Methyl 5-(acetyloxymethyl)-9-(oxan-4-yl)carbazole-2-carboxylate | 1047624-46-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: Methyl 5-(acetyloxymethyl)-9-(oxan-4-yl)carbazole-2-carboxylate
• CAS: 1047624-46-3
• 化学式: C₂₂H₂₃NO₅
• 分子量: 381.428
• InChiKey: HWNRCOMHHBINHF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  28
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  66.8
• 氢给体数：
  0
• 氢受体数：
  5

文献信息

• ACYLGUANIDINE DERIVATIVE
  申请人：Astellas Pharma Inc.

  公开号：EP2119704A1

  公开（公告）日：2009-11-18

  An object of the present invention is to provide a novel and excellent agent for treating or preventing dementia, schizophrenia and the like, based on the 5-HT5A receptor modulating action. It was confirmed that a compound characterized by a structure that a tricyclic hetero ring having a pyrrole ring at the center and guanidine are bonded via a carbonyl group has a potent 5-HT5A receptor modulating action and an excellent pharmacological action based thereon, and thus, it was found that the compound can be an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder, or attention deficit hyperactivity disorder, particularly for memory-related functional disorders such as cognitive impairments including dementia and schizophrenia, thereby completing the present invention.

  本发明的目的是提供一种基于 5-HT5A 受体调节作用的治疗或预防痴呆症、精神 分裂症等疾病的新型优良药物。经证实，一种化合物的结构特征是中心具有吡咯环的三环杂环与胍通过羰基键合，该化合物具有强效的 5-HT5A 受体调节作用和基于此的优异药理作用，因此、发现该化合物可作为治疗或预防痴呆症、精神分裂症、双相情感障碍或注意缺陷多动障碍的极佳药剂，尤其适用于与记忆相关的功能性障碍，如包括痴呆症和精神分裂症在内的认知障碍，从而完成了本发明。