3,6-anhydro-1,2-O-(1-methylethylidene)-5-O-(methylsulfonyl)-α-L-glucofuranose | 650577-71-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 呋喃类
• 英文名称: 3,6-anhydro-1,2-O-(1-methylethylidene)-5-O-(methylsulfonyl)-α-L-glucofuranose
• 英文别名: [(1R,2S,6S,8R,9S)-4,4-dimethyl-3,5,7,11-tetraoxatricyclo[6.3.0.02,6]undecan-9-yl] methanesulfonate
• CAS: 650577-71-2
• 化学式: C₁₀H₁₆O₇S
• 分子量: 280.299
• InChiKey: FIDGDSLUMONPSY-PQFOHKHZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.5
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  88.7
• 氢给体数：
  0
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  3,6-anhydro-1,2-O-(1-methylethylidene)-5-O-(methylsulfonyl)-α-L-glucofuranose 、 4-[(4-bromo-3-chlorophenyl)amino]-6-methyloxy-7-hydroxyquinazoline trifluoroacetate 在 potassium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 18.0h， 以121 mg的产率得到3,6-anhydro-5-O-[4-[(4-bromo-3-chlorophenyl)amino]-6-(methyloxy)quinazolin-7-yl]-1,2-O-(1-methylethylidene)-β-D-idofuranose
  参考文献：
  名称：

  Receptor-Type Kinase Modulators and Methods of Use

  摘要：

  本发明提供了用于调节受体激酶活性的化合物，特别是ephrin和EGFR，并利用这些化合物及其药物组合物治疗由受体激酶活性介导的疾病的方法。由受体激酶活性介导的疾病包括但不限于部分表现为细胞增殖异常水平（即肿瘤生长）、程序性细胞死亡（凋亡）、细胞迁移和侵袭以及与肿瘤生长相关的血管生成的疾病。本发明的化合物包括“谱选择性”激酶调节剂，这些化合物抑制、调节和/或调节跨受体型酪氨酸激酶亚家族的信号传导，包括ephrin和EGFR。

  公开号：

  US20160129032A1
• 作为产物：
  描述：

  1,4:3,6-dianhydro-2-deoxy-5-O-(phenylcarbonyl)-L-arabino-hex-1-enitol 在 N-甲基吗啉 、 吡啶 、 sodium hydroxide 、 四氧化锇 、 水 、 对甲苯磺酸 作用下， 以 甲醇 、 二氯甲烷 、 水 、 丙酮 、 苯 为溶剂， 反应 10.5h， 生成 3,6-anhydro-1,2-O-(1-methylethylidene)-5-O-(methylsulfonyl)-α-L-glucofuranose
  参考文献：
  名称：

  [EN] C-MET MODULATORS AND METHODS OF USE
  [FR] MODULATEURS DE C-MET ET PROCEDE D'UTILISATION

  摘要：

  公开号：

  WO2005030140A3

文献信息

• [EN] RECEPTOR-TYPE KINASE MODULATORS AND METHODS OF USE<br/>[FR] MODULATEURS DE KINASE DE TYPE RECEPTEUR ET PROCEDES D'UTILISATION
  申请人：EXELIXIS INC

  公开号：WO2004006846A2

  公开（公告）日：2004-01-22

  The present invention provides compounds for modulating receptor kinase activity, particularly ephrin and EGFR, and methods of treating diseases mediated by receptor kinase activity utilizing the compounds and pharmaceutical compositions thereof. Diseases mediated by receptor kinase activity include, but are not limited to, diseases characterized in part by abnormal levels of cell proliferation (i.e. tumor growth), programmed cell death ( apoptosis), cell migration and invasion and angiogenesis associated with tumor growth. Compounds of the invention include 'spectrum selective' kinase modulators, compounds that inhibit, regulate and/or mo dulate signal transduction across subfamilies of receptor-type tyrosine kinases, including ephrin and EGFR.

