N-(2-aminoethyl)-N methyl-2-naphthalenesulfonamide | 496946-75-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: N-(2-aminoethyl)-N methyl-2-naphthalenesulfonamide
• 英文别名: n-(2-Aminoethyl)-n-methyl-2-naphthalenesulfonamide；N-(2-aminoethyl)-N-methylnaphthalene-2-sulfonamide
• CAS: 496946-75-9
• 化学式: C₁₃H₁₆N₂O₂S
• 分子量: 264.348
• InChiKey: VNRBTVMMABONCU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  18
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  71.8
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  N-(2-aminoethyl)-N methyl-2-naphthalenesulfonamide 、 lithium 3-[4-(N-tert-butoxycarbonylaminomethyl)phenyl]propionate 在 盐酸 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 作用下， 以 乙醚 、 二氯甲烷 为溶剂， 反应 1.0h， 生成 N-[2-[N-[3-[4-(N-tert-butoxycarbonylaminomethyl)phenyl]propanoyl]amino]ethyl]-N-methyl-2-naphthalenesulfonamide
  参考文献：
  名称：

  NOVEL AMINE DERIVATIVE HAVING HUMAN BETA-TRYPTASE INHIBITORY ACTIVITY AND DRUGS CONTAINING THE SAME

  摘要：

  本发明旨在提供一种新型低分子量胺衍生物，该衍生物被很好地吸收，毒性低，并且具有极高选择性的优异人类β-色氨酸蛋白酶抑制活性，其药学上可接受的盐，以及含有该衍生物作为活性成分的药物。本发明的药物可作为一种预防/治疗剂，用于被认为是由β-色氨酸蛋白酶引起的危机和发展的疾病，例如呼吸道疾病、过敏性疾病、炎症性肠病、皮肤过度增生疾病、血管水肿和类风湿性关节炎。

  公开号：

  EP1445250A1

文献信息

• Novel amine derivative having human beta-tryptase inhibitory activity and drugs containing the same
  申请人：Kato Yutaka

  公开号：US20050043304A1

  公开（公告）日：2005-02-24

  It is intended to provide a novel low-molecular weight amine derivative, that is absorbed well, has low toxicity, and has an excellent human β-tryptase inhibitory activity with extremely high selectivity, a pharmaceutically acceptable salt thereof, and a medicine containing the same as an active ingredient. The medicine of the present invention is efficacious as a prophylactic/therapeutic agent for diseases in the crisis and evolution of which are considered to be attributed to β-tryptase, for example, respiratory diseases, allergic diseases, inflammatory bowel diseases, hyperprolliferative skin diseases, vascular edema and rheumatoid arthritis.
• NOVEL AMINE DERIVATIVE HAVING HUMAN BETA-TRYPTASE INHIBITORY ACTIVITY AND DRUGS CONTAINING THE SAME
  申请人：MOCHIDA PHARMACEUTICAL CO., LTD.

  公开号：EP1445250A1

  公开（公告）日：2004-08-11

  It is intended to provide a novel low-molecular weight amine derivative, that is absorbed well, has low toxicity, and has an excellent human β-tryptase inhibitory activity with extremely high selectivity, a pharmaceutically acceptable salt thereof, and a medicine containing the same as an active ingredient. The medicine of the present invention is efficacious as a prophylactic/therapeutic agent for diseases in the crisis and evolution of which are considered to be attributed to β-tryptase, for example, respiratory diseases, allergic diseases, inflammatory bowel diseases, hyperprolliferative skin diseases, vascular edema and rheumatoid arthritis.

  本发明旨在提供一种新型低分子量胺衍生物，该衍生物被很好地吸收，毒性低，并且具有极高选择性的优异人类β-色氨酸蛋白酶抑制活性，其药学上可接受的盐，以及含有该衍生物作为活性成分的药物。本发明的药物可作为一种预防/治疗剂，用于被认为是由β-色氨酸蛋白酶引起的危机和发展的疾病，例如呼吸道疾病、过敏性疾病、炎症性肠病、皮肤过度增生疾病、血管水肿和类风湿性关节炎。