10-fluoro-9-(4-fluoro-3-methylphenyl)-6,11-dihydro-5-oxa-11-aza-benzo[a]fluorene-3-carboxylic acid amide | 920303-01-1

• 分子结构分类: 有机化合物 - 有机杂环化合物
• 英文名称: 10-fluoro-9-(4-fluoro-3-methylphenyl)-6,11-dihydro-5-oxa-11-aza-benzo[a]fluorene-3-carboxylic acid amide
• 英文别名: 10-Fluoro-9-(4-fluoro-3-methylphenyl)-6,11-dihydrochromeno[4,3-b]indole-3-carboxamide
• CAS: 920303-01-1
• 化学式: C₂₃H₁₆F₂N₂O₂
• 分子量: 390.389
• InChiKey: AFGFCWCJBHUVDU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  29
• 可旋转键数：
  2
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.09
• 拓扑面积：
  68.1
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  C₂₃H₁₄F₂N₂O 在 lithium hydroxide 作用下， 生成 10-fluoro-9-(4-fluoro-3-methylphenyl)-6,11-dihydro-5-oxa-11-aza-benzo[a]fluorene-3-carboxylic acid amide
  参考文献：
  名称：

  Optimization of small molecule agonists of the thrombopoietin (Tpo) receptor derived from a benzo[a]carbazole hit scaffold

  摘要：

  The lead optimization of a novel series of benzo[a] carbazole-based small molecule agonists of the thrombopoietin (Tpo) receptor is reported. The chemical instability of the dihydro-benzo[a] carbazole lead 2 was successfully addressed in the design and evaluation of compounds which also demonstrated improved potency compared to 2. Members of the scaffold have been identified which are full agonists that demonstrate cellular functional potency < 50 nM. Analog 21 demonstrates equivalent efficacy in the human megakaryocyte differentiation (CFU-mega) assay compared to Eltrombopag(TM). (C) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2008.08.077

文献信息

• HETEROTETRACYCLIC COMPOUNDS AS TPO MIMETICS
  申请人：Alper Phillip B.

  公开号：US20090075996A1

  公开（公告）日：2009-03-19

  The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TPO activity, particularly diseases or disorders that involve thrombocytopenia.

  该发明提供了一类新颖的化合物，包括含有这些化合物的药物组合物，以及使用这些化合物来治疗或预防与TPO活性异常或失调相关的疾病或障碍的方法，尤其是涉及血小板减少症的疾病或障碍。
• HETEROTETRACYCLIC COMPOUNDS AS TPO MIMETICS
  申请人：IRM, LLC

  公开号：EP1910338B1

  公开（公告）日：2010-08-25
• US8153671B2
  申请人：——

  公开号：US8153671B2

  公开（公告）日：2012-04-10
• [EN] COMPOUNDS AND COMPOSITIONS AS TPO MIMETICS<br/>[FR] COMPOSES ET COMPOSITIONS UTILISES COMME MIMETIQUES DE LA TPO
  申请人：IRM LLC

  公开号：WO2007009120A2

  公开（公告）日：2007-01-18

  [EN] The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TPO activity, particularly diseases or disorders that involve thrombocytopenia.
  [FR] La présente invention concerne une nouvelle classe de composés, des compositions pharmaceutiques comprenant ces composés et des procédés d'utilisation de tels composés pour traiter ou prévenir des maladies ou des troubles associés à une activité anormale ou déréglée de la thrombopoïétine (TPO), en particulier des maladies ou des troubles impliquant la thrombocytopénie.