4-hydroxy-1,5-dimethyl-6-oxo-1,6-dihydropyridazine-3-carboxylic acid | 869357-54-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 4-hydroxy-1,5-dimethyl-6-oxo-1,6-dihydropyridazine-3-carboxylic acid
• 英文别名: 4-hydroxy-1,5-dimethyl-6-oxopyridazine-3-carboxylic acid
• CAS: 869357-54-0
• 化学式: C₇H₈N₂O₄
• 分子量: 184.152
• InChiKey: VHSWOYBVPBDEIX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  90.2
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  4-hydroxy-1,5-dimethyl-6-oxo-1,6-dihydropyridazine-3-carboxylic acid 在 N,N-二甲基甲酰胺 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 lithium hexamethyldisilazane 、 三氯氧磷 作用下， 以 四氢呋喃 、 N,N-二甲基甲酰胺 为溶剂， 反应 73.0h， 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 lithium hexamethyldisilazane 作用下， 以 四氢呋喃 为溶剂， 反应 1.5h， 以10.5 g的产率得到4-hydroxy-1,5-dimethyl-6-oxo-1,6-dihydropyridazine-3-carboxylic acid
  参考文献：
  名称：

  [EN] HERBICIDAL COMPOUNDS
  [FR] COMPOSÉS HERBICIDES

  摘要：

  本发明涉及公式（I）的化合物，或者该化合物的农学上可接受的盐，其中R1、R2、R3和R4如本文所定义。本发明还涉及包括公式（I）化合物的除草剂组合物，以及它们用于控制杂草的用途，特别是在有用植物作物中的用途。

  公开号：

  WO2017032786A1

文献信息

• Heterocyclic inhibitors of MEK and methods of use thereof
  申请人：Marlow L. Allison

  公开号：US20050256123A1

  公开（公告）日：2005-11-17

  Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R 1 , R 2 , R 7 , R 8 and R 9 , W, X and Y are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.

  本文披露了式I的化合物及其药用盐和前药，其中R1、R2、R7、R8和R9、W、X和Y的定义如规范中所述。这些化合物是MEK抑制剂，在哺乳动物中用于治疗高增殖性疾病，如癌症和炎症，以及炎症病症。还披露了在哺乳动物中治疗高增殖性疾病的方法以及含有这些化合物的药物组合物。
• 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。
• HETEROCYCLIC INHIBITORS OF MEK AND METHODS OF USE THEREOF
  申请人：Marlow Allison L.

  公开号：US20090215834A1

  公开（公告）日：2009-08-27

  Disclosed are compounds of the Formula V and pharmaceutically acceptable salts and prodrugs thereof, wherein R 1 , R 2 , R 7 , R 8 and R 9 , and W are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, and inflammatory conditions in mammals. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases and inflammatory conditions in mammals and pharmaceutical compositions containing such compounds.

  本发明涉及公式V的化合物，以及其药学上可接受的盐和前药，其中R1、R2、R7、R8和R9以及W在说明书中定义。这些化合物是MEK抑制剂，可用于治疗哺乳动物的高增殖性疾病，如癌症和炎症，以及炎症状况。本发明还涉及使用这些化合物治疗哺乳动物的高增殖性疾病和炎症状况的方法，以及含有这些化合物的制药组合物。
• 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。
• Heterocyclic Inhibitors of Mek and Methods of Use Thereof
  申请人：Marlow Allison L.

  公开号：US20080280957A1

  公开（公告）日：2008-11-13

  Disclosed are MEK inhibitors useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.

  本发明揭示了MEK抑制剂，其在哺乳动物的高增殖性疾病，如癌症和炎症，以及炎症状况的治疗中有用。还揭示了使用这些化合物治疗哺乳动物高增殖性疾病的方法和含有这些化合物的制药组成物。