公开(公告)号：US09802904B2

公开(公告)日：2017-10-31

申请号：US14655538

申请日：2013-12-26

申请人： The United States of America, as represented by the Secretary, Department of Health and Human Services ,  University of Delaware

发明人： David J. Maloney ,  Andrew S. Rosenthal ,  Ajit Jadhav ,  Thomas S. Dexheimer ,  Anton Simeonov ,  Zhihao Zhuang ,  Qin Liang ,  Diane K. Luci

IPC分类号： A61K31/505 ,  A61K31/506 ,  C07D239/42 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D239/94 ,  C07D405/14 ,  C07D405/12 ,  C07D409/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D495/04

CPC分类号： C07D239/94 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D495/04

摘要： Disclosed are inhibitors of the USP1/UAF1 deubiquitinase complex, for example. of formula (I), wherein R1, R2, and Q are as defined herein, which are useful in treating diseases such as cancer, and improving the efficacy of DNA damaging agents in cancer treatment. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least one compound of the invention, a method of method of inhibiting a heterodimeric deubiquitinase complex in a cell, and a method of enhancing the chemotherapeutic treatment of cancer in a mammal undergoing treatment with an anti cancer agent. Further disclosed is a method of preparing compounds of the invention.

公开(公告)号：US20150344443A1

公开(公告)日：2015-12-03

申请号：US14655538

申请日：2013-12-26

申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN ,  UNIVERSITY OF DELAWARE

发明人： David J. Maloney ,  Andrew S. Rosenthal ,  Ajit Jadhav ,  Thomas S. Dexheimer ,  Anton Simeonov ,  Zhihao Zhuang ,  Qin Liang ,  Diane K. Luci

IPC分类号： C07D239/94 ,  C07D405/12 ,  C07D495/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/12 ,  C07D401/12

CPC分类号： C07D239/94 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D495/04

摘要： Disclosed are inhibitors of the USP1/UAF1 deubiquitinase complex, for example. of formula (I), wherein R1, R2, and Q are as defined herein, which are useful in treating diseases such as cancer, and improving the efficacy of DNA damaging agents in cancer treatment. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least one compound of the invention, a method of method of inhibiting a heterodimeric deubiquitinase complex in a cell, and a method of enhancing the chemotherapeutic treatment of cancer in a mammal undergoing treatment with an anti cancer agent. Further disclosed is a method of preparing compounds of the invention.

摘要翻译： 公开了例如USP1 / UAF1去泛素化酶复合物的抑制剂。 式（I）的化合物，其中R1，R2和Q如本文所定义，其可用于治疗诸如癌症的疾病，以及提高DNA损伤剂在癌症治疗中的功效。 还公开了包含药学上合适的载体和本发明的至少一种化合物，抑制细胞中异二聚体脱蛋白酶复合物的方法的方法的组合物，以及在接受治疗的哺乳动物中增强癌症化学治疗的方法 抗癌剂。 进一步公开了制备本发明化合物的方法。