Amide compounds and use thereof

Details Amide compounds and use thereof Amide compounds and use thereof

C - Chemistry, Metallurgy

07

D

C07D 213/75 (2006.01) A61K 31/437 (2006.01) A61K 31/4409 (2006.01) A61K 31/4436 (2006.01) A61K 31/4709 (2006.01) A61K 31/55 (2006.01) A61P 9/00 (2006.01) A61P 9/08 (2006.01) A61P 9/10 (2006.01) A61P 9/12 (2006.01) A61P 11/06 (2006.01) A61P 15/06 (2006.01) A61P 15/10 (2006.01) A61P 15/18 (2006.01) A61P 19/00 (2006.01) A61P 19/10 (2006.01) A61P 25/00 (2006.01) A61P 27/02 (2006.01) A61P 27/06 (2006.01) A61P 29/00 (2006.01) A61P 31/00 (2006.01) A61P 35/00 (2006.01) A61P 35/04 (2006.01) A61P 37/06 (2006.01) C07D

Patent

CA 2403321

The present invention relates to an amide compound of the formula (see formula I) wherein R1 is a hydrogen and the like, R2 is a hydrogen and the like, X is SO2 and the like, Y is the formula (III) and the like and a is 2, an isomer thereof or pharmaceutically acceptable salts thereof. The compound of the present invention shows a remarkable and selective Rho kinase inhibitory action, is free of problematic toxicity, shows fine oral absorption and drug kinetics (absorption, distribution, metabolism, excretion and the like of the drug), and shows superior properties (e.g., stability etc.) as a compound. Accordingly, it can be used as a therapeutic drug for various diseases in which Rho kinase is involved.

L'invention concerne des composés d'amide représentés par la formule générale (I), leurs isomères et leurs sels acceptables sur le plan pharmaceutique. Dans cette formule, R<1> représente un atome d'hydrogène, etc., R<2> représente un atome d'hydrogène, etc., X représente SO2, etc., Y représente un groupe représenté par la formule (III), etc., et a prend la valeur de 2. Ces composés présentent un effet inhibiteur de kinase Rho sélectif et remarquable dépourvu de toxicité problématique et ont une excellente absorbabilité orale, de propriétés pharmacocinétiques (absorption de médicaments, distribution, métabolisme, excrétion, etc.) et physiques (stabilité, etc.) tel que les composés per se. Grâce à ces caractéristiques, ces composés sont utiles en tant que remèdes contre diverses maladies auxquelles la kinase Rho participe.

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