2,7-Bis-cyclohexyloxy-6-methoxy-quinoxaline | 216699-87-5

• 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: 2,7-Bis-cyclohexyloxy-6-methoxy-quinoxaline
• 英文别名: 2,7-dicyclohexyloxy-6-methoxyquinoxaline
• CAS: 216699-87-5
• 化学式: C₂₁H₂₈N₂O₃
• 分子量: 356.465
• InChiKey: VJIOUBTXSNPMNO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.1
• 重原子数：
  26
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  53.5
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  sodium;hydride 、 环己醇 、 2-氯-6,7-二甲氧基喹噁啉 在 氩 、 水 、 water-ethyl acetate 、 Brine 、 magnesium sulfate 、 EtOAc hexanes 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 3.67h， 以to provide a waxy white solid (m.p. 75-78° C.)的产率得到2,7-Bis-cyclohexyloxy-6-methoxy-quinoxaline
  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/喹喔啉化合物，以及包含这些化合物的药物组合物，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：

  US06821962B2

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。
• [EN] QUINOLINE AND QUINOXALINE COMPOUNDS AS PDGF-R AND/OR LCK TYROSINE KINASE INHIBITORS<br/>[FR] COMPOSES DE QUINOLINE ET DE QUINOXALINE AGISSANT COMME INHIBITEURS DU PDGG-R ET/OU DE LCK TYROSINE KINASE
  申请人：AVENTIS PHARM PROD INC

  公开号：WO2000031049A1

  公开（公告）日：2000-06-02

  This invention is directed to quinoline/quinoxaline compounds of formula (I) wherein X is L1OH or L2Z2; L1 is (CR3aR3b)r or (CR3aR3b)m-Z3-(CR3'aR3'b)n; L2 is (CR3aR3b)p-Z4-(CR3'aR3'b)q or ethenyl; Z1 is CH or N; Z2 is optionally substituted hydroxycycloalkyl, optionally substituted hydroxycycloalkenyl, optionally substituted hydroxyheterocyclyl or optionally substituted hydroxyheterocyclenyl; Z3 is O, NR4, S, SO or SO2; Z4 is O, NR4, S, SO, SO2 or a bond; m is 0 or 1; n is 2 or 3, and n + m = 2 or 3; p and q are independently 0, 1, 2, 3 or 4, and p + q = 0, 1, 2, 3 or 4 when Z4 is a bond, and p + q = 0, 1, 2 or 3 when Z4 is other than a bond; r is 2, 3 or 4; which inhibit platelet-derived growth factor or p56lck 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.

  本发明涉及公式（I）的喹啉/喹噁啉化合物，其中X为L1OH或L2Z2; L1为（CR3aR3b）r或（CR3aR3b）m-Z3-（CR3'aR3'b）n; L2为（CR3aR3b）p-Z4-（CR3'aR3'b）q或乙烯基; Z1为CH或N; Z2为可选择取代的羟基环烷基，可选择取代的羟基环烯基，可选择取代的羟基杂环基或可选择取代的羟基杂环烷基; Z3为O，NR4，S，SO或SO2; Z4为O，NR4，S，SO，SO2或键; m为0或1; n为2或3，且n + m = 2或3; p和q独立地为0、1、2、3或4，当Z4为键时，p + q = 0、1、2、3或4，当Z4不是键时，p + q = 0、1、2或3; r为2、3或4; 这些化合物抑制血小板来源生长因子或p56lck酪氨酸激酶活性，本发明还涉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/症状的患者的用途。
• [EN] QUINOLINE AND QUINOXALINE COMPOUNDS WHICH INHIBIT PLATELET-DERIVED GROWTH FACTOR AND/OR P56 TYROSINE KINASES<br/>[FR] COMPOSES QUINOLINE ET QUINOXALINE INHIBANT LE FACTEUR DE CROISSANCE DERIVE DES PLAQUETTES ET/OU LES TYROSINE-KINASES P56
  申请人：RHONE-POULENC RORER PHARMACEUTICALS, INC.

  公开号：WO1998054156A1

  公开（公告）日：1998-12-03

  (EN) This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor tyrosine kinase and/or Lck tyrosine kinase, 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.(FR) L'invention concerne des composés quinoline/quinoxaline inhibant la tyrosine-kynase de facteur de croissance dérivé des plaquettes et/ou la tyrosine-kinase Lck, des compositions pharmaceutiques renfermant ces composés, et l'utilisation de ces composés pour le traitement de patients souffrant ou sujets à des troubles/états associés à la différentiation et à la prolifération cellulaire, à la production de la matrice extracellulaire ou à la libération des médiateurs chimiques et/ou à l'activation et à la prolifération des lymphocytes T.

  该发明涉及抑制血小板衍生生长因子酪氨酸激酶和/或Lck酪氨酸激酶的喹啉/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细胞活化和增殖的疾病/病症的患者。
• 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。