N,N-dimethyl-(9-benzenesulfonyl-2,3,4,9-tetrahydro-1H-carbazol-3-yl)amine

• 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: N,N-dimethyl-(9-benzenesulfonyl-2,3,4,9-tetrahydro-1H-carbazol-3-yl)amine
• 英文别名: (9-benzenesulfonyl-2,3,4,9-tetrahydro-1H-carbazol-3-yl) dimethylamine；(9-Benzenesulfonyl-2,3,4,9-tetrahydro-1H-carbazol-3-yl)dimethylamine；9-(benzenesulfonyl)-N,N-dimethyl-1,2,3,4-tetrahydrocarbazol-3-amine
• 化学式: C₂₀H₂₂N₂O₂S
• 分子量: 354.473
• InChiKey: DXPHMVPLORWBKA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  25
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  50.7
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  (1,4-dioxa-spiro[4.5]dec-8-yl)dimethylamine 在 硫酸 、 potassium hydride 作用下， 以 四氢呋喃 、 水 、 mineral oil 为溶剂， 反应 3.0h， 生成 N,N-dimethyl-(9-benzenesulfonyl-2,3,4,9-tetrahydro-1H-carbazol-3-yl)amine
  参考文献：
  名称：

  N,N-Dimethyl-[9-(arylsulfonyl)-2,3,4,9-tetrahydro-1H-carbazol-3-yl]amines as novel, potent and selective 5-HT6 receptor antagonists

  摘要：

  The design, synthesis and SAR of novel tetrahydrocarbazole derivatives having 5-HT6 receptor antagonist activity is presented. The racemic compound 15e was found to possess desirable pharmacokinetic properties, adequate brain penetration and activity in animal models of cognition. (C) 2012 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2012.06.002

文献信息

• Carbazole Derivatives as Functional 5-HT6 Ligands
  申请人：Ramakrishna Venkata Satya Nirogi

  公开号：US20100189646A1

  公开（公告）日：2010-07-29

  The present invention provides carbazole derivatives of formula (I), useful in treatment of a CNS disorders related to or affected by the 5-HT 6 receptor. Pharmacological profile of these compounds includes high affinity binding with 5-HT 6 receptor along with good selectivity towards the said receptor. The present invention also includes the stereoisomers, the salts, methods of preparation and medicines containing the said carbazole derivatives.

  本发明提供了式(I)的Carbazole衍生物，用于治疗与5-HT6受体相关或受其影响的中枢神经系统疾病。这些化合物的药理特性包括与5-HT6受体的高亲和结合以及对该受体的良好选择性。本发明还包括立体异构体、盐、制备方法以及含有上述Carbazole衍生物的药物。
• Carbazole derivatives as functional 5-HT6 ligands
  申请人：Suven Life Sciences Limited

  公开号：US08143303B2

  公开（公告）日：2012-03-27

  Carbazole derivatives of formula (I), useful in treatment of a CNS disorders related to or affected by the 5-HT6 receptor are described. The pharmacological profile of these compounds includes high affinity binding with 5-HT6 receptor along with good selectivity towards the receptor. Stereoisomers, the salts, methods of preparation and medicines containing the carbazole derivatives are also described.

  本文描述了公式（I）的咔唑衍生物，可用于治疗与5-HT6受体相关或受其影响的中枢神经系统疾病。这些化合物的药理特性包括与5-HT6受体的高亲和力结合以及对受体的良好选择性。还描述了立体异构体、盐、制备方法和含有咔唑衍生物的药物。
• WO2007/46111
  申请人：——

  公开号：——

  公开（公告）日：——
• CARBAZOLE DERIVATIVES AS FUNCTIONAL 5-HT6 LIGANDS
  申请人：Suven Life Sciences Limited

  公开号：EP1948166A1

  公开（公告）日：2008-07-30
• US8143303B2
  申请人：——

  公开号：US8143303B2

  公开（公告）日：2012-03-27