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

被引：248
|
作者：
Eckhardt, Matthias [1 ]
Langkop, Elke [1 ]
Mark, Michael [2 ]
Tadayyon, Mob [2 ]
Thomas, Leo [2 ]
Nar, Herbert [3 ]
Pfrengle, Waldemar [4 ]
Guth, Brian [5 ]
Lotz, Ralf [5 ]
Sieger, Peter [5 ]
Fuchs, Holger [6 ]
Himmelsbach, Frank [1 ]
机构：
[1] Boehringer Ingelheim Pharm GmbH & Co KG, Dept Chem Res, D-88400 Biberach, Germany
[2] Boehringer Ingelheim Pharm GmbH & Co KG, Dept Metab Dis Res, D-88400 Biberach, Germany
[3] Boehringer Ingelheim Pharm GmbH & Co KG, Dept Lead Discovery, D-88400 Biberach, Germany
[4] Boehringer Ingelheim Pharm GmbH & Co KG, Dept Chem Dev, D-88400 Biberach, Germany
[5] Boehringer Ingelheim Pharm GmbH & Co KG, Dept Drug Discovery Support, D-88400 Biberach, Germany
[6] Boehringer Ingelheim Pharm GmbH & Co KG, Dept Drug Metab & Pharmacokinect, D-88400 Biberach, Germany
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2007年 / 50卷 / 26期
关键词：
D O I：
10.1021/jm701280z
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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.
引用
收藏
页码：6450 / 6453
页数：4
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