(4R,5R)-4-(5-amino-2-fluoro-phenyl)-5-fluoro-4,5-dimethyl-5,6-dihydro-4H-[1,3]oxazin-2-ylamine | 1402413-28-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: (4R,5R)-4-(5-amino-2-fluoro-phenyl)-5-fluoro-4,5-dimethyl-5,6-dihydro-4H-[1,3]oxazin-2-ylamine
• 英文别名: (4R,5R)-4-(5-amino-2-fluorophenyl)-5-fluoro-4,5-dimethyl-6H-1,3-oxazin-2-amine
• CAS: 1402413-28-8
• 化学式: C₁₂H₁₅F₂N₃O
• 分子量: 255.267
• InChiKey: WARLKRBMHZQDPT-NWDGAFQWSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  18
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  73.6
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  (4R,5R)-4-(5-amino-2-fluoro-phenyl)-5-fluoro-4,5-dimethyl-5,6-dihydro-4H-[1,3]oxazin-2-ylamine 、 4-Chloro-1-(2,2-difluoroethyl)-1H-pyrazole-3-carboxylic acid 生成 4-chloro-1-(2,2-difluoro-ethyl)-1H-pyrazole-3-carboxylic acid [3-((4R,5R)-2-amino-5-fluoro-4,5-dimethyl-5,6-dihydro-4H-[1,3]oxazin-4-yl)-4-fluoro-phenyl]amide
  参考文献：
  名称：

  1,3-Oxazines As Bace1 And/Or Bace2 Inhibitors

  摘要：

  本发明提供了具有BACE1和/或BACE2抑制活性的4-(3-氨基苯基)-5,6-二氢-4H-[1,3]噁唑-2-胺（式I），它们的制造，含有它们的药物组合物以及它们作为治疗活性物质的用途。本发明的活性化合物在治疗和/或预防例如阿尔茨海默病和2型糖尿病方面是有用的。

  公开号：

  US20150322054A1

文献信息

• [EN] 1,3-OXAZINES AS BACE1 AND/OR BACE2 INHIBITORS<br/>[FR] 1,3-OXAZINES EN TANT QU'INHIBITEURS DE BACE1 ET/OU DE BACE2
  申请人：HOFFMANN LA ROCHE

  公开号：WO2012156284A1

  公开（公告）日：2012-11-22

  The present invention provides compounds of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.

  本发明提供具有BACE1和/或BACE2抑制活性的式I化合物，它们的制备方法，含有它们的制药组合物以及它们作为治疗活性物质的用途。本发明的活性化合物可用于治疗和/或预防例如阿尔茨海默病和2型糖尿病等疾病。
• 1,3-OXAZINES AS BACE 1 AND/OR BACE2 INHIBITORS
  申请人：Hilpert Hans

  公开号：US20120295900A1

  公开（公告）日：2012-11-22

  The present invention provides compounds of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.

  本发明提供具有BACE1和/或BACE2抑制活性的化合物，它们的制备方法，含有它们的药物组合物以及它们作为治疗活性物质的用途。本发明的活性化合物在治疗和/或预防治疗例如阿尔茨海默病和2型糖尿病方面是有用的。
• 1,3-OXAZINES AS BACE1 AND/OR BACE2 INHIBITORS
  申请人：Hilpert Hans

  公开号：US20120258962A1

  公开（公告）日：2012-10-11

  The present invention provides 4-(3-Amino-phenyl)-5,6-dihydro-4H-[1,3]oxazin-2-ylamines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.

  本发明提供了具有BACE1和/或BACE2抑制活性的式I的4-(3-氨基苯基)-5,6-二氢-4H-[1,3]噁嗪-2-胺，其制备方法，含有它们的药物组合物以及它们作为治疗活性物质的用途。本发明的活性化合物在治疗和/或预防治疗阿尔茨海默病和2型糖尿病等疾病方面是有用的。
• [EN] 1,3 OXAZINES AS BACE1 AND/OR BACE2 INHIBITORS<br/>[FR] 1,3-OXAZINES À TITRE D'INHIBITEURS DE BACE1 ET/OU DE BACE2
  申请人：HOFFMANN LA ROCHE

  公开号：WO2012139993A1

  公开（公告）日：2012-10-18

  The present invention provides 4-(3-Amino-phenyl)-5,6-dihydro-4H-[1,3]oxazin-2-ylamines of formula (I) having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.

  本发明提供了具有BACE1和/或BACE2抑制活性的式(I)的4-(3-氨基苯基)-5,6-二氢-4H-[1,3]噁嗪-2-胺，以及它们的制备方法、含有它们的药物组合物和它们作为治疗活性物质的用途。本发明的活性化合物在治疗和/或预防治疗阿尔茨海默病和2型糖尿病等疾病方面是有用的。
• 1,3-oxazines as BACE1 and/or BACE2 inhibitors
  申请人：Hilpert Hans

  公开号：US08754075B2

  公开（公告）日：2014-06-17

  The present invention provides 4-(3-Amino-phenyl)-5,6-dihydro-4H-[1,3]oxazin-2-ylamines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.

  本发明提供了具有BACE1和/或BACE2抑制活性的式I的4-(3-氨基苯基)-5,6-二氢-4H-[1,3]噁唑-2-胺，以及它们的制造方法、含有它们的药物组合物和它们作为治疗活性物质的用途。本发明的活性化合物在治疗和/或预防阿尔茨海默病和2型糖尿病方面是有用的。