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13 条记录 (耗时 0.039 秒)

    Benzenesulfonamides and the use thereof to modulate the activity of endothelin
    5.
    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。

    Phosphoramidates, phosphinic amides and related compounds and the use thereof to modulate the activity of endothelin
    8.
    发明授权
    Phosphoramidates, phosphinic amides and related compounds and the use thereof to modulate the activity of endothelin 失效
    磷酰胺化物，次膦酰胺和相关化合物及其用于调节内皮素活性的用途

    公开(公告)号：US06384261B1

    公开(公告)日：2002-05-07

    申请号：US09146679

    申请日：1998-09-03

    申请人： Ming Fai Chan ,  Erik Joel Verner

    发明人： Ming Fai Chan ,  Erik Joel Verner

    IPC分类号： C07C6934

    CPC分类号： C07F9/247 ,  C07F9/650905 ,  C07F9/6512 ,  C07F9/653

    摘要： Phosphoramidates and phosphinic amides and related compounds are provided. Also provided are methods that use the compounds for modulating the activity of the endothelin family of peptides are provided. In particular, compounds having formula: in which A, B, R1 and R2 are as described are provided. Also provided are methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these compounds or prodrugs thereof. Methods for elucidating the physiological and pathophysiological roles of endothelin, as well as isolating endothelin receptors are also provided.

    摘要翻译： 提供了磷酰胺化物和次膦酰胺和相关化合物。 还提供了使用化合物调节肽的内皮素家族的活性的方法。 特别地，提供了具有下式的化合物：其中A，B，R 1和R 2如上所述。 还提供了通过施用有效量的一种或多种这些化合物或其前药来治疗内皮素介导的病症的方法。 还提供了阐明内皮素的生理和病理生理学作用以及分离内皮素受体的方法。

    Thieno-pyridine sulfonamides derivatives thereof and related compounds that modulate the activity of endothelin
    10.
    发明授权
    Thieno-pyridine sulfonamides derivatives thereof and related compounds that modulate the activity of endothelin 失效
    噻吩并吡啶磺酰胺衍生物和调节内皮素活性的相关化合物

    公开(公告)号：US5804585A

    公开(公告)日：1998-09-08

    申请号：US632586

    申请日：1996-04-15

    申请人： Erik Joel Verner

    发明人： Erik Joel Verner

    IPC分类号： A01N43/42 ,  A61K31/381 ,  A61K31/407 ,  A61K31/4365 ,  A61K31/4741 ,  A61K31/4743 ,  A61K31/4745 ,  C07D471/04 ,  C07D491/04 ,  C07D495/04 ,  A61K31/435

    CPC分类号： C07D471/04 ,  A61K31/381 ,  A61K31/407 ,  A61K31/4741 ,  A61K31/4743 ,  A61K31/4745 ,  C07D491/04 ,  C07D495/04

    摘要： Methods, compositions, and compounds for modulating the activity of an endothelin peptide are provided. The methods use compositions that contain compounds that include those of the formula: ##STR1## where X is selected from groups that include O, S, and NH; Y is selected from O.sup.+ and N, and R.sup.1 and R.sup.2 are each selected independently from among alkyl, lower alkenyl, lower alkynyl, lower haloalkyl, halide, pseudohalide or H, except that R.sup.2 is not halide. R.sup.3, R.sup.4 and R.sup.5 are selected from among groups that include hydrogen, halide, alkoxy, alkyl, haloalkyl; and R.sup.7 is selected from groups that include (CH.sub.2).sub.r R.sup.18, in which r is 0 to 6 and R.sup.18 is selected from groups that include aryl, particularly pyrmidinyl and phenyl. The methods are effected by contacting endothelin receptors with one or more of the compounds or with compositions containing one or more of the compounds prior to, simultaneously with, or subsequent to contacting the receptors with an endothelin peptide.

    摘要翻译： 提供了调节内皮素肽活性的方法，组合物和化合物。 该方法使用包含下列化合物的组合物：包括O，S和NH的化合物： Y选自O +和N，并且R 1和R 2各自独立地选自烷基，低级烯基，低级炔基，低级卤代烷基，卤化物，拟卤化物或H，除了R 2不是卤素。 R 3，R 4和R 5选自包括氢，卤素，烷氧基，烷基，卤代烷基的基团; 并且R 7选自包括（CH 2）r R 18的基团，其中r为0至6，R 18选自包括芳基，特别是嘧啶基和苯基的基团。 所述方法通过使内皮素受体与一种或多种化合物或含有一种或多种化合物的组合物在使受体与内皮素肽接触之前，同时或之后接触来实现。