This is a different class of inhibitors that was identified with HTS. Aromatic heterocyclic-based DPP-4 inhibitors have gained increased attention recently. The first patents describing xanthines (Figure 10) as DPP-4 inhibitors came from Boehringer-Ingelheim(BI) and Novo Nordisk.
When xanthine based DPP-4 inhibitors are compared with sitagliptin and vildagliptin it has shown a superior profile. Xanthines are believed to have higher potency, longer-lasting inhibition and longer-lasting improvement of glucose tolerance.