(R)-N-(2-fluoro-1-(2-fluorophenyl)ethylidene)-2-methylpropane-2-sulfinamide

• 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: (R)-N-(2-fluoro-1-(2-fluorophenyl)ethylidene)-2-methylpropane-2-sulfinamide
• 英文别名: (NE)-N-[2-fluoro-1-(2-fluorophenyl)ethylidene]-2-methylpropane-2-sulfinamide
• 化学式: C₁₂H₁₅F₂NOS
• 分子量: 259.32
• InChiKey: GOMMLNBARBYIIO-PTNGSMBKSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  17
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  48.6
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  (R)-N-(2-fluoro-1-(2-fluorophenyl)ethylidene)-2-methylpropane-2-sulfinamide 在 盐酸 、 lithium borohydride 、 ammonium chloride 、 碳酸氢钠 、 sodium carbonate 作用下， 以 四氢呋喃 、 1,4-二氧六环 、 甲醇 、 乙醇 、 水 、 乙酸乙酯 为溶剂， 生成 (S)-5,5-difluoro-4-(fluoromethyl)-4-(2-fluorophenyl)-5,6-dihydro-4H-1,3-oxazin-2-amine
  参考文献：
  名称：

  HALOGEN-ALKYL-1,3 OXAZINES AS BACE1 AND/OR BACE2 INHIBITORS

  摘要：

  本发明提供具有BACE1和/或BACE2抑制活性的化合物(I)的公式，它们的制备，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。

  公开号：

  US20140080819A1

文献信息

• 2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridines as BACE1 inhibitors
  申请人：H. Lundbeck A/S

  公开号：US10011596B2

  公开（公告）日：2018-07-03

  The present invention provides compounds of Formula I for the treatment of neurodegenerative or cognitive diseases. The method further provides for piperidine-2-one and piperidine-2-thione intermediates to compounds of formula I.

  本发明提供了式 I 的化合物 用于治疗神经退行性疾病或认知疾病。该方法进一步提供了式 I 化合物的哌啶-2-酮和哌啶-2-硫酮中间体。
• 2-amino-5,5-difluoro-6-(fluoromethyl)-6-phenyl-3,4,5,6-tetrahydropyridines as BACE1 inhibitors
  申请人：H. Lundbeck A/S

  公开号：US10058540B2

  公开（公告）日：2018-08-28

  The present invention is directed to compounds of Formula (I) which are inhibitors of the BACE1 enzyme. Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds to treat disorders for which the reduction of Aβ deposits is beneficial such as Alzheimer's disease.

  本发明涉及作为 BACE1 酶抑制剂的式 (I) 化合物。本发明的另一个方面涉及包含所述化合物的药物组合物，以及所述化合物用于治疗减少 Aβ 沉积有益的疾病（如阿尔茨海默病）的用途。
• BACE1 inhibitors
  申请人：Hoffmann-La Roche Inc.

  公开号：US10399969B2

  公开（公告）日：2019-09-03

  The present invention provides a compound of formula I, having BACE1 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.

  本发明提供了具有 BACE1 抑制活性的式 I 化合物、其制造方法、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可用于阿尔茨海默病等疾病的治疗和/或预防。
• 2-Amino-3-Fluoro-3-(Fluoromethyl)-6-Methyl-6-Phenyl-3,4,5,6-Tetrahydropyridines as BACE1 Inhibitors
  申请人：H. Lundbeck A/S

  公开号：US20170044151A1

  公开（公告）日：2017-02-16

  The present invention provides compounds of Formula I for the treatment of neurodegenerative or cognitive diseases. The method further provides for piperidine-2-one and piperidine-2-thione intermediates to compounds of formula I.
• 2-Amino-5,5-Difluoro-6-(Fluoromethyl)-6-Phenyl-3,4,5,6-Tetrahydropyridines as BACE1 Inhibitors
  申请人：H. Lundbeck A/S

  公开号：US20170340618A1

  公开（公告）日：2017-11-30

  The present invention is directed to compounds of Formula (I) which are inhibitors of the BACE1 enzyme. Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds to treat disorders for which the reduction of Aβ deposits is beneficial such as Alzheimer's disease.