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

页码：6450 / 6453

页数：4

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