RPR127963

• 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: RPR127963
• 英文别名: trans-4-(6,7-dimethoxyquinoxalin-2-ylamino)cyclohexanol；TKI963
• 化学式: C₁₆H₂₁N₃O₃
• 分子量: 303.361
• InChiKey: CYVRFHRDWQAJGA-XYPYZODXSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.36
• 重原子数：
  22.0
• 可旋转键数：
  4.0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  76.5
• 氢给体数：
  2.0
• 氢受体数：
  6.0

反应信息

• 作为反应物：
  描述：

  RPR127963 、 三苯基膦 、 偶氮二甲酸二乙酯 、 对硝基苯甲酸 在 silica gel 作用下， 以 四氢呋喃 为溶剂， 反应 2.0h， 以to give 250 mg (87.7%) of cyclohex-3-enyl-(6,7-dimethoxyquinoxalin-2-yl)-amine的产率得到Cyclohex-3-enyl-(6,7-dimethoxyquinoxalin-2-yl)-amine
  参考文献：
  名称：

  Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or p56lck tyrosine kinases

  摘要：

  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。

  公开号：

  US06696434B2
• 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， 生成 RPR127963
  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

• METHOD FOR ASSAY ON THE EFFECT OF VASCULARIZATION INHIBITOR
  申请人：Uenaka Toshimitsu

  公开号：US20100092490A1

  公开（公告）日：2010-04-15

  The present invention provides a method of predicting the antitumor effect of an angiogenesis inhibitor. It is possible to predict the antitumor effect of an angiogenesis inhibitor by evaluating the EGF dependency of a tumor cell for proliferation and/or survival and using the EGF dependency as an indicator. Since the antitumor effect of an angiogenesis inhibitor correlates with the EGF dependency of a tumor cell for proliferation and/or survival, the angiogenesis inhibitors is capable of producing excellent antitumor effect when combined with a substance having EGF inhibitory activity.

  本发明提供了一种预测抗血管生成抑制剂的抗肿瘤效果的方法。通过评估肿瘤细胞对表皮生长因子（EGF）增殖和/或存活的依赖性，并将其作为指标，可以预测抗血管生成抑制剂的抗肿瘤效果。由于抗血管生成抑制剂的抗肿瘤效果与肿瘤细胞对EGF增殖和/或存活的依赖性相关，因此当与具有EGF抑制活性的物质结合时，抗血管生成抑制剂能够产生出色的抗肿瘤效果。
• [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：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。
• Anti-vascular and anti-proliferation methods, therapies, and combinations employing specific tyrosine kinase inhibitors
  申请人：Nesbit Mark

  公开号：US20070197538A1

  公开（公告）日：2007-08-23

  This invention is directed to potent inhibitors of protein tyrosine kinase alone or in synergistic combination with antiangiogenic or chemotherapeutic agents for the abrogation of mature vasculature within chemotherapeutic refractory tumors, pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cell proliferation, and particularly treatment of brain cancer, ovarian cancer, pancreatic cancer prostate cancer, and human leukemias, such as CML, AML or ALL.

  本发明涉及针对蛋白酪氨酸激酶的强效抑制剂，单独或与抗血管生成或化疗药物协同使用，用于消除化疗难治性肿瘤内的成熟血管，以及包含这些化合物的制药组合物，并且用于治疗患有或患有涉及细胞增殖的疾病/病症的患者，特别是治疗脑癌、卵巢癌、胰腺癌、前列腺癌和人类白血病，如慢性髓细胞白血病、急性髓细胞白血病或急性淋巴细胞白血病。
• METHOD FOR PREDICTION OF THE EFFICACY OF VASCULARIZATION INHIBITOR
  申请人：Eisai R&D Management Co., Ltd.

  公开号：EP1925941A1

  公开（公告）日：2008-05-28

  It is an object of the present invention to find out a method of predicting the antitumor effect of an angiogenesis inhibitor. According to the present invention, it is possible to predict the antitumor effect of an angiogenesis inhibitor by determining the number of those blood vessels which are covered with pericytes in a tumor and using the resultant number as an indicator.

  本发明的目的是找到一种预测血管生成抑制剂抗肿瘤效果的方法。根据本发明，可以通过确定肿瘤中被周细胞覆盖的血管的数量，并以该数量作为指标，来预测血管生成抑制剂的抗肿瘤效果。