Ming Fai Chan - San Diego CA Chengde Wu - Houston TX Bore Gowda Raju - Sugar Land TX Timothy Kogan - Sugar Land TX Erik Joel Verner - Foster City CA Rosario Silvestre Castillo - San Diego CA Venkatachalapathi Yalamoori - San Diego CA Adam Kois - San Diego CA
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.
Benzenesulfonamides And The Use Thereof To Modulate The Activity Of Endothelin
Ming Fai Chan - San Diego CA Bore Gowda Raju - San Diego CA Adam Kois - San Diego CA Erik Joel Verner - San Diego CA Chengde Wu - San Diego CA Rosario Silvestre Castillo - San Diego CA Venkatachalapathi Yalamoori - San Diego CA
Assignee:
Texas Biotechnology Corporation - Houston TX
International Classification:
A61K 3142
US Classification:
514380, 514312, 548246, 546153
Abstract:
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.
N-Heteroaryl Aryl-Substituted Thienyl-Furyl-And Pyrrolyl-Sulfonamides And Derviatives Thereof That Modulate The Activity Of Endothelin
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.
Sulfonamides For Treatment Of Endothelin-Mediated Disorders
Chengde Wu - Houston TX Natalie Blok - Houston TX Timothy Kogan - late of Escondido CA Karin Keller - Houston TX Patricia Woodard - Escondido CA
Assignee:
Texas Biotechnology Corporation - Houston TX
International Classification:
A61K 3142
US Classification:
514380, 548245, 548246, 548247
Abstract:
Thienyl-, furyl- and pyrrolyl-sulfonamides, pharmaceutically-acceptable salts of sulfonamides, formulations of salts and the sulfonamides, and methods for modulating or altering the activity of the endothelin family of peptides using the formulations and sulfonamides are provided. In particular, formulations of sodium salts of N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides 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.
Formulation Of Sulfonamides For Treatment Of Endothelin-Mediated Disorders
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.
Benzenesulfonamides And The Use Thereof To Modulate The Activity Of Endothelin
Ming Fai Chan - Encinitas CA Bore Gowda Raju - Fremont CA Adam Kois - San Diego CA Erik Joel Verner - Foster City CA Chengde Wu - Pearland TX Rosario Silvestre Castillo - San Diego CA Venkatachalapathi Yalamoori - San Diego CA Vitukudi Narayanaiyengar Balaji - Bangalore, IN Kalyanaraman Ramnarayan - San Diego CA
Assignee:
Texas Biotechnology - Houston TX
International Classification:
A61K 3142
US Classification:
514380
Abstract:
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.
Sulfonamides And Derivatives Thereof That Modulate The Activity Of Endothelin
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.
Sulfonamides For Treatment Of Endothelin-Mediated Disorders
Chengde Wu - Houston TX Natalie Blok - Houston TX Timothy Kogan - late of Escondido CA Karin Keller - Austin TX
Assignee:
Texas Biotechnology Corporation - Houston TX
International Classification:
A61K 3142
US Classification:
514378, 548247, 424451, 424464, 424489, 424493
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.