methyl 4-(7-(4-morpholinophenyl)pyrido[4,3-b]pyrazin-5-yloxy)benzoate | 1613260-07-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 英文名称: methyl 4-(7-(4-morpholinophenyl)pyrido[4,3-b]pyrazin-5-yloxy)benzoate
• 英文别名: Methyl 4-(7-(4-morpholinophenyl)pyrido[4,3-b]pyrazin-5-yloxy)benzoate；methyl 4-[7-(4-morpholin-4-ylphenyl)pyrido[3,4-b]pyrazin-5-yl]oxybenzoate
• CAS: 1613260-07-3
• 化学式: C₂₅H₂₂N₄O₄
• 分子量: 442.474
• InChiKey: YQEFYRUQFQVHJC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  33
• 可旋转键数：
  6
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  86.7
• 氢给体数：
  0
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  methyl 4-(7-(4-morpholinophenyl)pyrido[4,3-b]pyrazin-5-yloxy)benzoate 在 lithium hydroxide monohydrate 作用下， 以 四氢呋喃 、 水 为溶剂， 以93 mg的产率得到4-(7-(4-morpholinophenyl)pyrido[4,3-b]pyrazin-5-yloxy)benzoic acid
  参考文献：
  名称：

  [EN] SUBSTITUTED PYRIDOPYRAZINES AS SYK INHIBITORS
  [FR] PYRIDOPYRAZINES SUBSTITUÉES UTILISÉES EN TANT QU'INHIBITEURS DE SYK

  摘要：

  本发明涉及式(I)的吡啶吡嗪化合物，以及其药物组合物和使用方法，其中R1、R2、R3、L、m、p和W如规范中所定义。

  公开号：

  WO2014086032A1
• 作为产物：
  描述：

  5,7-二氯吡啶并[4,3-b]吡嗪 在 (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride 、 potassium carbonate 、 caesium carbonate 作用下， 以 乙二醇二甲醚 、 水 、 N,N-二甲基甲酰胺 为溶剂， 反应 0.75h， 生成 methyl 4-(7-(4-morpholinophenyl)pyrido[4,3-b]pyrazin-5-yloxy)benzoate
  参考文献：
  名称：

  [EN] SUBSTITUTED PYRIDOPYRAZINES AS SYK INHIBITORS
  [FR] PYRIDOPYRAZINES SUBSTITUÉES UTILISÉES EN TANT QU'INHIBITEURS DE SYK

  摘要：

  本发明涉及式(I)的吡啶吡嗪化合物，以及其药物组合物和使用方法，其中R1、R2、R3、L、m、p和W如规范中所定义。

  公开号：

  WO2014086032A1

文献信息

• Substituted Pyridopyrazines as Syk Inhibitors
  申请人：HUTCHISON MEDIPHARMA LIMITED

  公开号：US20160002221A1

  公开（公告）日：2016-01-07

  The present invention relates to pyridopyrazine compounds of formula (I), pharmaceutical compositions thereof and methods of use therefore, wherein R 1 , R 2 , R 3 , L, m, p and W are as defined in the specification.

  本发明涉及式(I)的吡啶吡嗪化合物、其制药组合物和使用方法，其中R1、R2、R3、L、m、p和W如规范中所定义。
• SUBSTITUTED PYRIDOPYRAZINES AS SYK INHIBITORS
  申请人：HUTCHISON MEDIPHARMA LIMITED

  公开号：US20150307491A1

  公开（公告）日：2015-10-29

  The present invention relates to pyridopyrazine compounds of formula (I), pharmaceutical compositions thereof and methods of use therefore, wherein R 1 , R 2 , R 3 , L, m, p and W are as defined in the specification.

  本发明涉及式(I)的吡啶吡嗪化合物，其制药组合物和使用方法，其中R1、R2、R3、L、m、p和W如规范中所定义。
• SYK INHIBITORS
  申请人：Gilead Sciences, Inc.

  公开号：US20180071303A1

  公开（公告）日：2018-03-15

  The application provides methods reducing the side effects of chemotherapy and radiotherapy, including, hematopoietic toxicity, anemia, myelosuppression, pancytopenia, thrombocytopenia, neutropenia, lymphopenia, leukopenia, stomatitis and alopecia. The application provides a method for increasing the number of, neutrophil counts and platelet counts in a patient in need thereof, comprising administering an effective of an inhibitor of spleen tyrosine kinase (SYKi). The present application provides methods for treating myelosuppresive disorders by the administration of a SYKi. In certain embodiments, the myelosuppression is induced by the administration of one or more myelosuppressive agents, for example, anti-cancer drugs. The present application provides methods for treating AML/ALL in a patient with 11q23/MLL abnormalities comprising the step of administering an effective amount of a SYKi to said patient.
• [EN] SYK INHIBITORS<br/>[FR] INHIBITEURS DE SYK
  申请人：GILEAD SCIENCES INC

  公开号：WO2018053189A2

  公开（公告）日：2018-03-22

  The application provides methods reducing the side effects of chemotherapy and radiotherapy, including, hematopoietic toxicity, anemia, myelosuppression, pancytopenia, thrombocytopenia, neutropenia, lymphopenia, leukopenia, stomatitis and alopecia. The application provides a method for increasing the number of, neutrophil counts and platelet counts in a patient in need thereof, comprising administering an effective of an inhibitor of spleen tyrosine kinase (SYKi). The present application provides methods for treating myelosuppresive disorders by the administration of a SYKi. In certain embodiments, the myelosuppression is induced by the administration of one or more myelosuppressive agents, for example, anti-cancer drugs. The present application provides methods for treating AML/ALL in a patient with 11q23/MLL abnormalities comprising the step of administering an effective amount of a SYKi to said patient.
• [EN] SUBSTITUTED PYRIDOPYRAZINES AS SYK INHIBITORS<br/>[FR] PYRIDOPYRAZINES SUBSTITUÉES UTILISÉES EN TANT QU'INHIBITEURS DE SYK
  申请人：HUTCHISON MEDIPHARMA LTD

  公开号：WO2014086032A1

  公开（公告）日：2014-06-12

  The present invention relates to pyridopyrazine compounds of formula (I), pharmaceutical compositions thereof and methods of use therefore, wherein R1, R2, R3, L, m, p and W are as defined in the specification.

  本发明涉及式(I)的吡啶吡嗪化合物，以及其药物组合物和使用方法，其中R1、R2、R3、L、m、p和W如规范中所定义。