Design and synthesis of bicyclic heterocycles as potent γ-secretase modulators von Oehlrich, Daniel, Rombouts, Frederik J.R., Berthelot, Didier, Bischoff, François P., De Cleyn, Michel A.J., Jaroskova, Libuse, Macdonald, Gregor, Mercken, Marc, Surkyn, Michel, Trabanco, Andrés A., Tresadern, Gary, Van Brandt, Sven, Velter, Adriana I., Wu, Tongfei, Gijsen, Harrie J.M.

Volltext

Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example von Rombouts, Frederik J. R, Tovar, Fulgencio, Austin, Nigel, Tresadern, Gary, Trabanco, Andrés A

Volltext

Structure-Based Approaches to Improving Selectivity through Utilizing Explicit Water Molecules: Discovery of Selective β‑Secretase (BACE1) Inhibitors over BACE2 von Fujimoto, Kazuki, Yoshida, Shuhei, Tadano, Genta, Asada, Naoya, Fuchino, Kouki, Suzuki, Shinji, Matsuoka, Eriko, Yamamoto, Takahiko, Yamamoto, Shiho, Ando, Shigeru, Kanegawa, Naoki, Tonomura, Yutaka, Ito, Hisanori, Moechars, Diederik, Rombouts, Frederik J. R, Gijsen, Harrie J. M, Kusakabe, Ken-ichi

Volltext

Discovery of an Oral, Beyond-Rule-of-Five Mcl‑1 Protein–Protein Interaction Modulator with the Potential of Treating Hematological Malignancies von Romanov-Michailidis, Fedor, Hsiao, Chien-Chi, Urner, Lorenz M., Jerhaoui, Soufyan, Surkyn, Michel, Miller, Bradley, Vos, Ann, Dominguez Blanco, Maria, Bueters, Ruud, Vinken, Petra, Bekkers, Mariette, Walker, David, Pietrak, Beth, Eyckmans, Werner, Dores-Sousa, José Luís, Joo Koo, Seong, Lento, William, Bauser, Marcus, Philippar, Ulrike, Rombouts, Frederik J. R.

Volltext

JNJ-67569762, A 2‑Aminotetrahydropyridine-Based Selective BACE1 Inhibitor Targeting the S3 Pocket: From Discovery to Clinical Candidate von Rombouts, Frederik J. R, Kusakabe, Ken-ichi, Alexander, Richard, Austin, Nigel, Borghys, Herman, De Cleyn, Michel, Dhuyvetter, Deborah, Gijsen, Harrie J. M, Hrupka, Brian, Jacobs, Tom, Jerhaoui, Soufyan, Lammens, Lieve, Leclercq, Laurent, Tsubone, Koichi, Ueno, Tatsuhiko, Morimoto, Kenji, Einaru, Shunsuke, Sumiyoshi, Hirokazu, Van den Bergh, An, Vos, Ann, Surkyn, Michel, Teisman, Ard, Moechars, Diederik

Volltext

Clinical evaluation of [18F] JNJ-64326067, a novel candidate PET tracer for the detection of tau pathology in Alzheimer’s disease von Schmidt, Mark E., Janssens, Luc, Moechars, Diederik, Rombouts, Frederik J. R., Timmers, Maarten, Barret, Olivier, Constantinescu, Cristian C., Madonia, Jennifer, Russell, David S., Sandiego, Christine M., Kolb, Hartmuth

Volltext

Discovery of Extremely Selective Fused Pyridine-Derived β‑Site Amyloid Precursor Protein-Cleaving Enzyme (BACE1) Inhibitors with High In Vivo Efficacy through 10s Loop Interactions... von Ueno, Tatsuhiko, Matsuoka, Eriko, Asada, Naoya, Yamamoto, Shiho, Kanegawa, Naoki, Ito, Mana, Ito, Hisanori, Moechars, Diederik, Rombouts, Frederik J. R, Gijsen, Harrie J. M, Kusakabe, Ken-ichi

Volltext

1,4-Oxazine β‑Secretase 1 (BACE1) Inhibitors: From Hit Generation to Orally Bioavailable Brain Penetrant Leads von Rombouts, Frederik J. R, Tresadern, Gary, Delgado, Oscar, Martínez-Lamenca, Carolina, Van Gool, Michiel, García-Molina, Aránzazu, Alonso de Diego, Sergio A, Oehlrich, Daniel, Prokopcova, Hana, Alonso, José Manuel, Austin, Nigel, Borghys, Herman, Van Brandt, Sven, Surkyn, Michel, De Cleyn, Michel, Vos, Ann, Alexander, Richard, Macdonald, Gregor, Moechars, Dieder, Gijsen, Harrie, Trabanco, Andrés A

Volltext

Discovery of N‑(Pyridin-4-yl)-1,5-naphthyridin-2-amines as Potential Tau Pathology PET Tracers for Alzheimer’s Disease von Rombouts, Frederik J. R, Andrés, José-Ignacio, Ariza, Manuela, Alonso, José Manuel, Austin, Nigel, Bottelbergs, Astrid, Chen, Lu, Chupakhin, Vladimir, Cleiren, Erna, Fierens, Katleen, Fontana, Alberto, Langlois, Xavier, Leenaerts, Joseph E, Mariën, Jonas, Martínez Lamenca, Carolina, Salter, Rhys, Schmidt, Mark E, Te Riele, Paula, Wintmolders, Cindy, Trabanco, Andrés A, Zhang, Wei, Macdonald, Gregor, Moechars, Dieder

Volltext

Modulating physicochemical properties of tetrahydropyridine-2-amine BACE1 inhibitors with electron-withdrawing groups: A systematic study von Rombouts, Frederik J.R., Hsiao, Chien-Chi, Bache, Solène, De Cleyn, Michel, Heckmann, Pauline, Leenaerts, Jos, Martinéz-Lamenca, Carolina, Van Brandt, Sven, Peschiulli, Aldo, Vos, Ann, Gijsen, Harrie J.M.

