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

  • J Med Chem. 2007 Dec 27;50(26):6450-3. doi: 10.1021/jm701280z.
Matthias Eckhardt  1 ,  Elke Langkopf ,  Michael Mark ,  Moh Tadayyon ,  Leo Thomas ,  Herbert Nar ,  Waldemar Pfrengle ,  Brian Guth ,  Ralf Lotz ,  Peter Sieger ,  Holger Fuchs ,  Frank Himmelsbach
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PMID: 18052023 DOI: 10.1021/jm701280z
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.

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