spiro[6-(3-trifluoromethyl-phenyl)-imidazo[1,2-a]pyridin-2-one-3,1'-cyclohexane]

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并吡啶类
• 英文名称: spiro[6-(3-trifluoromethyl-phenyl)-imidazo[1,2-a]pyridin-2-one-3,1'-cyclohexane]
• 英文别名: 6-(3-trifluoromethyl-phenyl)-3,3-spiro[cyclohexane]-imidazo[1,2-a]pyridin-2-one；6'-[3-(Trifluoromethyl)phenyl]spiro[cyclohexane-1,3'-imidazo[1,2-a]pyridine]-2'-one
• 化学式: C₁₉H₁₇F₃N₂O
• 分子量: 346.352
• InChiKey: BNURYHPGPOCBJE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  25
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.37
• 拓扑面积：
  32.7
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  2-氨基-5-溴吡啶 在 四(三苯基膦)钯 sodium methylate 、 sodium ethanolate 、 potassium carbonate 作用下， 以 1,4-二氧六环 、 甲醇 、 乙醇 、 水 为溶剂， 反应 16.0h， 生成 spiro[6-(3-trifluoromethyl-phenyl)-imidazo[1,2-a]pyridin-2-one-3,1'-cyclohexane]
  参考文献：
  名称：

  3,3-二烷基-6-苯基-咪唑并吡啶酮的简易合成

  摘要：

  摘要 一系列带有 6-芳基的新型 3,3-二烷基化咪唑并吡啶酮被设计为活性孕酮拮抗剂 3,3-二取代-5-芳基吲哚的模拟物。描述了四步合成路线。关键步骤是碱催化环化、碱催化烷基化和 Suzuki 偶联反应。

  DOI：

  10.1080/00397910701215957

文献信息

• Pyridine Imidazoles and Aza-indoles as Progesterone Receptor Modulators
  申请人：Jiang Weiqin

  公开号：US20100016266A1

  公开（公告）日：2010-01-21

  The present invention is directed to novel heteroatom containing tetracyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders mediated by one or more estrogen receptors. The compounds of the invention are useful in the treatment of disorders associated with the depletion of estrogen such as hot flashes, vaginal dryness, osteopenia and osteoporosis; hormone sensitive cancers and hyperplasia of the breast, endometrium, cervix and prostate; endometriosis, uterine fibroids, osteoarthritis and as contraceptive agents, alone or in combination with a progestogen or progestogen antagonist.

  本发明涉及一种新型含杂原子的四环衍生物，以及包含它们的制药组合物，以及它们在治疗由一个或多个雌激素受体介导的疾病中的应用。本发明的化合物在治疗与雌激素耗竭有关的疾病方面具有用途，例如潮热、阴道干燥、骨质疏松和骨质疏松症；激素敏感性癌症和乳腺、子宫内膜、宫颈和前列腺的增生；子宫内膜异位症、子宫肌瘤、骨关节炎以及作为避孕剂，单独或与孕激素或孕激素拮抗剂联合使用。
• PYRIDINE IMIDAZOLES AND AZA-INDOLES AS PROGESTERONE RECEPTOR MODULATORS
  申请人：Jiang Weiqin

  公开号：US20080119500A1

  公开（公告）日：2008-05-22

  The present invention is directed to novel heteroatom containing tetracyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders mediated by one or more estrogen receptors. The compounds of the invention are useful in the treatment of disorders associated with the depletion of estrogen such as hot flashes, vaginal dryness, osteopenia and osteoporosis; hormone sensitive cancers and hyperplasia of the breast, endometrium, cervix and prostate; endometriosis, uterine fibroids, osteoarthritis and as contraceptive agents, alone or in combination with a progestogen or progestogen antagonist.

  本发明涉及新颖的含杂原子的四环衍生物，含有它们的制药组合物以及它们在治疗由一个或多个雌激素受体介导的疾病中的应用。本发明的化合物可用于治疗与雌激素耗竭有关的疾病，如潮热、阴道干燥、骨质疏松和骨质疏松症；激素敏感性癌症和乳腺、子宫内膜、宫颈和前列腺的增生；子宫内膜异位症、子宫肌瘤、骨关节炎以及作为避孕剂，单独使用或与孕激素或孕激素拮抗剂联合使用。
• Pyridine imidazoles and aza-indoles as progesterone receptor modulators
  申请人：Janssen Pharmaceutica NV

  公开号：EP2502925A1

  公开（公告）日：2012-09-26

  The present invention is directed to novel pyrimidine imidazoles and aza-indoles according to formulae (I) and (II), pharmaceutical compositions containing them and their use in the treatment of disorders mediated by one or more estrogen receptors. The compounds of the invention are useful in the treatment of disorders associated with the depletion of estrogen such as hot flashes, vaginal dryness, osteopenia and osteoporosis; hormone sensitive cancers and hyperplasia of the breast, endometrium, cervix and prostate; endometriosis, uterine fibroids, osteoarthritis and as contraceptive agents, alone or in combination with a progestogen or progestogen antagonist

  本发明涉及符合式(I)和(II)的新型嘧啶咪唑和氮杂吲哚、含有它们的药物组合物以及它们在治疗由一种或多种雌激素受体介导的疾病中的用途。本发明的化合物可用于治疗与雌激素耗竭有关的疾病，如潮热、阴道干燥、骨质疏松和骨质疏松症；对激素敏感的癌症和乳腺、子宫内膜、宫颈和前列腺增生；子宫内膜异位症、子宫肌瘤、骨关节炎；以及单独或与孕激素或孕激素拮抗剂合用作为避孕药物。
• US7348432B2
  申请人：——

  公开号：US7348432B2

  公开（公告）日：2008-03-25
• US7608712B2
  申请人：——

  公开号：US7608712B2

  公开（公告）日：2009-10-27