4-[3-(4-oxo-6,7-dihydro-5H-indol-1-yl)propanoylamino]benzoic acid

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 4-[3-(4-oxo-6,7-dihydro-5H-indol-1-yl)propanoylamino]benzoic acid
• 化学式: C₁₈H₁₈N₂O₄
• 分子量: 326.3
• InChiKey: RTCZEILINJEGQX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  24
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  88.4
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• Methods for Treating Cognitive/Attention Deficit Disorders Using Tetrahydroindolone Analogues and Derivatives
  申请人：Glasky Alvin J.

  公开号：US20120070385A1

  公开（公告）日：2012-03-22

  The present specification discloses tetrahydroindolone derivatives or analogues and methods for treating cognitive/attention deficit disorders using such tetrahydroindolone derivatives and analogues.

  本说明书公开了四氢吲哚酮衍生物或类似物，并使用这些四氢吲哚酮衍生物和类似物治疗认知/注意力缺陷障碍的方法。
• METHODS FOR TREATING COGNITIVE /ATTENTION DEFICIT DISORDERS USING TETRAHYDROINDOLONE ANALOGUES AND DERIVATIVES
  申请人：Glasky Alvin J.

  公开号：US20090192319A1

  公开（公告）日：2009-07-30

  Methods for treating cognitive/attention deficit disorders in general using tetrahydroindolone derivatives and analogues, particularly tetrahydroindolone derivatives or analogues in which the tetrahydroindolone derivative or analogue is covalently linked to another moiety to form a bifunctional conjugate are disclosed. More specifically, methods and compositions for treating attention deficit disorder and attention deficit hyperactivity disorders in adults and children as well as mild cognitive impairment and dementia are provided. The compounds used to treat and/or palliate cognitive/attention deficit disorders in general include a tetrahydroindolone derivative or analogue comprises a 9-atom bicyclic moiety, moiety A, linked through a linker L to a moiety B, where B is a carboxylic acid, a carboxylic acid ester, or a moiety of the structure N(Y 1 )-D, where Y 1 can be one of a variety of substituents, including hydrogen or alkyl, and D is a moiety that enhances the pharmacological effects, promotes absorption or blood-brain barrier penetration of the derivative or analogue. The moiety A has a six-membered ring fused to a five-membered ring. The moiety A can have one, two, or three nitrogen atoms in the five membered ring. The moiety A can be a tetrahydroindolone moiety. The moiety B can be one of a variety of moieties, including moieties having nootropic activity or other biological or physiological activity.

  本文披露了使用四氢吲哚酮衍生物和类似物治疗认知/注意力缺陷障碍的方法，特别是使用四氢吲哚酮衍生物或类似物，其中四氢吲哚酮衍生物或类似物与另一物质共价连接形成双功能结合物的方法。更具体地，本文提供了治疗成人和儿童的注意力缺陷障碍和注意力缺陷多动障碍以及轻度认知障碍和痴呆症的方法和组合物。用于治疗和/或缓解认知/注意力缺陷障碍的化合物包括四氢吲哚酮衍生物或类似物，其包括一个9原子的双环基团，基团A，通过连接剂L与基团B连接，其中B是羧酸，羧酸酯或结构N（Y1）-D的基团，其中Y1可以是多种取代基之一，包括氢或烷基，D是增强衍生物或类似物的药理效应，促进吸收或血脑屏障渗透的基团。基团A具有融合到五元环的六元环。基团A可以在五元环中有一个、两个或三个氮原子。基团A可以是四氢吲哚酮基团。基团B可以是多种基团之一，包括具有诺普力活性或其他生物或生理活性的基团。
• SYNTHESIS AND METHODS OF USE OF TETRAHYDROINDOLONE ANALOGUES AND DERIVATIVES
  申请人：Spectrum Pharmaceuticals, Inc.

  公开号：EP1383742B1

  公开（公告）日：2010-10-27
• US8063233B2
  申请人：——

  公开号：US8063233B2

  公开（公告）日：2011-11-22
• US8377456B2
  申请人：——

  公开号：US8377456B2

  公开（公告）日：2013-02-19