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TRICYCLIC INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE
专利权人:
发明人:
SHEN, WANG,沈旺,沈旺,MAUNG, JACK,满 杰克,滿 杰克,ZHANG, AIMIN,张爱民,張愛民,ZHENG, XIAOLING,郑晓玲,鄭曉玲
申请号:
TW101119653
公开号:
TWI577693B
申请日:
2012.05.31
申请国别(地区):
TW
年份:
2017
代理人:
摘要:
The invention provides for compositions comprising phosphorous containing tricyclic compounds, including phthalazin-1(2H)-one derivatives. The compounds are potent inhibitors of the enzyme poly(ADP-ribose)polymerase (PARP), particularly PARP-1 and potentially PARP-2. The also show good cellular activity in inhibiting poly(ADP- ribose) oligomer formation. The compounds may be useful as mono-therapy or in combination with other therapeutic agents in the treatment conditions where PARP is implicated, such as cancer, inflammatory diseases and ischemic conditions. Thus, also provided are methods for the treatment of a condition where PARP is implicated comprising administering to an effective amount of a compound of the invention to an individual in need thereof.本發明提供包含含磷三環化合物(包括酞嗪-1(2H)-酮衍生物)之組合物。該等化合物係聚(ADP-核糖)聚合酶(PARP)、尤其PARP-1及潛在PARP-2之強效抑制劑。其亦在抑制聚(ADP-核糖)寡聚體形成中顯示良好細胞活性。該等化合物可作為單一療法或與其他治療劑組合用於治療與PARP有關之病況,例如癌症、發炎疾病及缺血性病況。因此,本發明亦提供治療與PARP有關病況的方法,其包含向有需要之個體投與有效量之本發明化合物。
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/
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