Selective androgen receptor degrader (SARD) ligands and methods of use thereof
US10654809B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Mar 16, 2018 |
| Grant date | May 19, 2020 |
| Priority date | — |
| Expiry date | Mar 16, 2038 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D401/12
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including heterocyclic anilide rings and their synthetic precursors, R-isomers, and non-hydroxylated and/or non-chiral propanamides, and pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic 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.