The present invention relates to novel 2-aryl and 4-aryl substituted pyridines, which are highly selective and potent inhibitors of the dipeptidyl peptidase IV enzyme, and which are useful in the treatment and prevention of multiple diseases and disorders mediated by dipeptidyl peptidase IV, such as diabetes, particularly type II diabetes. The invention also relates to procedures for synthesis of such compounds and pharmaceutical compositions thereof. In view of the rapid increase of diabetes there is a considerable demand for the development of new agents in this field. There is particularly a need for agents with superior efficacy, high selectivity, long duration of action, better bioavailability, and physiological compatibility, which supplement the conventional therapies. The provided compounds are usable as really effective agents, exhibiting precious pharmacological properties as well as an excellent safety profile, for treatment and prophylaxis of diseases mediated by dipeptidyl peptidase IV, such as diabetes, particularly type II diabetes and related diseases.
