N-(benzo-2,1,3-thiadiazol-5-yl)-2-(3-hydroxymethyl-2,4,6-trimethylphenylaminocarbonyl)thiophene-3-sulfonamide | 205516-53-6

• 分子结构分类: 有机化合物 - 有机杂环化合物
• 英文名称: N-(benzo-2,1,3-thiadiazol-5-yl)-2-(3-hydroxymethyl-2,4,6-trimethylphenylaminocarbonyl)thiophene-3-sulfonamide
• 英文别名: 3-(2,1,3-benzothiadiazol-5-ylsulfamoyl)-N-[3-(hydroxymethyl)-2,4,6-trimethylphenyl]thiophene-2-carboxamide
• CAS: 205516-53-6
• 化学式: C₂₁H₂₀N₄O₄S₃
• 分子量: 488.612
• InChiKey: OYNPUCOYMOSIHO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  32
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  186
• 氢给体数：
  3
• 氢受体数：
  9

文献信息

• Sulfonamides and derivatives thereof that modulate the activity of endothelin
  申请人：——

  公开号：US20030208084A1

  公开（公告）日：2003-11-06

  Thienyl-, furyl- and pyrrolyl-sulfonamides, formulations of pharmaceutically-acceptable salts thereof and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides, formulations thereof and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit the activity of endothelin are also provided.

  本文提供了噻吩基、呋喃基和吡咯基磺酰胺、其药学上可接受的盐的配方以及调节或改变内皮素家族肽活性的方法。特别地，提供了N-(异恶唑基)噻吩基磺酰胺、N-(异恶唑基)呋喃基磺酰胺和N-(异恶唑基)吡咯基磺酰胺及其配方，以及使用这些磺酰胺通过与受体接触来抑制内皮素肽与内皮素受体的结合的方法。还提供了通过给予这些磺酰胺或其前药的有效剂量来治疗内皮素介导的疾病的方法，这些磺酰胺或其前药抑制内皮素的活性。
• US6420567B1
  申请人：——

  公开号：US6420567B1

  公开（公告）日：2002-07-16
• US6632829B2
  申请人：——

  公开号：US6632829B2

  公开（公告）日：2003-10-14
• [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.