3,5-Dihydro-imidazo[4,5-d]pyridazin-4-ones: A class of potent DPP-4 inhibitors

Systematic variations of the xanthine scaffold in close analogs of development compound BI 1356 led to the class of 3,5-dihydro-imidazo[4,5-d]pyridazin-4-ones which provided, after substituent screening, a series of highly potent DPP-4 inhibitors.

Graphical abstractSystematic variations of the xanthine scaffold in BI 1356 leading to the potent DPP-4 inhibitor 12-(R) are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide