5-(6,7-dimethoxyquinazolin-4-yl)-N2-(4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)thiazole-2,4-diamine | 1035994-38-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 5-(6,7-dimethoxyquinazolin-4-yl)-N2-(4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)thiazole-2,4-diamine
• 英文别名: 5-(6,7-dimethoxyquinazolin-4-yl)-2-N-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-1,3-thiazole-2,4-diamine
• CAS: 1035994-38-7
• 化学式: C₂₅H₂₈N₆O₃S
• 分子量: 492.602
• InChiKey: WSKNGLXYSYCKAY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  35
• 可旋转键数：
  9
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  136
• 氢给体数：
  2
• 氢受体数：
  10

反应信息

• 作为产物：
  描述：

  氰胺 、 4-bromomethyl-6,7-dimethoxyquinazoline 、 4-(2-pyrrolidin-1-ylethoxy)phenyl isothiocyanate 在 正丁基锂 作用下， 以 乙腈 、 叔丁醇 、 四氢呋喃 、 hexanes 为溶剂， 反应 7.5h， 生成 5-(6,7-dimethoxyquinazolin-4-yl)-N2-(4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)thiazole-2,4-diamine
  参考文献：
  名称：

  WO2008/80134

  摘要：

  公开号：

文献信息

• DIAMINOTHIAZOLES USEFUL AS AXL INHIBITORS
  申请人：Goff Dane

  公开号：US20080227789A1

  公开（公告）日：2008-09-18

  Diaminothiazoles and pharmaceutical compositions containing them are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the diaminothiazoles in treating diseases or conditions associated with Axl activity are also disclosed.

  本发明揭示了二氨基噻唑类化合物和含有它们的药物组合物，作为抑制受体蛋白酪氨酸激酶Axl活性的有用药物。还揭示了使用二氨基噻唑类化合物治疗与Axl活性相关的疾病或病症的方法。
• Diaminothiazoles useful as Axl inhibitors
  申请人：Rigel Pharmaceuticals, Inc.

  公开号：US07879856B2

  公开（公告）日：2011-02-01

  Diaminothiazoles and pharmaceutical compositions containing them are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the diaminothiazoles in treating diseases or conditions associated with Axl activity are also disclosed.

  本发明公开了含有二氨基噻唑的药物组合物，这些组合物可用于抑制受体蛋白酪氨酸激酶Axl的活性。还公开了使用二氨基噻唑治疗与Axl活性相关的疾病或症状的方法。
• DIANHYDROGALACTITOL TOGETHER WITH RADIATION TO TREAT NON-SMALL-CELL CARCINOMA OF THE LUNG AND GLIOBLASTOMA MULTIFORME
  申请人：Del Mar Pharmaceuticals

  公开号：EP3217970A1

  公开（公告）日：2017-09-20
• USE OF DIANHYDROGALACTITOL AND ANALOGS AND DERIVATIVES THEREOF, TOGETHER WITH RADIATION, TO TREAT NON-SMALL-CELL CARCINOMA OF THE LUNG AND GLIOBLASTOMA MULTIFORME AND SUPPRESS PROLIFERATION OF CANCER STEM CELLS
  申请人：DelMar Pharmaceuticals, Inc.

  公开号：US20190015379A1

  公开（公告）日：2019-01-17

  The use of dianhydrogalactitol provides a novel therapeutic modality for the treatment of non-small-cell lung carcinoma (NSCLC) and for the treatment of glioblastoma multiforme (GBM). Dianhydrogalactitol acts as an alkylating agent on DNA that creates N7 methylation. Dianhydrogalactitol is effective in suppressing the growth of cancer stem cells and is active against tumors that are refractory to temozolomide; the drug acts independently of the MGMT repair mechanism.
• US7879856B2
  申请人：——

  公开号：US7879856B2

  公开（公告）日：2011-02-01