Selective androgen receptor degrader (SARD) ligands and methods of use thereof

US9814698B2 · kind B2 · utility

Assignees

• University of Tennessee Research Foundation · US
• GTX Corp · US

Inventors

• Ramesh Narayanan · Cordova, US
• Duane D. Miller · Germantown, US
• Thamarai Ponnusamy · Memphis, US
• Dong-Jin Hwang · Arlington, US
• Jayaprakash Pagadala · Boca Raton, US
• Charles B. Duke · Memphis, US
• Christopher C. Coss · Upper Arlington, US
• James T. Dalton · Columbus, US
• Yali He · Germantown, US

Key dates

• Filing date: Apr 21, 2016
• Grant date: Nov 14, 2017
• Expiry date: Apr 21, 2036

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D487/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

This invention provides novel indole, indazole, benzimidazole, indoline, quinolone, isoquinoline, and carbazole selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, androgenic alopecia or other hyper androgenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), and uterine fibroids, and to methods for reducing the levels of 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.