2,1-oxazoline and 1,2-pyrazoline-based inhibitors of...

C - Chemistry – Metallurgy – 07 – D

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C07D 261/02 (2006.01) A61K 31/415 (2006.01) A61K 31/42 (2006.01) A61K 45/06 (2006.01) A61P 3/04 (2006.01) A61P 3/06 (2006.01) A61P 3/10 (2006.01) C07D 231/04 (2006.01) C07D 231/06 (2006.01)

Patent

CA 2444465

Dipeptidyl peptidase IV (DP 4) inhibiting compounds are provided having the formula where n is 0 or 1; X is H or CN; Y is N, NH or O; Z is CH2 when Y is O or N-H, with Y-Z forming a single bond, and Z is CH when Y is N, with Y-Z forming a double bond; 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 d'inhibition de la dipeptidyl peptidase IV (DP 4) de formule (1) dans laquelle n est égal à 0 ou 1; X désigne H ou CN; Y représente N, NH ou O; Z désigne CH¿2? quand Y représente O ou N-H, Y-Z formant une liaison simple et Z représente CH quand Y désigne N, Y-Z formant une liaison double; et dans laquelle R?1¿, R?2¿, R?3¿ et R?4¿ sont tels que définis dans la description. L'invention concerne également une méthode de traitement de diabètes et de maladies associées, notamment les diabètes de type II et d'autres maladies telles que définies dans la description, par mise en oeuvre d'un inhibiteur DP 4 ou d'une combinaison d'un tel inhibiteur DP 4 et d'un ou de plusieurs autres agents anti-diabétiques, tels que la metformine, le glyburide, la troglitazone, la pioglitazone, la rosiglitazone et/ou l'insuline et/ou un ou plusieurs agents parmi les agents hypolipidémiques et/ou anti-obésité et/ou d'autres agents thérapeutiques.

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