发明申请
WO2009061781A1 NOVEL MODULATORS OF CELL CYCLE CHECKPOINTS AND THEIR USE IN COMBINATION WITH CHECKPOINT KINASE INHIBITORS
审中-公开
基本信息:
- 专利标题： NOVEL MODULATORS OF CELL CYCLE CHECKPOINTS AND THEIR USE IN COMBINATION WITH CHECKPOINT KINASE INHIBITORS
- 专利标题（中）：细胞周期检测点的新型调节因子及其与检测点激酶抑制剂的组合使用
- 申请号：PCT/US2008/082429 申请日：2008-11-05
- 公开(公告)号：WO2009061781A1 公开(公告)日：2009-05-14
- 发明人： GUZI, Timothy, J. , PARRY, David, A. , LABROLI, Marc, A. , DWYER, Michael, P. , PARUCH, Kamil , ROSNER, Kristen, E. , SHEN, Ruichao , POPOVICI-MULLER, Janeta
- 申请人： SCHERING CORPORATION , GUZI, Timothy, J. , PARRY, David, A. , LABROLI, Marc, A. , DWYER, Michael, P. , PARUCH, Kamil , ROSNER, Kristen, E. , SHEN, Ruichao , POPOVICI-MULLER, Janeta
- 申请人地址： 2000 Galloping Hill Road Kenilworth, NJ 07033 US
- 专利权人： SCHERING CORPORATION,GUZI, Timothy, J.,PARRY, David, A.,LABROLI, Marc, A.,DWYER, Michael, P.,PARUCH, Kamil,ROSNER, Kristen, E.,SHEN, Ruichao,POPOVICI-MULLER, Janeta
- 当前专利权人： SCHERING CORPORATION,GUZI, Timothy, J.,PARRY, David, A.,LABROLI, Marc, A.,DWYER, Michael, P.,PARUCH, Kamil,ROSNER, Kristen, E.,SHEN, Ruichao,POPOVICI-MULLER, Janeta
- 当前专利权人地址： 2000 Galloping Hill Road Kenilworth, NJ 07033 US
- 代理机构： KALYANARAMAN, Palaiyur, S.
- 优先权： US60/986,089 20071107
- 主分类号： C07H19/073
- IPC分类号： C07H19/073 ; C07H19/067 ; A61K31/7068 ; A61P35/00
摘要：
In its many embodiments, the present invention provides a novel class of pyrimidine analogs of formula (V) as targeted mechanism-based modulators of cell cycle checkpoints. Cancers and/or malignancies can be treated by administration of a cell cycle checkpoint modulator of the invention. Also discussed are suitable combinations of the cell cycle checkpoint modulator with a checkpoint kinase inhibitor to produce synergistic apoptosis in cancer cells. The invention includes methods of treating cancers by administering the combination of the cell cycle checkpoint modulator and the checkpoint kinase inhibitor, pharmaceutical compositions comprising the activator as well as the combination and pharmaceutical kits.
摘要（中）：
在其许多实施方案中，本发明提供了一类新颖的式（V）嘧啶类似物作为细胞周期检查点的靶向基于机制的调节剂。 可以通过施用本发明的细胞周期检查点调节剂来治疗癌症和/或恶性肿瘤。 还讨论了细胞周期检查点调节剂与检查点激酶抑制剂的合适组合，以在癌细胞中产生协同凋亡。 本发明包括通过施用细胞周期检查点调节剂和检查点激酶抑制剂的组合，包含活化剂的药物组合物以及组合药物试剂盒来治疗癌症的方法。
IPC结构图谱:
| C | 化学；冶金 |
| --C07 | 有机化学 |
| ----C07H | 糖类；及其衍生物；核苷；核苷酸；核酸 |
| ------C07H19/00 | 含有杂环与糖化物基团共有1个杂环原子的化合物；核苷；单核苷酸类；及其脱水衍生物 |
| --------C07H19/02 | .共有氮 |
| ----------C07H19/04 | ..仅含有氮作为杂环原子的杂环基 |
| ------------C07H19/06 | ...嘧啶基 |
| --------------C07H19/073 | ....以2-脱氧核糖基作为糖化物基 |