1-butoxypyrido[4,3-c]-1,6-naphthyridin-6-ol | 868997-87-9

• 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: 1-butoxypyrido[4,3-c]-1,6-naphthyridin-6-ol
• 英文别名: 1-butoxy-5H-pyrido[4,3-c][1,6]naphthyridin-6-one
• CAS: 868997-87-9
• 化学式: C₁₅H₁₅N₃O₂
• 分子量: 269.303
• InChiKey: FWJPDDCQIZGEBJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  20
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  64.1
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  1-butoxypyrido[4,3-c]-1,6-naphthyridin-6-ol 在 N,N-二乙基苯胺 、 三氯氧磷 、 三乙胺 作用下， 以 乙腈 为溶剂， 生成 1,6-dichloropyrido[4,3-c]-1,6-naphthyridine
  参考文献：
  名称：

  WO2008/112217

  摘要：

  公开号：
• 作为产物：
  描述：

  4'-Amino-2'-butoxy-N,N-diisopropyl-3,3'-bipyridine-4-carboxamide 在 sodium hexamethyldisilazane 作用下， 以 四氢呋喃 为溶剂， 生成 1-butoxypyrido[4,3-c]-1,6-naphthyridin-6-ol
  参考文献：
  名称：

  The discovery of tricyclic pyridone JAK2 inhibitors. Part 1: Hit to lead

  摘要：

  This paper describes the discovery and design of a novel class of JAK2 inhibitors. Furthermore, we detail the optimization of a screening hit using ligand binding efficiency and log D. These efforts led to the identification of compound 41, which demonstrates in vivo activity in our study. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2010.10.031

文献信息

• [EN] TETRACYCLIC INHIBITORS OF JANUS KINASES<br/>[FR] INHIBITEURS TETRACYCLIQUES DE JANUS KINASES
  申请人：INCYTE CORP

  公开号：WO2005105814A1

  公开（公告）日：2005-11-10

  The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.

  本发明提供了能调节雅努斯激酶活性并且在治疗与雅努斯激酶活性相关的疾病方面有用的化合物，例如免疫相关疾病和癌症。
• Tetracyclic inhibitors of Janus kinases
  申请人：Rodgers D. James

  公开号：US20060106020A1

  公开（公告）日：2006-05-18

  The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.

  本发明提供了一种调节Janus激酶活性的化合物，可用于治疗与Janus激酶活性相关的疾病，例如免疫相关疾病和癌症。
• INHIBITORS OF JANUS KINASES AND/OR 3-PHOSPHOINOSITIDE-DEPENDENT PROTEIN KINASE-1
  申请人：Siu Tony

  公开号：US20100160309A1

  公开（公告）日：2010-06-24

  The instant invention provides for compounds that inhibit JAK2 tyrosine kinase and/or PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting JAK2 tyrosine kinase activity and/or PDK1 kinase inhibitory activity by administering the compound to a patient in need of treatment or prevention of myeloproliferative disorders or cancer.

  本发明提供了抑制JAK2酪氨酸激酶和/或PDK1的化合物。本发明还提供了包含这些抑制化合物的组合物，并通过将该化合物给予需要治疗或预防骨髓增生性疾病或癌症的患者来抑制JAK2酪氨酸激酶活性和/或PDK1激酶抑制活性的方法。
• Inhibitors of janus kinases and/or 3-phosphoinositide-dependent protein kinase-1
  申请人：Merck Sharp & Dohme Corp.

  公开号：US08329722B2

  公开（公告）日：2012-12-11

  The instant invention provides for compounds that inhibit JAK2 tyrosine kinase and/or PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting JAK2 tyrosine kinase activity and/or PDK1 kinase inhibitory activity by administering the compound to a patient in need of treatment or prevention of myeloproliferative disorders or cancer.

  本发明提供了抑制JAK2酪氨酸激酶和/或PDK1的化合物。本发明还提供了包含这种抑制剂化合物的组合物，并通过向需要治疗或预防骨髓增生性疾病或癌症的患者施用该化合物来抑制JAK2酪氨酸激酶活性和/或PDK1激酶抑制活性的方法。
• TETRACYCLIC INHIBITORS OF JANUS KINASES
  申请人：Rodgers James D.

  公开号：US20090215766A1

  公开（公告）日：2009-08-27

  The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.

  本发明提供了一种可以调节Janus激酶活性的化合物，这些化合物可用于治疗与Janus激酶活性相关的疾病，例如免疫相关疾病和癌症。