4-amino-5-chloro-N-[5-(hydroxymethyl)pyrrolidin-3-yl]-2-methoxybenzamide

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 4-amino-5-chloro-N-[5-(hydroxymethyl)pyrrolidin-3-yl]-2-methoxybenzamide
• 化学式: C₁₃H₁₈ClN₃O₃
• 分子量: 299.75
• InChiKey: VWLVWKBJYFEAEJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  20
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  96.6
• 氢给体数：
  4
• 氢受体数：
  5

文献信息

• Medicinal composition
  申请人：Kitajima Akihiko

  公开号：US20050239861A1

  公开（公告）日：2005-10-27

  The present invention relates to an ameliorant for improving the movement of the digestive tract comprising, as an active ingredient, 4-amino-5-chloro-2-methoxy-N-[(2S,4S)-2-hydroxymethyl-4-pirrolidinyl]benzamide or an acid addition salt thereof which is a metabolite of 4-amino-5-chloro-2-methoxy-N-[(2S,4S)-1-ethyl-2-hydroxymethyl-4-pyrrolidinyl]benzamide or an acid addition salt thereof, having high biding affinity for a serotonin receptor 4 (5HT 4 ) and causing no arteritis and thrombus formation; a medicinal composition for improving the movement of the digestive tract comprising the said ameliorant and a pharmaceutically acceptable carrier; and a treating method for promoting the movement of the digestive tract, which comprises using the said medicinal composition for improving the movement of the digestive tract.

  本发明涉及一种改善消化道运动的改良剂，包括作为活性成分的4-氨基-5-氯-2-甲氧基-N-[(2S,4S)-2-羟甲基-4-吡咯烷基]苯甲酰胺或其酸加成盐，该化合物是4-氨基-5-氯-2-甲氧基-N-[(2S,4S)-1-乙基-2-羟甲基-4-吡咯烷基]苯甲酰胺或其酸加成盐的代谢物，具有高亲和力结合5-羟色胺受体4（5HT4），不引起动脉炎和血栓形成；一种用于改善消化道运动的药物组合物，包括上述改良剂和药学上可接受的载体；以及一种促进消化道运动的治疗方法，该方法包括使用上述用于改善消化道运动的药物组合物。
• MEDICINAL COMPOSITION
  申请人：Nagase Chemtex Corporation

  公开号：EP1547593A1

  公开（公告）日：2005-06-29

  The present invention relates to an ameliorant for improving the movement of the digestive tract comprising, as an active ingredient, 4-amino-5-chloro-2-methoxy-N-[(2S,4S)-2-hydroxymethyl-4-pirrolidinyl]benzamide or an acid addition salt thereof which is a metabolite of 4-amino-5-chloro-2-methoxy-N-[(2S,4S)-1-ethyl-2-hydroxymethyl-4-pyrrolidinyl]benzamide or an acid addition salt thereof , having high biding affinity for a serotonin receptor 4 (5HT4) and causing no arteritis and thrombus formation; a medicinal composition for improving the movement of the digestive tract comprising the said ameliorant and a pharmaceutically acceptable carrier; and a treating method for promoting the movement of the digestive tract, which comprises using the said medicinal composition for improving the movement of the digestive tract.

  本发明涉及一种改善消化道运动的改良剂，其活性成分包括 4-氨基-5-氯-2-甲氧基-N-[(2S,4S)-2-羟甲基-4-吡咯烷基]苯甲酰胺或其酸加成盐，后者是 4-氨基-5-氯-2-甲氧基-N-[(2S、4-氨基-5-氯-2-甲氧基-N-[(2S, 4S)-1-乙基-2-羟甲基-4-吡咯烷基]苯甲酰胺或其酸加成盐，对5-羟色胺受体4 (5HT4)有很高的结合亲和力，不会引起动脉炎和血栓形成；一种用于改善消化道运动的药物组合物，包括上述改善剂和药学上可接受的载体；以及一种促进消化道运动的治疗方法，其中包括使用上述用于改善消化道运动的药物组合物。
• US7485665B2
  申请人：——

  公开号：US7485665B2

  公开（公告）日：2009-02-03