Structure Report for: 2RGU

Eckhardt, M., Langkopf, E., Mark, M., Taddayon, M., Thomas, L., Nar, H., Pfrengle, W., Guth, B., Lotz, R., Sieger, P., Fuchs, H., Himmelsbach, F.

Title: 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylme thyl)-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 and Himmelsbach F <2 more author(s)> Eckhardt M, Langkopf E, Mark M, Tadayyon M, Thomas L, Nar H, Pfrengle W, Guth B, Lotz R, Sieger P, Fuchs H, Himmelsbach F (- 2)
Ref: Journal of Medicinal Chemistry, 50:6450, 2007 : PubMed
Abstract


ESTHER: Eckhardt_2007_J.Med.Chem_50_6450
PubMedSearch: Eckhardt 2007 J.Med.Chem 50 6450
PubMedID: 18052023
Gene_locus related to this paper: human-DPP4
Inhibitor(s) related to this paper: Linagliptin

Abstract

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.