7-bromo-1,2,3,4-tetrahydro-1,8-naphthyridin-4-ol | 957196-47-3

• 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: 7-bromo-1,2,3,4-tetrahydro-1,8-naphthyridin-4-ol
• CAS: 957196-47-3
• 化学式: C₈H₉BrN₂O
• 分子量: 229.076
• InChiKey: PCEUOVAXVRZOGS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  45.2
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  7-bromo-1,2,3,4-tetrahydro-1,8-naphthyridin-4-ol 在 甲醇 、 正丁基锂 作用下， 以 四氢呋喃 为溶剂， 反应 20.0h， 生成 1,2,3,4-Tetrahydro-1,8-naphthyridin-4-OL
  参考文献：
  名称：

  Synthesis and structure–activity relationships of 1,2,3,4-tetrahydropyrido[2,3-b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase

  摘要：

  Dysregulation of the anaplastic lymphoma kinase (ALK) is implicated in a variety of cancers. A series of tetrahydropyrido[2,3-b]pyrazines was constructed as ring-constrained analogs of a known aminopyridine kinase scaffold. Chemistry was developed to rapidly elaborate the SAR, structural elements impacting ALK inhibitory activity were exploited, and kinase selective analogs were identified that inhibit ALK with IC50 values similar to 10 nM (enzyme) and similar to 150 nM (cell). (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2010.04.087
• 作为产物：
  描述：

  7-溴-2,3-二氢-1,8-萘啶-4(1h)-酮 在 sodium tetrahydroborate 作用下， 以 四氢呋喃 为溶剂， 反应 2.0h， 生成 7-bromo-1,2,3,4-tetrahydro-1,8-naphthyridin-4-ol
  参考文献：
  名称：

  [EN] RING-FUSED BICYCLIC PYRIDYL DERIVATIVES AS FGFR4 INHIBITORS
  [FR] DÉRIVÉS PYRIDYLE BICYCLIQUES À ANNEAUX FUSIONNÉS UTILISÉS EN TANT QU'INHIBITEURS DE FGFR4

  摘要：

  本发明提供了化合物(I)或其药学上可接受的盐；制备该化合物的方法及其治疗用途。本发明还提供了药理活性剂的组合物和包含该化合物的药物组合物。

  公开号：

  WO2015059668A1

文献信息

• Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
  申请人：Buschmann Nicole

  公开号：US20150119385A1

  公开（公告）日：2015-04-30

  The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.

  本发明提供了化合物(I)或其药学上可接受的盐；制造该化合物的方法及其治疗用途。本发明还提供了药理活性剂的组合物和包括该化合物的药物组合。
• [EN] RING-FUSED BICYCLIC PYRIDYL DERIVATIVES AS FGFR4 INHIBITORS<br/>[FR] DÉRIVÉS PYRIDYLE BICYCLIQUES À ANNEAUX FUSIONNÉS UTILISÉS EN TANT QU'INHIBITEURS DE FGFR4
  申请人：NOVARTIS AG

  公开号：WO2015059668A1

  公开（公告）日：2015-04-30

  The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.

  本发明提供了化合物(I)或其药学上可接受的盐；制备该化合物的方法及其治疗用途。本发明还提供了药理活性剂的组合物和包含该化合物的药物组合物。
• Pyridopyrazines and derivatives thereof as alk and c-Met inhibitors
  申请人：Dorsey D. Bruce

  公开号：US20080032972A1

  公开（公告）日：2008-02-07

  The present invention provides a compound of Formula I or a pharmaceutically acceptable salt form thereof, wherein A, L 1 , R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , and X are as defined herein. The compounds of Formula I have ALK and/or c-Met inhibitory activity, and may be used to treat ALK- or c-Met-mediated disorders or conditions.

  本发明提供了化合物I的结构或其药学上可接受的盐形式，其中A、L1、R1、R2、R3、R4、R5、R6和X的定义如本文所述。化合物I具有ALK和/或c-Met抑制活性，并可用于治疗ALK或c-Met介导的疾病或病症。
• PYRIDOPYRAZINES AND DERIVATIVES THEREOF AS ALK AND c-MET INHIBITORS
  申请人：Dorsey Bruce D.

  公开号：US20100048576A1

  公开（公告）日：2010-02-25

  The present invention provides a compound of Formula I or a pharmaceutically acceptable salt form thereof, wherein A, L 1 , R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , and X are as defined herein. The compounds of Formula I have ALK and/or c-Met inhibitory activity, and may be used to treat ALK- or c-Met-mediated disorders or conditions.

  本发明提供了I式化合物或其药学上可接受的盐形式，其中A、L1、R1、R2、R3、R4、R5、R6和X的定义如本文所述。I式化合物具有ALK和/或c-Met抑制活性，可用于治疗ALK或c-Met介导的疾病或病状。
• Pyridopyrazines and derivatives thereof as ALK and c-Met inhibitors
  申请人：Cephalon, Inc.

  公开号：US08080561B2

  公开（公告）日：2011-12-20

  The present invention provides a compound of Formula I or a pharmaceutically acceptable salt form thereof, wherein A, L1, R1, R2, R3, R4, R5, R6, and X are as defined herein. The compounds of Formula I have ALK and/or c-Met inhibitory activity, and may be used to treat ALK- or c-Met-mediated disorders or conditions.

  本发明提供了公式I的化合物或其药学上可接受的盐形式，其中A，L1，R1，R2，R3，R4，R5，R6和X的定义如本文所述。公式I的化合物具有ALK和/或c-Met抑制活性，并可用于治疗ALK或c-Met介导的疾病或病况。