Inhibitors of post-proline cleaving proteases

C - Chemistry – Metallurgy – 07 – D

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C07D 417/14 (2006.01) A61K 31/40 (2006.01) A61K 31/426 (2006.01) A61K 31/427 (2006.01) A61K 31/4427 (2006.01) A61K 31/445 (2006.01) A61K 31/4523 (2006.01) A61K 31/4709 (2006.01) A61K 31/53 (2006.01) A61K 31/5375 (2006.01) A61K 31/54 (2006.01) A61K 31/541 (2006.01) A61P 3/10 (2006.01) C07D 207/10 (2006.01) C07D 207/16 (2006.01) C07D 207/335 (2006.01) C07D 211/14 (2006.01) C07D 211/38 (2006.01) C07D 211/62 (2006.01) C07D 213/38 (2006.01) C07D 213/74 (2006.01) C07D 213/82 (2006.01) C07D 215/12 (2006.01) C07D 2

Patent

CA 2464254

Novel compounds that are inhibitors of one or most post-proline cleaving proteases, e.g. dipeptidyl peptidase IV, according to general formula (1). R1 is H or CN, X1 is O, S, CH2, CHF, CF2, CH(CH3), C(CH3)2 or CH(CN), and b is 1 or 2. G1 is H or a group according to the formula -CH2-X2-(CH2)a-G3 and G2 is H or a group according to the formula -CH2-(CH29a-G3, provided that one of G1 and G2 is H and the other is not H. X2 is O, S, or CH2, and a is 0, 1 or 2, provided that when a is 1 then X2 is CH2. G3 is a group according to one of general formulae 2-4., where the variables have meaning given in the description. The compounds are useful in the treatment of i.a. type 2 diabetes and impaired glucose tolerance.

L'invention concerne des nouveaux composés qui sont des inhibiteurs d'une ou de plusieurs protéases de clivage post-proline, par exemple la dipeptidyl peptidase IV, selon la formule générale (1), dans laquelle R?1¿ représente H ou CN, X?1¿ désigne O, S, CH¿2?, CHF, CF¿2?, CH(CH¿3?), C(CH¿3?)¿2? ou CH(CN) et b est égal à 1 ou 2. G?1¿ représente H ou un groupe selon la formule -CH¿2?-X?2¿-(CH¿2?)¿a?-G?3¿ et G?2¿ représente H ou un groupe selon la formule -CH¿2?-(CH¿2?)¿a?-G?3¿, pour autant que un parmi G?1¿ et G?2¿ représente H et que l'autre ne désigne pas H. X?2¿ représente O, S ou CH¿2? et a est égal à 0, 1 ou 2, pour autant que quand a est égal à 1, X¿2? représente CH¿2?. G?3¿ désigne un groupe selon une des formules générales 2-4, les variables ayant les significations expliquées dans la description. Les composés sont utiles dans le traitement, par exemple, des diabètes de type 2 et d'une tolérance altérée au glucose.

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