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    Benzenesulfonamides and the use thereof to modulate the activity of endothelin
    1.
    发明授权
    Benzenesulfonamides and the use thereof to modulate the activity of endothelin 失效
    苯磺酰胺及其用途来调节内皮素的活性

    公开(公告)号：US06376523B1

    公开(公告)日：2002-04-23

    申请号：US09439802

    申请日：1999-11-12

    申请人： Ming Fai Chan ,  Bore Gowda Raju ,  Adam Kois ,  Erik Joel Verner ,  Chengde Wu ,  Rosario Silvestre Castillo ,  Venkatachalapathi Yalamoori ,  Vitukudi Narayanaiyengar Balaji

    发明人： Ming Fai Chan ,  Bore Gowda Raju ,  Adam Kois ,  Erik Joel Verner ,  Chengde Wu ,  Rosario Silvestre Castillo ,  Venkatachalapathi Yalamoori ,  Vitukudi Narayanaiyengar Balaji

    IPC分类号： A61K3142

    CPC分类号： A61K31/42 ,  A61K31/47 ,  C07D261/16

    摘要： N-(5-isoxazolyl)benzenesulfonamides and N-(3-isoxazolyl)benzenesulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(5-isoxazolyl)biphenylsulfonamides and N-(3-isoxazolyl)biphenylsulfonamides and methods for inhibiting the binding of an endothelin peptide to an endothelin receptor or increasing the activity of endothelin peptides by contacting the receptor with a sulfonamide are provided. N-isoxzolyl-4-biphenylsulfonamides are particularly preferred. These compounds exhibit activity as endothelin receptor B antagonists. Methods for treating endothelin-mediated disorders, particularly inflammatory diseases, such as asthma, 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.

    摘要翻译： 提供N-（5-异恶唑基）苯磺酰胺和N-（3-异恶唑基）苯磺酰胺以及调节或改变肽内皮素家族活性的方法。 特别地，提供N-（5-异恶唑基）联苯磺酰胺和N-（3-异恶唑基）联苯磺酰胺以及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或增加内皮素肽活性的方法 。 N-异恶唑基-4-联苯磺酰胺是特别优选的。 这些化合物表现出作为内皮素受体B拮抗剂的活性。 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药来治疗内皮素介导的疾病，特别是炎性疾病如哮喘的方法。

    Benzenesulfonamides and the use thereof to modulate the activity of endothelin
    7.
    发明授权
    Benzenesulfonamides and the use thereof to modulate the activity of endothelin 失效
    苯磺酰胺及其用途来调节内皮素的活性

    公开(公告)号：US6030991A

    公开(公告)日：2000-02-29

    申请号：US730633

    申请日：1996-12-06

    申请人： Ming Fai Chan ,  Bore Gowda Raju ,  Adam Kois ,  Erik Joel Verner ,  Chengde Wu ,  Rosario Silvestre Castillo ,  Venkatachalapathi Yalamoori ,  Vitukudi Narayanaiyengar Balaji

    发明人： Ming Fai Chan ,  Bore Gowda Raju ,  Adam Kois ,  Erik Joel Verner ,  Chengde Wu ,  Rosario Silvestre Castillo ,  Venkatachalapathi Yalamoori ,  Vitukudi Narayanaiyengar Balaji

    IPC分类号： A61K31/42 ,  C07D261/10

    CPC分类号： A61K31/42 ,  C07D261/10

    摘要： N-(5-isoxazolyl)benzenesulfonamides and N-(3-isoxazolyl) benzene-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(5-isoxazolyl)-biphenylsulfonamides and N-(3-isoxazolyl)biphenylsulfonamides and methods for inhibiting the binding of an endothelin peptide to an endothelin receptor or increasing the activity of endothelin peptides by contacting the receptor with a sulfonamide are provided. N-isoxzolyl-4-biphenylsulfonamides are particularly preferred. These compounds exhibit activity as endothelin receptor B antagonists. Methods for treating endothelin-mediated disorders, particularly inflammatory diseases, such as asthma, 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.

    摘要翻译： 提供N-（5-异恶唑基）苯磺酰胺和N-（3-异恶唑基）苯磺酰胺以及调节或改变肽内皮素家族活性的方法。 特别地，N-（5-异恶唑基） - 联苯磺酰胺和N-（3-异恶唑基）联苯磺酰胺和通过使受体与磺酰胺接触来抑制内皮素肽与内皮素受体的结合或增加内皮素肽的活性的方法是 提供。 N-异恶唑基-4-联苯磺酰胺是特别优选的。 这些化合物表现出作为内皮素受体B拮抗剂的活性。 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药来治疗内皮素介导的疾病，特别是炎性疾病如哮喘的方法。

    Sulfonamides and derivatives thereof that modulate the activity of endothelin
    9.
    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。

    N-heteroaryl aryl-substituted thienyl-furyl-and pyrrolyl-sulfonamides and derviatives thereof that modulate the activity of endothelin
    10.
    发明授权
    N-heteroaryl aryl-substituted thienyl-furyl-and pyrrolyl-sulfonamides and derviatives thereof that modulate the activity of endothelin 失效
    N-杂芳基芳基取代的噻吩基 - 呋喃基和吡咯基磺酰胺及其衍生物，其调节内皮素的活性

    公开(公告)号：US06420567B1

    公开(公告)日：2002-07-16

    申请号：US08938325

    申请日：1997-09-26

    申请人： Chengde Wu ,  Bore Gowda Raju ,  Timothy Kogan ,  Natalie Blok

    发明人： Chengde Wu ,  Bore Gowda Raju ,  Timothy Kogan ,  Natalie Blok

    IPC分类号： C07D26104

    CPC分类号： C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

    摘要： 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.

    摘要翻译： 提供噻吩基，呋喃基和吡咯基磺酰胺，其药学上可接受的盐的制剂和调节或改变肽内皮素家族的活性的方法。 特别地，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）吡咯烷磺酰胺，其制剂和使用这些磺酰胺用于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 被提供。 还提供了通过施用有效量的一种或多种这些抑制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。