- 专利标题: Selective androgen receptor degrader (SARD) ligands and methods of use thereof
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申请号: US16556828申请日: 2019-08-30
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公开(公告)号: US11273147B2公开(公告)日: 2022-03-15
- 发明人: Ramesh Narayanan , Duane D. Miller , Thamarai Ponnusamy , Dong-Jin Hwang , Yali He , Jayaprakash Pagadala , Christopher C. Coss , James T. Dalton , Charles B. Duke
- 申请人: University of Tennessee Research Foundation
- 申请人地址: US TN Knoxville
- 专利权人: University of Tennessee Research Foundation
- 当前专利权人: University of Tennessee Research Foundation
- 当前专利权人地址: US TN Knoxville
- 代理机构: Knobbe, Martens, Olson & Bear, LLP
- 主分类号: A61K31/404
- IPC分类号: A61K31/404 ; A61K31/437 ; A61K31/4184 ; A61K31/47 ; A61P35/00 ; A61K31/403 ; A61K31/416 ; A61K31/4192 ; A61K31/472
摘要:
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.
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