SELECTIVE ANDROGEN RECEPTOR COVALENT ANTAGONISTS (SARCAS) AND METHODS OF USE THEREOF
Abstract:
This invention relates to selective androgen receptor covalent antagonists, synthetic intermediates and by-products, and related compounds, and compositions comprising the same, and uses thereof 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.
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