4-(4-bromo-2-fluorophenylamino)-1,5-dimethyl-6-oxo-1,6-dihydropyridazine-3-carboxylic acid | 934639-05-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 4-(4-bromo-2-fluorophenylamino)-1,5-dimethyl-6-oxo-1,6-dihydropyridazine-3-carboxylic acid
• 英文别名: 4-(4-bromo-2-fluoroanilino)-1,5-dimethyl-6-oxopyridazine-3-carboxylic acid
• CAS: 934639-05-1
• 化学式: C₁₃H₁₁BrFN₃O₃
• 分子量: 356.151
• InChiKey: BKHNGKAEURZUQN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  21
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.15
• 拓扑面积：
  82
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  O-[2-(乙烯氧基)乙基]羟胺 、 4-(4-bromo-2-fluorophenylamino)-1,5-dimethyl-6-oxo-1,6-dihydropyridazine-3-carboxylic acid 在 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 三乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 3.0h， 生成 4-(4-溴-2-氟苯基氨基)-1,5-二甲基-6-氧代-N-(2-(乙烯基氧基)乙氧基)-1,6-二氢哒嗪-3-甲酰胺
  参考文献：
  名称：

  WO2008/120004

  摘要：

  公开号：
• 作为产物：
  描述：

  diethyl 2-(2-methyl-2-propionylhydrazono)malonate 在 N,N-二甲基甲酰胺 lithium hexamethyldisilazane 、 三氯氧磷 作用下， 以 四氢呋喃 为溶剂， 反应 91.5h， 生成 4-(4-bromo-2-fluorophenylamino)-1,5-dimethyl-6-oxo-1,6-dihydropyridazine-3-carboxylic acid
  参考文献：
  名称：

  WO2008/120004

  摘要：

  公开号：

文献信息

• COMBINATION 059
  申请人：SMITH Paul David

  公开号：US20090099174A1

  公开（公告）日：2009-04-16

  This invention relates to a combination product, as defined herein, comprising a MEK inhibitor and a mTOR-selective inhibitor, and to methods for the production of an anti-cancer effect in a patient, which is accordingly useful in the treatment of cancer in a patient. More specifically the present invention relates to; a combination product, as defined herein, comprising a MEK inhibitor and a mTOR-selective inhibitor; a combination product, as defined herein, comprising a kit of parts comprising a MEK inhibitor and a mTOR-selective inhibitor; use of the combination product, as defined herein, in the treatment of cancer; a method of treating cancer comprising administering the combination product, as defined herein, to a patient. The combination product, as defined herein, and methods of the invention are also useful in the treatment of other diseases associated with the activity of MEK, and/or mTOR.

  本发明涉及一种组合产品，其定义为包括MEK抑制剂和mTOR选择性抑制剂，并且涉及在患者中产生抗癌效果的方法，因此在治疗患者的癌症方面非常有用。更具体地，本发明涉及：一种组合产品，其定义为包括MEK抑制剂和mTOR选择性抑制剂；一种组合产品，其定义为包括MEK抑制剂和mTOR选择性抑制剂的组件套件；使用此组合产品在癌症治疗中的方法；一种治疗癌症的方法，包括向患者投与此组合产品。此组合产品和本发明的方法也适用于治疗与MEK和/或mTOR活性相关的其他疾病。
• COMBINATION COMPRISING A MEK INHIBITOR AND AN AURORA KINASE INHIBITOR 188
  申请人：Mundt Kirsten Elisabeth

  公开号：US20100004247A1

  公开（公告）日：2010-01-07

  The present invention relates to a therapeutic combination comprising a MEK inhibitor and an Aurora kinase inhibitor, and to methods for the production of an anti-cancer effect in a patient, which is accordingly useful in the treatment of cancer in a patient. More specifically the present invention relates to: a therapeutic combination comprising a MEK inhibitor and an Aurora kinase inhibitor; a combination product comprising a MEK inhibitor and an Aurora kinase inhibitor, a kit of parts comprising a MEK inhibitor and an Aurora kinase inhibitor; use of a therapeutic combination, combination product or kit of parts in the treatment of cancer; a method of treating cancer comprising administering the therapeutic combination, combination product or kit of parts to a patient. The therapeutic combination and methods of the invention are also useful in the treatment of conditions in which the inhibition of MEK and/or Aurora kinase is beneficial.

  本发明涉及一种治疗组合物，包括MEK抑制剂和Aurora激酶抑制剂，以及在患者中产生抗癌效果的方法，因此在患者的癌症治疗中有用。更具体地，本发明涉及：一种治疗组合物，包括MEK抑制剂和Aurora激酶抑制剂；一种组合产品，包括MEK抑制剂和Aurora激酶抑制剂；一种零件套件，包括MEK抑制剂和Aurora激酶抑制剂；使用治疗组合物、组合产品或零件套件治疗癌症的方法；将治疗组合物、组合产品或零件套件输注给患者治疗癌症的方法。本发明的治疗组合物和方法也适用于治疗MEK和/或Aurora激酶抑制有益的情况。
• WO2007/44084
  申请人：——

  公开号：——

  公开（公告）日：——
• COMBINATIONS OF MEK INHIBITORS WITH MTOR INHIBITORS
  申请人：AstraZeneca AB

  公开号：EP2217234A2

  公开（公告）日：2010-08-18
• [EN] COMBINATION 059<br/>[FR] COMBINAISON 059
  申请人：ASTRAZENECA AB

  公开号：WO2009050506A2

  公开（公告）日：2009-04-23

  This invention relates to a combination product, as defined herein, comprising a MEK inhibitor and a mTOR-selective inhibitor, and to methods for the production of an anti-cancer effect in a patient, which is accordingly useful in the treatment of cancer in a patient. More specifically the present invention relates to; a combination product, as defined herein, comprising a MEK inhibitor and a mTOR-selective inhibitor; a combination product, as defined herein, comprising a kit of parts comprising a MEK inhibitor and a mTOR-selective inhibitor; use of the combination product, as defined herein, in the treatment of cancer; a method of treating cancer comprising administering the combination product, as defined herein, to a patient. The combination product, as defined herein, and methods of the invention are also useful in the treatment of other diseases associated with the activity of MEK, and/or mTOR.