Selective androgen receptor degrader (SARD) ligands and methods of use thereof
US11230523B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | May 29, 2019 |
| Grant date | Jan 25, 2022 |
| Priority date | — |
| Expiry date | May 29, 2039 |
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 cyclic and heterocyclic anilide rings and their synthetic precursors, and mono-, di-, or multi-substituted N-heterocyclic rings, R-isomers, non-hydroxylated and/or non-chiral propanamides in treating androgen receptor dependent diseases and conditions such as hyperproliferations of the prostate including pre-malignancies and benign prostatic hyperplasia, 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.