17-Hydroexemestane | 140461-66-1

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 类固醇和类固醇衍生物
• 英文名称: 17-Hydroexemestane
• 英文别名: 17-dihydroexemestane；(8R,9S,10R,13S,14S)-17-hydroxy-10,13-dimethyl-6-methylidene-8,9,11,12,14,15,16,17-octahydro-7H-cyclopenta[a]phenanthren-3-one
• CAS: 140461-66-1
• 化学式: C₂₀H₂₆O₂
• 分子量: 298.425
• InChiKey: NFDPYPMRHKQTDM-IMAGCOIZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  22
• 可旋转键数：
  0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.65
• 拓扑面积：
  37.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  丁二酸酐 、 17-Hydroexemestane 在 4-二甲氨基吡啶 、 三乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 48.0h， 以47%的产率得到
  参考文献：
  名称：

  An aromatase inhibitor in combination with Zinc(II) phthalocyanine for targeted therapy of post-menopausal breast cancer

  摘要：

  DOI：

  10.1016/j.dyepig.2022.110281
• 作为产物：
  描述：

  依西美坦 在 sodium tetrahydroborate 、 溶剂黄146 、 三氟乙酸 作用下， 以 二氯甲烷 、 乙腈 为溶剂， 以39%的产率得到17-Hydroexemestane
  参考文献：
  名称：

  An aromatase inhibitor in combination with Zinc(II) phthalocyanine for targeted therapy of post-menopausal breast cancer

  摘要：

  DOI：

  10.1016/j.dyepig.2022.110281

文献信息

• NOVEL COMPOSITION TO INCREASE LIBIDO
  申请人：Farber Michael

  公开号：US20090017107A1

  公开（公告）日：2009-01-15

  The present invention relates to a composition for increasing testosterone physiological levels comprising a sufficient amount of at least two ketosteroid derivatives of testosterone metabolism in association with a liposomal carrier bound to a saliva-absorbing carrier, wherein said increase in testosterone levels increases libido.

  本发明涉及一种用于增加睾酮生理水平的组合物，该组合物包含足够量的至少两种睾酮代谢的酮固醇衍生物与结合到唾液吸收载体的脂质体载体，其中睾酮水平的增加会增加性欲。
• Methods relating to aromatase inhibitor pharmacogenetics
  申请人：Lazarus Philip

  公开号：US08476023B2

  公开（公告）日：2013-07-02

  Methods for aiding in determining therapeutic efficacy of an aromatase inhibitor in a subject are provided according to embodiments of the present invention which include detecting expression and/or function of at least one UDP-glucuronosyltransferase having activity to modify at least one aromatase inhibitor and/or metabolite of the aromatase inhibitor by glucuronidation, wherein detection of expression and/or function of the UDP-glucuronosyltransferase is correlated with therapeutic efficacy of the aromatase inhibitor in the subject. Detection of UDP-glucuronosyltransferase expression and/or function includes detection of a UDP-glucuronosyltransferase gene deletion polymorphism in the subject.

  本发明的实施例提供了用于帮助确定受体内芳香化酶抑制剂的治疗效果的方法，其包括检测至少一种UDP-葡萄糖醛酸转移酶的表达和/或功能，该UDP-葡萄糖醛酸转移酶具有通过葡萄糖醛酸化修饰至少一种芳香化酶抑制剂和/或芳香化酶抑制剂代谢物的活性，其中检测UDP-葡萄糖醛酸转移酶的表达和/或功能与受体内芳香化酶抑制剂的治疗效果相关。检测UDP-葡萄糖醛酸转移酶的表达和/或功能包括检测受体内UDP-葡萄糖醛酸转移酶基因缺失多态性。
• METHODS RELATING TO AROMATASE INHIBITOR PHARMACOGENETICS
  申请人：LAZARUS PHILIP

  公开号：US20110033856A1

  公开（公告）日：2011-02-10

  Methods for aiding in determining therapeutic efficacy of an aromatase inhibitor in a subject are provided according to embodiments of the present invention which include detecting expression and/or function of at least one UDP-glucuronosyltransferase having activity to modify at least one aromatase inhibitor and/or metabolite of the aromatase inhibitor by glucuronidation, wherein detection of expression and/or function of the UDP-glucuronosyltransferase is correlated with therapeutic efficacy of the aromatase inhibitor in the subject. Detection of UDP-glucuronosyltransferase expression and/or function includes detection of a UDP-glucuronosyltransferase gene deletion polymorphism in the subject

  本发明的实施例提供了用于辅助确定芳香化酶抑制剂在受试者中的治疗效果的方法，其中包括检测至少一种UDP-葡萄糖醛酸转移酶的表达和/或功能，该酶具有通过葡萄糖醛酸化修饰至少一种芳香化酶抑制剂和/或芳香化酶抑制剂代谢产物的活性，在该受试者中检测UDP-葡萄糖醛酸转移酶的表达和/或功能与芳香化酶抑制剂的治疗效果相关联。检测UDP-葡萄糖醛酸转移酶的表达和/或功能包括检测受试者中的UDP-葡萄糖醛酸转移酶基因缺失多态性。
• NOVEL COMPOSITION TO INCREASE MUSCLE STRENGTH
  申请人：FARBER Mike

  公开号：US20080153788A1

  公开（公告）日：2008-06-26

  The present invention relates to a composition comprising a sufficient amount of at least two ketosteroid derivatives of testosterone's metabolism in association with a pharmaceutically acceptable carrier for increasing testosterone's physiological levels in a male subject.