4-(5-methoxy-1H-indol-1-yl)-2,6-dimethylfuro[2,3-d]pyrimidine | 1392880-22-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 4-(5-methoxy-1H-indol-1-yl)-2,6-dimethylfuro[2,3-d]pyrimidine
• 英文别名: 4-(5-methoxyindol-1-yl)-2,6-dimethylfuro[2,3-d]pyrimidine
• CAS: 1392880-22-6
• 化学式: C₁₇H₁₅N₃O₂
• 分子量: 293.325
• InChiKey: UDKMOAHOTPOVJU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  22
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  53.1
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  2,6-dimethylfuro[2,3-d]pyrimidin-4(3H)-one 在 sodium hydride 、 三氯氧磷 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 4.5h， 生成 4-(5-methoxy-1H-indol-1-yl)-2,6-dimethylfuro[2,3-d]pyrimidine
  参考文献：
  名称：

  [EN] CONFORMATIONALLY RESTRICTED 4-SUBSTITUTED-2,6-DIMETHYLFURO[2,3-d]PYRIMIDINES AS ANTITUMOR AGENTS
  [FR] 2,6-DIMÉTHYLFURO[2,3-D]PYRIMIDINES 4-SUBSTITUÉES À CONFORMATION RESTREINTE À TITRE D'AGENTS ANTITUMORAUX

  摘要：

  本发明提供构象限制的4-取代2,6-二甲基呋喃[2,3-d]嘧啶化合物和包含这些化合物的制药组合物。优选地，这些化合物表现出微管组装和受体酪氨酸激酶的双重抑制作用。本发明还公开了治疗癌症的方法，包括向患者施用至少一种构象限制的4-取代2,6-二甲基呋喃[2,3-d]嘧啶化合物的治疗有效剂量。

  公开号：

  WO2016100495A1

文献信息

• Conformationally Restricted 4-Substituted-2,6-dimethylfuro[2,3-d]pyrimidines as Multi-targeted Receptor Tyrosine Kinase Inhibitors and Microtubule Targeting Antitumor Agents
  申请人：Duquesne University of the Holy Spirit

  公开号：US20160176891A1

  公开（公告）日：2016-06-23

  Compounds of Formula I: and compounds of Formula II: are provided. Pharmaceutical compositions comprising either the compound of Formula I or Formula II are disclosed. Methods of treating patients having cancer are provided by administering to the patient a therapeutically effective amount of one or more compounds having Formula I or Formula II to treat the patient. The compounds of Formula I or II are preferably conformationally restricted furo[2,3-d]pyrimidines having dual inhibition of microtubule assembly and receptor tyrosine kinases.

  提供了化学式I和化学式II的化合物。揭示了包含化学式I或化学式II化合物的制药组合物。通过向患有癌症的患者投与具有化学式I或化学式II的一个或多个化合物的治疗有效量来治疗患者的方法。化学式I或II的化合物通常是具有微管组装和受体酪氨酸激酶双重抑制作用的构象限制的呋喃[2,3-d]嘧啶类化合物。
• Conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as anti-tumor agents
  申请人：DUQUESNE UNIVERSITY OF THE HOLY SPIRIT

  公开号：US10189853B2

  公开（公告）日：2019-01-29

  The present invention provides conformationally restricted 4-substituted 2,6-dimethylfuro[2,3-d]pyrimidine compounds and pharmaceutical compositions comprising these compounds. Preferably, the compounds exhibit dual inhibition of microtubule assembly and receptor tyrosine kinases. Methods of treating cancer comprising administering a therapeutically effective amount of at least one conformationally restricted 4-substituted 2,6-dimethylfuro[2,3-d]pyrimidine compound to a patient is disclosed.

  本发明提供了构象受限的 4-取代 2,6-二甲基呋喃并[2,3-d]嘧啶化合物以及包含这些化合物的药物组合物。优选地，这些化合物表现出对微管组装和受体酪氨酸激酶的双重抑制作用。本发明公开了治疗癌症的方法，包括向患者施用治疗有效量的至少一种构象受限的 4-取代 2,6-二甲基呋喃并[2,3-d]嘧啶化合物。
• CONFORMATIONALLY RESTRICTED 4-SUBSTITUTED-2,6-DIMETHYLFURO[2,3-d]PYRIMIDINES AS ANTI-TUMOR AGENTS
  申请人：DUQUESNE UNIVERSITY OF THE HOLY SPIRIT

  公开号：US20170369500A1

  公开（公告）日：2017-12-28

  The present invention provides conformationally restricted 4-substituted 2,6-dimethylfuro[2,3-d]pyrimidine compounds and pharmaceutical compositions comprising these compounds. Preferably, the compounds exhibit dual inhibition of microtubule assembly and receptor tyrosine kinases. Methods of treating cancer comprising administering a therapeutically effective amount of at least one conformationally restricted 4-substituted 2,6-dimethylfuro[2,3-d]pyrimidine compound to a patient is disclosed.
• US9777012B2
  申请人：——

  公开号：US9777012B2

  公开（公告）日：2017-10-03
• [EN] CONFORMATIONALLY RESTRICTED 4-SUBSTITUTED-2,6-DIMETHYLFURO[2,3-d]PYRIMIDINES AS ANTITUMOR AGENTS<br/>[FR] 2,6-DIMÉTHYLFURO[2,3-D]PYRIMIDINES 4-SUBSTITUÉES À CONFORMATION RESTREINTE À TITRE D'AGENTS ANTITUMORAUX
  申请人：UNIV HOLY GHOST DUQUESNE

  公开号：WO2016100495A1

  公开（公告）日：2016-06-23

  The present invention provides conformationally restricted 4-substituted 2,6-dimethylfuro[2,3-d]pyrimidine compounds and pharmaceutical compositions comprising these compounds. Preferably, the compounds exhibit dual inhibition of microtubule assembly and receptor tyrosine kinases. Methods of treating cancer comprising administering a therapeutically effective amount of at least one conformationally restricted 4-substituted 2,6-dimethylfuro[2,3-d]pyrimidine compound to a patient is disclosed.

  本发明提供构象限制的4-取代2,6-二甲基呋喃[2,3-d]嘧啶化合物和包含这些化合物的制药组合物。优选地，这些化合物表现出微管组装和受体酪氨酸激酶的双重抑制作用。本发明还公开了治疗癌症的方法，包括向患者施用至少一种构象限制的4-取代2,6-二甲基呋喃[2,3-d]嘧啶化合物的治疗有效剂量。