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A POLY (ADP-RIBOSE) POLYMERASE-1 (PARP-1) INHIBITOR AND USES THEREFOR

机译：POLY（ADP-核糖）POLYMERASE-1（PARP-1）抑制剂及其用途

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摘要

Disclosed are Poly (ADP-ribose) polymerase-1 (PARP-1) inhibitors. Further disclosed are methods of synthesis. Of the compounds synthesized, 2-[p-(2-Fluoroethoxy)phenyl]-1.3.10-triazatricyclo[6.4.1.0^4,13]trideca-2,4(13),5,7-tetraen-9-one (12) had the highest inhibition potency for PARP-1 (IC₅₀ = 6.3 nM).

机译：公开了聚（ADP-核糖）聚合酶-1（PARP-1）抑制剂。进一步公开了合成方法。在合成的化合物中，2- [对-（2-氟乙氧基）苯基] -1.3.10-三氮杂三环[6.4.1.0 ^{4,13 ] trideca-2,4（13），5,7 -tetraen-9-one（ 12）对PARP-1的抑制能力最高（IC _{50 = 6.3 nM）。}} 展开▼

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公开/公告号EP3424909A1

专利类型

公开/公告日2019-01-09

原文格式PDF

申请/专利权人 WASHINGTON UNIVERSITY;
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申请/专利号EP20180190718

发明设计人 MACH ROBERT;CHU WENHUA;ZHOU DONG;MICHEL LOREN;CHEN DELPHINE;
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申请日2015-01-05

分类号C07D243/24;C07D235/26;A61K36/55;C07D263/62;C07D277/62;C07D411/04;A01N43/52;A01N43/76;A01N43/78;

国家 EP

入库时间 2022-08-21 12:25:45

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