| 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_2007_J.Med.Chem_50_6450 |
| 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 |
| Ref : Journal of Medicinal Chemistry , 50 :6450 , 2007 |
|
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. |
| PubMedSearch : Eckhardt_2007_J.Med.Chem_50_6450 |
| PubMedID: 18052023 |
| Gene_locus related to this paper: human-DPP4 |
| Inhibitor | Linagliptin |
| Gene_locus | human-DPP4 |
| Structure | 2RGU |
Eckhardt M, Langkopf E, Mark M, Tadayyon M, Thomas L, Nar H, Pfrengle W, Guth B, Lotz R, Sieger P, Fuchs H, Himmelsbach F (2007)
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
Journal of Medicinal Chemistry
50 :6450
Eckhardt M, Langkopf E, Mark M, Tadayyon M, Thomas L, Nar H, Pfrengle W, Guth B, Lotz R, Sieger P, Fuchs H, Himmelsbach F (2007)
Journal of Medicinal Chemistry
50 :6450