3-Thiophen-3-yl-1,4-dihydroindeno[1,2-c]pyrazol-5-amine | 866851-37-8

• 分子结构分类: 有机化合物 - 苯类化合物
• 英文名称: 3-Thiophen-3-yl-1,4-dihydroindeno[1,2-c]pyrazol-5-amine
• CAS: 866851-37-8
• 化学式: C₁₄H₁₁N₃S
• 分子量: 253.327
• InChiKey: YEEVIOSNBWPLGL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  18
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  82.9
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  3-Thiophen-3-yl-1,4-dihydroindeno[1,2-c]pyrazol-5-amine 、 2-(4-methylpiperazin 1-yl)acetyl chloride 在 吡啶 作用下， 反应 0.17h， 生成 2-(4-methyl-piperazin-1-yl)-N-(3-thiophen-3-yl-2,4-dihydro-indeno[1,2-c]pyrazol-5-yl)-acetamide
  参考文献：
  名称：

  Synthesis and biological evaluation of 5-substituted 1,4-dihydroindeno[1,2-c]pyrazoles as multitargeted receptor tyrosine kinase inhibitors

  摘要：

  We report the synthesis and biological evaluation of 5-substituted 1,4-dihydroindeno[1,2-c]pyrazoles as multitargeted kinase inhibitors. Initial efforts focused on the development of selective KDR inhibitors, while later strategies involved the improvement of potency toward multiple kinase targets. Thus, several compounds were identified as potent KDR, Flt1, Flt3, and c-Kit inhibitors. (C) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2007.03.031
• 作为产物：
  描述：

  2',3'-dihydrospiro[1,3-dioxolane-2,1'-inden]-4'-amine 在 盐酸 、 水 、 sodium hydride 、 对甲苯磺酸 、 一水合肼 作用下， 以 吡啶 、 甲醇 、 乙醇 、 丙酮 、 苯 为溶剂， 反应 5.5h， 生成 3-Thiophen-3-yl-1,4-dihydroindeno[1,2-c]pyrazol-5-amine
  参考文献：
  名称：

  Synthesis and biological evaluation of 5-substituted 1,4-dihydroindeno[1,2-c]pyrazoles as multitargeted receptor tyrosine kinase inhibitors

  摘要：

  We report the synthesis and biological evaluation of 5-substituted 1,4-dihydroindeno[1,2-c]pyrazoles as multitargeted kinase inhibitors. Initial efforts focused on the development of selective KDR inhibitors, while later strategies involved the improvement of potency toward multiple kinase targets. Thus, several compounds were identified as potent KDR, Flt1, Flt3, and c-Kit inhibitors. (C) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2007.03.031

文献信息

• [EN] TRICYCLIC PYRAZOLE KINASE INHIBITORS<br/>[FR] INHIBITEURS DE KINASES A BASE DE TYRAZOLES TRICYCLIQUES
  申请人：ABBOTT LAB

  公开号：WO2005095387A1

  公开（公告）日：2005-10-13

  Compounds of the present invention are useful for inhibiting protein tyrosine kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

  本发明的化合物对抑制蛋白酪氨酸激酶具有用处。还公开了制备这些化合物的方法、含有这些化合物的组合物以及使用这些化合物进行治疗的方法。
• Tricyclic pyrazole kinase inhibitors
  申请人：Arnold D. Lee

  公开号：US20060014816A1

  公开（公告）日：2006-01-19

  Compounds of the present invention are useful for inhibiting protein tyrosine kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

  本发明的化合物可用于抑制蛋白酪氨酸激酶。还公开了制备该化合物的方法，含有该化合物的组合物，以及使用该化合物的治疗方法。
• TRICYCLIC PYRAZOLE KINASE INHIBITORS
  申请人：AbbVie Inc.

  公开号：EP1740579B1

  公开（公告）日：2015-08-19
• US7468371B2
  申请人：——

  公开号：US7468371B2

  公开（公告）日：2008-12-23
• Synthesis and biological evaluation of 5-substituted 1,4-dihydroindeno[1,2-c]pyrazoles as multitargeted receptor tyrosine kinase inhibitors
  作者：Irini Akritopoulou-Zanze、Daniel H. Albert、Peter F. Bousquet、George A. Cunha、Christopher M. Harris、Maria Moskey、Jurgen Dinges、Kent D. Stewart、Thomas J. Sowin

  DOI：10.1016/j.bmcl.2007.03.031

  日期：2007.6

  We report the synthesis and biological evaluation of 5-substituted 1,4-dihydroindeno[1,2-c]pyrazoles as multitargeted kinase inhibitors. Initial efforts focused on the development of selective KDR inhibitors, while later strategies involved the improvement of potency toward multiple kinase targets. Thus, several compounds were identified as potent KDR, Flt1, Flt3, and c-Kit inhibitors. (C) 2007 Elsevier Ltd. All rights reserved.