发明申请
WO2008075007A1 MORPHOLINO-SUBSTITUTED BICYCLOHETEROARYL COMPOUNDS AND THEIR USE AS ANTI CANCER AGENTS
审中-公开
基本信息:
- 专利标题： MORPHOLINO-SUBSTITUTED BICYCLOHETEROARYL COMPOUNDS AND THEIR USE AS ANTI CANCER AGENTS
- 专利标题（中）：吗啡取代的双环蛋白化合物及其作为抗癌剂的用途
- 申请号：PCT/GB2007/004819 申请日：2007-12-14
- 公开(公告)号：WO2008075007A1 公开(公告)日：2008-06-26
- 发明人： COLLINS, Ian , READER, John, Charles , CHEUNG, Kwai, Ming , MATTHEWS, Thomas, Peter , PROISY, Nicolas , KLAIR, Sukhbinder, Singh
- 申请人： CANCER RESEARCH TECHNOLOGY LIMITED , COLLINS, Ian , READER, John, Charles , CHEUNG, Kwai, Ming , MATTHEWS, Thomas, Peter , PROISY, Nicolas , KLAIR, Sukhbinder, Singh
- 申请人地址： Sardinia House Sardinia Street London Greater London WC2A 3NL GB
- 专利权人： CANCER RESEARCH TECHNOLOGY LIMITED,COLLINS, Ian,READER, John, Charles,CHEUNG, Kwai, Ming,MATTHEWS, Thomas, Peter,PROISY, Nicolas,KLAIR, Sukhbinder, Singh
- 当前专利权人： CANCER RESEARCH TECHNOLOGY LIMITED,COLLINS, Ian,READER, John, Charles,CHEUNG, Kwai, Ming,MATTHEWS, Thomas, Peter,PROISY, Nicolas,KLAIR, Sukhbinder, Singh
- 当前专利权人地址： Sardinia House Sardinia Street London Greater London WC2A 3NL GB
- 代理机构： WYTENBURG, Wilhelmus et al.
- 优先权： GB0625633.3 20061221; US60/876,137 20061221
- 主分类号： C07D471/04
- IPC分类号： C07D471/04 ; C07D473/34 ; C07D487/04 ; A61K31/52 ; A61K31/519 ; A61K31/437 ; A61P35/00 ; A61P29/00
摘要：
The present invention pertains generally to the field of therapeutic compounds, and mor specifically to certain morpholino-substituted bicydoheteroaryl compounds (referred to herein as MBHA compounds), of the following formula: and especially certain morpholino-substituted 7H- pyrrolo[2,3-dlpyrimidine and moφholino-substituted 1H-pyrazolo[3.4-b]pyridine compounds, which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or Il inhibitor, (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.
摘要（中）：
本发明一般涉及治疗化合物领域，具体涉及下列通式的某些吗啉代取代的双环杂芳基化合物（本文称为MBHA化合物），特别是某些吗啉代取代的7H-吡咯并[2,3- dl嘧啶和吗啉代取代的1H-吡唑并[3,4-b]吡啶化合物，其特别是抑制检测点激酶1（CHK1）激酶功能。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内都用于抑制CHK1激酶功能以及治疗由CHK1介导的疾病和病症的用途，其被改善 通过抑制CHK1激酶功能等，包括增殖条件如癌症等，任选地与另一种试剂组合，例如（a）DNA拓扑异构酶I或II抑制剂，（b）DNA损伤剂; （c）抗代谢物或TS抑制剂; （d）微管靶向剂; 和（e）电离辐射。
IPC结构图谱:
| C | 化学；冶金 |
| --C07 | 有机化学 |
| ----C07D | 杂环化合物 |
| ------C07D471/00 | 在稠环系中含有氮原子作为仅有的杂环原子、其中至少1个环是含有1个氮原子的六元环的杂环化合物，C07D451/00至C07D463/00不包括的 |
| --------C07D471/02 | .在稠环系中含两个杂环 |
| ----------C07D471/04 | ..邻位稠环系 |