16-05-2019 дата публикации
Номер: US20190144387A1
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. 4. The compound of claim 1 , wherein W claim 1 , W claim 1 , W claim 1 , W claim 1 , W claim 1 , and Ware CH.5. The compound of claim 1 , wherein Wis N and W claim 1 , W claim 1 , W claim 1 , W claim 1 , and Ware CH.6. The compound of claim 1 , wherein Wis N and W claim 1 , W claim 1 , W claim 1 , W claim 1 , and Ware CH.7. The compound of claim 1 , wherein Wis N and W claim 1 , W claim 1 , W claim 1 , W claim 1 , Ware CH.8. The compound of claim 1 , wherein only one of X claim 1 , X claim 1 , X claim 1 , X claim 1 , and Xare N.9. The compound of claim 1 , wherein Xor Xis N.10. The compound of claim 1 , wherein Xor Xis N.11. The compound of claim 1 , wherein Xis N.12. The compound of claim 1 , wherein Xis N and X claim 1 , X claim 1 , X claim 1 , and Xare CH.14. The compound of claim 1 , wherein Q is H claim 1 , NO claim 1 , COR claim 1 , alkyl claim 1 , alkoxy claim 1 , aryl claim 1 , CN claim 1 , CF claim 1 , F claim 1 , Cl claim 1 , Br or I.15. The compound of claim 1 , wherein Z is CN.16. The compound of claim 1 , wherein Y is Cl or CF.18. ...
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