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Discovery of 3-({5-Chloro-1-[3-(methylsulfonyl)propyl]-1H-indol-2-yl}methyl)-1-(2,2,2-trifluoroethyl)-1,3-dihydro-2H-imidazo[4,5-c]pyridin-2-one (JNJ-53718678), a Potent and Orally Bioavailable Fusion Inhibitor of Respiratory Syncytial Virus.
Vendeville S, Tahri A, Hu L, Demin S, Cooymans L, Vos A, Kwanten L, Van den Berg J, Battles MB, McLellan JS, Koul A, Raboisson P, Roymans D, Jonckers THM. Vendeville S, et al. Among authors: jonckers thm. J Med Chem. 2020 Aug 13;63(15):8046-8058. doi: 10.1021/acs.jmedchem.0c00226. Epub 2020 Jun 15. J Med Chem. 2020. PMID: 32407115
Discovery and selection of TMC114, a next generation HIV-1 protease inhibitor.
Surleraux DL, Tahri A, Verschueren WG, Pille GM, de Kock HA, Jonckers TH, Peeters A, De Meyer S, Azijn H, Pauwels R, de Bethune MP, King NM, Prabu-Jeyabalan M, Schiffer CA, Wigerinck PB. Surleraux DL, et al. J Med Chem. 2005 Mar 24;48(6):1813-22. doi: 10.1021/jm049560p. J Med Chem. 2005. PMID: 15771427
2'-Deoxy-2'-spirocyclopropylcytidine revisited: a new and selective inhibitor of the hepatitis C virus NS5B polymerase.
Jonckers TH, Lin TI, Buyck C, Lachau-Durand S, Vandyck K, Van Hoof S, Vandekerckhove LA, Hu L, Berke JM, Vijgen L, Dillen LL, Cummings MD, de Kock H, Nilsson M, Sund C, Rydegård C, Samuelsson B, Rosenquist A, Fanning G, Van Emelen K, Simmen K, Raboisson P. Jonckers TH, et al. J Med Chem. 2010 Nov 25;53(22):8150-60. doi: 10.1021/jm101050a. Epub 2010 Oct 29. J Med Chem. 2010. PMID: 21033671
Antiviral activity and mode of action of TMC647078, a novel nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
Berke JM, Vijgen L, Lachau-Durand S, Powdrill MH, Rawe S, Sjuvarsson E, Eriksson S, Götte M, Fransen E, Dehertogh P, Van den Eynde C, Leclercq L, Jonckers TH, Raboisson P, Nilsson M, Samuelsson B, Rosenquist Å, Fanning GC, Lin TI. Berke JM, et al. Antimicrob Agents Chemother. 2011 Aug;55(8):3812-20. doi: 10.1128/AAC.00214-11. Epub 2011 May 16. Antimicrob Agents Chemother. 2011. PMID: 21576430 Free PMC article.
Discovery of 4'-azido-2'-deoxy-2'-C-methyl cytidine and prodrugs thereof: a potent inhibitor of Hepatitis C virus replication.
Nilsson M, Kalayanov G, Winqvist A, Pinho P, Sund C, Zhou XX, Wähling H, Belfrage AK, Pelcman M, Agback T, Benckestock K, Wikström K, Boothee M, Lindqvist A, Rydegård C, Jonckers TH, Vandyck K, Raboisson P, Lin TI, Lachau-Durand S, de Kock H, Smith DB, Martin JA, Klumpp K, Simmen K, Vrang L, Terelius Y, Samuelsson B, Rosenquist S, Johansson NG. Nilsson M, et al. Bioorg Med Chem Lett. 2012 May 1;22(9):3265-8. doi: 10.1016/j.bmcl.2012.03.021. Epub 2012 Mar 16. Bioorg Med Chem Lett. 2012. PMID: 22472694
Molecular mechanism of respiratory syncytial virus fusion inhibitors.
Battles MB, Langedijk JP, Furmanova-Hollenstein P, Chaiwatpongsakorn S, Costello HM, Kwanten L, Vranckx L, Vink P, Jaensch S, Jonckers TH, Koul A, Arnoult E, Peeples ME, Roymans D, McLellan JS. Battles MB, et al. Nat Chem Biol. 2016 Feb;12(2):87-93. doi: 10.1038/nchembio.1982. Epub 2015 Dec 7. Nat Chem Biol. 2016. PMID: 26641933 Free PMC article.
Discovery of 1-((2R,4aR,6R,7R,7aR)-2-Isopropoxy-2-oxidodihydro-4H,6H-spiro[furo[3,2-d][1,3,2]dioxaphosphinine-7,2'-oxetan]-6-yl)pyrimidine-2,4(1H,3H)-dione (JNJ-54257099), a 3'-5'-Cyclic Phosphate Ester Prodrug of 2'-Deoxy-2'-Spirooxetane Uridine Triphosphate Useful for HCV Inhibition.
Jonckers TH, Tahri A, Vijgen L, Berke JM, Lachau-Durand S, Stoops B, Snoeys J, Leclercq L, Tambuyzer L, Lin TI, Simmen K, Raboisson P. Jonckers TH, et al. J Med Chem. 2016 Jun 23;59(12):5790-8. doi: 10.1021/acs.jmedchem.6b00382. Epub 2016 Jun 3. J Med Chem. 2016. PMID: 27181575
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: jonckers thm. 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
31 results