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Synthesis, SAR, and series evolution of novel oxadiazole-containing 5-lipoxygenase activating protein inhibitors: discovery of 2-[4-(3-{(r)-1-[4-(2-amino-pyrimidin-5-yl)-phenyl]-1-cyclopropyl-ethyl}-[1,2,4]oxadiazol-5-yl)-pyrazol-1-yl]-N,N-dimethyl-acetamide (BI 665915).
Takahashi H, Riether D, Bartolozzi A, Bosanac T, Berger V, Binetti R, Broadwater J, Chen Z, Crux R, De Lombaert S, Dave R, Dines JA, Fadra-Khan T, Flegg A, Garrigou M, Hao MH, Huber J, Hutzler JM, Kerr S, Kotey A, Liu W, Lo HY, Loke PL, Mahaney PE, Morwick TM, Napier S, Olague A, Pack E, Padyana AK, Thomson DS, Tye H, Wu L, Zindell RM, Abeywardane A, Simpson T. Takahashi H, et al. Among authors: simpson t. J Med Chem. 2015 Feb 26;58(4):1669-90. doi: 10.1021/jm501185j. Epub 2015 Feb 11. J Med Chem. 2015. PMID: 25671290
4-aryl piperazine and piperidine amides as novel mGluR5 positive allosteric modulators.
Xiong H, Brugel TA, Balestra M, Brown DG, Brush KA, Hightower C, Hinkley L, Hoesch V, Kang J, Koether GM, McCauley JP Jr, McLaren FM, Panko LM, Simpson TR, Smith RW, Woods JM, Brockel B, Chhajlani V, Gadient RA, Spear N, Sygowski LA, Zhang M, Arora J, Breysse N, Wilson JM, Isaac M, Slassi A, King MM. Xiong H, et al. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7381-4. doi: 10.1016/j.bmcl.2010.10.036. Epub 2010 Oct 21. Bioorg Med Chem Lett. 2010. PMID: 21067920
Discovery and optimization of oxadiazole-based FLAP inhibitors.
Bartolozzi A, Abeywardane A, Bosanac T, Broadwater JA, Chen Z, Hutzler JM, Huber JD, Nemoto P, Olague A, Riether D, Simpson T, Takahashi H, Wu L, Zhang Y, Zindell RM. Bartolozzi A, et al. Among authors: simpson t. Bioorg Med Chem Lett. 2017 Oct 15;27(20):4652-4659. doi: 10.1016/j.bmcl.2017.09.007. Epub 2017 Sep 8. Bioorg Med Chem Lett. 2017. PMID: 28927794
The potent and selective RIPK2 inhibitor BI 706039 improves intestinal inflammation in the TRUC mouse model of inflammatory bowel disease.
Ermann J, Matmusaev M, Haley EK, Braun C, Jost F, Mayer-Wrangowski S, Hsiao P, Ting N, Li L, Terenzio D, Chime J, Lukas S, Patnaude L, Panzenbeck M, Csordas D, Zheng J, Mierz D, Simpson T, King FJ, Klimowicz AP, Mbow ML, Fine JS, Miller CA, Fogal SE, Byrne FR. Ermann J, et al. Among authors: simpson t. Am J Physiol Gastrointest Liver Physiol. 2021 Nov 1;321(5):G500-G512. doi: 10.1152/ajpgi.00163.2021. Epub 2021 Sep 8. Am J Physiol Gastrointest Liver Physiol. 2021. PMID: 34494462 Free article.
Combined PET/DCE-MRI in a Rabbit Model of Atherosclerosis: Integrated Quantification of Plaque Inflammation, Permeability, and Burden During Treatment With a Leukotriene A4 Hydrolase Inhibitor.
Calcagno C, Lairez O, Hawkins J, Kerr SW, Dugas MS, Simpson T, Epskamp J, Robson PM, Eldib M, Bander I, K-Raman P, Ramachandran S, Pruzan A, Kaufman A, Mani V, Ehlgen A, Niessen HG, Broadwater J, Fayad ZA. Calcagno C, et al. Among authors: simpson t. JACC Cardiovasc Imaging. 2018 Feb;11(2 Pt 2):291-301. doi: 10.1016/j.jcmg.2017.11.030. JACC Cardiovasc Imaging. 2018. PMID: 29413439 Free article.
1,017 results