4-methoxy-3-trichloroacetyl-1H-indole

• 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: 4-methoxy-3-trichloroacetyl-1H-indole
• 英文别名: 2,2,2-trichloro-1-(4-methoxy-1H-indol-3-yl)ethanone
• 化学式: C₁₁H₈Cl₃NO₂
• 分子量: 292.549
• InChiKey: NQZMLIDJRBOWKO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  42.1
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  4-甲氧基吲哚 、 三氯乙酰氯 在 吡啶 作用下， 以 甲醇 、 二氯甲烷 为溶剂， 生成 4-methoxy-3-trichloroacetyl-1H-indole
  参考文献：
  名称：

  Certain fused pyrrolecarboxanilides and their use as GABA brain receptor

  摘要：

  本发明涵盖了以下结构的化合物I：其中：W代表取代或未取代的芳基；X为氢、羟基或较低的烷基；T为氢、卤素、羟基、氨基或烷基；R.sub.3为氢或有机基团；R.sub.4为氢或取代或未取代的有机取代基；R.sub.5和R.sub.6代表有机和无机取代基；n为1、2、3或4。这些化合物是GABAa脑受体的高度选择性激动剂、拮抗剂或逆拮抗剂，或者是GABAa脑受体的激动剂、拮抗剂或逆拮抗剂的前药。这些化合物在焦虑、睡眠和癫痫障碍的诊断和治疗、苯二氮䓬类药物过量和增强记忆方面具有用途。

  公开号：

  US05484944A1

文献信息

• Certain pyrrolo pyridine-3-carboxamides; a new class of GABA brain
  申请人：Neurogen Corporation

  公开号：US05750702A1

  公开（公告）日：1998-05-12

  The present invention encompasses structures of the formula: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## wherein: W represents substituted or unsubstituted phenyl; X is hydrogen, hydroxy or lower alkyl; T is hydrogen, halogen, hydroxy, nitro, amino or alkyl; R.sub.3 is hydrogen or an organic group; R.sub.4 is hydrogen or substituted or unsubstituted organic substituent; R.sub.5 and R.sub.6 represent organic, and inorganic substituents; and n is 1, 2, 3, or 4, 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.

  本发明涵盖了以下结构的化合物：##STR1##或其药学上可接受的非毒性盐，其中：##STR2##其中：W代表取代或未取代的苯基；X为氢、羟基或较低的烷基；T为氢、卤素、羟基、硝基、氨基或烷基；R.sub.3为氢或有机基团；R.sub.4为氢或取代或未取代的有机取代基；R.sub.5和R.sub.6代表有机和无机取代基；n为1、2、3或4，这些化合物是GABAa脑受体的高度选择性激动剂、拮抗剂或逆拮抗剂，或者是GABAa脑受体激动剂、拮抗剂或逆拮抗剂的前药。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是有用的。
• Certain fused pyrrolecarboxamides a new class of GABA brain receptor
  申请人：Neurogen Corporation

  公开号：US05723462A1

  公开（公告）日：1998-03-03

  Disclosed are compounds of formula I: ##STR1## wherein R.sub.8 and R.sub.9 independently represent hydrogen or organic substituents; W represents optionally substituted thiazolyl or quinoxalinyl; X is hydrogen, hydroxy or lower alkyl; and T is hydrogen, halogen, hydroxy, nitro, amino or 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 receptor. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.

  化合物的结构式为I：##STR1## 其中R.sub.8和R.sub.9独立地代表氢或有机取代基；W代表可选择取代的噻唑基或喹喔啉基；X为氢、羟基或低碳基；T为氢、卤素、羟基、硝基、氨基或烷基，这些化合物是GABAa脑受体的高选择性激动剂、拮抗剂或逆拮抗剂，或者是GABAa脑受体激动剂、拮抗剂或逆拮抗剂的前药。这些化合物在焦虑、睡眠和癫痫障碍、苯二氮卓类药物过量和增强记忆的诊断和治疗中很有用。
• Certain fused pyrrolecarboxanilides; a new class of GABA brain receptor
  申请人：Neurogen Corporation

  公开号：US05608079A1

  公开（公告）日：1997-03-04

  The present invention encompasses structures of the formula I: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## wherein: W represents substituted or unsubstituted aryl groups; X is hydrogen, hydroxy or lower alkyl; T is hydrogen, halogen, hydroxyl, amino or alkyl; R.sub.3 is hydrogen or an organic group; R.sub.4 is hydrogen or substituted or unsubstituted organic substituent; R.sub.5 and R.sub.6 represent organic, and inorganic substituents; and n is 1, 2, 3, or 4. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain recpetors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.

  本发明涵盖了I式结构和其药学上可接受的无毒盐，其中：W代表取代或未取代的芳基基团；X为氢、羟基或低碳基；T为氢、卤素、羟基、氨基或烷基；R3为氢或有机基团；R4为氢或取代或未取代的有机取代基；R5和R6代表有机和无机取代基；n为1、2、3或4。这些化合物是高度选择性的GABAa脑受体激动剂、拮抗剂或反向激动剂，或是GABAa脑受体激动剂、拮抗剂或反向激动剂的前药。这些化合物在焦虑、睡眠和癫痫障碍、苯二氮平类药物过量和增强记忆方面的诊断和治疗中有用。
• Certain fused pyrrolecarboxamides; a new class of GABA brain receptor
  申请人：Neurogen Corporation

  公开号：US06096887A1

  公开（公告）日：2000-08-01

  The present invention encompasses structures of the formula I: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## W represents substituted or unsubstituted heteroaryl; X is hydrogen, hydroxy or lower alkyl; T is hydrogen, halogen, hydroxy, nitro, amino or alkyl; R.sub.3 is hydrogen or an organic group; R.sub.4 is hydrogen or substituted or unsubstituted organic substituent; R.sub.5 and R.sub.6 represent organic, and inorganic substituents; and n is 1,2,3, or 4, 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.

  本发明涵盖以下结构的化合物I式：##STR1##或其药学上可接受的无毒盐，其中：##STR2##W代表取代或未取代的杂环芳基；X为氢、羟基或较低的烷基；T为氢、卤素、羟基、硝基、氨基或烷基；R.sub.3为氢或有机基团；R.sub.4为氢或取代或未取代的有机取代基；R.sub.5和R.sub.6代表有机和无机取代基；n为1、2、3或4。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。
• Certain fused pyrrolecarboxanilides; a new class of gaba brain receptor
  申请人：Neurogen Corporation

  公开号：US05925770A1

  公开（公告）日：1999-07-20

  The present invention encompasses structures of the formula: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## wherein: W represents substituted or unsubstituted phenyl; X is hydrogen, T is hydrogen, and n is 3, 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.

  本发明涵盖以下结构的化合物：## STR1 ## 或其药学上可接受的非毒性盐，其中：## STR2 ## 其中：W代表取代或未取代的苯基；X为氢，T为氢，n为3，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GABAa脑受体激动剂，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，苯二氮平类药物过量和增强记忆方面有用。