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Pharmacological characterization of the selective 11β-hydroxysteroid dehydrogenase 1 inhibitor, BI 135585, a clinical candidate for the treatment of type 2 diabetes.
Hamilton BS, Himmelsbach F, Nar H, Schuler-Metz A, Krosky P, Guo J, Guo R, Meng S, Zhao Y, Lala DS, Zhuang L, Claremon DA, McGeehan GM. Hamilton BS, et al. Among authors: himmelsbach f. Eur J Pharmacol. 2015 Jan 5;746:50-5. doi: 10.1016/j.ejphar.2014.10.053. Epub 2014 Nov 8. Eur J Pharmacol. 2015. PMID: 25445047
Discovery of BI 135585, an in vivo efficacious oxazinanone-based 11β hydroxysteroid dehydrogenase type 1 inhibitor.
Zhuang L, Tice CM, Xu Z, Zhao W, Cacatian S, Ye YJ, Singh SB, Lindblom P, McKeever BM, Krosky PM, Zhao Y, Lala D, Kruk BA, Meng S, Howard L, Johnson JA, Bukhtiyarov Y, Panemangalore R, Guo J, Guo R, Himmelsbach F, Hamilton B, Schuler-Metz A, Schauerte H, Gregg R, McGeehan GM, Leftheris K, Claremon DA. Zhuang L, et al. Among authors: himmelsbach f. Bioorg Med Chem. 2017 Jul 15;25(14):3649-3657. doi: 10.1016/j.bmc.2017.04.033. Epub 2017 Apr 29. Bioorg Med Chem. 2017. PMID: 28528082
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: himmelsbach f. J Med Chem. 2007 Dec 27;50(26):6450-3. doi: 10.1021/jm701280z. Epub 2007 Dec 1. J Med Chem. 2007. PMID: 18052023
SGLT6 - A pharmacological target for the treatment of obesity?
Baader-Pagler T, Eckhardt M, Himmelsbach F, Sauer A, Stierstorfer BE, Hamilton BS. Baader-Pagler T, et al. Among authors: himmelsbach f. Adipocyte. 2018;7(4):277-284. doi: 10.1080/21623945.2018.1516098. Epub 2018 Oct 11. Adipocyte. 2018. PMID: 30161013 Free PMC article.
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: himmelsbach f. 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
(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: himmelsbach f. 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
Sequential C-H Arylation and Enantioselective Hydrogenation Enables Ideal Asymmetric Entry to the Indenopiperidine Core of an 11β-HSD-1 Inhibitor.
Wei X, Qu B, Zeng X, Savoie J, Fandrick KR, Desrosiers JN, Tcyrulnikov S, Marsini MA, Buono FG, Li Z, Yang BS, Tang W, Haddad N, Gutierrez O, Wang J, Lee H, Ma S, Campbell S, Lorenz JC, Eckhardt M, Himmelsbach F, Peters S, Patel ND, Tan Z, Yee NK, Song JJ, Roschangar F, Kozlowski MC, Senanayake CH. Wei X, et al. Among authors: himmelsbach f. J Am Chem Soc. 2016 Nov 30;138(47):15473-15481. doi: 10.1021/jacs.6b09764. Epub 2016 Nov 17. J Am Chem Soc. 2016. PMID: 27794616 Free PMC article.
25 results