jm701280z_si_001.pdf (363.02 kB)
8-(3-(R)-Aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a Highly Potent, Selective, Long-Acting, and Orally Bioavailable DPP-4 Inhibitor for the Treatment of Type 2 Diabetes
journal contributionposted on 2007-12-27, 00:00 authored by Matthias Eckhardt, Elke Langkopf, Michael Mark, Moh Tadayyon, Leo Thomas, Herbert Nar, Waldemar Pfrengle, Brian Guth, Ralf Lotz, Peter Sieger, Holger Fuchs, Frank Himmelsbach
A new chemical class of potent DPP-4 inhibitors structurally derived from the xanthine scaffold for the treatment of type 2 diabetes has been discovered and evaluated. Systematic structural variations have led to 1 (BI 1356), a highly potent, selective, long-acting, and orally active DPP-4 inhibitor that shows considerable blood glucose lowering in different animal species. 1 is currently undergoing clinical phase IIb trials and holds the potential for once-daily treatment of type 2 diabetics.