7-methoxy-4-methyl-3-(1-oxy-pyridin-4-yl)-chromen-2-one | 902130-92-1

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 香豆素及其衍生物
• 英文名称: 7-methoxy-4-methyl-3-(1-oxy-pyridin-4-yl)-chromen-2-one
• 英文别名: 7-Methoxy-4-methyl-3-(1-oxidopyridin-1-ium-4-yl)chromen-2-one
• CAS: 902130-92-1
• 化学式: C₁₆H₁₃NO₄
• 分子量: 283.284
• InChiKey: ZJFDHRKNONEZGJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  21
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  61
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  7-methoxy-4-methyl-3-pyridin-4-yl-2H-chromen-2-one 在 间氯过氧苯甲酸 作用下， 以 二氯甲烷 为溶剂， 生成 7-methoxy-4-methyl-3-(1-oxy-pyridin-4-yl)-chromen-2-one
  参考文献：
  名称：

  WO2006/78834

  摘要：

  公开号：

文献信息

• Novel heterocyclic benzo[c]chromene derivatives useful as modulators of the estrogen receptors
  申请人：Zhang Xuqing

  公开号：US20060205741A1

  公开（公告）日：2006-09-14

  The present invention is directed to novel heterocyclic benzo[c]chromene 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.

  本发明涉及新型杂环苯并[c]色烯衍生物、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。本发明的化合物在治疗与雌激素耗竭相关的疾病方面有用，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药物，单独或与孕激素或孕激素拮抗剂联合使用。
• NOVEL HETEROCYCLIC BENZO[C]CHROMENE DERIVATIVES USEFUL AS MODULATORS OF THE ESTROGEN RECEPTORS
  申请人：Zhang Xuqing

  公开号：US20080221125A1

  公开（公告）日：2008-09-11

  The present invention is directed to novel heterocyclic benzo[c]chromene 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.

  本发明涉及新型杂环苯并[c]色烯衍生物，包括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方面的用途。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、骨质疏松症和骨质疏松症；激素敏感性癌症和乳腺、子宫内膜、子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。
• NOVEL HETEROCYCLIC BENZOY[C]CHROMENE DERIVATIVES USEFUL AS MODULATORS OF THE ESTROGEN RECEPTORS
  申请人：JANSSEN PHARMACEUTICA N.V.

  公开号：EP1846397A1

  公开（公告）日：2007-10-24
• US7399767B2
  申请人：——

  公开号：US7399767B2

  公开（公告）日：2008-07-15
• [EN] NOVEL HETEROCYCLIC BENZO[C]CHROMENE DERIVATIVES USEFUL AS MODULATORS OF THE ESTROGEN RECEPTORS<br/>[FR] NOUVEAUX DERIVES DE BENZO[C]CHROMENE HETEROCYCLIQUES UTILES EN TANT QUE MODULATEURS DES RECEPTEURS AUX OESTROGENES
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2006078834A1

  公开（公告）日：2006-07-27

  [EN] The present invention is directed to novel heterocyclic benzo[c]chromene derivatives of Formula (I), 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.
  [FR] La présente invention se rapporte à de nouveaux dérivés de benzo[c]chromène hétérocycliques de la formule (I), à des compositions pharmaceutiques les contenant, et à leur utilisation pour traiter des troubles causés par un ou plusieurs récepteurs aux oestrogènes. Les composés selon l'invention sont utiles pour traiter : les troubles associés au manque d'oestrogène, tels que les bouffées de chaleurs, la sécheresse vaginale, l'ostéopénie et l'ostéoporose ; les cancers hormonosensibles et l'hyperplasie du sein, de l'endomètre, du col de l'utérus et de la prostate ; l'endométriose, les léiomyomes utérins, l'arthrose. Lesdits composés peuvent également être utilisés comme agents contraceptifs, seuls ou en combinaison avec un progestagène ou un antagoniste du progestagène.