基本信息:
- 专利标题： NOVEL 1,2,4-BENZOTRIAZINE-1,4-DIOXIDES
- 专利标题（中）：新的1,2,4-苯并噻唑-1,4-二氧化物
- 申请号：PCT/NZ2005/000034 申请日：2005-03-01
- 公开(公告)号：WO2005082867A1 公开(公告)日：2005-09-09
- 发明人： DENNY, William, Alexander , HAY, Michael, Patrick , HICKS, Kevin, Owen , PRUIJN, Frederik, Bastiaan , WILSON, William, Robert , PCHALEK, Karin
- 申请人： AUCKLAND UNISERVICES LIMITED , DENNY, William, Alexander , HAY, Michael, Patrick , HICKS, Kevin, Owen , PRUIJN, Frederik, Bastiaan , WILSON, William, Robert , PCHALEK, Karin
- 申请人地址： Level 10,, 70 Symonds Street,, NZ-1001 Auckland NZ
- 专利权人： AUCKLAND UNISERVICES LIMITED,DENNY, William, Alexander,HAY, Michael, Patrick,HICKS, Kevin, Owen,PRUIJN, Frederik, Bastiaan,WILSON, William, Robert,PCHALEK, Karin
- 当前专利权人： AUCKLAND UNISERVICES LIMITED,DENNY, William, Alexander,HAY, Michael, Patrick,HICKS, Kevin, Owen,PRUIJN, Frederik, Bastiaan,WILSON, William, Robert,PCHALEK, Karin
- 当前专利权人地址： Level 10,, 70 Symonds Street,, NZ-1001 Auckland NZ
- 代理机构： BALDWINS
- 优先权： NZ531499 20040301
- 主分类号： C07D253/10
- IPC分类号： C07D253/10
摘要：
The present invention provides a simplified set of characteristics that can be used to select 1,2,4 benzotriazine 1,4 dioxide compounds (TPZ analogues) with therapeutic activity against hypoxic cells in human tumour xenografts, and to further provide a novel class of 1,2,4-benzotriazine-1,4-dioxides (TPZ analogues) with predicted in vivo activity against tumours, to their preparation, and to their use as hypoxia-selective cytotoxic drugs and radiosensitizers for cancer therapy, both alone or in combination with radiation and/or other anticancer drugs.
摘要（中）：
本发明提供了可用于选择具有针对人肿瘤异种移植物中缺氧细胞的治疗活性的1,2,4苯并三嗪二氧化物化合物（TPZ类似物）的简化的特征集，并进一步提供新的1类 ，具有预测的肿瘤体内活性的2,4-苯并三嗪-1,4-二氧化物（TPZ类似物），其制备及其作为用于癌症治疗的缺氧选择性细胞毒性药物和放射增敏剂的用途，单独或与 辐射和/或其他抗癌药物。
IPC结构图谱:
| C | 化学；冶金 |
| --C07 | 有机化学 |
| ----C07D | 杂环化合物 |
| ------C07D253/00 | 杂环化合物，含六元环、有3个氮原子作为仅有的杂环原子，C07D251/00组不包含的 |
| --------C07D253/02 | .不和其他环稠合 |
| ----------C07D253/10 | ..稠合的1,2,4-三嗪；氢化的稠合1,2,4-三嗪 |