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BI 456906: Discovery and preclinical pharmacology of a novel GCGR/GLP-1R dual agonist with robust anti-obesity efficacy.
Zimmermann T, Thomas L, Baader-Pagler T, Haebel P, Simon E, Reindl W, Bajrami B, Rist W, Uphues I, Drucker DJ, Klein H, Santhanam R, Hamprecht D, Neubauer H, Augustin R. Zimmermann T, et al. Among authors: thomas l. Mol Metab. 2022 Dec;66:101633. doi: 10.1016/j.molmet.2022.101633. Epub 2022 Nov 7. Mol Metab. 2022. PMID: 36356832 Free PMC article.
Design, synthesis and evaluation of MCH receptor 1 antagonists--Part III: Discovery of pre-clinical development candidate BI 186908.
Oost T, Heckel A, Kley JT, Lehmann T, Müller S, Roth GJ, Rudolf K, Arndt K, Budzinski R, Lenter M, Lotz RR, Maier GM, Markert M, Thomas L, Stenkamp D. Oost T, et al. Among authors: thomas l. Bioorg Med Chem Lett. 2015 Aug 15;25(16):3275-80. doi: 10.1016/j.bmcl.2015.05.065. Epub 2015 May 29. Bioorg Med Chem Lett. 2015. PMID: 26105194
(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. 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
Chronic treatment with the dipeptidyl peptidase-4 inhibitor BI 1356 [(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] increases basal glucagon-like peptide-1 and improves glycemic control in diabetic rodent models.
Thomas L, Tadayyon M, Mark M. Thomas L, et al. J Pharmacol Exp Ther. 2009 Feb;328(2):556-63. doi: 10.1124/jpet.108.143966. Epub 2008 Oct 29. J Pharmacol Exp Ther. 2009. PMID: 18971371
5,368 results