methyl 3-[4-fluoro-4-({[(6-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-1-yl)carbonyl]amino}methyl)piperidin-1-yl]-2,2-dimethylpropanoate | 908140-13-6

• 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 3-[4-fluoro-4-({[(6-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-1-yl)carbonyl]amino}methyl)piperidin-1-yl]-2,2-dimethylpropanoate
• 英文别名: Methyl 3-[4-fluoro-4-[[(6-fluoro-3,3-dimethyl-2-oxoindole-1-carbonyl)amino]methyl]piperidin-1-yl]-2,2-dimethylpropanoate
• CAS: 908140-13-6
• 化学式: C₂₃H₃₁F₂N₃O₄
• 分子量: 451.514
• InChiKey: FPQRDIWZLYXYOE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  32
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.61
• 拓扑面积：
  79
• 氢给体数：
  1
• 氢受体数：
  7

文献信息

• Oxyindole derivatives
  申请人：Uchida Chikara

  公开号：US20060194842A1

  公开（公告）日：2006-08-31

  This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: A, R 1 , R 2 , R 3 , R 4 and R 5 are each as described herein or a pharmaceutically acceptable salt, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT 4 agonistic activity such as, but not limited to, as gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageal disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes or apnea syndrome.

  这项发明涉及以下式（I）的化合物： 或其药学上可接受的盐，其中： A，R1，R2，R3，R4和R5分别如本文所述或药学上可接受的盐，以及含有这种化合物的组合物和利用这种化合物治疗由5-HT 4 激动活性介导的疾病的用途，例如但不限于胃食管反流病、胃肠疾病、胃动力障碍、非溃疡性消化不良、功能性消化不良、肠易激综合征（IBS）、便秘、消化不良、食管炎、胃食管疾病、恶心、中枢神经系统疾病、阿尔茨海默病、认知障碍、呕吐、偏头痛、神经系统疾病、疼痛、心血管疾病、心力衰竭、心律失常、糖尿病或呼吸暂停综合征。
• OXYINDOLE DERIVATIVES
  申请人：Uchida Chikara

  公开号：US20100173925A1

  公开（公告）日：2010-07-08

  This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: A, R 1 , R 2 , R 3 , R 4 and R 5 are each as described herein or a pharmaceutically acceptable salt, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5 -HT 4 agonistic activity such as, but not limited to, as gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageal disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes or apnea syndrome.

  本发明涉及式(I)化合物或其药学上可接受的盐，其中： A，R1，R2，R3，R4和R5如本文所述或其药学上可接受的盐，以及含有这种化合物的组合物以及在治疗由5-HT4激动剂活性介导的病症中使用这种化合物，例如，但不限于，胃食管反流病、胃肠疾病、胃动力障碍、非溃疡性消化不良、功能性消化不良、肠易激综合征（IBS）、便秘、消化不良、食管炎、胃食管疾病、恶心、中枢神经系统疾病、阿尔茨海默病、认知障碍、呕吐、偏头痛、神经系统疾病、疼痛、心血管疾病、心力衰竭、心律失常、糖尿病或呼吸暂停综合征。
• OXYINDOLE DERIVATIVES AS 5HT4 RECEPTOR AGONISTS
  申请人：Pfizer, Inc.

  公开号：EP1856110A1

  公开（公告）日：2007-11-21
• US7589109B2
  申请人：——

  公开号：US7589109B2

  公开（公告）日：2009-09-15
• [EN] OXYINDOLE DERIVATIVES AS 5HT4 RECEPTOR AGONISTS<br/>[FR] DERIVES D'OXYINDOLE UTILISES COMME AGONISTES DU RECEPTEUR 5HT4
  申请人：PFIZER JAPAN INC

  公开号：WO2006090279A1

  公开（公告）日：2006-08-31

  [EN] This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: A, R¹ , R², R³ , ^R4 and R⁵ are each as described herein or a pharmaceutically acceptable salt, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT₄ agonisitic activity such as, but not limited to, as gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes or apnea syndrome.
  [FR] L'invention concerne des composés de formule (I) ou un de leurs sels pharmaceutiquement acceptables où : A, R1, R2, R3, R4 et R5 sont décrits dans la description, ou un sel pharmaceutiquement acceptable, et des compositions contenant ces composés ainsi que leur utilisation dans le traitement d'un état à médiation par une activité de récepteur 5-HT₄ tel que (mais de façon non restrictive) le reflux oeso-gastrique, la maladie gastro-intestinale, le trouble de motilité gastrique, la dyspepsie non ulcéreuse, la dyspepsie fonctionnelle, le syndrome du côlon irritable (IBS), la constipation, la dyspepsie, l'oesophagite, la maladie oeso-gastrique, la nausée, la maladie du système nerveux central, la maladie d'Alzheimer, le trouble cognitif, le vomissement, la migraine, le trouble neurologique, la douleur, les troubles cardiovasculaires, l'insuffisance cardiaque, l'arythmie, le diabète et le syndrome d'apnée