(1S,4R,5S,15R)-19-[3,5-bis(trifluoromethyl)phenyl]-5-[(3,5-difluorophenyl)methyl]-4-hydroxy-14-oxa-2,6-diazatricyclo[13.6.1.016,21]docosa-11,16(21),17,19-tetraen-7-one

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 大环内酰胺类
• 英文名称: (1S,4R,5S,15R)-19-[3,5-bis(trifluoromethyl)phenyl]-5-[(3,5-difluorophenyl)methyl]-4-hydroxy-14-oxa-2,6-diazatricyclo[13.6.1.016,21]docosa-11,16(21),17,19-tetraen-7-one
• 化学式: C₃₄H₃₂F₈N₂O₃
• 分子量: 668.6
• InChiKey: WZOZNJNPXMBUSM-SYQUUIDJSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6.4
• 重原子数：
  47
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  70.6
• 氢给体数：
  3
• 氢受体数：
  12

文献信息

• DIAMINOPROPANE DERIVED MACROCYCLES AS INHIBITORS OF BETA AMYLOID PRODUCTION
  申请人：Marcin Lawrence R.

  公开号：US20080194535A1

  公开（公告）日：2008-08-14

  There is provided a series of macrocyclic diaminopropanes of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , m, n, W, X, Y, Z and L as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.

  提供一系列宏环脂肪二胺丙烷化合物的化学式（I）或其立体异构体；或其药用盐， 其中R1，R2，R3，m，n，W，X，Y，Z和L如本文所定义，它们的药物组合物和使用方法。这些新化合物抑制β-分泌酶对淀粉样前体蛋白（APP）的加工，更具体地说，抑制Aβ-肽的产生。本公开涉及对治疗与β-淀粉样蛋白产生相关的神经系统疾病的化合物，如阿尔茨海默病和其他受抗淀粉样活性影响的疾病。
• US7772221B2
  申请人：——

  公开号：US7772221B2

  公开（公告）日：2010-08-10