Eckhardt_2007_J.Med.Chem_50_6450

Reference

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

Related information

Inhibitor Linagliptin
Gene_locus Linagliptin    human-DPP4
Structure Linagliptin    human-DPP4    2RGU

Citations formats

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