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Page 1
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
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
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
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
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
Correction to 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, Martinez-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, Urmaliya V, Teisman A, Moechars D. Gijsen HJM, et al. Among authors: dhuyvetter d. J Med Chem. 2018 Dec 27;61(24):11415. doi: 10.1021/acs.jmedchem.8b01859. Epub 2018 Dec 7. J Med Chem. 2018. PMID: 30525600 No abstract available.
Discovery of an Extremely Potent Thiazine-Based β-Secretase Inhibitor with Reduced Cardiovascular and Liver Toxicity at a Low Projected Human Dose.
Tadano G, Komano K, Yoshida S, Suzuki S, Nakahara K, Fuchino K, Fujimoto K, Matsuoka E, Yamamoto T, Asada N, Ito H, Sakaguchi G, Kanegawa N, Kido Y, Ando S, Fukushima T, Teisman A, Urmaliya V, Dhuyvetter D, Borghys H, Van Den Bergh A, Austin N, Gijsen HJM, Yamano Y, Iso Y, Kusakabe KI. Tadano G, et al. Among authors: dhuyvetter d. J Med Chem. 2019 Oct 24;62(20):9331-9337. doi: 10.1021/acs.jmedchem.9b01140. Epub 2019 Oct 8. J Med Chem. 2019. PMID: 31549838
Trifluoromethyl Dihydrothiazine-Based β-Secretase (BACE1) Inhibitors with Robust Central β-Amyloid Reduction and Minimal Covalent Binding Burden.
Anan K, Iso Y, Oguma T, Nakahara K, Suzuki S, Yamamoto T, Matsuoka E, Ito H, Sakaguchi G, Ando S, Morimoto K, Kanegawa N, Kido Y, Kawachi T, Fukushima T, Teisman A, Urmaliya V, Dhuyvetter D, Borghys H, Austin N, Van Den Bergh A, Verboven P, Bischoff F, Gijsen HJM, Yamano Y, Kusakabe K. Anan K, et al. Among authors: dhuyvetter d. ChemMedChem. 2019 Nov 20;14(22):1894-1910. doi: 10.1002/cmdc.201900478. Epub 2019 Nov 12. ChemMedChem. 2019. PMID: 31657130
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
24 results