C-21 thioethers as glucocorticoid receptor agonists

Details C-21 thioethers as glucocorticoid receptor agonists C-21 thioethers as glucocorticoid receptor agonists

C - Chemistry, Metallurgy

07

J

C07J 43/00 (2006.01) A61K 31/573 (2006.01) A61K 31/58 (2006.01) A61P 5/44 (2006.01) C07J 31/00 (2006.01) C07J 71/00 (2006.01)

Patent

CA 2710240

The present invention provides compounds of Formula (VII) and 11-keto analogs thereof, and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, and isomers of said compounds and said 11-keto analogs, having the gener-al structure formula (VII) wherein L, R1, R2, R3, R4, and R5 are selected mdependently of each other and as defined herem Also provided are pharmaceutical compositions, methods of preparing, and methods of usmg such compounds m the treatment and pro-phylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions The novel compounds of the present invention possess useful pharmacological activity while having unexpectedly low systemic activiy Thus, the compounds of the invention represent a safer alternative to those known glucocorticoids which have poor side-effect profiles

L'invention concerne des composés de formules (VII) et 11-céto analogues de ceux-ci, et des sels, des solvates, des esters, des promédicaments, des tautomères et des isomères pharmaceutiquement acceptables de ces composés et de ces 11-céto analogues, possédant la formule de structure générale (VII); dans laquelle L, R1, R2, R3, R4 et R5 sont sélectionnés de manière indépendantes les uns des autres et tels que défini dans la formule. Elle concerne également des compositions pharmaceutiques, des procédés de préparation et des procédés d'utilisation de ces composés dans le traitement et la prophylaxie d'une large gamme de troubles et de maladies immunitaires, auto-immunes et inflammatoires. Les nouveaux composés de cette invention ont une activité pharmacologique utile tout en ayant une activité systémique incroyablement faible. Ainsi, les composés de l'invention représentent une alternative plus sûre aux glucocorticoïdes connus possédant des profils d'effets secondaires réduits.

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