4'-(1-carboxy)ethoxy-N-(3-methoxy-5-methylpyrazin-2-yl)2-biphenylsulphonamide | 186651-51-4

• 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'-(1-carboxy)ethoxy-N-(3-methoxy-5-methylpyrazin-2-yl)2-biphenylsulphonamide
• 英文别名: 2-[4-[2-[(3-Methoxy-5-methylpyrazin-2-yl)sulfamoyl]phenyl]phenoxy]propanoic acid
• CAS: 186651-51-4
• 化学式: C₂₁H₂₁N₃O₆S
• 分子量: 443.48
• InChiKey: QTAMLIBDIYBRMZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  31
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  136
• 氢给体数：
  2
• 氢受体数：
  9

反应信息

• 作为产物：
  描述：

  N-(isobutoxycarbonyl)-4'-(1-methoxycarbonyl)ethoxy-N-(3-methoxy-5-methylpyrazin-2-yl)-2-biphenylsulphonamide 在 lithium hydroxide 作用下， 以 四氢呋喃 、 甲醇 、 水 为溶剂， 生成 4'-(1-carboxy)ethoxy-N-(3-methoxy-5-methylpyrazin-2-yl)2-biphenylsulphonamide
  参考文献：
  名称：

  N-heterocyclic sulfonamides having endothelin receptor activity

  摘要：

  这项发明涉及公式I的药用化合物，其中R.sup.1、R.sup.2、R.sup.3、n、m和Het具有本文中定义的任何含义，以及它们的药用盐和含有它们的药物组合物。这些新化合物具有内皮素受体拮抗活性，并且在治疗内皮素水平升高或异常导致重要病因的疾病或医学状况中具有用途。该发明还涉及新化合物的制造过程以及在医疗治疗中使用这些化合物的方法。

  公开号：

  US05668137A1

文献信息

• N-Heterocyclyl biphenyl sulfonamides
  申请人：ZENECA LIMITED

  公开号：EP0749964A1

  公开（公告）日：1996-12-27

  The invention concerns pharmaceutically useful compounds of the formula I, in which R1, R2, R3, n, m and Het have any of the meanings defined herein, and their pharmaceutically-acceptable salts, and pharmaceutical compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful, for example, in the treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role. The invention further concerns processess for the manufacture of the novel compounds and the use of the compounds in medical treatment.

  本发明涉及式 I 的药用化合物（其中 R1、R2、R3、n、m 和 Het 具有本文所定义的任 何含义）及其药学上可接受的盐类，以及含有它们的药物组合物。这些新型化合物具有内皮素受体拮抗剂活性，可用于治疗内皮素水平升高或异常起重要致病作用的疾病或病症。本发明还涉及新型化合物的生产工艺以及这些化合物在医疗中的应用。
• US5668137A
  申请人：——

  公开号：US5668137A

  公开（公告）日：1997-09-16
• [EN] PHARMACEUTICAL AND VETERINARY USES OF ENDOTHELIN ANTAGONISTS<br/>[FR] UTILISATIONS PHARMACEUTIQUES ET VETERINAIRES D'ANTAGONISTES DE L'ENDOTHELINE ET APPLICATIONS ASSOCIEES
  申请人：TEXAS BIOTECHNOLOGY CORP

  公开号：WO2001049289A1

  公开（公告）日：2001-07-12

  Pharmaceutical and veterinary uses of endothelin antagonists are provided. In particular, methods of treatment of laminitis, such as equine and bovine laminitis, by administration of one or more endothelin antagonists are provided. Methods of treatment, prevention, or amelioration of one or more symptoms of menopause; osteoporosis and metabolic bone disorders; climacteric disorders including hot flushes or flashes, abnormal clotting patterns, urogenital discomfort and increased incidence of cardiovascular disease, and other disorders associated with the reduction in ovarian function in women; pre-eclampsia; and control and management of labor during pregnancy by administration of endothelin antagonists are also provided.
• N-heterocyclic sulfonamides having endothelin receptor activity
  申请人：Zeneca Ltd.

  公开号：US05668137A1

  公开（公告）日：1997-09-16

  The invention concerns pharmaceutically useful compounds of the formula I, in which R.sup.1, R.sup.2, R.sup.3, n, m and Het have any of the meanings defined herein, and their pharmaceutically-acceptable salts, and pharmaceutical compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful, for example, in the treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role. The invention further concerns processess for the manufacture of the novel compounds and the use of the compounds in medical treatment.

  这项发明涉及公式I的药用化合物，其中R.sup.1、R.sup.2、R.sup.3、n、m和Het具有本文中定义的任何含义，以及它们的药用盐和含有它们的药物组合物。这些新化合物具有内皮素受体拮抗活性，并且在治疗内皮素水平升高或异常导致重要病因的疾病或医学状况中具有用途。该发明还涉及新化合物的制造过程以及在医疗治疗中使用这些化合物的方法。