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

University of Texas System

University of California

Yeong Sang Kim

Jane B Neckers

Leonard M Neckers

Marc Cox

Aki Iwai

Heather A Balsiger

Vineet Kumar

Robert J Fletterick

Jane B Trepel

Yangmin Ning

Sunmin Lee

Sanjay V Malhotra

Johanny Kugelman-Tonos

Johanny Tonos De Leon

Marc B Cox

Johanny Meneses De Leon

Disclosed are compounds which are nuclear receptor modulators that can act as antagonists to the androgen receptor, for example, a compound of Formula I: wherein Rto Rand Xto Xare as described herein, as well as pharmaceutically acceptable salts, solvates, and stereoisomers thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment for cancers, including prostate cancers, other nuclear receptor mediated cancers, and other conditions, are also disclosed.

Nuclear receptor modulators and their use for the treatment and prevention of cancer

Disclosed are compounds which are nuclear receptor modulators that can act as antagonists to the androgen receptor, for example, a compound of Formula I: wherein Rto Rand Xto Xare as described herein, as well as pharmaceutically acceptable salts, solvates, and stereoisomers thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment for cancers, including prostate cancers, other nuclear receptor mediated cancers, and other conditions, are also disclosed. 

Pharmaceutical compositions that bind to a predicted FK506 Binding Protein 52 (FKBP52) interaction surface on the androgen receptor hormone binding domain, otherwise known as FKBP52 Targeting Agents (FTAs) are provided. These compositions of the present invention are found to specifically recognize the FKBP52 regulatory surface on the androgen receptor and inhibit FKBP52 from functionally interacting with the androgen receptor. Compositions comprising the pharmaceutical composition, as well as methods of use, treatment and screening are also provided.

Pharmaceutical compositions which inhibit FKBP52-mediated regulation of androgen receptor function and methods of using same

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Gaithersburg, MD, United States of America

Yeong Sang Kim