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.
Eckhardt M,
Langkopf E,
Mark M,
Tadayyon M,
Thomas L,
Nar H,
Pfrengle W,
Guth B,
Lotz R,
Sieger P,
Fuchs H,
Himmelsbach F.
Boehringer Ingelheim Pharma GmbH & Co. KG, Biberach, Germany. matthias.eckhardt@boehringer-ingelheim.com
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.
PMID: 18052023 [PubMed - indexed for MEDLINE]