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SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF

机译:选择性雄激素受体降解剂(SARD)配体及其使用方法

摘要

This invention is directed to selective androgen receptor degrader (SARD) compounds including heterocyclic rings 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.
机译:本发明涉及选择性雄激素受体降解剂(SARD)化合物,包括杂环环和药物组合物及其用途,用于治疗前列腺癌,晚期前列腺癌,抗阉割前列腺癌,三重阴性乳腺癌,表达雄激素受体的其他癌症,雄激素癌症或其他高肾性皮肤病,肯尼迪的疾病,肌萎缩侧面硬化(ALS),腹主动脉瘤(AAA)和子宫肌瘤,以及降低包括致病或抗性突变的雄激素受体 - 全长(AR-FL)水平的方法,在受试者中的Ar - 剪接变体(Ar-SV)和致病性聚谷氨酰胺(PolyQ)多态性。

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