(2R)-2-[3-chloro-4-(2,5-dihydropyrrol-1-yl)phenyl]propanamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯啉
• 英文名称: (2R)-2-[3-chloro-4-(2,5-dihydropyrrol-1-yl)phenyl]propanamide
• 化学式: C₁₃H₁₅ClN₂O
• 分子量: 250.72
• InChiKey: FVBGLQFOTOEXTJ-SECBINFHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  46.3
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• Amide of r-2-(aminoaryl)-propionic acid for use in theprevention of leucocyte activation
  申请人：——

  公开号：US20040186146A1

  公开（公告）日：2004-09-23

  N-(2-aminoaryl-propionyl)-amides of formula (1) are described. 1 The process for their preparation and pharmaceutical preparations thereof are also described. The amides of the invention are useful in the prevention and treatment of tissue damage due to the exacerbate recruitment of polymorphonuclear neutrophils (leukocytes PMN) at the inflammatory sites. In particular, the invention relates to the R enantiomers of 2-(aminoaryl)-propionyl amides of formula (1) for use in the ihibition of the chemotaxis of neutrophils induced by IL-8. The compounds of the invention are used in the treatment of psoriasis, ulcerative cholitis, glomerular nephritis, acute respiratory insufficiency, idiopathic fibrosis, and rheumatoid arthritis.

  描述了式（1）的N-(2-氨基芳基丙酰基)-酰胺。还描述了它们的制备过程和制药制剂。本发明的酰胺在预防和治疗由于炎症部位过度招募多形核中性粒细胞（白细胞PMN）引起的组织损伤方面是有用的。特别地，本发明涉及式（1）的2-(氨基芳基)-丙酰基酰胺的R对映体，用于抑制IL-8诱导的中性粒细胞趋化。本发明的化合物用于治疗牛皮癣、溃疡性结肠炎、肾小球肾炎、急性呼吸功能不全、特发性纤维化和类风湿性关节炎。
• AMIDES OF R-2-(AMINOARYL)-PROPIONIC ACIDS FOR USE IN THEPREVENTION OF LEUCOCYTE ACTIVATION"
  申请人：Dompé S.P.A.

  公开号：EP1276732A1

  公开（公告）日：2003-01-22
• US7217707B2
  申请人：——

  公开号：US7217707B2

  公开（公告）日：2007-05-15
• [EN] "AMIDES OF R-2-(AMINOARYL)-PROPIONIC ACIDS FOR USE IN THEPREVENTION OF LEUCOCYTE ACTIVATION"<br/>[FR] AMIDES D'ACIDES R-2-(AMINOARYL)-PROTONIQUES PREVENANT L'ACTIVATION DES LEUCOCYTES
  申请人：DOMPE SPA

  公开号：WO2001079189A2

  公开（公告）日：2001-10-25

  N-(2-aminoaryl-propionyl)-amides of formula (1) are described. The process for their preparation and pharmaceutical preparations thereof are also described. The amides of the invention are useful in the prevention and treatment of tissue damage due to the exacerbate recruitment of polymorphonuclear neutrophils (leukocytes PMN) at the inflammatory sites. In particular, the invention relates to the R enantiomers of 2-(aminoaryl)-propionyl amides of formula (1) for use in the inhibition of the chemotaxis of neutrophils induced by IL-8. The compounds of the invention are used in the treatment of psoriasis, ulcerative cholitis, glomerular nephritis, acute respiratory insufficiency, idiopathic fibrosis, and rheumatoid arthritis.