(2S)-1-[(2S)-2-[(2-aminoacetyl)amino]-3-phenylpropanoyl]pyrrolidine-2-carboxamide

• 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: (2S)-1-[(2S)-2-[(2-aminoacetyl)amino]-3-phenylpropanoyl]pyrrolidine-2-carboxamide
• 化学式: C₁₆H₂₂N₄O₃
• 分子量: 318.37
• InChiKey: KREXGEDWNVJURM-STQMWFEESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.4
• 重原子数：
  23
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  119
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• Tripeptides and tripeptide derivatives for the treatment of postlesional diseases of the nervous system
  申请人：Rapin Jean

  公开号：US20050080016A1

  公开（公告）日：2005-04-14

  The invention relates to the use of specific tripeptides for the treatment of postlesional diseases of ischemic, traumatic or toxic origin. The tripeptide derivatives satisfy the following formula (I): (see formula I as in paper form) wherein X represents OH, (C 1-5 ) alkoxy, NH 2 , NH—C 1-5 -alkyl, N(C 1-5 alkyl) 2 ; R 1 is a residue derived from one of the amino acids Phe, Tyr, Trp, Pro, which each may be optionally substituted with one or more (C 1-5 ) alkoxy groups, (C 1-5 ) alkyl groups or halogen atoms, as well as Ala, Val, Leu or Ile; R 2 is a residue derived from one of the amino acids Gly, Ala, Ile, Val, Ser, Thr, and Pro; Y 1 and Y 2 independently from each other represent H or (C 1-5 ) alkyl; R 3 and R 4 independently from each other represent H, OH, (C 1-5 ) alkyl or (C 1-5 ) alkoxy, provided that R 3 and R 4 are not both OH or (C 1-5 ) alkoxy; and R 5 represents H, OH, (C 1-5 ) alkyl or (C 1-5 ) alkoxy; or a pharmaceutically acceptable salt thereof.

  本发明涉及使用特定三肽治疗缺血性、创伤性或毒性后损伤性疾病。该三肽衍生物满足以下式子（I）：（见论文中的式子I） 其中，X代表OH、（C1-5）烷氧基、NH2、NH-C1-5-烷基、N（C1-5烷基）2；R1是来自苯丙氨酸、酪氨酸、色氨酸、脯氨酸中的一种氨基酸残基，每个氨基酸残基都可以选择性地用一个或多个（C1-5）烷氧基、（C1-5）烷基或卤原子取代，以及丙氨酸、缬氨酸、亮氨酸或异亮氨酸；R2是来自甘氨酸、丙氨酸、异亮氨酸、缬氨酸、丝氨酸、苏氨酸和脯氨酸中的一种氨基酸残基；Y1和Y2分别表示H或（C1-5）烷基；R3和R4分别表示H、OH、（C1-5）烷基或（C1-5）烷氧基，前提是R3和R4不同时为OH或（C1-5）烷氧基；R5表示H、OH、（C1-5）烷基或（C1-5）烷氧基；或其药学上可接受的盐。
• Tripeptides and tripeptide derivatives for the treatment of neurodegenerative diseases
  申请人：Rapin Jean

  公开号：US20050101538A1

  公开（公告）日：2005-05-12

  The invention relates to the use of specific tripeptides for the treatment of neurodegenerative diseases, and to pharmaceutical compositions comprising the tripeptides. The tripeptide derivatives satisfy the following formula (I): wherein X represents OH, (C 1-5 ) alkoxy, NH 2 , NH—C 1-5 -alkyl, N(C 1-5 alkyl) 2 ; R 1 is a residue derived from one of the amino acids Phe, Tyr, Trp, Pro, which each may be optionally substituted with one or more (C 1-5 )alkoxy groups, (C 1-5 )alkyl groups or halogen atoms, as well as Ala, Val, Leu or Ile; R 2 is a residue derived from one of the amino acids Gly, Ala, Ile, Val, Ser, Thr, Leu and Pro; Y 1 and Y 2 independently from each other represent H or (C 1-5 )alkyl; R 3 and R 4 independently from each other represent H, OH, (C 1-5 )alkyl or (C 1-5 )alkoxy, provided that R 3 and R 4 are not both OH or (C 1-5 )alkoxy; and R 5 represents H, OH, (C 1-5 )alkyl or (C 1-5 )alkoxy; or a pharmaceutically acceptable salt thereof.

  本发明涉及使用特定三肽治疗神经退行性疾病，以及包含该三肽的药物组合物。该三肽衍生物满足以下公式（I）：其中X代表OH，（C1-5）烷氧基，NH2，NH-（C1-5）烷基，N（C1-5烷基）2；R1是从苯丙氨酸，酪氨酸，色氨酸，脯氨酸中的一个衍生的残基，每个残基可选择地用一个或多个（C1-5）烷氧基，（C1-5）烷基或卤素原子取代，以及丙氨酸，缬氨酸，亮氨酸或异亮氨酸；R2是从甘氨酸，丙氨酸，异亮氨酸，缬氨酸，丝氨酸，苏氨酸，亮氨酸和脯氨酸中的一个衍生的残基；Y1和Y2各自独立地表示H或（C1-5）烷基；R3和R4各自独立地表示H，OH，（C1-5）烷基或（C1-5）烷氧基，前提是R3和R4不是OH或（C1-5）烷氧基；R5表示H，OH，（C1-5）烷基或（C1-5）烷氧基；或其药学上可接受的盐。
• TRIPEPTIDES AND TRIPEPTIDE DERIVATIVES FOR THE TREATMENT OF POSTLESIONAL DISEASES OF THE NERVOUS SYSTEM
  申请人：Neurotell AG

  公开号：EP1363656A2

  公开（公告）日：2003-11-26
• TRIPEPTIDES AND TRIPEPTIDE DERIVATIVES FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
  申请人：Neurotell AG

  公开号：EP1359934B1

  公开（公告）日：2006-11-08
• US7122524B2
  申请人：——

  公开号：US7122524B2

  公开（公告）日：2006-10-17