915086-45-2Relevant academic research and scientific papers
Discovery of JNJ-63576253: A Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC)
Zhang, Zhuming,Connolly, Peter J.,Lim, Heng Keang,Pande, Vineet,Meerpoel, Lieven,Teleha, Christopher,Branch, Jonathan R.,Ondrus, Janine,Hickson, Ian,Bush, Tammy,Luistro, Leopoldo,Packman, Kathryn,Bischoff, James R.,Ibrahim, Salam,Parrett, Christopher,Chong, Yolanda,Gottardis, Marco M.,Bignan, Gilles
supporting information, p. 909 - 924 (2021/02/06)
Persistent androgen receptor (AR) activation drives therapeutic resistance to second-generation AR pathway inhibitors and contributes to the progression of advanced prostate cancer. One resistance mechanism is point mutations in the ligand binding domain
SUBSTITUTED HYDANTOIN AND THIOHYDANTOIN DERIVATIVES AS ANDROGEN RECEPTOR ANTAGONISTS
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Page/Page column 72, (2018/09/25)
Disclosed are compounds, compositions and methods for treating of disorders that are affected by the antagonism of one or more androgen receptor types. Such compounds are represented by Formula (I), wherein R1, R2a, R,2b,Z
SUBSTITUTED THIOHYDANTOIN DERIVATIVES AS ANDROGEN RECEPTOR ANTAGONISTS
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Page/Page column 188; 189; 190, (2017/08/07)
Disclosed are compounds, compositions and methods for treating of disorders that are affected by the antagonism of one or more androgen receptor types. Such compounds are represented by Formula (I) as follows: Formula (I) wherein R1 and G are defined herein.
Structure-activity relationship for thiohydantoin androgen receptor antagonists for castration-resistant prostate cancer (CRPC)
Jung, Michael E.,Ouk, Samedy,Yoo, Dongwon,Sawyers, Charles L.,Chen, Charlie,Tran, Chris,Wongvipat, John
experimental part, p. 2779 - 2796 (2010/09/05)
A structure-activity relationship study was carried out on a series of thiohydantoins and their analogues 14 which led to the discovery of 92 (MDV3100) as the clinical candidate for the treatment of hormone refractory prostate cancer.
DIARYLHYDANTOIN COMPOUNDS
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Page/Page column 31, (2008/06/13)
The present invention relates to diarylhydantoin compounds, including diarylthiohydantoins, and methods for syntheszing them and using them in the treatment of hormone refractory prostate cancer.
