Development of two diastereoselective routes towards trans-4-aminomethyl-piperidin-3-ol building blocks
Gijsen, Harrie J.M., De Cleyn, Michel J.A., Love, Christopher J., Surkyn, Michel, Van Brandt, Sven F.A., Verdonck, Marc G.C., Moens, Luc, Cuypers, Jef, Bosmans, Jean-Paul R.M.A.
Published in Tetrahedron (03.03.2008)
Published in Tetrahedron (03.03.2008)
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Discovery of an Oral, Beyond-Rule-of-Five Mcl‑1 Protein–Protein Interaction Modulator with the Potential of Treating Hematological Malignancies
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.
Published in Journal of medicinal chemistry (11.05.2023)
Published in Journal of medicinal chemistry (11.05.2023)
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JNJ-67569762, A 2‑Aminotetrahydropyridine-Based Selective BACE1 Inhibitor Targeting the S3 Pocket: From Discovery to Clinical Candidate
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
Published in Journal of medicinal chemistry (14.10.2021)
Published in Journal of medicinal chemistry (14.10.2021)
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1,4-Oxazine β‑Secretase 1 (BACE1) Inhibitors: From Hit Generation to Orally Bioavailable Brain Penetrant Leads
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
Published in Journal of medicinal chemistry (22.10.2015)
Published in Journal of medicinal chemistry (22.10.2015)
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Journal Article
Design and Synthesis of a Novel Series of Bicyclic Heterocycles As Potent γ-Secretase Modulators
Bischoff, Francois, Berthelot, Didier, De Cleyn, Michel, Macdonald, Gregor, Minne, Garrett, Oehlrich, Daniel, Pieters, Serge, Surkyn, Michel, Trabanco, Andrés A, Tresadern, Gary, Van Brandt, Sven, Velter, Ingrid, Zaja, Mirko, Borghys, Herman, Masungi, Chantal, Mercken, Marc, Gijsen, Harrie J. M
Published in Journal of medicinal chemistry (08.11.2012)
Published in Journal of medicinal chemistry (08.11.2012)
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Journal Article
Design and synthesis of a novel series of cyanoindole derivatives as potent γ-secretase modulators
Bischoff, François P., Velter, Adriana Ingrid, Minne, Garrett, Pieters, Serge, Berthelot, Didier, De Cleyn, Michel, Gijsen, Harrie J.M., Macdonald, Gregor, Surkyn, Michel, Van Brandt, Sven, Van Roosbroeck, Yves, Zavattaro, Chiara, Mercken, Marc, Austin, Nigel, Dhuyvetter, Deborah, Borghys, Herman, Ahmad, Ishtiyaque, Samanta, Swapan Kumar
Published in Bioorganic & medicinal chemistry letters (15.07.2019)
Published in Bioorganic & medicinal chemistry letters (15.07.2019)
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Journal Article
Optimization of 1,4-Oxazine β‑Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate
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
Published in Journal of medicinal chemistry (28.06.2018)
Published in Journal of medicinal chemistry (28.06.2018)
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Journal Article
Evaluation of a Series of β‑Secretase 1 Inhibitors Containing Novel Heteroaryl-Fused-Piperazine Amidine Warheads
Oehlrich, Daniel, Peschiulli, Aldo, Tresadern, Gary, Van Gool, Michiel, Vega, Juan Antonio, De Lucas, Ana Isabel, Alonso de Diego, Sergio A, Prokopcova, Hana, Austin, Nigel, Van Brandt, Sven, Surkyn, Michel, De Cleyn, Michel, Vos, Ann, Rombouts, Frederik J. R, Macdonald, Gregor, Moechars, Dieder, Gijsen, Harrie J. M, Trabanco, Andrés A
Published in ACS medicinal chemistry letters (08.08.2019)
Published in ACS medicinal chemistry letters (08.08.2019)
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Journal Article
A Brain-Penetrant and Bioavailable Pyrazolopiperazine BACE1 Inhibitor Elicits Sustained Reduction of Amyloid β In Vivo
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
Published in ACS medicinal chemistry letters (13.01.2022)
Published in ACS medicinal chemistry letters (13.01.2022)
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Journal Article
Correction to Optimization of 1,4-Oxazine β‑Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate
Gijsen, Harrie J. M, Alonso de Diego, Sergio A, De Cleyn, Michel, García-Molina, Aránzazu, Macdonald, Gregor J, Martinez-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, Urmaliya, Vijay, Teisman, Ard, Moechars, Diederik
Published in Journal of medicinal chemistry (27.12.2018)
Published in Journal of medicinal chemistry (27.12.2018)
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Anilinotriazoles as potent gamma secretase modulators
Velter, Adriana I., Bischoff, Francois P., Berthelot, Didier, De Cleyn, Michel, Oehlrich, Daniel, Jaroskova, Libuse, Macdonald, Gregor, Minne, Garrett, Pieters, Serge, Rombouts, Frederik, Van Brandt, Sven, Van Roosbroeck, Yves, Surkyn, Michel, Trabanco, Andres A., Tresadern, Gary, Wu, Tongfei, Borghys, Herman, Mercken, Marc, Masungi, Chantal, Gijsen, Harrie
Published in Bioorganic & medicinal chemistry letters (15.12.2014)
Published in Bioorganic & medicinal chemistry letters (15.12.2014)
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Design and synthesis of bicyclic heterocycles as potent γ-secretase modulators
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.
