3{[(4-chloro-3-methyl-5-isoxazolyl)amino]sulfonyl}-N-methoxymethyl-2-thiophenecarboxylic acid methoxymethyl ester | 349453-52-7

• 分子结构分类: 有机化合物 - 有机杂环化合物
• 英文名称: 3{[(4-chloro-3-methyl-5-isoxazolyl)amino]sulfonyl}-N-methoxymethyl-2-thiophenecarboxylic acid methoxymethyl ester
• 英文别名: Methoxymethyl 3-[(4-chloro-3-methyl-1,2-oxazol-5-yl)-(methoxymethyl)sulfamoyl]thiophene-2-carboxylate
• CAS: 349453-52-7
• 化学式: C₁₃H₁₅ClN₂O₇S₂
• 分子量: 410.856
• InChiKey: LPBIOHLGLWNOPV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  25
• 可旋转键数：
  9
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  145
• 氢给体数：
  0
• 氢受体数：
  10

文献信息

• Sulfonamides and derivatives thereof that modulate the activity of endothelin
  申请人：Texas Biotechnology Corporation

  公开号：US20010056183A1

  公开（公告）日：2001-12-27

  Thienyl-, furyl-, pyrrolyl- and phenylsulfonamides, formulations of pharmaceutically-acceptable derivatives 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, N-(isoxazolyl)pyrrolylsulfonamides and N-(isoxazolyl)phenylsulfonamides, 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 pharmaceutically acceptable derivatives thereof that inhibit the activity of endothelin are also provided.

  提供了噻吩基、呋喃基、吡咯基和苯基磺酰胺，以及其药学上可接受的衍生物的配方和调节或改变内皮素家族肽活性的方法。具体而言，提供了N-(异噁唑基)噻吩基磺酰胺、N-(异噁唑基)呋喃基磺酰胺、N-(异噁唑基)吡咯基磺酰胺和N-(异噁唑基)苯基磺酰胺，以及这些磺酰胺的配方和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药学上可接受的抑制内皮素活性的衍生物的有效量来治疗内皮素介导的疾病的方法。
• SULFONAMIDES AND DERIVATIVES THEREOF THAT MODULATE THE ACTIVITY OF ENDOTHELIN
  申请人：ENCYSIVE PHARMACEUTICALS INC.

  公开号：EP1244657B1

  公开（公告）日：2004-12-29
• US6686382B2
  申请人：——

  公开号：US6686382B2

  公开（公告）日：2004-02-03
• [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.
• [EN] SULFONAMIDES AND DERIVATIVES THEREOF THAT MODULATE THE ACTIVITY OF ENDOTHELIN<br/>[FR] SULFONAMIDES ET LEURS DERIVES MODULANT L'ACTIVITE DE L'ENDOTHELINE
  申请人：TEXAS BIOTECHNOLOGY CORP

  公开号：WO2001049685A2

  公开（公告）日：2001-07-12

  Thienyl-, furyl-, pyrrolyl- and phenylsulfonamides, formulations of pharmaceutically-acceptable derivatives 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, N-(isoxazolyl)pyrrolylsulfonamides and N-(isoxazoly)phenylsulfonamides, 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 pharmaceutically acceptable derivatives thereof that inhibit the activity of endothelin are also provided.