N-(1,3-benzodioxol-5-yl)-4-oxo-6-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并间二氧杂环戊烯类
• 英文名称: N-(1,3-benzodioxol-5-yl)-4-oxo-6-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide
• 英文别名: N-(1,3-benzodioxol-5-yl)-6-methyl-4-oxo-1,5,6,7-tetrahydroindole-3-carboxamide
• 化学式: C₁₇H₁₆N₂O₄
• 分子量: 312.325
• InChiKey: ZVZGIDNLEMOGON-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  23
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  80.4
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• Fused pyrrolecarboxamides: GABA brain receptor ligands
  申请人：Albaugh Pamela

  公开号：US20050014939A1

  公开（公告）日：2005-01-20

  Substituted pyrrolecarboxamide compounds are disclosed. These compounds are highly selective agonists, antagonists or inverse agonists for GABA A brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABA A brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Alzheimer's dementia, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABA A receptors in tissue samples.

  揭示了取代吡咯甲酰胺化合物。这些化合物是高度选择性的GABAA脑受体的激动剂、拮抗剂或逆向激动剂，或者是GABAA脑受体的激动剂、拮抗剂或逆向激动剂的前药，因此在焦虑、抑郁、阿尔茨海默病痴呆、睡眠和癫痫障碍、苯二氮卓类药物过量以及增强记忆的诊断和治疗中非常有用。此外，还提供了包括包装的药物组合物在内的制药组合物。该发明的化合物还可用作定位组织样本中GABAA受体的探针。
• Fused pyrrolecarboxamides; a new class of GABA brain receptor ligands
  申请人：Neurogen

  公开号：US20010029299A1

  公开（公告）日：2001-10-11

  Disclosed are compounds of the formula: 1 or the pharmaceutically acceptable non-toxic salts thereof wherein: G, X, T, n, and R 3 -R 6 are as defined herein, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.

  本发明涉及以下公式的化合物：1或其药学上可接受的非毒性盐，其中：G、X、T、n和R3-R6的定义如本文所述，这些化合物是高度选择性的GABAa脑受体的激动剂、拮抗剂或反向激动剂，或是GABAa脑受体的激动剂、拮抗剂或反向激动剂的前药。这些化合物在焦虑、睡眠和癫痫障碍的诊断和治疗、苯二氮卓类药物过量和增强记忆方面有用。
• NOVEL FUSED PYRROLECARBOXAMIDES; A NEW CLASS OF GABA BRAIN RECEPTOR LIGANDS
  申请人：NEUROGEN CORPORATION

  公开号：EP1019372A1

  公开（公告）日：2000-07-19
• FUSED PYRROLECARBOXAMIDES; A NEW CLASS OF GABA BRAIN RECEPTOR LIGANDS
  申请人：NEUROGEN CORPORATION

  公开号：EP1019372B1

  公开（公告）日：2006-04-05
• US5804686A
  申请人：——

  公开号：US5804686A

  公开（公告）日：1998-09-08