基本信息:
- 专利标题： ISOQUINOLIN-1 (2H) -ONE DERIVATIVES AS PARP-1 INHIBITORS
- 专利标题（中）：作为PARP-1抑制剂的异喹啉-1（2H） - 酮衍生物
- 申请号：PCT/EP2010/056921 申请日：2010-05-19
- 公开(公告)号：WO2010133647A1 公开(公告)日：2010-11-25
- 发明人： PAPEO, Gianluca Mariano Enrico , BERTRAND, Jay Aaron , CERVI, Giovanni , FORTE, Barbara , LUPI, Rosita , MONTAGNOLI, Alessia , SCOLARO, Alessandra , ZUCCOTTO, Fabio , ORSINI, Paolo , POSTERI, Helena
- 申请人： NERVIANO MEDICAL SCIENCES S.r.l. , PAPEO, Gianluca Mariano Enrico , BERTRAND, Jay Aaron , CERVI, Giovanni , FORTE, Barbara , LUPI, Rosita , MONTAGNOLI, Alessia , SCOLARO, Alessandra , ZUCCOTTO, Fabio , ORSINI, Paolo , POSTERI, Helena
- 申请人地址： PO Box 11 Viale Pasteur, 10 I-20014 Nerviano (MI) IT
- 专利权人： NERVIANO MEDICAL SCIENCES S.r.l.,PAPEO, Gianluca Mariano Enrico,BERTRAND, Jay Aaron,CERVI, Giovanni,FORTE, Barbara,LUPI, Rosita,MONTAGNOLI, Alessia,SCOLARO, Alessandra,ZUCCOTTO, Fabio,ORSINI, Paolo,POSTERI, Helena
- 当前专利权人： NERVIANO MEDICAL SCIENCES S.r.l.,PAPEO, Gianluca Mariano Enrico,BERTRAND, Jay Aaron,CERVI, Giovanni,FORTE, Barbara,LUPI, Rosita,MONTAGNOLI, Alessia,SCOLARO, Alessandra,ZUCCOTTO, Fabio,ORSINI, Paolo,POSTERI, Helena
- 当前专利权人地址： PO Box 11 Viale Pasteur, 10 I-20014 Nerviano (MI) IT
- 代理机构： NERVIANO MEDICAL SCIENCES S.r.l.
- 优先权： EP09160869.5 20090521
- 主分类号： C07D217/24
- IPC分类号： C07D217/24 ; C07D401/04 ; A61K31/472 ; A61K31/4725 ; A61P9/00 ; A61P25/00 ; A61P29/00 ; A61P35/00
摘要：
There are provided substituted isoquinolin-1(2H)-one derivatives which selectively inhibit the activity of poly (ADP- ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of the present invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds. A screening method for the identification of compounds capable of binding several PARP proteins, as well the probes used in such method, are further objects of the invention.
摘要（中）：
提供了相对于聚（ADP-核糖）聚合酶PARP-2选择性地抑制聚（ADP-核糖）聚合酶PARP-1的活性的取代的异喹啉-1（2H） - 酮衍生物。 因此，本发明的化合物可用于治疗诸如癌症，心血管疾病，中枢神经系统损伤和不同形式的炎症的疾病。 本发明还提供了制备这些化合物的方法，包含这些化合物的药物组合物，以及利用包含这些化合物的药物组合物治疗疾病的方法。 用于鉴定能够结合若干PARP蛋白的化合物的筛选方法以及在该方法中使用的探针是本发明的另外的目的。
IPC结构图谱:
| C | 化学；冶金 |
| --C07 | 有机化学 |
| ----C07D | 杂环化合物 |
| ------C07D217/00 | 杂环化合物，含异喹啉或氢化异喹啉环系 |
| --------C07D217/02 | .只有氢原子或仅含碳或氢原子的基直接连在含氮环的碳原子上：烷撑-双-异喹啉 |
| ----------C07D217/24 | ..氧原子 |