AG 1433 | 168836-03-1

• 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: AG 1433
• 英文别名: 2-(3,4-dihydroxyphenyl)-6,7-dimethylquinoxaline；4-(6,7-dimethylquinoxalin-2-yl)benzene-1,2-diol；tyrphostin AG 1433；tyrphostin AG1433；ALX-270-277；2-(3,4-dihydroxyphenyl)-6,7-dimethyl-quinoxaline
• CAS: 168836-03-1
• 化学式: C₁₆H₁₄N₂O₂
• 分子量: 266.299
• InChiKey: SMKFYHOKXJUJOT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  20
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  66.2
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  3,4-二羟基-2'-氯苯乙酮 、 水 、 4，5-二甲基-1，2-苯二胺 以 二甲基亚砜 为溶剂， 以67%的产率得到AG 1433
  参考文献：
  名称：

  Compounds for the treatment of disorders related to vasculogenesis

  摘要：

  本发明涉及有机分子，能够调节酪氨酸激酶信号传导，特别是KDR/FLK-1受体信号传导，以调节和/或调节血管生成和血管新生。该发明部分基于KDR/FLK-1酪氨酸激酶受体表达与内皮细胞相关，并且将血管内皮生长因子（VEGF）确定为FLK-1的高亲和力配体的证明。这些结果表明KDR/FLK-1在血管生成和血管新生过程中的信号系统中起着重要作用。本发明还描述了表达FLK-1的宿主细胞的工程化以及利用表达的FLK-1来评估和筛选参与FLK-1调节的药物和VEGF类似物的用途，无论是通过激动剂还是拮抗剂活性。该发明还涉及使用所披露的化合物治疗与血管生成和血管新生相关的疾病，包括癌症、糖尿病、血管瘤和卡波西肉瘤。

  公开号：

  US05763441A1

文献信息

• Targeted multivalent macromolecules
  申请人：TARGESOME, INC.

  公开号：US20030129223A1

  公开（公告）日：2003-07-10

  Targeted therapeutic agents, comprising a linking carrier, a therapeutic entity associated with the linking carrier, and at least one targeting entity are provided, as well as methods for their preparation and use.

  靶向治疗剂，包括一个连接载体，与连接载体相关联的治疗实体，以及至少一个靶向实体，以及它们的制备和使用方法。
• Quinazoline compounds and compositions thereof for the treatment of
  申请人：Sugen, Inc.

  公开号：US05792771A1

  公开（公告）日：1998-08-11

  The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction and particularly KDR/FLK-1 receptor signal transduction in order to regulate and/or modulate vasculogenesis and angiogenesis. The invention is based, in part, on the demonstration that KDR/FLK-1 tyrosine kinase receptor expression is associated with endothelial cells and the identification of vascular endothelial growth factor (VEGF) as the high affinity ligand of FLK-1. These results indicate a major role for KDR/FLK-1 in the signaling system during vasculogenesis and angiogenesis. Engineering of host cells that express FLK-1 and the uses of expressed FLK-1 to evaluate and screen for drugs and analogs of VEGF involved in FLK-1 modulation by either agonist or antagonist activities is also described. The invention also relates to the use of the disclosed compounds in the treatment of disorders, including cancer, diabetes, hemangioma and Kaposi's sarcoma, which are related to vasculogenesis and angiogenesis.

  本发明涉及有机分子，能够调节酪氨酸激酶信号传导，特别是KDR/FLK-1受体信号传导，以调节和/或调节血管生成和血管新生。该发明部分基于KDR/FLK-1酪氨酸激酶受体表达与内皮细胞相关，并确定血管内皮生长因子（VEGF）为FLK-1的高亲和力配体的论证。这些结果表明KDR/FLK-1在血管生成和血管新生过程中的信号系统中起着重要作用。描述了表达FLK-1的宿主细胞的工程化，以及利用表达的FLK-1评估和筛选参与FLK-1调节的VEGF的药物和类似物，无论是通过激动剂还是拮抗剂活性。该发明还涉及使用所披露的化合物治疗与血管生成和血管新生相关的疾病，包括癌症、糖尿病、血管瘤和卡波西肉瘤。
• Substituted aryl-amine derivatives and methods of use
  申请人：Yuan Chenguang Chester

  公开号：US20060040966A1

  公开（公告）日：2006-02-23

  Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds of Formula I and II wherein R, R 1 and R 2 for each formula are defined herein. The invention further includes analogs, prodrugs and pharmaceutically acceptable salts and derivatives of Formulas I and II, as well as pharmaceutical compositions, medicaments and methods thereof for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

  选定的胺类化合物对于预防和治疗由血管生成介导的疾病等疾病有效。该发明涵盖了式I和式II的新型化合物，其中每个式中的R、R1和R2如本文所定义。该发明还包括式I和式II的类似物、前药和药物可接受的盐和衍生物，以及用于预防和治疗涉及癌症等疾病和其他疾病或病症的药物组合物、药物和方法。该发明还涉及制备这种化合物的工艺以及在这种工艺中有用的中间体。
• Methods and compositions for treating diseases associated with pathogenic proteins
  申请人：Chiang K. Peter

  公开号：US20070179123A1

  公开（公告）日：2007-08-02

  Methods and compositions are provided comprising a therapeutically effective amount of a compound of formula I wherein R 1-4 , W, X, Y and Z are as defined in the specification, for inhibiting and treating diseases and disorders associated with pathogenic proteins causing neurodegenerative diseases and amyloid diseases, such as protease resistant prion proteins (PrP Sc ) and those associated with transmissible spongiform encephalopathies (TSEs), Alzheimer's Disease, amyloidosis, and the like.

  提供了一种方法和组合物，包括公式I中化合物的治疗有效量，其中R1-4，W，X，Y和Z如规范中所定义，用于抑制和治疗与致病蛋白质相关的疾病和障碍，这些致病蛋白质导致神经退行性疾病和淀粉样疾病，如蛋白酶抵抗性朊病毒蛋白（PrPSc）和与可传播性海绵状脑病（TSEs），阿尔茨海默病，淀粉样变性等相关的蛋白质。
• Specific binding agents to hepatocyte growth factor
  申请人：Amgen, Inc

  公开号：EP2341067A1

  公开（公告）日：2011-07-06

  Specific binding agents that interact with hepatocyte growth factor (HGF) are described. Methods of treating cancer by administering a pharmaceutically effective amount of a specific binding agent to HGF are described. Methods of detecting the amount of HGF in a sample using a specific binding agent to HGF are described.

  描述了与肝细胞生长因子（HGF）相互作用的特异性结合剂。描述了通过施用药学有效量的 HGF 特异性结合剂治疗癌症的方法。介绍了使用与 HGF 的特异性结合剂检测样品中 HGF 含量的方法。