Selective androgen receptor degrader (SARD) ligands and methods of use thereof
US10865184B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Sep 5, 2018 |
| Grant date | Dec 15, 2020 |
| Priority date | — |
| Expiry date | Sep 5, 2038 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D471/04
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.