6-phenyl-7H-thieno[2,3-b]pyridin-4-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 6-phenyl-7H-thieno[2,3-b]pyridin-4-one
• 化学式: C₁₃H₉NOS
• 分子量: 227.28
• InChiKey: ZAUVSAUDLZNZQL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  57.3
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• Aryl fused substituted 4-oxy-pyridines
  申请人：——

  公开号：US20020035121A1

  公开（公告）日：2002-03-21

  Disclosed are compounds of the formula: 1 wherein X, Q, W and 2 are as defined herein. These compounds are 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, Down Syndrome, 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.

  本发明揭示了化合物的公式：1，其中X，Q，W和2如定义所述。这些化合物是GABAA脑受体的激动剂，拮抗剂或反向激动剂，或者是GABAA脑受体激动剂，拮抗剂或反向激动剂的前药，因此在焦虑，抑郁，唐氏综合症，睡眠和癫痫障碍，苯二氮卓类药物过量和记忆增强的诊断和治疗中有用。此外，还提供了包括包装的制药组合物在内的制药组合物。本发明的化合物还可用作组织样本中GABAA受体定位的探针。
• Heterocyclic amino substituted heteroaryl fused pyridines; GABA brain receptor ligands
  申请人：Neurogen

  公开号：US20020077474A1

  公开（公告）日：2002-06-20

  Disclosed are compounds of the formula 1 or the pharmaceutically acceptable non-toxic salts thereof wherein: n is an integer from 0 to 3; the C ring is aryl or heteroaryl; X is CH, N, or O Z represents an electron pair, hydrogen, or (un)substituted heterocycle, aryl, or amido; W is (un)substituted alkyl, aryl, or heteroaryl; A and B are hydrogen or lower alkyl, 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, Down Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness.

  本发明涉及如下公式1的化合物或其药学上可接受的非毒性盐： 其中，n为0至3的整数；C环为芳基或杂环芳基；X为CH、N或O；Z代表电子对、氢或（未）取代的杂环、芳基或酰胺基；W为（未）取代的烷基、芳基或杂环芳基；A和B为氢或低碳基。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，或者是GABAa脑受体激动剂、拮抗剂或反向激动剂的前药。这些化合物可用于诊断和治疗焦虑症、唐氏综合症、睡眠、认知和癫痫障碍，以及苯二氮平类药物过量和提高警觉性。
• US6103903A
  申请人：——

  公开号：US6103903A

  公开（公告）日：2000-08-15
• US6166203A
  申请人：——

  公开号：US6166203A

  公开（公告）日：2000-12-26
• US6380209B1
  申请人：——

  公开号：US6380209B1

  公开（公告）日：2002-04-30