Published in Bioorganic & medicinal chemistry letters (01.09.2013)
Published in Bioorganic & medicinal chemistry letters (01.09.2013)
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Design and synthesis of bicyclic heterocycles as potent I3-secretase modulators
Oehlrich, Daniel, Rombouts, Frederik, Berthelot, Didier, Bischoff, Francois, Cleyn, Michel, Jaroskova, Libuse, Macdonald, Gregor, Mercken, Marc, Surkyn, Michel, Trabanco, Andres, Tresadern, Gary, Brandt, Sven, Velter, Adriana, Wu, Tongfei, Gijsen, Harrie
Published in Bioorganic & medicinal chemistry letters (01.09.2013)
Published in Bioorganic & medicinal chemistry letters (01.09.2013)
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5-Sulfonyl-benzimidazoles as selective CB2 agonists-Part 2
Gijsen, Harrie J.M., De Cleyn, Michel A.J., Surkyn, Michel, Van Lommen, Guy R.E., Verbist, Bie M.P., Nijsen, Marjoleen J.M.A., Meert, Theo, Wauwe, Jean Van, Aerssens, Jeroen
Published in Bioorganic & medicinal chemistry letters (01.01.2012)
Published in Bioorganic & medicinal chemistry letters (01.01.2012)
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5-Sulfonyl-benzimidazoles as selective CB2 agonists
Verbist, Bie M.P., De Cleyn, Michel A.J., Surkyn, Michel, Fraiponts, Erwin, Aerssens, Jeroen, Nijsen, Marjoleen J.M.A., Gijsen, Harrie J.M.
Published in Bioorganic & medicinal chemistry (15.04.2008)
Published in Bioorganic & medicinal chemistry (15.04.2008)
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SUBSTITUTED TRIAZOLE AND IMIDAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS
SVEN FRANCISCUS ANNA VAN BRANDT, WU TONGFEI, MICHEL SURKYN, FREDERIK JAN RITA ROMBOUTS, FRANCOIS PAUL BISCHOFF, GARRETT BERLOND MINNE, SERGE MARIA ALOYSIUS PIETERS, HENRICUS JACOBUS MARIA GIJSEN, DANIEL OEHLRICH, ADRIANA INGRID VELTER, MICHEL ANNA JOZEF DE CLEYN, DIDIER JEAN-CLAUDE BERTHELOT
Year of Publication 16.07.2015
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Year of Publication 16.07.2015
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MACROCYCLIC BRANCHED 3-FLUORO-BUT-3-ENAMIDES AS INHIBITORS OF MCL-1
ROMBOUTS, Frederik Jan Rita, HSIAO, Meng-Yang, JOUFFROY, Matthieu Dominique, JERHAOUI, Soufyan, SURKYN, Michel
Year of Publication 14.03.2024
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Year of Publication 14.03.2024
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MACROCYCLIC 2-ALLYLTETRAHYDROFURANS AS INHIBITORS OF MCL-1
HSIAO, Meng-Yang, URNER, Lorenz, ROMBOUTS, Frederik, JERHAOUI, Soufyan, SURKYN, Michel, ROMANOV MICHAILIDIS, Fedor, DIELS, Gaston
Year of Publication 14.12.2023
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Year of Publication 14.12.2023
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MACROCYCLIC BRANCHED 3-FLUORO-BUT-3-ENAMIDES AS INHIBITORS OF MCL-1
HSIAO, Meng-Yang, JOUFFROY, Matthieu, Dominique, ROMBOUTS, Frederik, Jan, Rita, JERHAOUI, Soufyan, SURKYN, Michel
Year of Publication 25.10.2023
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Year of Publication 25.10.2023
Patent