Volltext

Industrial medicinal chemistry insights: neuroscience hit generation at Janssen von Tresadern, Gary, Rombouts, Frederik J.R., Oehlrich, Daniel, Macdonald, Gregor, Trabanco, Andres A.

Volltext

Macrocyclic Carbon-Linked Pyrazoles As Novel Inhibitors of MCL‑1 von Demin, Samuël, Peschiulli, Aldo, Velter, Adriana I., Vos, Ann, De Boeck, Benoît, Miller, Bradley, Rombouts, Frederik J. R., Reuillon, Tristan, Lento, William, Blanco, Maria Dominguez, Jouffroy, Matthieu, Steyvers, Helena, Bekkers, Mariette, Altrocchi, Cristina, Pietrak, Beth, Koo, Seong Joo, Szewczuk, Lawrence, Attar, Ricardo, Philippar, Ulrike

Volltext

Optimization of 1,4-Oxazine β‑Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate von Gijsen, Harrie J. M, Alonso de Diego, Sergio A, De Cleyn, Michel, García-Molina, Aránzazu, Macdonald, Gregor J, Martínez-Lamenca, Carolina, Oehlrich, Daniel, Prokopcova, Hana, Rombouts, Frederik J. R, Surkyn, Michel, Trabanco, Andrés A, Van Brandt, Sven, Van den Bossche, Dries, Van Gool, Michiel, Austin, Nigel, Borghys, Herman, Dhuyvetter, Deborah, Moechars, Diederik

Volltext

Pyrido[4,3‑e][1,2,4]triazolo[4,3‑a]pyrazines as Selective, Brain Penetrant Phosphodiesterase 2 (PDE2) Inhibitors von Rombouts, Frederik J. R, Tresadern, Gary, Buijnsters, Peter, Langlois, Xavier, Tovar, Fulgencio, Steinbrecher, Thomas B, Vanhoof, Greet, Somers, Marijke, Andrés, José-Ignacio, Trabanco, Andrés A

Volltext

A Brain-Penetrant and Bioavailable Pyrazolopiperazine BACE1 Inhibitor Elicits Sustained Reduction of Amyloid β In Vivo von Peschiulli, Aldo, Oehlrich, Daniel, Van Gool, Michiel, Austin, Nigel, Van Brandt, Sven, Surkyn, Michel, De Cleyn, Michel, Vos, Ann, Tresadern, Gary, Rombouts, Frederik J. R, Macdonald, Gregor J, Moechars, Diederik, Trabanco, Andrés A, Gijsen, Harrie J. M

Volltext

Synthesis of a conformationally restricted dipeptide analogue and its evaluation as a β-turn mimic von De Borggraeve, Wim M, Rombouts, Frederik J.R, Van der Eycken, Erik V, Toppet, Suzanne M, Hoornaert, Georges J

Volltext

Structure-Based Design of a Potent, Selective, and Brain Penetrating PDE2 Inhibitor with Demonstrated Target Engagement von Buijnsters, Peter, De Angelis, Meri, Langlois, Xavier, Rombouts, Frederik J. R, Sanderson, Wendy, Tresadern, Gary, Ritchie, Alison, Trabanco, Andrés A, VanHoof, Greet, Roosbroeck, Yves Van, Andrés, José-Ignacio

Volltext

Discovery of N-(4-[18F]Fluoro-5-methylpyridin-2-yl)isoquinolin-6-amine (JNJ-64326067), a New Promising Tau Positron Emission Tomography Imaging Tracer von Rombouts, Frederik J.R, Declercq, Lieven, Andres, Jose-Ignacio, Bottelbergs, Astrid, Chen, Lu, Iturrino, Laura, Leenaerts, Joseph E, Marien, Jonas, Song, Fengbin, Wintmolders, Cindy, Wuyts, Stijn, Xia, Chunfang A, te Riele, Paula, Bormans, Guy, Vandenberghe, Rik, Kolb, Hartmuth, Moechars, Diederik

Volltext

Synthesis and conformational analysis of Substance P antagonist analogues based on a 1,7-naphthyridine scaffold von Rombouts, Frederik J.R, Van den Bossche, Jeroen, Toppet, Suzanne M, Compernolle, Frans, Hoornaert, Georges J

Volltext

Intramolecular Diels–Alder reactions of N-alkenyl-2(1 H)-pyrazinones: generation of a novel type of cis-1,7-naphthyridine von Rombouts, Frederik J.R, De Borggraeve, Wim, Toppet, Suzanne M, Compernolle, Frans, Hoornaert, Georges J

Volltext