The United States of America, as Represented by the Secretary, Department of Health and Human Services

The University of Texas System

University of California

Jane B Neckers

Leonard M Neckers

Yeong Sang Kim

Marc Cox

Aki Iwai

Yangmin Ning

Sunmin Lee

Heather A Balsiger

John A Beutler

W Marston Linehan

Vineet Kumar

Robert J Fletterick

Bradley T Scroggins

Johanny Kugelman-Tonos

Sanjay V Malhotra

Min-Jung Lee

Carole Ac Sourbier

Johanny Tonos De Leon

Carole Sourbier

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

Disclosed is a method of activating protein kinase C theta (PKC&#x3b8;) in an HIV or HTLV infected animal comprising administering to the animal an effective amount of a compound of formula (I): Formula (I), or an epimer thereof; wherein Ar and R-Rare described herein. Examples of diseases or conditions associated with PKC&#x3b8; include HIV1 infection, AIDS, HTLV infection, and adult T cell leukemia/lymphoma. 

Methods of treating patients infected with HIV and HTLV

Disclosed are methods of treating an animal for insulin resistance and associated diseases or conditions, activating the transcriptional activity of heat shock factor 1 (HSF1), or inducing the expression of heat shock protein 70 (HSP70) in an animal in need thereof, wherein the methods involve administering an effective amount of one or more compounds of formula (I) or an epimer thereof, wherein Ar, and R-Rare described herein. Examples of diseases or conditions associated with insulin resistance include diabetes, obesity, inflammation, metabolic syndrome, polycystic ovary disease, arteriosclerosis, non-alcoholic fatty liver disease, reproductive abnormality in a female, and growth abnormality. 

Methods of treating or preventing insulin resistance and associated diseases and conditions

Growing community of inventors

Bethesda, MD, United States of America

Jane B Neckers