7-[(R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-3-(1,2,3,6-tetrahydropyridin-4-yl)-furo[3,2-c]pyridin-6-ylamine | 1175296-62-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 呋喃吡啶类
• 英文名称: 7-[(R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-3-(1,2,3,6-tetrahydropyridin-4-yl)-furo[3,2-c]pyridin-6-ylamine
• 英文别名: 7-[(R)-1-(2,6-Dichloro-3-fluorophenyl)ethoxy]-3-(1,2,3,6-tetrahydropyridin-4-yl)furo[3,2-c]pyridin-6-ylamine；7-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-3-(1,2,3,6-tetrahydropyridin-4-yl)furo[3,2-c]pyridin-6-amine
• CAS: 1175296-62-4
• 化学式: C₂₀H₁₈Cl₂FN₃O₂
• 分子量: 422.286
• InChiKey: TWIKWMMVTICGGP-SNVBAGLBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  28
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  73.3
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  7-[(R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-3-(1,2,3,6-tetrahydropyridin-4-yl)-furo[3,2-c]pyridin-6-ylamine 在 钯 碳 、 氮气 、 氢气 、 钯 、 氨 、 甲醇 、 二氯甲烷 作用下， 以 乙酸乙酯 为溶剂， 反应 1.0h， 生成 7-[(R)-1-(2,6-Dichloro-3-fluorophenyl)-ethoxy]-3-piperidin-4-yl-furo[3,2-c]pyridin-6-ylamine
  参考文献：
  名称：

  Furo[3,2-C]pyridines

  摘要：

  本发明涉及式I的Furo[3,2-c]吡啶和Thieno[3,2-c]吡啶化合物，以及其药学上可接受的盐、制备方法、中间体、制药组合物和用途，例如在疾病治疗中，包括癌症，包括涉及EMT的病症，包括由蛋白激酶活性介导的病症，例如RON和/或MET。

  公开号：

  US08022206B2
• 作为产物：
  描述：

  N-Boc-1,2,5,6-四氢吡啶-4-硼酸频哪醇酯 在 盐酸 、 四(三苯基膦)钯 、 potassium carbonate 作用下， 以 1,4-二氧六环 、 水 为溶剂， 生成 7-[(R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-3-(1,2,3,6-tetrahydropyridin-4-yl)-furo[3,2-c]pyridin-6-ylamine
  参考文献：
  名称：

  Novel 6-aminofuro[3,2-c]pyridines as potent, orally efficacious inhibitors of cMET and RON kinases

  摘要：

  A series of novel 6-aminofuro[3,2-c]pyridines as kinase inhibitors is described, most notably, OSI-296 (6). We discuss our exploration of structure-activity relationships and optimization leading to OSI-296 and disclose its pharmacological activity against cMET and RON in cellular assays. OSI-296 is a potent and selective inhibitor of cMET and RON kinases that shows in vivo efficacy in tumor xenografts models upon oral dosing and is well tolerated. (C) 2013 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2013.05.074

文献信息

• Furo- and Thieno [3,2-c] Pyridines
  申请人：Li An-Hu

  公开号：US20090197864A1

  公开（公告）日：2009-08-06

  Furo[3,2-c]Pyridine and Thieno[3,2-c]pyridine compounds of Formula I, and pharmaceutically acceptable salts thereof, preparation, intermediates, pharmaceutical compositions, and use, such as in disease treatment, including cancers, including conditions in which EMT is involved, including conditions mediated by protein kinase activity such as RON and/or MET.

  Furo[3,2-c]吡啶和Thieno[3,2-c]吡啶的化合物I的制备、中间体、药用可接受的盐、药物组合物以及用途，例如在疾病治疗中的应用，包括癌症，包括涉及EMT的疾病，包括由蛋白激酶活性介导的疾病，如RON和/或MET。
• FURO-AND THIENO[3,2-C]PYRIDINES
  申请人：OSI Pharmaceuticals, Inc.

  公开号：EP2265616B1

  公开（公告）日：2013-11-20
• US8022206B2
  申请人：——

  公开号：US8022206B2

  公开（公告）日：2011-09-20
• [EN] FURO-AND THIENO[3,2-C] PYRIDINES<br/>[FR] FURO-[3,2-20090813WO03059913A1BAYER AG [US], et al20030724WA1-42AWO2007027855A2ARRAY BIOPHARMA INC [US], et al20070308WA1-42AWO2007124181A2AMGEN INC [US], et al20071101WA1-42AWO03059913A1BAYER AG [US], et al20030724WO2007027855A2ARRAY BIOPHARMA INC [US], et al20070308WO2007124181A2AMGEN INC [US], et al20071101
  申请人：OSI PHARM INC

  公开号：WO2009100282A1

  公开（公告）日：2009-08-13

  Furo[3,2-c]Pyridine and Thieno[3,2-c]pyridine compounds of Formula (I), and pharmaceutically acceptable salts thereof, preparation, intermediates, pharmaceutical compositions, and use, such as in disease treatment, including cancers, including conditions in which EMT is involved, including conditions mediated by protein kinase activity such as RON and/or MET.
• Novel 6-aminofuro[3,2-c]pyridines as potent, orally efficacious inhibitors of cMET and RON kinases
  作者：Arno G. Steinig、An-Hu Li、Jing Wang、Xin Chen、Hanqing Dong、Caterina Ferraro、Meizhong Jin、Mridula Kadalbajoo、Andrew Kleinberg、Kathryn M. Stolz、Paula A. Tavares-Greco、Ti Wang、Mark R. Albertella、Yue Peng、Linda Crew、Jennifer Kahler、Julie Kan、Ryan Schulz、Andy Cooke、Mark Bittner、Roy W. Turton、Maryland Franklin、Prafulla Gokhale、Darla Landfair、Christine Mantis、Jen Workman、Robert Wild、Jonathan Pachter、David Epstein、Mark J. Mulvihill

  DOI：10.1016/j.bmcl.2013.05.074

  日期：2013.8

  A series of novel 6-aminofuro[3,2-c]pyridines as kinase inhibitors is described, most notably, OSI-296 (6). We discuss our exploration of structure-activity relationships and optimization leading to OSI-296 and disclose its pharmacological activity against cMET and RON in cellular assays. OSI-296 is a potent and selective inhibitor of cMET and RON kinases that shows in vivo efficacy in tumor xenografts models upon oral dosing and is well tolerated. (C) 2013 Elsevier Ltd. All rights reserved.