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Page 1
Novel Pyrimidine Toll-like Receptor 7 and 8 Dual Agonists to Treat Hepatitis B Virus.
McGowan D, Herschke F, Pauwels F, Stoops B, Last S, Pieters S, Scholliers A, Thoné T, Van Schoubroeck B, De Pooter D, Mostmans W, Khamlichi MD, Embrechts W, Dhuyvetter D, Smyej I, Arnoult E, Demin S, Borghys H, Fanning G, Vlach J, Raboisson P. McGowan D, et al. Among authors: dhuyvetter d. J Med Chem. 2016 Sep 8;59(17):7936-49. doi: 10.1021/acs.jmedchem.6b00747. Epub 2016 Aug 23. J Med Chem. 2016. PMID: 27513093
Identification and Optimization of Pyrrolo[3,2-d]pyrimidine Toll-like Receptor 7 (TLR7) Selective Agonists for the Treatment of Hepatitis B.
McGowan DC, Herschke F, Pauwels F, Stoops B, Smyej I, Last S, Pieters S, Embrechts W, Khamlichi MD, Thoné T, Van Schoubroeck B, Mostmans W, Wuyts D, Verstappen D, Scholliers A, De Pooter D, Dhuyvetter D, Borghys H, Tuefferd M, Arnoult E, Hong J, Fanning G, Bollekens J, Urmaliya V, Teisman A, Horton H, Jonckers THM, Raboisson P. McGowan DC, et al. Among authors: dhuyvetter d. J Med Chem. 2017 Jul 27;60(14):6137-6151. doi: 10.1021/acs.jmedchem.7b00365. Epub 2017 Jul 14. J Med Chem. 2017. PMID: 28671847
2,4-Diaminoquinazolines as Dual Toll-like Receptor (TLR) 7/8 Modulators for the Treatment of Hepatitis B Virus.
Embrechts W, Herschke F, Pauwels F, Stoops B, Last S, Pieters S, Pande V, Pille G, Amssoms K, Smyej I, Dhuyvetter D, Scholliers A, Mostmans W, Van Dijck K, Van Schoubroeck B, Thone T, De Pooter D, Fanning G, Jonckers THM, Horton H, Raboisson P, McGowan D. Embrechts W, et al. Among authors: dhuyvetter d. J Med Chem. 2018 Jul 26;61(14):6236-6246. doi: 10.1021/acs.jmedchem.8b00643. Epub 2018 Jul 17. J Med Chem. 2018. PMID: 29965759
Design and synthesis of a novel series of cyanoindole derivatives as potent γ-secretase modulators.
Bischoff FP, Velter AI, Minne G, Pieters S, Berthelot D, De Cleyn M, Gijsen HJM, Macdonald G, Surkyn M, Van Brandt S, Van Roosbroeck Y, Zavattaro C, Mercken M, Austin N, Dhuyvetter D, Borghys H, Ahmad I, Samanta SK. Bischoff FP, et al. Among authors: dhuyvetter d. Bioorg Med Chem Lett. 2019 Jul 15;29(14):1737-1745. doi: 10.1016/j.bmcl.2019.05.023. Epub 2019 May 15. Bioorg Med Chem Lett. 2019. PMID: 31122869
Optimization of 1,4-Oxazine β-Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate.
Gijsen HJM, Alonso de Diego SA, De Cleyn M, García-Molina A, Macdonald GJ, Martínez-Lamenca C, Oehlrich D, Prokopcova H, Rombouts FJR, Surkyn M, Trabanco AA, Van Brandt S, Van den Bossche D, Van Gool M, Austin N, Borghys H, Dhuyvetter D, Moechars D. Gijsen HJM, et al. Among authors: dhuyvetter d. J Med Chem. 2018 Jun 28;61(12):5292-5303. doi: 10.1021/acs.jmedchem.8b00304. Epub 2018 Jun 11. J Med Chem. 2018. PMID: 29809004
JNJ-67569762, A 2-Aminotetrahydropyridine-Based Selective BACE1 Inhibitor Targeting the S3 Pocket: From Discovery to Clinical Candidate.
Rombouts FJR, Kusakabe KI, Alexander R, Austin N, Borghys H, De Cleyn M, Dhuyvetter D, Gijsen HJM, Hrupka B, Jacobs T, Jerhaoui S, Lammens L, Leclercq L, Tsubone K, Ueno T, Morimoto K, Einaru S, Sumiyoshi H, Van den Bergh A, Vos A, Surkyn M, Teisman A, Moechars D. Rombouts FJR, et al. Among authors: dhuyvetter d. J Med Chem. 2021 Oct 14;64(19):14175-14191. doi: 10.1021/acs.jmedchem.1c00935. Epub 2021 Sep 23. J Med Chem. 2021. PMID: 34553934
Discovery of Potent and Centrally Active 6-Substituted 5-Fluoro-1,3-dihydro-oxazine β-Secretase (BACE1) Inhibitors via Active Conformation Stabilization.
Nakahara K, Fuchino K, Komano K, Asada N, Tadano G, Hasegawa T, Yamamoto T, Sako Y, Ogawa M, Unemura C, Hosono M, Ito H, Sakaguchi G, Ando S, Ohnishi S, Kido Y, Fukushima T, Dhuyvetter D, Borghys H, Gijsen HJM, Yamano Y, Iso Y, Kusakabe KI. Nakahara K, et al. Among authors: dhuyvetter d. J Med Chem. 2018 Jul 12;61(13):5525-5546. doi: 10.1021/acs.jmedchem.8b00011. Epub 2018 Jun 14. J Med Chem. 2018. PMID: 29775538
Rational Design of Novel 1,3-Oxazine Based β-Secretase (BACE1) Inhibitors: Incorporation of a Double Bond To Reduce P-gp Efflux Leading to Robust Aβ Reduction in the Brain.
Fuchino K, Mitsuoka Y, Masui M, Kurose N, Yoshida S, Komano K, Yamamoto T, Ogawa M, Unemura C, Hosono M, Ito H, Sakaguchi G, Ando S, Ohnishi S, Kido Y, Fukushima T, Miyajima H, Hiroyama S, Koyabu K, Dhuyvetter D, Borghys H, Gijsen HJM, Yamano Y, Iso Y, Kusakabe KI. Fuchino K, et al. Among authors: dhuyvetter d. J Med Chem. 2018 Jun 28;61(12):5122-5137. doi: 10.1021/acs.jmedchem.8b00002. Epub 2018 May 23. J Med Chem. 2018. PMID: 29733614
A translational assessment of preclinical versus clinical tools for the measurement of cardiac contractility: comparison of LV dP/dt(max) with echocardiography in telemetry implanted beagle dogs.
Cools F, Dhuyvetter D, Vanlommel A, Janssens S, Borghys H, Geys H, Gallacher DJ. Cools F, et al. Among authors: dhuyvetter d. J Pharmacol Toxicol Methods. 2014 Jan-Feb;69(1):17-23. doi: 10.1016/j.vascn.2013.10.003. Epub 2013 Oct 16. J Pharmacol Toxicol Methods. 2014. PMID: 24140387
24 results