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CN104685072A 用于确定抵抗雄激素受体疗法的方法和组合物 无效 - 驳回 复审申请

用于确定抵抗雄激素受体疗法的方法和组合物
摘要：
本文描述了经修饰的雄激素受体多肽，其对雄激素受体抑制剂的抑制作用具有抵抗性。本文描述了含有所述经修饰的雄激素受体多肽的组合物、组合和试剂盒，以及使用所述经修饰的雄激素受体多肽的方法。本文还描述了使用所述经修饰的雄激素受体多肽作为筛选剂来鉴定和设计第三代雄激素受体调节剂的方法。本文还描述了抑制所述经修饰的雄激素受体多肽的活性的第三代雄激素受体调节剂。还描述了包含本文描述的化合物的药物组合物和药剂，以及单独使用或与其他化合物组合地使用此类雄激素受体调节剂来治疗疾病或病症的方法，所述疾病或病症包括由雄激素受体介导或依赖于雄激素受体的癌症，诸如去势抵抗性前列腺癌。
摘要（英）：

Described herein are modified androgen receptor polypeptides that are resistant to inhibition by an androgen receptor inhibitor. Described herein are compositions, combinations, and kits containing the modified androgen receptor polypeptides and methods of using the modified androgen receptor polypeptides. Also described herein are methods of using the modified androgen receptor polypeptides as screening agents for the identification and design of third-generation androgen receptor modulators. Also described herein are third-generation androgen receptor modulators that inhibit the activity of the modified androgen receptor polypeptides. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such androgen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions, including cancers, such as castration resistant prostate cancers, that are mediated or dependent upon androgen receptors.

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