Substituted arylalcanoic acid derivatives as ppar pan...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 209/82 (2006.01) A61K 31/185 (2006.01) A61K 31/335 (2006.01) A61K 31/403 (2006.01) A61K 31/422 (2006.01) A61K 31/426 (2006.01) A61K 31/538 (2006.01) A61K 31/5415 (2006.01) A61K 31/55 (2006.01) A61P 1/18 (2006.01) A61P 3/04 (2006.01) A61P 3/10 (2006.01) C07D 209/86 (2006.01) C07D 213/50 (2006.01) C07D 279/22 (2006.01) C07D 401/12 (2006.01) C07D 471/04 (2006.01)

Patent

CA 2504718

Disclosed is the preparation and pharmaceutical use of substituted arylalcanoic acid derivatives of Formula I, wherein ring A, ring B, Rl, R2, R3, R4, R5, X, Alkl, Alk2, Arl, and Ar2 are as defined in the specification. These compounds, as selective agonists activating peroxisome proliferator- activated receptors (PPAR), in particularly the RXR/PPARalpha, RXR/PPARgamma, and RXRJPPARdelta heterodimers, are useful in the treatment and/or prevention of type 2 diabetes and associated metabolic syndrome such as hypertension, obesity, insulin resistance, hyperlipidemia, hyperglycemia, hypercholesterolemia, atherosclerosis, coronary artery disease, and other cardiovascular disorders with improved side effects profile commonly associated with conventional PPARgamma agonists.

L'invention concerne la préparation et utilisation pharmaceutique de dérivés d'acides arylalcanoïques substitués de formule (I) dans laquelle le cycle A, le cycle B, R?1¿, R?2¿, R?3¿, R?4¿, R?5¿, X, Alk?1¿, Alk?2¿, Ar?1¿ et Ar?2¿ sont tels que définis dans le descriptif. Ces composés, servant d'agonistes sélectifs, activant les récepteurs activés par les proliférateurs de peroxysome (PPAR), plus particulièrement les hétérodimères RXR/PPARalpha, et RXR/PPARgamma et RXRJPPARdelta qui sont utiles dans le traitement et/ou la prévention du diabète de type 2 et du syndrome métabolique associé, à savoir l'hypertension, l'obésité, l'insulino-résistance, l'hyperlipidémie, l'hyperglycémie, l'hypercholestérolémie, l'athérosclérose, les maladies coronariennes et d'autres troubles cardio-vasculaires présentent un profil d'effets secondaires amélioré associé communément aux agonistes habituels PPARgamma.

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