2-Amino-3, 4-dihydroquinazolines as inhibitors of BACE-1 (β-site APP cleaving enzyme): use of structure based design to convert a micromolar hit into a nanomolar lead EW Baxter, KA Conway, L Kennis, F Bischoff, MH Mercken, HL De Winter, ... Journal of medicinal chemistry 50 (18), 4261-4264, 2007 | 187 | 2007 |
New 2-substituted 1, 2, 3, 4-tetrahydrobenzofuro [3, 2-c] pyridine having highly active and potent central α2-antagonistic activity as potential antidepressants LEJ Kennis, FP Bischoff, CJ Mertens, CJ Love, FAF Van den Keybus, ... Bioorganic & medicinal chemistry letters 10 (1), 71-74, 2000 | 76 | 2000 |
Design and synthesis of a novel series of bicyclic heterocycles as potent γ-secretase modulators F Bischoff, D Berthelot, M De Cleyn, G Macdonald, G Minne, D Oehlrich, ... Journal of medicinal chemistry 55 (21), 9089-9106, 2012 | 68 | 2012 |
Pyrimidine derivatives for the treatment of viral infections D Mc Gowan, PJMB Raboisson, W Embrechts, THM Jonckers, SJ Last, ... US Patent 9,422,250, 2016 | 67 | 2016 |
Synthesis and Pharmacological Characterization of Two Novel, Brain Penetrating P2X7 Antagonists MA Letavic, B Lord, F Bischoff, NA Hawryluk, S Pieters, JC Rech, Z Sales, ... ACS medicinal chemistry letters 4 (4), 419-422, 2013 | 60 | 2013 |
Quinazoline derivatives for the treatment of viral infections and further diseases D McGowan, PJMB Raboisson, THM Jonckers, SJ Last, W Embrechts, ... US Patent 8,916,575, 2014 | 40 | 2014 |
Novel pyrimidine toll-like receptor 7 and 8 dual agonists to treat hepatitis B virus D McGowan, F Herschke, F Pauwels, B Stoops, S Last, S Pieters, ... Journal of Medicinal Chemistry 59 (17), 7936-7949, 2016 | 39 | 2016 |
Pyrrolo [3, 2-] pyrimidine derivatives for the treatment of viral infections and other diseases DC McGowan, SJ Last, SMA Pieters, W Embrechts, THM Jonckers, ... US Patent 9,499,549, 2016 | 37 | 2016 |
2, 4-Diaminoquinazolines as dual toll-like receptor (TLR) 7/8 modulators for the treatment of hepatitis B virus W Embrechts, F Herschke, F Pauwels, B Stoops, S Last, S Pieters, ... Journal of Medicinal Chemistry 61 (14), 6236-6246, 2018 | 27 | 2018 |
Heterocyclic substituted 2-amino quinazoline derivatives for the treatment of viral infections SJ Last, DC McGowan, W Embrechts, SMA Pieters, THM Jonckers, ... US Patent 9,663,474, 2017 | 27 | 2017 |
Glyoxamide substituted pyrrolamide derivatives and the use thereof as medicaments for the treatment of hepatitis B K Vandyck, BRR Kesteleyn, SMA Pieters, G Rombouts, WG Verschueren, ... US Patent 10,450,270, 2019 | 20 | 2019 |
Anilinotriazoles as potent gamma secretase modulators AI Velter, FP Bischoff, D Berthelot, M De Cleyn, D Oehlrich, L Jaroskova, ... Bioorganic & Medicinal Chemistry Letters 24 (24), 5805-5813, 2014 | 20 | 2014 |
Cyclized sulfamoylarylamide derivatives and the use thereof as medicaments for the treatment of hepatitis B SMH Vendeville, SJ Last, SD Demin, SC Grosse, GYP Haché, L Hu, ... US Patent 10,875,876, 2020 | 18 | 2020 |
Identification and Optimization of Pyrrolo[3,2-d]pyrimidine Toll-like Receptor 7 (TLR7) Selective Agonists for the Treatment of Hepatitis B DC McGowan, F Herschke, F Pauwels, B Stoops, I Smyej, S Last, ... Journal of Medicinal Chemistry 60 (14), 6137-6151, 2017 | 18 | 2017 |
2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE) FP Bischoff, M Braeken, SMA Pieters, MH Mercken, HLJ De Winter, ... US Patent 8,436,006, 2013 | 16 | 2013 |
Pyrrolo [3, 2-d] pyrimidine derivatives for the treatment of viral infections and other diseases DC McGowan, SMA Pieters, SJ Last, W Embrechts, THM Jonckers, ... US Patent 10,385,054, 2019 | 13 | 2019 |
Discovery of selective 2, 4-diaminoquinazoline toll-like receptor 7 (TLR 7) agonists S Pieters, D McGowan, F Herschke, F Pauwels, B Stoops, S Last, ... Bioorganic & Medicinal Chemistry Letters 28 (4), 711-719, 2018 | 13 | 2018 |
Alkylaminobenzothiazole and-benzoxazole derivatives LEJ Kennis, JC Mertens, SMA Pieters US Patent 6,224,849, 2001 | 13 | 2001 |
Substituted bicyclic heterocyclic compounds as gamma secretase modulators HJM Gijsen, AI Velter, GJ MacDonald, FP Bischoff, T Wu, SFA Van Brandt, ... US Patent 8,946,426, 2015 | 9 | 2015 |
Glyoxamide substituted pyrrolamide derivatives and the use thereof as medicaments for the treatment of hepatitis B K Vandyck, BRR Kesteleyn, SMA Pieters, G Rombouts, WG Verschueren, ... | 8 | 2018 |