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

Eckhardt, Matthias; Langkopf, Elke; Mark, Michael; Tadayyon, Moh; Thomas, Leo; Nar, Herbert; Pfrengle, Waldemar; Guth, Brian; Lotz, Ralf; Sieger, Peter; Fuchs, Holger; Himmelsbach, Frank

doi:10.1021/jm701280z.s001

jm701280z_si_001.pdf (363.02 kB)

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

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posted on 2007-12-27, 00:00 authored by Matthias Eckhardt, Elke Langkopf, Michael Mark, Moh Tadayyon, Leo Thomas, Herbert Nar, Waldemar Pfrengle, Brian Guth, Ralf Lotz, Peter Sieger, Holger Fuchs, Frank Himmelsbach

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.

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

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