N-((3-chloro-5-propoxybenzylamino)(amino)methylene)-5-methyl-3-(4-methoxyphenyl)isoxazole 4-carboxamide | 917386-34-6

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: N-((3-chloro-5-propoxybenzylamino)(amino)methylene)-5-methyl-3-(4-methoxyphenyl)isoxazole 4-carboxamide
• 英文别名: N-[N'-[(3-chloro-5-propoxyphenyl)methyl]carbamimidoyl]-3-(4-methoxyphenyl)-5-methyl-1,2-oxazole-4-carboxamide
• CAS: 917386-34-6
• 化学式: C₂₃H₂₅ClN₄O₄
• 分子量: 456.929
• InChiKey: JGVCTRTYDJNIME-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  32
• 可旋转键数：
  9
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  112
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• Aminoacetamide acyl guanidines as beta-secretase inhibitors
  申请人：Gerritz Samuel

  公开号：US20060287287A1

  公开（公告）日：2006-12-21

  There is provided a series of substituted acyl guanidines of Formula (Ik) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R 2 , R 3 , R 4 , R 5 , R 25 , R 26 and R 27 as defined herein, their pharmaceutical compositions and methods of use. These 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.

  提供了一系列的取代酰基胍类化合物，符合以下化学式（Ik）或其立体异构体；或其药学上可接受的盐，其中R2、R3、R4、R5、R25、R26和R27如本文所定义，它们的药物组合物和使用方法。这些化合物抑制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β-淀粉样蛋白产生相关的神经疾病的治疗有用的化合物，如阿尔茨海默氏病和其他受抗淀粉样活性影响的病症。
• Acyl guanidines as beta-secretase inhibitors
  申请人：Gerritz Samuel

  公开号：US20070015754A1

  公开（公告）日：2007-01-18

  There is provided a series of substituted acyl guanidines of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , R 4 and R 5 as defined herein, their pharmaceutical compositions and methods of use. These 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.

  提供了一系列的取代酰基鸟氨酸化合物（I）或其立体异构体；或其药学上可接受的盐，其中R1、R2、R3、R4和R5如本文所定义，以及它们的药物组合物和使用方法。这些化合物抑制β-分泌酶对淀粉样前体蛋白（APP）的加工，更具体地抑制Aβ-肽的产生。本公开涉及用于治疗与β-淀粉样蛋白产生有关的神经系统疾病，例如阿尔茨海默病和其他受抗淀粉样蛋白活性影响的疾病的化合物。
• US7273882B2
  申请人：——

  公开号：US7273882B2

  公开（公告）日：2007-09-25
• US7612069B2
  申请人：——

  公开号：US7612069B2

  公开（公告）日：2009-11-03
• [EN] ACYL GUANIDINES AS BETA-SECRETASE INHIBITORS<br/>[FR] ACYLGUANIDINES EN TANT QU'INHIBITEUR DE BETA-SECRETASE
  申请人：BRISTOL MYERS SQUIBB CO

  公开号：WO2007002214A2

  公开（公告）日：2007-01-04

  [EN] There is provided a series of substituted acyl guanidines of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R₁, R₂. R₃, R₄ and R₅ as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by Beta-secretase and, more specifically, inhibit the production of ABeta-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to Beta-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
  [FR] L'invention concerne une série de guanidines à substitution acyle représentées par la formule (I) ou un de leurs stéréoisomères ou un de leurs sels acceptables sur le plan pharmaceutique, dans laquelle R₁, R₂. R₃, R₄ et R₅ correspondent à leur définition dans le descriptif, leurs compositions pharmaceutiques et méthodes d'utilisation. Ces composés inhibent l'effet exercé sur la protéine précurseur d'amyloïde (APP) par béta-sécrétase et, de façon plus spécifique, inhibent la production du Abéta-peptide. L'invention concerne des composés utiles pour le traitement de troubles neurologiques relatifs à la production des béta-amyloïdes, tels que la maladie d'Alzheimer ou d'autres états associés à l'activité anti-amyloïde.