(7-chlorothieno[3,2-b]pyridin-2-yl)(4-methylpiperazin-1-yl)methanone | 1033276-77-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻吩并吡啶类
• 英文名称: (7-chlorothieno[3,2-b]pyridin-2-yl)(4-methylpiperazin-1-yl)methanone
• 英文别名: (7-chlorothieno[3,2-b]pyridin-2-yl)-(4-methylpiperazin-1-yl)methanone
• CAS: 1033276-77-5
• 化学式: C₁₃H₁₄ClN₃OS
• 分子量: 295.793
• InChiKey: ZTHOMFKELLPQPQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  19
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  64.7
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (7-chlorothieno[3,2-b]pyridin-2-yl)(4-methylpiperazin-1-yl)methanone 在 ammonium chloride 、 sodium carbonate 、 magnesium sulfate 、 锌 作用下， 以 Ph₂O 、 水 为溶剂， 生成 (7-(4-amino-2-fluorophenoxy)thieno[3,2-b]pyridin-2-yl)(4-methylpiperazin-1-yl)methanone
  参考文献：
  名称：

  Inhibitors of Protein Tyrosine Kinase Activity

  摘要：

  本发明涉及抑制蛋白酪氨酸激酶活性的化合物。特别是，本发明涉及抑制生长因子受体的蛋白酪氨酸激酶活性的化合物，从而抑制受体信号传导，例如，抑制VEGF受体信号传导。本发明还提供了用于治疗细胞增殖性疾病和条件以及眼科疾病、障碍和条件的化合物、组合物和方法。

  公开号：

  US20110257100A1
• 作为产物：
  描述：

  N-甲基哌嗪 、 7-chlorothieno[3,2-b] pyridine-2-carbonyl chloride 在 ammonium chloride 、 三乙胺 作用下， 以 4-(dicyanomethylene)-2-methyl-6-(p-dimethylaminostyryl)-4H-pyran 为溶剂， 生成 (7-chlorothieno[3,2-b]pyridin-2-yl)(4-methylpiperazin-1-yl)methanone
  参考文献：
  名称：

  Inhibitors of Protein Tyrosine Kinase Activity

  摘要：

  本发明涉及抑制蛋白酪氨酸激酶活性的化合物。特别是，本发明涉及抑制生长因子受体的蛋白酪氨酸激酶活性的化合物，从而抑制受体信号传导，例如，抑制VEGF受体信号传导。本发明还提供了用于治疗细胞增殖性疾病和条件以及眼科疾病、障碍和条件的化合物、组合物和方法。

  公开号：

  US20110257100A1

文献信息

• METHODS OF TREATMENT OF CELL PROLIFERATIVE AND/OR OPHTHALMIC DISEASES, DISORDERS AND CONDITIONS USING INHIBITORS OF PROTEIN TYROSINE KINASE ACTIVITY
  申请人：MethylGene Inc.

  公开号：US20140315801A1

  公开（公告）日：2014-10-23

  This invention relates to methods for treating cell proliferative diseases and conditions and ophthalmic diseases, disorders and conditions using compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to the methods of treatment which utilize compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling.

  本发明涉及使用抑制蛋白酪氨酸激酶活性的化合物治疗细胞增殖性疾病和病况以及眼科疾病、障碍和病况的方法。特别地，本发明涉及使用抑制生长因子受体蛋白酪氨酸激酶活性的化合物的治疗方法，从而抑制受体信号传导，例如抑制VEGF受体信号传导。
• Inhibitors of protein tyrosine kinase activity
  申请人：Raeppel Stéphane

  公开号：US08906852B2

  公开（公告）日：2014-12-09

  This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions and ophthalmic diseases, disorders and conditions.

  本发明涉及抑制蛋白酪氨酸激酶活性的化合物。特别是，本发明涉及抑制生长因子受体的蛋白酪氨酸激酶活性的化合物，从而抑制受体信号传导，例如抑制VEGF受体信号传导。本发明还提供了用于治疗细胞增殖性疾病和状况以及眼科疾病、疾患和状况的化合物、组合物和方法。
• Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases
  作者：Stephen Claridge、Franck Raeppel、Marie-Claude Granger、Naomy Bernstein、Oscar Saavedra、Lijie Zhan、David Llewellyn、Amal Wahhab、Robert Deziel、Jubrail Rahil、Normand Beaulieu、Hannah Nguyen、Isabelle Dupont、Annie Barsalou、Carole Beaulieu、Ian Chute、Serge Gravel、Marie-France Robert、Sylvain Lefebvre、Marja Dubay、Roussen Pascal、Jeff Gillespie、Zhiyun Jin、James Wang、Jeffrey M. Besterman、A. Robert MacLeod、Arkadii Vaisburg

  DOI：10.1016/j.bmcl.2008.04.009

  日期：2008.5

  A series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases is described. The compounds demonstrated potency with IC50 values in the low nanomolar range in vitro while the lead compound also showed in vivo activity against various human tumor xenograft models in mice. Further exploration of this class of compounds is underway. (c) 2008 Elsevier Ltd. All rights reserved.
• US8906852B2
  申请人：——

  公开号：US8906852B2

  公开（公告）日：2014-12-09
• [EN] INHIBITORS OF PROTEIN TYROSINE KINASE ACTIVITY<br/>[FR] INHIBITEURS DE L'ACTIVITÉ PROTÉINE TYROSINE KINASE
  申请人：METHYLGENE INC

  公开号：WO2011127567A1

  公开（公告）日：2011-10-20

  Compounds that inhibit protein tyrosine kinase activity are disclosed, preferably of Formulae (II) and (III). In particular, said compounds inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling. The invention also provides said compounds, compositions thereof and methods for treating cell proliferative diseases and conditions and ophthalmic diseases, disorders and conditions.