3-amino-5-morpholin-4-ylbenzamide | 945397-25-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 英文名称: 3-amino-5-morpholin-4-ylbenzamide
• CAS: 945397-25-1
• 化学式: C₁₁H₁₅N₃O₂
• 分子量: 221.259
• InChiKey: OQQPVALJCHOSOS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  81.6
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  3-Morpholin-4-yl-5-nitro-benzamide 在 palladium 10% on activated carbon 、 氢气 作用下， 以 乙醇 为溶剂， 生成 3-amino-5-morpholin-4-ylbenzamide
  参考文献：
  名称：

  Inhibitors of the tyrosine kinase EphB4. Part 2: Structure-based discovery and optimisation of 3,5-bis substituted anilinopyrimidines

  摘要：

  Crystallographic studies of a range of 3-substituted anilinopyrimidine inhibitors of EphB4 have highlighted two alternative C-2 aniline conformations and this discovery has been exploited in the design of a highly potent series of 3,5-disubstituted anilinopyrimidines. The observed range of cellular activities has been rationalised on the basis of physicochemical and structural characteristics.

  DOI：

  10.1016/j.bmcl.2008.09.087

文献信息

• PYRIMIDINE DERIVATIVES
  申请人：Kettle Jason Grant

  公开号：US20110046108A1

  公开（公告）日：2011-02-24

  The invention concerns benzamide compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R 1 , ring A, n, R 3 , and R 4 are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of EphB4, and/or EphA2 and/or Src kinases.

  这项发明涉及Formula (I)的苯甲酰胺化合物或其药用可接受的盐，其中R1、环A、n、R3和R4如描述中所定义。本发明还涉及制备这种化合物的方法、含有它们的药物组合物以及它们在制造用作抗增殖剂的药物中的用途，用于预防或治疗对EphB4、EphA2和/或Src激酶抑制敏感的肿瘤或其他增殖病症。
• [EN] PYRIMIDINE DERIVATIVES<br/>[FR] DERIVES DE PYRIMIDINE
  申请人：ASTRAZENECA AB

  公开号：WO2007085833A2

  公开（公告）日：2007-08-02

  [EN] The invention concerns benzamide compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R¹, ring A, n, R³, and R⁴ are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of EphB4, and/or EphA2 and/or Src kinases.
  [FR] La présente invention concerne des composés de benzamide de Formule (I) ou un sel dérivé pharmaceutiquement acceptable, où R¹, le cycle A, n, R³, et R⁴ sont tels qu'énoncés dans la description. La présente invention a aussi trait à des processus de préparation de tels composés, à des compositions pharmaceutiques les contenant et à leur utilisation dans la fabrication d'un médicament à utiliser comme agent antiproliférateur pour la prévention ou le traitement de tumeurs ou d'autres conditions prolifératrices qui sont sensibles à l'inhibition des kinases EphB4, et/ou EphA2 et/ou Src.
• [EN] QUINAZOLINES FOR PDK1 INHIBITION<br/>[FR] QUINAZOLINES DESTINÉS À L'INHIBITION DE PDK1
  申请人：NOVARTIS VACCINES & DIAGNOSTIC

  公开号：WO2008079988A2

  公开（公告）日：2008-07-03

  (EN) The invention provides novel compounds that are inhibitors of PDK1. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions.(FR) Cette invention concerne de nouveaux composés qui sont des inhibiteurs de PDK1. Elle concerne également des compositions pharmaceutiques contenant ces composés, et des méthodes utilisant ces composés et compositions pour le traitement de maladies à évolution chronique comme le cancer.