GTx, Inc.;University of Tennessee Research Foundation
发明人:
Ramesh Narayanan,Duane D. Miller,Thamarai Ponnusamy,Dong-Jin Hwang,Jayaprakash Pagadala,Charles B. Duke,Christopher C. Coss,James T. Dalton,Yali He
申请号：
US15331777
公开号：
US10035763B2
申请日:
2016.10.21
申请国别(地区):
US
年份:
2018
代理人:
摘要：
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, 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.
