| 943970-13-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并咪唑类
• CAS: 943970-13-6
• 化学式: C₂₉H₃₁ClN₈O
• 分子量: 543.071
• InChiKey: DZHMNRMMNFEUNL-MEMLXQNLSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.01
• 重原子数：
  39.0
• 可旋转键数：
  5.0
• 环数：
  7.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  110.77
• 氢给体数：
  2.0
• 氢受体数：
  8.0

反应信息

• 作为产物：
  描述：

  trans-3-iodo-1-(4-morpholin-4-yl-cyclohexyl)-1H-pyrazolo[3,4-d]pyrimidin-4-ylamine 、 2-(2-chlorobenzyl)-6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1Hbenzo[d]imidazole 在 bis-triphenylphosphine-palladium(II) chloride 、 sodium carbonate 作用下， 以 乙二醇二甲醚 、 水 为溶剂， 生成
  参考文献：
  名称：

  Development of multitargeted inhibitors of both the insulin-like growth factor receptor (IGF-IR) and members of the epidermal growth factor family of receptor tyrosine kinases

  摘要：

  Emerging clinical and pre-clinical data indicate that both insulin-like growth factor receptor (IGF-IR) and members of the epidermal growth factor (EGF) family of receptor tyrosine kinases (RTKs) exhibit significant cross-talk in human cancers. Therefore, a small molecule that successfully inhibits the signaling of both classes of oncogenic kinases might provide an attractive agent for chemotherapeutic use. Herein, we disclose the structure activity relationships that led to the synthesis and biological characterization of 14, a novel small molecule inhibitor of both IGF-IR and members of the epidermal growth factor family of RTKs. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.01.086

文献信息

• PROTEIN KINASE INHIBITORS
  申请人：Sheppard S. George

  公开号：US20070203143A1

  公开（公告）日：2007-08-30

  Compounds that inhibit protein kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.

  抑制蛋白激酶的化合物、含有这些化合物的组合物以及利用这些化合物治疗疾病的方法被披露。
• METHODS FOR THE TREATMENT OF SCLERODERMA AND RELATED CONDITIONS
  申请人：HZNP Limited

  公开号：US20210253686A1

  公开（公告）日：2021-08-19

  Provided herein are antibodies against insulin-like growth factor 1 receptor (IGF-1R) and their use in methods of treatment of, and achievement of clinical outcomes in, scleroderma and forms thereof, including diffuse cutaneous systemic sclerosis.
• METHODS FOR THE TREATMENT OF THYROID EYE DISEASE
  申请人：HZNP Limited

  公开号：US20210253719A1

  公开（公告）日：2021-08-19

  Provided herein are methods of treating or reducing the severity of thyroid eye disease (TED), also known as thyroid-associated ophthalmopathy (TAO), or Graves' ophthalmopathy or orbitopathy (GO), as well as antibodies, or antigen binding fragments thereof, and pharmaceutical compositions comprising them, useful in the methods.
• US7772231B2
  申请人：——

  公开号：US7772231B2

  公开（公告）日：2010-08-10
• Development of multitargeted inhibitors of both the insulin-like growth factor receptor (IGF-IR) and members of the epidermal growth factor family of receptor tyrosine kinases
  作者：Robert D. Hubbard、Nwe Y. Bamaung、Steve D. Fidanze、Scott A. Erickson、Fabio Palazzo、Julie L. Wilsbacher、Qian Zhang、Lora A. Tucker、Xiaoming Hu、Peter Kovar、Donald J. Osterling、Eric F. Johnson、Jennifer Bouska、Jieyi Wang、Steven K. Davidsen、Randy L. Bell、George S. Sheppard

  DOI：10.1016/j.bmcl.2009.01.086

  日期：2009.3

  Emerging clinical and pre-clinical data indicate that both insulin-like growth factor receptor (IGF-IR) and members of the epidermal growth factor (EGF) family of receptor tyrosine kinases (RTKs) exhibit significant cross-talk in human cancers. Therefore, a small molecule that successfully inhibits the signaling of both classes of oncogenic kinases might provide an attractive agent for chemotherapeutic use. Herein, we disclose the structure activity relationships that led to the synthesis and biological characterization of 14, a novel small molecule inhibitor of both IGF-IR and members of the epidermal growth factor family of RTKs. (C) 2009 Elsevier Ltd. All rights reserved.