  本发明提供了用于调节受体激酶活性的化合物，特别是调节ephrin和EGFR，以及利用这些化合物和其制剂治疗受受体激酶活性介导的疾病的方法。受受体激酶活性介导的疾病包括但不限于部分由细胞增殖异常水平（即肿瘤生长）、程序性细胞死亡（凋亡）、细胞迁移和侵袭以及与肿瘤生长相关的血管生成所特征化的疾病。本发明的化合物包括“光谱选择性”激酶调节剂，这些化合物抑制、调节和/或调节受体型酪氨酸激酶亚家族之间的信号转导，包括ephrin和EGFR。
• Receptor-type kinase modulators and methods of use
  申请人：Rice D Kenneth

  公开号：US20060069077A1

  公开（公告）日：2006-03-30

  The present invention provides compounds for modulating receptor kinase activity, particularly ephrin and EGFR, and methods of treating diseases mediated by receptor kinase activity utilizing the compounds and pharmaceutical compositions thereof. Diseases mediated by receptor kinase activity include, but are not limited to, diseases characterized in part by abnormal levels of cell proliferation (i.e. tumor growth), programmed cell death (apoptosis), cell migration and invasion and angiogenesis associated with tumor growth. Compounds of the invention include “spectrum selective” kinase modulators, compounds that inhibit, regulate and/or modulate signal transduction across subfamilies of receptor-type tyrosine kinases, including ephrin and EGFR.

  本发明提供了用于调节受体激酶活性的化合物，特别是调节ephrin和EGFR等受体激酶活性的化合物，并利用这些化合物和其制剂治疗由受体激酶活性介导的疾病的方法。由受体激酶活性介导的疾病包括但不限于部分表现为细胞增殖异常水平（即肿瘤生长）、程序性细胞死亡（凋亡）、细胞迁移和侵袭以及与肿瘤生长相关的血管生成的疾病。本发明的化合物包括“光谱选择性”激酶调节剂，可以抑制、调节和/或调节受体型酪氨酸激酶亚家族之间的信号转导，包括ephrin和EGFR。
• c-MET MODULATORS AND METHOD OF USE
  申请人：BANNEN CANNE LYNNE

  公开号：US20070244116A1

  公开（公告）日：2007-10-18

  The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.

  本发明提供了用于调节蛋白激酶酶活性，以调节细胞活动，如增殖、分化、程序性细胞死亡、迁移和化学侵袭的化合物。更具体地，本发明提供了喹唑啉和喹啉，这些化合物抑制、调节和/或调节激酶受体，特别是c-Met、KDF、c-Kit、flt-3和flt-4，与上述细胞活动变化相关的信号转导途径，包含这些化合物的组合物，以及使用它们治疗激酶依赖性疾病和病况的方法。本发明还提供制备上述化合物的方法和包含这些化合物的组合物。
• C-MET MODULATORS AND METHOD OF USE
  申请人：Bannen Canne Lynne

  公开号：US20070225307A1

  公开（公告）日：2007-09-27

  The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.

  本发明提供了用于调节蛋白激酶酶活性以调节细胞活动（如增殖、分化、程序性细胞死亡、迁移和化学入侵）的化合物。更具体地，该发明提供了喹唑啉和喹啉，它们能够抑制、调节和/或调节激酶受体，特别是c-Met、KDF、c-Kit、flt-3和flt-4，与上述细胞活动变化相关的信号转导途径，包含这些化合物的组合物，以及使用它们治疗激酶依赖性疾病和病况的方法。本发明还提供了制备上述化合物和包含这些化合物的组合物的方法。
• c-Met modulators and methods of use
  申请人：Bannen Canne Lynne

  公开号：US20070054928A1

  公开（公告）日：2007-03-08

  The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate and/or modulate kinase receptor, particularly c-Met, KDR, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.

  本发明提供了用于调节蛋白激酶酶活性以调节细胞活动（如增殖、分化、程序性细胞死亡、迁移和化学入侵）的化合物。更具体地，本发明提供了能够抑制、调节和/或调节激酶受体，特别是c-Met、KDR、c-Kit、flt-3和flt-4，与上述细胞活动变化相关的信号转导途径的喹唑啉和喹啉，以及包含这些化合物的组合物和使用它们治疗激酶依赖性疾病和病况的方法。本发明还提供了制备上述化合物和包含这些化合物的组合物的方法。