2-(6,7-Dimethoxy-quinoxalin-2-yl)-2-aza-bicyclo[2.2.2]octan-3-one | 217093-53-3

• 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: 2-(6,7-Dimethoxy-quinoxalin-2-yl)-2-aza-bicyclo[2.2.2]octan-3-one
• 英文别名: 2-(6,7-dimethoxyquinoxalin-2-yl)-2-azabicyclo[2.2.2]octan-3-one
• CAS: 217093-53-3
• 化学式: C₁₇H₁₉N₃O₃
• 分子量: 313.356
• InChiKey: QTJOJAJAJFVICY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  23
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  64.6
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  2-(6,7-Dimethoxy-quinoxalin-2-yl)-2-aza-bicyclo[2.2.2]octan-3-one 在 水 作用下， 生成 4-(6,7-Dimethoxy-quinoxalin-2-ylamino)-cyclohexanecarboxylic acid
  参考文献：
  名称：

  Potent quinoxaline-Based inhibitors of PDGF receptor tyrosine kinase activity. Part 2: the synthesis and biological activities of RPR127963 an orally bioavailable inhibitor

  摘要：

  RPR127963 demonstrates an excellent pharmacokinetic profile in several species and was found to be efficacious in the prevention of restenosis in a Yucatan mini-pig model upon oral administration of 1-5 mg/kg. The in vitro selectivity profile and SAR of the highly optimized PDGF-R tyrosine kinase inhibitor are highlighted. (C) 2003 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(03)00655-3
• 作为产物：
  描述：

  1,2-二氨基-4,5-二甲氧基苯 在 三氯氧磷 作用下， 以 四氢呋喃 为溶剂， 生成 2-(6,7-Dimethoxy-quinoxalin-2-yl)-2-aza-bicyclo[2.2.2]octan-3-one
  参考文献：
  名称：

  Potent quinoxaline-Based inhibitors of PDGF receptor tyrosine kinase activity. Part 2: the synthesis and biological activities of RPR127963 an orally bioavailable inhibitor

  摘要：

  RPR127963 demonstrates an excellent pharmacokinetic profile in several species and was found to be efficacious in the prevention of restenosis in a Yucatan mini-pig model upon oral administration of 1-5 mg/kg. The in vitro selectivity profile and SAR of the highly optimized PDGF-R tyrosine kinase inhibitor are highlighted. (C) 2003 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(03)00655-3

文献信息

• [EN] QUINOLINE AND QUINOXALINE COMPOUNDS AS PDGF-RECEPTOR AND/OR LCK TYROSINE KINASE INHIBITORS<br/>[FR] COMPOSES DE QUINOLEINE ET QUINOXALINE UTILISES COMME INHIBITEURS DU RECEPTEUR PDGF ET/OU DE LA TYROSINE KINASE LCK
  申请人：AVENTIS PHARM PROD INC

  公开号：WO2000031051A1

  公开（公告）日：2000-06-02

  This invention is directed to quinoline/quinoxaline compounds of formula (I), which inhibit platelet-derived growth factor or p56lck tyrosine kinase activity, to pharmaceutical compositions comprising theses compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or T cell activation and proliferation.

  本发明涉及公式（I）的喹啉/喹噁啉化合物，其抑制血小板来源性生长因子或p56lck酪氨酸激酶活性，以及包含这些化合物的制药组合物，并且用于治疗患有或受到涉及细胞分化、增殖、细胞外基质产生或介质释放和/或T细胞激活和增殖的疾病/症状的患者。
• Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or p56lck tyrosine kinases
  申请人：——

  公开号：US20030130285A1

  公开（公告）日：2003-07-10

  This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor or p56 lck tyrosine kinase activity, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or T cell activation and proliferation.

  本发明涉及抑制血小板源性生长因子或p56lck酪氨酸激酶活性的喹啉/喹噁啉化合物，以及包含这些化合物的制药组合物，以及使用这些化合物治疗患有或患有涉及细胞分化、增殖、细胞外基质产生或介质释放和/或T细胞激活和增殖的疾病/症状的患者。
• Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and /or p56lck tyrosine kinases
  申请人：——

  公开号：US20030139400A1

  公开（公告）日：2003-07-24

  This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor or p56 lck tyrosine kinase activity, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or T cell activation and proliferation.

  本发明涉及抑制血小板源性生长因子或p56lck酪氨酸激酶活性的喹啉/喹噁啉化合物，以及包含这些化合物的制药组合物，并且涉及使用这些化合物治疗患有或存在细胞分化、增殖、细胞外基质产生或介质释放和/或T细胞激活和增殖的疾病/状况的患者。
• US06180632B2
  申请人：——

  公开号：——

  公开（公告）日：——
• QUINOLINE AND QUINOXALINE COMPOUNDS WHICH INHIBIT PLATELET-DERIVED GROWTH FACTOR AND/OR p56lck TYROSINE KINASES
  申请人：Aventis Pharmaceuticals Inc.

  公开号：EP1001945B1

  公开（公告）日：2011-03-02