the functional role of EAAT-2 has been hampered by the lack of potent and selective pharmacological tools. In this study, we describe the synthesis and biological activities of novel aryl-ether, biaryl-, and fluorene-aspartic acid and diaminopropionic acid analogs as potent inhibitors of EAAT-2. Compound (16) represents one of the most potent (IC50 = 85 +/- 5 nM) and selective inhibitors of EAAT-2 identified to date. (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2005.08.003

文献信息

• [EN] NOVEL ASPARTYLAMIDE INHIBITORS OF EXCITATORY AMINO ACID TRANSPORTERS<br/>[FR] NOUVEAUX INHIBITEURS D'ASPARTYLAMIDE DE TRANSPORTEURS D'ACIDE AMINÉ EXCITATEURS
  申请人：UNIV MONTANA

  公开号：WO2013134241A1

  公开（公告）日：2013-09-12

  The compounds of the invention are inhibitors of excitatory amino acid transporters (EAAT) that penetrate the blood-brain barrier to access the central nervous system. The compounds of the invention follow the structural formula: or a salt, ester or prodrug thereof, wherein X is a halogen, such as fluorine, or a radionuclide, such as fluorine-18. The compounds and methods described herein can be used for the treatment of, e.g., neurodegenerative disorders (e.g., amyotrophic lateral sclerosis), ischemia, spinal cord injury, and traumatic brain injury in a patient (e.g., a human). The invention further provides compounds and methods for the synthesis and use of radiographic tracers to diagnose and follow the progression of such disorders.

  本发明的化合物是兴奋性氨基酸转运体（EAAT）的抑制剂，能穿过血脑屏障进入中枢神经系统。本发明的化合物遵循以下结构式：或其盐、酯或前药，其中X是卤素，如氟，或放射性核素，如氟-18。本文描述的化合物和方法可用于治疗神经退行性疾病（例如肌萎缩侧索硬化症）、缺血、脊髓损伤和创伤性脑损伤等患者（例如人类）。本发明还提供了用于合成和使用放射示踪剂以诊断和追踪这些疾病进展的化合物和方法。
• Steroid receptor modulator compounds and methods
  申请人：——

  公开号：US20040186132A1

  公开（公告）日：2004-09-23

  Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.

  本文披露了高亲和力、高选择性的非类固醇化合物，可作为类固醇受体调节剂。同时也披露了包含这些化合物的药物组合物，以及使用这些化合物和组合物治疗需要类固醇受体激动剂或拮抗剂治疗的患者的方法，还包括制备这些化合物的中间体和制备类固醇受体调节剂化合物的方法。
• Novel Aspartylamide Inhibitors of Excitatory Amino Acid Transporters
  申请人：THE UNIVERSITY OF MONTANA

  公开号：US20150023878A1

  公开（公告）日：2015-01-22

  The compounds of the invention are inhibitors of excitatory amino acid transporters (EAAT) that penetrate the blood-brain barrier to access the central nervous system. The compounds of the invention follow the structural formula: or a salt, ester or prodrug thereof, wherein X is a halogen, such as fluorine, or a radionuclide, such as fluorine-18. The compounds and methods described herein can be used for the treatment of, e.g., neurodegenerative disorders (e.g., amyotrophic lateral sclerosis), ischemia, spinal cord injury, and traumatic brain injury in a patient (e.g., a human). The invention further provides compounds and methods for the synthesis and use of radiographic tracers to diagnose and follow the progression of such disorders.

  本发明的化合物是兴奋性氨基酸转运体（EAAT）的抑制剂，能够穿过血脑屏障进入中枢神经系统。本发明的化合物遵循以下结构式：或其盐、酯或前药，其中X是卤素，如氟，或放射性核素，如氟-18。本发明所描述的化合物和方法可用于治疗神经退行性疾病（例如肌萎缩性侧索硬化症）、缺血、脊髓损伤和创伤性脑损伤等患者（例如人类）。本发明还提供了化合物和方法，用于合成和使用放射性示踪剂诊断和跟踪这些疾病的进展。
• Methods for the preparation of coumarine derivatives
  申请人：LIGAND PHARMACEUTICALS INCORPORATED

  公开号：EP1041071A1

  公开（公告）日：2000-10-04

  Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.

  本发明公开了对类固醇受体具有高亲和力、高选择性调节作用的非类固醇化合物。还公开了含有此类化合物的药物组合物、使用所公开化合物和组合物治疗需要类固醇受体激动剂或拮抗剂治疗的患者的方法、制备化合物时有用的中间体以及制备类固醇受体调节剂化合物的工艺。
• Nonsteroidal progesterone receptor antagonists based on a conformationally-restricted subseries of 6-aryl-1,2-dihydro-2,2,4-trimethylquinolines
  作者：Lawrence G. Hamann、David T. Winn、Charlotte L.F. Pooley、Christopher M. Tegley、Sarah J. West、Luc.J. Farmer、Lin Zhi、James P. Edwards、Keith B. Marschke、Dale E. Mais、Mark E. Goldman、Todd K. Jones

  DOI：10.1016/s0960-894x(98)00482-x

  日期：1998.10

  A series of nonsteroidal human progesterone receptor (hPR) antagonists based on conformationally-restricted analogues of a 6-aryl-1,2-dihydro-2,2,4-trimethylquinoline pharmacophore were synthesized and evaluated for their ability to bind to the human progesterone receptor and inhibit progesterone-stimulated reporter gene expression in mammalian cells, (C) 1998 Elsevier Science Ltd. AU rights reserved.