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1. 发明申请

WO2015089338A2 GLUCOCORTICOID INHIBITORS FOR TREATMENT OF PROSTATE CANCER 审中-公开
标题翻译：糖皮质激素抑制剂治疗前列腺癌
公开(公告)号：WO2015089338A2
公开(公告)日：2015-06-18
申请号：PCT/US2014069854
申请日：2014-12-11
申请人： SLOAN KETTERING INST CANCER
发明人： ARORA VIVEK , SAWYERS CHARLES L , EVANS MICHAEL J , VEACH DARREN R
IPC分类号： A61K31/573
CPC分类号： C07J17/00 , A61K31/416 , A61K31/4166 , A61K31/4439 , A61K31/5375 , A61K31/573 , A61K31/575 , A61K31/58 , A61K31/7105 , A61K31/713 , A61K45/06 , C07J9/00 , C07J43/003 , G01N33/743 , A61K2300/00
摘要： The present invention encompasses the recognition that reproducible and detectable changes in the level and or activity of Glucocorticoid Receptor (GR) are associated with incidence and/or risk of Castration Resistant Prostate Cancer (CRPC) and/or doubly resistant prostate cancer, specifically in individuals having prostate cancer and on antiandrogen therapy, and provides for the use of GR inhibitors to treat and/or reduce risk of CRPC and/or doubly resistant prostate cancer. In some embodiments, GR inhibitors also have Androgen Receptor (AR) inhibitory activity or are administered in conjunction with AR inhibitors. The present invention also provides technologies for identification and/or characterization of agents to treat and/or reduce risk of CRPC and/or doubly resistant prostate cancer; in some embodiments such agents alter level and/or activity of a GR. In some embodiments, provided agents show effects on a GR's activity of regulating transcription of one or more target genes. The present invention also provides systems for using such agents, for example to treat and/or reduce risk of CRPC and/or doubly resistant prostate cancer.
摘要翻译：本发明包括认识到糖皮质激素受体（GR）的水平和或活性的可重现和可检测的改变与去势抵抗性前列腺癌（CRPC）和/或双重抗性前列腺癌（特别是在个体中）的发病率和/或风险相关患有前列腺癌和抗雄激素疗法，并且提供GR抑制剂用于治疗和/或降低CRPC和/或双重抗性前列腺癌的风险的用途。在一些实施方案中，GR抑制剂还具有雄激素受体（AR）抑制活性或与AR抑制剂联合施用。本发明还提供了用于鉴定和/或表征治疗和/或降低CRPC和/或双重抗性前列腺癌风险的药剂的技术; 在一些实施方案中，这样的试剂改变GR的水平和/或活性。在一些实施方案中，提供的试剂显示对GR调节一种或多种靶基因转录的活性的作用。本发明还提供了使用这些药剂的系统，例如用于治疗和/或降低CRPC和/或双重抗性前列腺癌的风险。

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