公开(公告)号：US06248767B1

公开(公告)日：2001-06-19

申请号：US08938444

申请日：1997-09-26

Applicant: Natalie Blok ,  Chengde Wu ,  Patricia Woodard ,  Karin Keller ,  Timothy Kogan

Inventor： Natalie Blok ,  Chengde Wu ,  Patricia Woodard ,  Karin Keller ,  Timothy Kogan

IPC: A61K3142

CPC classification number: C07D413/14 ,  C07D261/16 ,  C07D409/12 ,  C07D413/12 ,  C07D417/14

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

Abstract translation: 提供噻吩基，呋喃基和吡咯基磺酰胺的药学上可接受的盐的制剂以及使用制剂调节或改变肽的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）吡咯烷磺酰胺的钠盐的制剂和使用这些磺酰胺盐通过使受体接触来抑制内皮素肽与内皮素受体结合的方法 与磺酰胺盐。 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盐或其前体来治疗内皮素介导的病症的方法。

公开(公告)号：US06683103B2

公开(公告)日：2004-01-27

申请号：US10029561

申请日：2001-12-20

Applicant: Chengde Wu ,  Natalie Blok ,  Timothy Kogan ,  Karin Keller

Inventor： Chengde Wu ,  Natalie Blok ,  Timothy Kogan ,  Karin Keller

IPC: A61K3142

CPC classification number: C07D413/14 ,  C07D261/16 ,  C07D409/12 ,  C07D413/12 ,  C07D417/14

Abstract: Thienylsulfonamides and their pharmaceutically acceptable derivatives, pharmaceutical compositions, articles of manufacture, combinations, lyophilized powders and methods for the treatment of endothelin diseases using these formulations and sulfonamides are provided. A process of preparing an alkali metal salt of a hydrophobic sulfonamide is provided. The process includes the step of dissolving a free sulfonamide in an organic solvent in the presence of a saturated alkali metal salt solution and recovering the formed sulfonamide salt from the organic phase.

Abstract translation: 提供噻吩磺酰胺及其药学上可接受的衍生物，药物组合物，制品，组合，冻干粉末以及使用这些制剂和磺酰胺治疗内皮素疾病的方法。 提供了制备疏水性磺酰胺的碱金属盐的方法。 该方法包括在饱和碱金属盐溶液存在下将游离磺酰胺溶解在有机溶剂中并从有机相中回收所形成的磺酰胺盐的步骤。

公开(公告)号：US06613804B2

公开(公告)日：2003-09-02

申请号：US10006256

申请日：2001-12-04

Applicant: Ming Fai Chan ,  Timothy Kogan ,  Erik Joel Verner ,  Adam Kois ,  Vitukudi Narayanaiyengar Balaji

Inventor： Ming Fai Chan ,  Timothy Kogan ,  Erik Joel Verner ,  Adam Kois ,  Vitukudi Narayanaiyengar Balaji

IPC: A61K3118

CPC classification number: C07D413/14 ,  C07D261/14 ,  C07D261/16 ,  C07D413/12

Abstract: Biphenylsulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, bicyclic or tricyclic carbon or heterocyclic ring biphenylsulfonamides 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.

公开(公告)号：US06458805B2

公开(公告)日：2002-10-01

申请号：US09792237

申请日：2001-02-23

Applicant: Natalie Blok ,  Chengde Wu ,  Patricia Woodard ,  Karin Keller ,  Timothy Kogan

Inventor： Natalie Blok ,  Chengde Wu ,  Patricia Woodard ,  Karin Keller ,  Timothy Kogan

IPC: A61K3147

CPC classification number: C07D413/14 ,  C07D261/16 ,  C07D409/12 ,  C07D413/12 ,  C07D417/14

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

Abstract translation: 提供噻吩基，呋喃基和吡咯基磺酰胺的药学上可接受的盐的制剂以及使用制剂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） - 吡咯烷磺酰胺的钠盐的制剂和使用这些磺酰胺盐的方法，用于通过接触来抑制内皮素肽与内皮素受体的结合 提供了具有磺酰胺盐的受体。 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盐或其前体来治疗内皮素介导的病症的方法。

公开(公告)号：US06342610B2

公开(公告)日：2002-01-29

申请号：US08913331

申请日：1997-11-07

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

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

IPC: C07D20736

CPC classification number: C07D413/12 ,  C07D261/14 ,  C07D261/16 ,  C07D261/20 ,  C07D413/14 ,  C07D417/12

Abstract: Thienyl-, furyl- and pyrrolyl-sulfonamides 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 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.

Abstract translation: 提供噻吩基，呋喃基和吡咯基磺酰胺以及调节或改变肽内皮素家族的活性的方法。 特别地，提供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，以及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。 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。