Patent · US Active

Selective androgen receptor degrader (SARD) Ligands and methods of use thereof

US10441570B2 · kind B2 · utility

9Cited by
17References
66Claims
0Family size

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Key dates

Filing dateMay 16, 2018
Grant dateOct 15, 2019
Priority date
Expiry dateMay 24, 2038

Classification

  • Technology area (CPC A)Human Necessities
  • CPC primaryA61P35/00
  • 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.