发明名称 |
PARP MODULATORS AND TREATMENT OF CANCER |
摘要 |
The invention relates to a method of modulating poly(ADP-ribose)polymerase-l (PARP-I) activity in a mammal comprising administering to a mammal an effective amount of an organic aromatic compound having from 4 to about 35 carbon atoms, wherein said organic aromatic compound is capable of binding the arginine-34 moiety located in Zinc finger- 1 of the PARP-I enzyme and wherein said organic aromatic compound has electron donating capabilities such that it's tr-electron system will interact with the positively charged (cationic) guanidinium moiety of the specific arginine-34 residue of the Zinc-1 finger of PARP-I and does not contain benzamide or lactam substituents. In particular, substituted benzopyrones and substituted indoles and their pharmaceutical compositions containing such compounds that modulate the activity of PARP-I, are described. The invention is also directed to the composition of matter, kits and methods for their therapeutic and/or prophylactic use in treating diseases and disorders described herein, by administering effective amounts of such compounds. Preferably, the compositions and methods provided herein inhibit PARP activity. |
申请公布号 |
WO2006135873(A3) |
申请公布日期 |
2007.04.26 |
申请号 |
WO2006US22907 |
申请日期 |
2006.06.12 |
申请人 |
BIPAR SCIENCES, INC.;KUN, ERNEST;MENDELEYEV, JEROME;BAUER, PAL |
发明人 |
KUN, ERNEST;MENDELEYEV, JEROME;BAUER, PAL |
分类号 |
C07D295/00;C12P13/00 |
主分类号 |
C07D295/00 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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