Massachusetts Institute of Technology

Nicholas B Struntz

Angela N Koehler

Andrew Raymond Chen

Francisco Caballero

Eric Stefan

Dylan Vijith Neel

Helen L Evans

Shelby Doyle

David C Freeman

Andre Richters

Provided herein are compounds useful for modulating the activity of an androgen receptor, or a variant thereof, and related compositions and methods. Compounds of the invention are useful for antagonizing the androgen receptor splice variant AR-v7, and for the treatment of castration-resistant prostate cancer.

Small molecule modulators of the androgen receptor

The present disclosure provides compounds of Formula (I'), Formula (I), Formula (II), Formula (II-A), Formula (III), and Formula (IV). The compounds described herein are MAX binders and/or modulators of Myc, Mad, or Mxi1 (e.g., inhibitors of Myc, Mad, or Mxi1), and may be useful in treating a subject with a disease associated with Myc, such as proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions and kits including the compounds described herein, as well as methods of using and uses of the compounds, compositions, and kits. 

Max binders as MYC modulators and uses thereof

Growing community of inventors

Cambridge, MA, United States of America

Nicholas B Struntz