Sulfonamides and derivatives thereof that modulate the...

C - Chemistry – Metallurgy – 07 – D

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C07D 413/12 (2006.01) A61K 31/41 (2006.01) A61K 31/42 (2006.01) A61K 31/44 (2006.01) A61K 31/495 (2006.01) A61K 31/70 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01) C07D 409/14 (2006.01) C07D 413/14 (2006.01) C07D 417/12 (2006.01) C07H 15/26 (2006.01)

Patent

CA 2261760

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 the endothelin are also provided.

L'invention concerne des thiényl-, furyl- et pyrrolyl-sulfonamides, des formulations de sels pharmaceutiquement acceptables de ceux-ci et des procédés de modulation ou de modification de peptides de la famille de l'endothéline. Elle porte notamment sur des N-(isoxazolyl)thiénylsulfonamides, des N-(isoxazolyl)furylsulfonamides et des N-(isoxazolyl)pyrrolylsulfonamides, des formulations de ceux-ci et des procédés dans lesquels ces sulfonamides sont utilisés pour l'inhibition de la liaison d'un peptide d'endothéline à un récepteur de l'endothéline par la mise en contact du récepteur avec le sulfonamide. Elle se rapporte encore à des procédés de traitement de troubles dont l'endothéline est à l'origine, qui consistent à administrer des doses efficaces d'un ou plusieurs de ces sulfonamides ou promédicaments de ces derniers, qui inhibent l'activité de l'endothéline.

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