3-(1-hydroxyethyl)-1,2,4-benzotriazine 1-oxide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 三嗪类
• 英文名称: 3-(1-hydroxyethyl)-1,2,4-benzotriazine 1-oxide
• 英文别名: 1-(1-Oxido-1,2,4-benzotriazin-1-ium-3-yl)ethanol
• 化学式: C₉H₉N₃O₂
• 分子量: 191.189
• InChiKey: LOVQYKKKQCCVNO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.2
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  71.5
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  3-chloro-1,2,4-benzotriazine 1-oxide 、 tritoluyl phosgene 、 钯 在 三乙胺 作用下， 以 乙腈 为溶剂， 生成 3-(1-hydroxyethyl)-1,2,4-benzotriazine 1-oxide 、 3-vinyl-1,2,4-benzotriazine-1-oxide
  参考文献：
  名称：

  Method of treating a mammal having a solid tumor susceptible to

  摘要：

  治疗患有对顺铂治疗敏感的实体肿瘤的哺乳动物的方法包括：向哺乳动物施用有效量的3-氨基-1,2,4-苯并三氮唑-1,4-二氧化物；并在向哺乳动物施用3-氨基-1,2,4-苯并三氮唑-1,4-二氧化物后约0.5至约五小时内向哺乳动物施用有效量的顺铂。

  公开号：

  US05484612A1

文献信息

• Method of tumor treatment
  申请人：THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY

  公开号：EP0649658A1

  公开（公告）日：1995-04-26

  The present invention provides methods for increasing the cytotoxicity of a chemotherapy agent towards a solid tumor, such tumor susceptible to treatment with the chemotherapy agent, comprising administering to a mammal having such a tumor, from about one half hour to about twenty-four hours prior to administering the chemotherapy agent, or from about one hour to about two hours after administering the chemotherapy agent, a cytotoxicity-enhancing amount of a compound of Formula I. The invention also provides kits for treatment of such tumors which comprise a chemotherapy agent and a cytotoxicity-enhancing amount of a 1,2,4-benzotriazine oxide as defined in Formula I. The present invention also provides the use of a compound of Formula I capable of exerting a cytotoxic-enhancing effect on a cancer tumor for the manufacture of a medicament, for the therapeutic administration to a mammal having such a tumour from about one half hour to about twenty-four hours prior to treatment of said tumor with a chemotherapy agent.

  本发明提供了增加化疗剂对实体瘤的细胞毒性的方法，这种肿瘤易受化疗剂的治疗，包括在施用化疗剂前约半小时至约二十四小时，或在施用化疗剂后约一小时至约两小时，向患有这种肿瘤的哺乳动物施用增强细胞毒性量的式Ⅰ化合物。本发明还提供了用于治疗此类肿瘤的试剂盒，该试剂盒包含化疗剂和细胞毒性增强量的如式Ⅰ所定义的1,2,4-苯并三嗪氧化物。 本发明还提供了能够对癌症肿瘤产生细胞毒性增强作用的式 I 化合物用于制造药物，以便在用化疗剂治疗所述肿瘤前约半小时至约二十四小时内对患有此类肿瘤的哺乳动物进行治疗给药。
• Use of 1,2,4-benzotriazine oxides for the preparation of a medicament for the treatment of tumours
  申请人：THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY

  公开号：EP0972517A2

  公开（公告）日：2000-01-19

  The present invention provides methods for treating mammalian cancer tumors, preferably solid tumors, comprising administering to a mammal in need of such treatment an effective amount of a 1,2,4-benzotriazine oxide as defined in Formula I or pharmacologically acceptable salts of said compound; and administering to the mammal from about one half hour to about twenty-four hours after administering the 1,2,4-benzotriazine oxide an effective amount of a chemotherapy agent to which the tumor is susceptible. The invention also provides kits for treatment of such tumors which comprise a chemotherapy agent and a cytotoxicity-enhancing amount of a 1,2,4-benzotriazine oxide as defined in Formula I.

  本发明提供了治疗哺乳动物癌症肿瘤，优选实体瘤的方法，包括给需要这种治疗的哺乳动物施用有效量的如式I所定义的1，2，4-苯并三嗪氧化物或所述化合物的药理学上可接受的盐；以及在施用1，2，4-苯并三嗪氧化物后约半小时至约二十四小时内给哺乳动物施用有效量的肿瘤易感的化疗剂。本发明还提供了用于治疗此类肿瘤的试剂盒，该试剂盒包括化疗剂和细胞毒性增强量的如式Ⅰ所定义的1，2，4-苯并三嗪氧化物。
• Use of 1,2,4-benzotriazine oxides for the manufacture of a medicament for the treatment of tumors
  申请人：THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY

  公开号：EP0649658B1

  公开（公告）日：2000-06-14
• Use of 1,2,4-benzotriazine oxides for the preparation of a medicament for the treatment of tumors
  申请人：THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY

  公开号：EP0972517B1

  公开（公告）日：2004-07-07
• US5484612A
  申请人：——

  公开号：US5484612A

  公开（公告）日：1996-01-16