2-[(Pyridin-2(1H)-on-5-yl)methyl]amino-N-(benzo[d]pyrazol-5-yl)-3-pyridinecarboxamide | 352228-04-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡唑类
• 英文名称: 2-[(Pyridin-2(1H)-on-5-yl)methyl]amino-N-(benzo[d]pyrazol-5-yl)-3-pyridinecarboxamide
• 英文别名: N-(1H-indazol-5-yl)-2-[(6-oxo-1H-pyridin-3-yl)methylamino]pyridine-3-carboxamide
• CAS: 352228-04-7
• 化学式: C₁₉H₁₆N₆O₂
• 分子量: 360.375
• InChiKey: NXHMUFFLBNEBCE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  27
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.05
• 拓扑面积：
  112
• 氢给体数：
  4
• 氢受体数：
  5

文献信息

• 2-Amino-nicotinamide derivatives and their use as vegf-receptor tyrosine kinase inhibitors
  申请人：——

  公开号：US20030032656A1

  公开（公告）日：2003-02-13

  The invention relates to the use of 2-amino-nicotinamide derivatives of formula (I) wherein n is from 1 up to and including 6; W is O or S; R 1 and R 3 represent independently of each other hydrogen, lower alkyl or lower acyl; R 2 represents a cycloalkyl group, an aryl group, or a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms and 0, 1 or 2 heteroatoms independently from each other selected from the group consisting of oxygen and sulfur, which groups in each case are unsubstituted or mono- or polysubstituted; R and R′ are independently of each other hydrogen or lower alkyl; X represents an aryl group, or a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms and 0, 1 or 2 heteroatoms independently from each other selected from the group consisting of oxygen and sulfur, which groups in each case are unsubstituted or mono- or polysubstituted; or a N-oxide, a possible tautomer thereof or a pharmaceutically acceptale salt of such a compound, alone or in combination with one or more other pharmaceutically active compounds for the preparation of a pharmaceutical composition for use for therapy of a disease which responds to an inhibition of the VEGF-receptor tyrosine kinase activity; and to new 2-amino-nicotinamide derivatives of formula (I) and processes for the preparation thereof. 1

  本发明涉及使用公式（I）中的2-氨基烟酰胺衍生物，其中n为1至6，包括1和6；W为O或S；R1和R3分别表示氢、低烷基或低酰基；R2表示环烷基、芳基或含有一个或多个环氮原子和0、1或2个异原子的单环或双环杂芳基，这些基团在每种情况下都未取代或单取代或多取代；R和R'独立地表示氢或低烷基；X表示芳基或含有一个或多个环氮原子和0、1或2个异原子的单环或双环杂芳基，这些基团在每种情况下都未取代或单取代或多取代；或其N-氧化物、可能的互变异构体或其药学上可接受的盐，单独或与一个或多个其他药物活性化合物结合，用于制备用于治疗对抗VEGF受体酪氨酸激酶活性的抑制有反应的疾病的制剂；以及公式（I）的新型2-氨基烟酰胺衍生物及其制备方法。
• 2-AMINO-NICOTINAMIDE DERIVATIVES AND THEIR USE AS VEGF-RECEPTOR TYROSINE KINASE INHIBITORS
  申请人：Novartis AG

  公开号：EP1259487B1

  公开（公告）日：2009-12-23
• EP2168948B1
  申请人：——

  公开号：EP2168948B1

  公开（公告）日：2014-05-07
• Combination Of A Vegf Receptor Inhibitor Or With A Chemotherapeutic Agent
  申请人：Bold Guido

  公开号：US20080085902A1

  公开（公告）日：2008-04-10

  The present invention relates to a combination therapy for treating patients suffering from proliferative diseases or diseases associated with persistent angiogenesis. The patient is treated with a VEGF inhibitor compound; and one or more chemotherapeutic agents.
• US6624174B2
  申请人：——

  公开号：US6624174B2

  公开（公告）日：2003-09-23