National Institutes of Health, a Component of the US Dept. of Health & Human Services

Other

University of Delaware

Elias Set Jenö Arnér

Arner, Elias Set Jeno

Thomas S Dexheimer

Anton Simeonov

David Joseph Maloney

Ajit Jadhav

Diane K Luci

William Chester Stafford

Nathan Patrick Coussens

Elias Set Arner

Diane Karen Luci

Yves Pommier

Christophe Marchand

Zhihao Zhuang

Andrew S Rosenthal

Qin Liang

Periyasamy Selvam

Kasthuraiah Maddali

Nathan Coussens

There is provided compounds of formula (I) or pharmaceutically-acceptable salts thereof, wherein W, X, Y, Z, R, Rand Rhave meanings provided in the description, which compounds are useful in the treatment of cancers. 

Pyridazinones and their use in the treatment of cancer

There is provided compounds of formula (I) or pharmaceutically-acceptable salts thereof, wherein L, R, R, R, Rand n have meanings provided in the description, which compounds are useful in the treatment of cancers. 

Pyridines and their use in the treatment of cancer

There is provided compounds of formula (I), or pharmaceutically-acceptable salts thereof, wherein X, Y, Z, Rand Rhave meanings provided in the description, which compounds are useful in the treatment of cancers. 

Tricyclic compounds and their use in the treatment of cancer

Disclosed are inhibitors of the USP1/UAF1 deubiquitinase complex, for example. of formula (I), wherein R, R, 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.

Inhibitors of the USP1/UAF1 deubiquitinase complex and uses thereof

A method for treating cancer in a subject, comprising administering to a subject having cancer a therapeutically effective amount of (i) a fluoroquinolone derivative that inhibits tyrosyl-DNA-phosphodiesterase 1 (Tdp1) activity or (ii) a sulfonamide moiety-containing compound that inhibits tyrosyl-DNA-phosphodiesterase 1 (Tdp1) activity, thereby treating the cancer in the subject. In certain embodiments, the fluoroquinolone derivative or sulfonamide moiety-containing compound is co-administered with a topoisomerase I (TopI) inhibitor.

Fluoroquinolone derivatives or sulfonamide moiety-containing compounds as inhibitors of tyrosyl-dnaphosphodiesterase (TDP1)

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Lansing, MI, United States of America

Thomas S Dexheimer