2-Benzyl-3-ME-1-piperazin-1-YL-benzo(4,5)imidazo(1,2-A)pyridine-4-carbonitrile

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 2-Benzyl-3-ME-1-piperazin-1-YL-benzo(4,5)imidazo(1,2-A)pyridine-4-carbonitrile
• 英文别名: 2-benzyl-3-methyl-1-piperazin-1-ylpyrido[1,2-a]benzimidazole-4-carbonitrile
• 化学式: C₂₄H₂₃N₅
• 分子量: 381.5
• InChiKey: KFUXDPTVDFRJJC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5
• 重原子数：
  29
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  56.4
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• IMIDAZO[1,2-a]PYRIDINE DERIVATIVE
  申请人：Astellas Pharma Inc.

  公开号：US20130053363A1

  公开（公告）日：2013-02-28

  [Problem] To provide a compound useful as medicine having PDE4B inhibitory activity, in particular, as an active ingredient of a composition for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like. [Measures for Solution] The present inventors examined compounds having PDE4B inhibitory activity and found that a tricyclic or tetracyclic imidazo[1,2-a]pyridine derivative or salts thereof had a superior PDE4B inhibitory activity, thereby completing the present invention. The imidazo[1,2-a]pyridine derivative can be used as an agent for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like.

  [问题]提供一种作为药物有PDE4B抑制活性的化合物，特别是作为治疗或预防精神分裂症、阿尔茨海默病、痴呆、抑郁症等组合物的活性成分。[解决方案措施]本发明人研究了具有PDE4B抑制活性的化合物，发现三环或四环咪唑[1,2-a]吡啶衍生物或其盐具有卓越的PDE4B抑制活性，从而完成了本发明。咪唑[1,2-a]吡啶衍生物可用作治疗或预防精神分裂症、阿尔茨海默病、痴呆、抑郁症等的药物。
• HETEROCYCLIC INHIBITORS OF PDE4
  申请人：Govek Steven P.

  公开号：US20090275586A1

  公开（公告）日：2009-11-05

  The present invention is directed to potent and selective heterocyclic compounds, useful as inhibitors of phosphodiesterase 4 (PDE4), compositions comprising the same, and their application as pharmaceuticals for the treatment of disease. Methods of inhibition of PDE4 activity are also provided, as well as methods for the treatment of inflammatory diseases and other diseases in which PDE4 or one of its isoforms may play a role.
• US8822688B2
  申请人：——

  公开号：US8822688B2

  公开（公告）日：2014-09-02
• [EN] HETEROCYCLIC INHIBITORS OF PDE4<br/>[FR] INHIBITEURS HÉTÉROCYCLIQUES DE PDE4
  申请人：KALYPSYS INC

  公开号：WO2008045664A2

  公开（公告）日：2008-04-17

  [EN] The present invention is directed to potent and selective heterocyclic compounds, useful as inhibitors of phosphodiesterase 4 (PDE4), compositions comprising the same, and their application as pharmaceuticals for the treatment of disease. Methods of inhibition of PDE4 activity are also provided, as well as methods for the treatment of inflammatory diseases and other diseases in which PDE4 or one of its isoforms may play a role.
  [FR] L'invention concerne des composés hétérocycliques puissants et sélectifs, servant d'inhibiteurs de la phosphodiestérase 4 (PDE4), des compositions comprenant ces composés, et leur application en tant que substances pharmaceutiques destinées à traiter des maladies. L'invention concerne également des procédés d'inhibition de l'activité de PDE4, ainsi que des procédés visant à traiter des maladies inflammatoires ou d'autres maladies dans lesquelles PDE4 ou l'une de ses isoformes peut jouer un rôle.