Publication number: 20180360805
Abstract: This invention provides novel indole, indazole, benzimidazole, benzotriazole, indoline, quinolone, isoquinoline, and carbazole selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating hyperproliferations of the prostate including pre-malignancies and benign prostatic hyperplasia, prostate cancer, advanced prostate cancer, castration resistant prostate cancer, other AR-expressing cancers, androgenic alopecia or other hyper androgenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels (through degradation) and/or activity (through inhibition) of any androgen receptor including androgen receptor-full length (AR-FL) including pathogenic and/or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.
Type:
Application
Filed:
May 16, 2018
Publication date:
December 20, 2018
Applicants:
GTx, Inc., University of Tennessee Research Foundation
Inventors:
Ramesh NARAYANAN, Duane D. MILLER, Thamarai PONNUSAMY, Dong-Jin HWANG, Yali HE, Jayaprakash PAGADALA, Charles B, DUKE, Christopher C. COSS, James T. DALTON