(RS)-4-(3-bromo-phenyl)-4-(4-methyl-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)-4,5-dihydro-oxazol-2-ylamine | 1180016-38-9

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 新黄酮类化合物
• 英文名称: (RS)-4-(3-bromo-phenyl)-4-(4-methyl-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)-4,5-dihydro-oxazol-2-ylamine
• 英文别名: 4-(3-bromophenyl)-4-(4-methyl-2,3-dihydro-1,4-benzoxazin-6-yl)-5H-1,3-oxazol-2-amine
• CAS: 1180016-38-9
• 化学式: C₁₈H₁₈BrN₃O₂
• 分子量: 388.264
• InChiKey: OAVOBVZAHLTHHA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  24
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  60.1
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• 4,5-DIHYDRO-OXAZOL-2-YL AMINE DERIVATIVES
  申请人：Andreini Matteo

  公开号：US20090209529A1

  公开（公告）日：2009-08-20

  The present invention relates to a compounds of formula I wherein R 1 , R 1′ , R 2 , R 3 , R 4 , X, Ar, and m are as defined in the specification and claims and pharmaceutically active acid addition salts thereof. Compounds of the invention have Asp2 (β-secretase, BACE 1 or Memapsin-2) inhibitory activity and are useful for the treatment of diseases characterized by elevated β-amyloid levels or β-amyloid deposits, particularly Alzheimer's disease.

  本发明涉及一种具有以下式I的化合物 其中R 1 ，R 1′ ，R 2 ，R 3 ，R 4 ，X，Ar和m如规范和索赔中定义，并且其药用活性酸盐。本发明的化合物具有Asp2（β-分泌酶，BACE 1或Memapsin-2）抑制活性，并且对于治疗由β-淀粉样蛋白水平升高或β-淀粉样蛋白沉积所特征的疾病，特别是阿尔茨海默病，是有用的。
• 4, 5-DIHYDRO-OXAZOL-2-YL AMINE DERIVATIVES
  申请人：F. Hoffmann-La Roche AG

  公开号：EP2245019A1

  公开（公告）日：2010-11-03
• US7989449B2
  申请人：——

  公开号：US7989449B2

  公开（公告）日：2011-08-02
• [EN] 4, 5-DIHYDRO-OXAZOL-2-YL AMINE DERIVATIVES<br/>[FR] DÉRIVÉS DE 4,5-DIHYDROOXAZOL-2-YLAMINE
  申请人：HOFFMANN LA ROCHE

  公开号：WO2009103626A1

  公开（公告）日：2009-08-27

  The present invention relates to a compounds of formula I or a pharmaceutically active acid addition salts thereof. It has been found that the present compounds have Asp2 (β-sccretasc, BACE 1 or Mcmapsin-2) inhibitory activity and that the compounds may therefore be used in the treatment of diseases characterised by elevated β-amyloid levels or β-amyloid deposits, particularly Alzheimer's disease.
• [EN] ANTICOAGULANT ANTIDOTES<br/>[FR] ANTIDOTES D'ANTICOAGULANTS
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2011089183A2

  公开（公告）日：2011-07-28

  The present invention relates to antibody molecules against anticoagulants, in particular dabigatran, and their use as antidotes of such anticoagulants.