Fused bicyclic heterocycles useful as dipeptidyl peptidase-IV inhibitors

摘要

The present invention is directed to novel bicyclic heterocycles of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.;

主权项

1. A compound of structural formula I:or a pharmaceutically acceptable salt thereof; wherein X1 and X2 are independently selected from the group consisting of —N— and —CR5—;
R1 is selected from the group consisting of hydrogen, C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, aryl, heterocycle, aroyl, heteroaroyl and C3-C10cycloalkyl; wherein the C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, aryl, heterocycle, aroyl, heteroaroyl and C3-C10cycloalkyl are unsubstituted or substituted with 1-3 substituents from R5; R2 is selected from the group consisting of C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, benzyl, heterocycle and C1-C6alkylheterocycle; wherein the C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, benzyl, heterocycle and C1-C6alkylheterocycle are unsubstituted or substituted with 1-3 substituents each independently selected from R3, R4 and R5; R3 is selected from the group consisting of hydrogen, C1-C6alkyl and aryl, wherein the C1-C6alkyl and aryl are unsubstituted or substituted with 1-3 substituents selected from R5; R4 is selected from the group consisting of hydrogen and C1-C6alkyl; R5 is selected from the group consisting of hydrogen, halogen, C1-C6alkyl, halogen-substitutedC1-C6alkyl, —OH, C1-C6alkylOH, halogen-substitutedC1-C6alkylOH, —OC1-C6alkyl, —Ohalogen-substitutedC1-C6alkyl, —COOH, —COOC1-C6alkyl, —C1-C6alkylCOOC1-C6alkyl, —C1-C6alkylCOOH, —CN, C1-C6alkylCN, NHC1-C6alkyl, N(C1-C6alkyl)2, C1-C6alkylCONH2, —CONH2, —CONHC1-C6alkyl, —NHCOC1-C6alkyl, —CON(C1-C6alkyl)2, —NHSO2C1-C6alkyl, SO2aryl, —SO2C1-C6alkyl, C1-C6alkylSO2C1-C6alkyl, aryl, —NHCOaryl, and —NHCOheterocycle; and n is 0-4.