Novel dipeptidyl peptidase iv inhibitors, pharmaceutical...

C - Chemistry – Metallurgy – 07 – D

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Details

C07D 403/12 (2006.01) A61K 31/40 (2006.01) A61K 31/41 (2006.01) C07D 207/16 (2006.01)

Patent

CA 2583457

The present invention relates to novel compounds useful as dipeptidyl peptidase IV (DPP-IV) inhibitors of the formula: (I) wherein Y is -S(O)m, -CH2- , CHF, or -CF2; m is 0, 1, or 2; X is a bond, C1-C5 alkyl (e.g., -CH2-), or - C(=0)-; the dotted line [----] in the carbocyclic ring represents an optional double bond; R1 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heterocyclic ring, substituted or unsubstituted heterocyclylalkyl, substituted or unsubstituted heteroarylalkyl, CN, -COOR3, CONR3R4, -OR3, -NR3R4, or NR3COR3; R2 is hydrogen, cyano, COOH, or an isostere of a carboxylic acid (such as SO3H, CONOH, B(OH)2, PO3R3R4, SO2NR3R4, tetrazole, -COOR3, -CONR3R4, NR3COR4, or -COOCOR3).

La présente invention a trait à de nouveaux composés utiles en tant qu'inhibiteurs de la dipeptidyle peptidase IV (DPP-IV) de formule (I), dans laquelle: Y est -S(O)m, -CH2-, CHF, ou -CF2; m est 0, 1, ou 2; X est une liaison, alkyle en C1-C5 (par exemple, -CH2-), ou -C(=O)-; la ligne en pointillé [-----] dans le noyau carbocyclique représente une double liaison éventuelle; R1 est cycloalkyle substitué ou non substitué, cycloalkylalkyle substitué ou non substitué, cycloalkényle substitué ou non substitué, aryle substitué ou non substitué, arylalkyle substitué ou non substitué, hétéroaryle substitué ou non substitué, noyau hétérocyclique substitué ou non substitué, hétérocyclylalkyle substitué ou non substitué, hétéroarylalkyle substitué ou non substitué, CN, -COOR3, CONR3R4, -OR3, -NR3R4, ou NR3COR3; R2 est hydrogène, cyano, COOH, ou un isostère d'un acide carboxylique (tel que SO3H, CONOH, B(OH)2, PO3R3R4, SO2NR3R4, tétrazole, -COOR3, -CONR3R4, NR3COR4, ou -COOCOR3).

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