Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl...

C - Chemistry – Metallurgy – 07 – D

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C07D 209/52 (2006.01) A61K 31/403 (2006.01) A61P 3/04 (2006.01) A61P 3/06 (2006.01) A61P 3/10 (2006.01)

Patent

CA 2402894

Dipeptidyl peptidase IV (DP 4) inhibiting compounds are provided having the formula (I) where x is 0 or 1 and y is 0 or 1 (provided that x = 1 when y = 0 and x = 0 when y = 1); n is 0 or 1; X is H or CN; and wherein R1, R2, R3 and R4 are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, and other diseases as set out herein, employing such DP 4 inhibitor or a combination of such DP 4 inhibitor and one or more of another antidiabetic agent such as metformin, glyburide, troglitazone, pioglitazone, rosiglitazone and/or insulin and/or one or more of a hypolipidemic agent and/or anti-obesity agent and/or other therapeutic agent.

L'invention concerne des composés inhibant la dipeptidyl peptidase IV (DP4), de formule (I) dans laquelle x vaut 0 ou 1 et y vaut 0 ou 1 (à condition que x=1 lorsque y=0 et que x=0 lorsque y=1) ; n vaut 0 ou 1 ; X représente H ou CN ; R?1¿, R?2¿, R?3¿ et R?4¿ sont tels que décrits. L'invention porte également sur un procédé de traitement des diabètes et de maladies associées, notamment du diabète du type II et d'autres maladies définies dans le dossier, au moyen dudit inhibiteur de DP4 ainsi que d'un ou plusieurs autres agents antidiabétiques, tels que metformine, glyburide, troglitazone, pioglitazone, rosiglitazone et/ou l'insuline et/ou un agent hypolipidémique et/ou un agent anti-obésité et/ou un autre agent thérapeutique.

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