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    Sulfonamides and derivatives thereof that modulate the activity of endothelin
    5.
    发明授权
    Sulfonamides and derivatives thereof that modulate the activity of endothelin 失效
    调节内皮素活性的磺酰胺及其衍生物

    公开(公告)号：US5571821A

    公开(公告)日：1996-11-05

    申请号：US247072

    申请日：1994-05-20

    申请人： Ming Fai Chan ,  Bore G. Raju ,  Adam Kois ,  Erik J. Verner ,  Chengde Wu ,  Rosario S. Castillo ,  Venkatachalapathi Yalamoori ,  Vitukudi N. Balaji ,  Kalyanaraman Ramnarayan

    发明人： Ming Fai Chan ,  Bore G. Raju ,  Adam Kois ,  Erik J. Verner ,  Chengde Wu ,  Rosario S. Castillo ,  Venkatachalapathi Yalamoori ,  Vitukudi N. Balaji ,  Kalyanaraman Ramnarayan

    IPC分类号： C07D261/14 ,  C07D261/16 ,  C07D261/20 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  A61K31/47

    CPC分类号： C07D413/12 ,  C07D261/14 ,  C07D261/16 ,  C07D261/20 ,  C07D413/14 ,  C07D417/12

    摘要： Sulfonamides 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 or increase the activity of endothelin are also provided. The sulfonamides have formula I: ##STR1## in which Ar.sup.1 is a 3- or 5-isoxazolyl and Ar.sup.2 is selected from among alkyl, including straight and branched chains, aromatic rings, fused aromatic rings and heterocyclic rings, including 5-membered heterocycles with one, two or more heteroatoms and fused ring analogs thereof and 6-membered rings with one, two or more heteroatoms and fused ring analogs thereof. Ar.sup.2 is preferably thiophenyl, furyl, pyrrolyl, naphthyl, and phenyl. Compounds in which Ar.sup.1 is a 4-halo-substituted isoxazole are more active than the corresponding alkyl-substituted compound and compounds in which Ar.sup.1 is substituted at this position with a higher alkyl tend to exhibit greater affinity for ET.sub.B receptors than the corresponding lower alkyl-substituted compound.

    摘要翻译： 提供磺酰胺和使用这些磺酰胺通过使受体与磺酰胺接触来抑制内皮素肽与内皮素受体结合的方法。 还提供了通过施用有效量的一种或多种这些抑制或增加内皮素活性的磺酰胺或其前体来治疗内皮素介导的病症的方法。 磺酰胺具有式I：其中Ar 1是3-或5-异恶唑基，Ar 2选自烷基，包括直链和支链，芳环，稠合芳环和杂环，其中包括5- 与一个，两个或更多个杂原子及其稠环类似物和六元环与一个，两个或更多个杂原子和稠合环类似物结合。 Ar 2优选为噻吩基，呋喃基，吡咯基，萘基和苯基。 其中Ar1是4-卤素取代的异恶唑的化合物比相应的烷基取代的化合物更有活性，其中Ar1在该位置被高级烷基取代的化合物倾向于对ETB受体表现出比相应的低级烷基取代的化合物更大的亲和力， 取代的化合物。