rac-4-(3-(4-cyano-3-(trifluoromethyl)phenyl)-7,7-dimethyl-4-oxo-2-thioxo-1,3-diazaspiro[4.5]decan-1-yl)-2-fluoro-N-methylbenzamide | 1607853-88-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑烷类
• 英文名称: rac-4-(3-(4-cyano-3-(trifluoromethyl)phenyl)-7,7-dimethyl-4-oxo-2-thioxo-1,3-diazaspiro[4.5]decan-1-yl)-2-fluoro-N-methylbenzamide
• 英文别名: 4-(3-(4-cyano-3-(trifluoromethyl)phenyl)-7,7-dimethyl-4-oxo-2-thioxo-1,3-diazaspiro[4.5]decan-1-yl)-2-fluoro-N-methylbenzamide；4-[3-[4-cyano-3-(trifluoromethyl)phenyl]-7,7-dimethyl-4-oxo-2-sulfanylidene-1,3-diazaspiro[4.5]decan-1-yl]-2-fluoro-N-methylbenzamide
• CAS: 1607853-88-2
• 化学式: C₂₆H₂₄F₄N₄O₂S
• 分子量: 532.562
• InChiKey: SDCCTWOPPMGNLK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.4
• 重原子数：
  37
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  109
• 氢给体数：
  1
• 氢受体数：
  8

文献信息

• ANDROGEN RECEPTOR VARIANTS AND METHODS FOR MAKING AND USING
  申请人：MEMORIAL SLOAN-KETTERING CANCER CENTER

  公开号：US20150265587A1

  公开（公告）日：2015-09-24

  The present invention encompasses the recognition that an F876L mutation of the androgen receptor (AR) gene confers resistance to the antiandrogens enzalutamide (MDV3100) and ARN-509 and is associated with incidence and/or risk of castration resistant prostate cancer (CRPC). The present invention also provides other AR polypeptide sequences associated with increased incidence and/or risk of CRPC. The present invention also provides screening methods for identification and/or characterization of novel AR polypeptide sequences associated with increased incidence and/or risk of CRPC via exposure to antiandrogens and for identification and/or characterization of agents to treat and/or reduce risk of CRPC by virtue of their effect on AR transcriptional activation.

  本发明涵盖了一种认识到雄激素受体（AR）基因的F876L突变赋予抗雄激素恩扎鲁胺（MDV3100）和ARN-509的耐药性，并与去势抵抗性前列腺癌（CRPC）的发生率和/或风险相关的方法。本发明还提供了与增加CRPC发生率和/或风险相关的其他AR多肽序列。本发明还提供了筛选方法，用于通过暴露于抗雄激素并确定和/或表征与增加CRPC发生率和/或风险相关的新AR多肽序列，并通过其对AR转录激活的影响确定和/或表征治疗和/或降低CRPC风险的药剂。
• Androgen receptor variants and methods for making and using
  申请人：MEMORIAL SLOAN-KETTERING CANCER CENTER

  公开号：US10206911B2

  公开（公告）日：2019-02-19

  The present invention encompasses the recognition that an F876L mutation of the androgen receptor (AR) gene confers resistance to the antiandrogens enzalutamide (MDV3100) and ARN-509 and is associated with incidence and/or risk of castration resistant prostate cancer (CRPC). The present invention also provides other AR polypeptide sequences associated with increased incidence and/or risk of CRPC. The present invention also provides screening methods for identification and/or characterization of novel AR polypeptide sequences associated with increased incidence and/or risk of CRPC via exposure to antiandrogens and for identification and/or characterization of agents to treat and/or reduce risk of CRPC by virtue of their effect on AR transcriptional activation.

  本发明包括认识到雄激素受体（AR）基因的 F876L 突变可产生对抗雄激素恩杂鲁胺（MDV3100）和 ARN-509 的耐药性，并与阉割抵抗性前列腺癌（CRPC）的发病率和/或风险有关。本发明还提供了与 CRPC 发病率和/或风险增加有关的其他 AR 多肽序列。本发明还提供了筛选方法，用于鉴定和/或表征与通过暴露于抗雄激素而增加CRPC发病率和/或风险相关的新型AR多肽序列，以及鉴定和/或表征通过影响AR转录激活而治疗和/或降低CRPC风险的药物。
• Modulators of resistant androgen receptor
  申请人：Memorial Sloan-Kettering Cancer Center

  公开号：US10450294B2

  公开（公告）日：2019-10-22

  The present invention provides compounds useful as modulators, agonists or antagonists of androgen receptor (AR), compositions thereof, and methods of making and using the same.

  本发明提供了可用作雄激素受体（AR）的调节剂、激动剂或拮抗剂的化合物、其组合物及其制造和使用方法。
• MODULATORS OF RESISTANT ANDROGEN RECEPTOR
  申请人：MEMORIAL SLOAN-KETTERING CANCER CENTER

  公开号：US20150274693A1

  公开（公告）日：2015-10-01

  The present invention provides compounds useful as modulators, agonists or antagonists of androgen receptor (AR), compositions thereof, and methods of making and using the same. Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful in medicine, and particularly for treating any of a variety of diseases, disorders or conditions.
• US9365542B2
  申请人：——

  公开号：US9365542B2

  公开（公告）日：2016-06-14