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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 M, Langkopf E, Mark M, Tadayyon M, Thomas L, Nar H, Pfrengle W, Guth B, Lotz R, Sieger P, Fuchs H, Himmelsbach F. Eckhardt M, et al. Among authors: langkopf e. J Med Chem. 2007 Dec 27;50(26):6450-3. doi: 10.1021/jm701280z. Epub 2007 Dec 1. J Med Chem. 2007. PMID: 18052023
(R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione (BI 1356), a novel xanthine-based dipeptidyl peptidase 4 inhibitor, has a superior potency and longer duration of action compared with other dipeptidyl peptidase-4 inhibitors.
Thomas L, Eckhardt M, Langkopf E, Tadayyon M, Himmelsbach F, Mark M. Thomas L, et al. Among authors: langkopf e. J Pharmacol Exp Ther. 2008 Apr;325(1):175-82. doi: 10.1124/jpet.107.135723. Epub 2008 Jan 25. J Pharmacol Exp Ther. 2008. PMID: 18223196
3,5-Dihydro-imidazo[4,5-d]pyridazin-4-ones: a class of potent DPP-4 inhibitors.
Eckhardt M, Hauel N, Himmelsbach F, Langkopf E, Nar H, Mark M, Tadayyon M, Thomas L, Guth B, Lotz R. Eckhardt M, et al. Among authors: langkopf e. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3158-62. doi: 10.1016/j.bmcl.2008.04.075. Epub 2008 May 1. Bioorg Med Chem Lett. 2008. PMID: 18485703