N-(5-cyclopropyl-2H-pyrazol-3-yl)-2-[2-(3,5-difluoro-phenyl)-acetylamino]-propionamide | 681487-53-6

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: N-(5-cyclopropyl-2H-pyrazol-3-yl)-2-[2-(3,5-difluoro-phenyl)-acetylamino]-propionamide
• 英文别名: (2S)-N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-[[2-(3,5-difluorophenyl)acetyl]amino]propanamide
• CAS: 681487-53-6
• 化学式: C₁₇H₁₈F₂N₄O₂
• 分子量: 348.352
• InChiKey: QICKFMGLBJHRRZ-VIFPVBQESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  25
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  86.9
• 氢给体数：
  3
• 氢受体数：
  5

文献信息

• Acylated amino acid amidyl pyrazoles and related compounds
  申请人：Tung S. Jay

  公开号：US20070197624A1

  公开（公告）日：2007-08-23

  This invention is directed to acylated amino acid amidyl pyrazoles and related compounds of Formula I. The invention is also directed to a pharmaceutical formation comprising such compound or in a pharmaceutically acceptable salt form thereof. The invention is further directed to a method for inhibiting β-amyloid peptide release and/or synthesis, a method for inhibiting γ-secretase activity, and a method for treating neurological disorders associated with β-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.

  本发明涉及公式I中的酰化氨基酸酰胺基吡唑及相关化合物。本发明还涉及包含该化合物或其药学上可接受的盐形式的制药组合物。本发明还涉及一种抑制β-淀粉样肽释放和/或合成的方法，一种抑制γ-分泌酶活性的方法，以及一种治疗与β-淀粉样肽产生相关的神经疾病的方法。该方法包括向宿主施用包含公式I中化合物的有效量的制药配方。公式I中的化合物对预防和治疗阿尔茨海默病有用。
• ACYLATED AMINO ACID AMIDYL PYRAZOLES AND RELATED COMPOUNDS
  申请人：Tung Jay S.

  公开号：US20100280066A1

  公开（公告）日：2010-11-04

  This invention is directed to acylated amino acid amidyl pyrazoles and related compounds of Formula I. The invention is also directed to a pharmaceutical formation comprising such compound or in a pharmaceutically acceptable salt form thereof. The invention is further directed to a method for inhibiting β-amyloid peptide release and/or synthesis, a method for inhibiting γ-secretase activity, and a method for treating neurological disorders associated with β-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.

  本发明涉及式I的酰化氨基酸酰胺基吡唑及其相关化合物。本发明还涉及包括该化合物或其药学上可接受的盐形式的制药组合物。本发明还涉及一种抑制β-淀粉样肽释放和/或合成的方法，一种抑制γ-分泌酶活性的方法，以及一种治疗与β-淀粉样肽产生相关的神经系统疾病的方法。该方法包括向宿主施用包含式I化合物的有效量的制药配方。式I的化合物在预防和治疗阿尔茨海默病方面很有用。
• 3-((N-ACYLATED AMINOACYL)AMINO)PYRAZOLES AS INHIBITORS OF BETA-AMYLOID PEPTIDE PRODUCTION USEFUL FOR THE TREATMENT OF ALZHEIMER'S DISEASE
  申请人：Elan Pharmaceuticals Inc.

  公开号：EP2511267A1

  公开（公告）日：2012-10-17

  This invention is directed to 3-((N-acylated aminoacyl)amino)pyrazoles of Formula (I). The invention is also directed to a pharmaceutical formulation comprising such compound or a pharmaceutically acceptable salt thereof. The invention is further directed to a method for inhibiting beta-amyloid peptide release and/or synthesis, a method for inhibiting gamma-secretase activity, and a method for treating neurological disorders associated with beta-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula (I). The compounds of Formula (I) are useful in the prevention and treatment of Alzheimer's disease.

  本发明涉及式(I)的 3-((N-酰化氨基酰)氨基)吡唑。本发明还涉及一种包含这种化合物或其药学上可接受的盐的药物制剂。本发明进一步涉及一种抑制β-淀粉样肽释放和/或合成的方法，一种抑制γ-分泌酶活性的方法，以及一种治疗与β-淀粉样肽产生相关的神经系统疾病的方法。该方法包括向宿主施用包含有效量式（I）化合物的药物制剂。式（I）化合物可用于预防和治疗阿尔茨海默病。
• EP1633350A4
  申请人：——

  公开号：EP1633350A4

  公开（公告）日：2008-11-26
• US7759382B2
  申请人：——

  公开号：US7759382B2

  公开（公告）日：2010-07-20