Discovery and Characterization of Potent, Efficacious, Orally Available Antimalarial Plasmepsin X Inhibitors and Preclinical Safety Assessment of UCB7362
Lowe, Martin A., Cardenas, Alvaro, Valentin, Jean-Pierre, Zhu, Zhaoning, Abendroth, Jan, Castro, Jose L., Class, Reiner, Delaunois, Annie, Fleurance, Renaud, Gerets, Helga, Gryshkova, Vitalina, King, Lloyd, Lorimer, Donald D., MacCoss, Malcolm, Rowley, Julian H., Rosseels, Marie-Luce, Royer, Leandro, Taylor, Richard D., Wong, Melanie, Zaccheo, Oliver, Chavan, Vishal P., Ghule, Gokul A., Tapkir, Bapusaheb K., Burrows, Jeremy N., Duffey, Maëlle, Rottmann, Matthias, Wittlin, Sergio, Angulo-Barturen, Iñigo, Jiménez-Díaz, María Belén, Striepen, Josefine, Fairhurst, Kate J., Yeo, Tomas, Fidock, David A., Cowman, Alan F., Favuzza, Paola, Crespo-Fernandez, Benigno, Gamo, Francisco Javier, Goldberg, Daniel E., Soldati-Favre, Dominique, Laleu, Benoît, de Haro, Teresa
Published in Journal of medicinal chemistry (27.10.2022)
Published in Journal of medicinal chemistry (27.10.2022)
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Journal Article
Deconvoluting and derisking QRS complex widening to improve cardiac safety profile of novel plasmepsin X antimalarials
Delaunois, Annie, Cardenas, Alvaro, de Haro, Teresa, Gerets, Helga H J, Gryshkova, Vitalina, Hebeisen, Simon, Korlowski, Chloé, Laleu, Benoit, Lowe, Martin A, Valentin, Jean-Pierre
Published in Toxicological sciences (01.10.2024)
Published in Toxicological sciences (01.10.2024)
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Journal Article
Assessing the interplay between off-target promiscuity, cytotoxicity, and tolerability in rodents to improve the safety profile of novel anti-malarial plasmepsin X inhibitors
Gerets, Helga H J, Delaunois, Annie, Cardenas, Alvaro, Class, Reiner, Fleurance, Renaud, de Haro, Teresa, Laleu, Benoît, Lowe, Martin A, Rosseels, Marie-Luce, Valentin, Jean-Pierre
Published in Toxicological sciences (01.10.2024)
Published in Toxicological sciences (01.10.2024)
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Journal Article
Palladium-Mediated Annulation of Vinyl Aziridines with Michael Acceptors: Stereocontrolled Synthesis of Substituted Pyrrolidines and Its Application in a Formal Synthesis of (−)-α-Kainic Acid
Lowe, Martin A., Ostovar, Mehrnoosh, Ferrini, Serena, Chen, C. Chun, Lawrence, Paul G., Fontana, Francesco, Calabrese, Andrew A., Aggarwal, Varinder K.
Published in Angewandte Chemie International Edition (04.07.2011)
Published in Angewandte Chemie International Edition (04.07.2011)
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Journal Article
Design of Novel Series of Antimalarial PMX Inhibitors with Increased Half-Life via Molecular Property Optimization
Sakata, Komei, Lowe, Martin A., Xuan, Mengyang, Bruffaerts, Jeffrey, Stasi, Luigi P., Lallemand, Benedicte, Cardenas, Alvaro, Taylor, Richard D., Vidler, Lewis R., King, Lloyd, Valentin, Jean-Pierre, Laleu, Benoit, de Haro, Teresa
Published in ACS medicinal chemistry letters (09.11.2023)
Published in ACS medicinal chemistry letters (09.11.2023)
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Journal Article
Fused thiophene derivatives as MEK inhibitors
Laing, Victoria E., Brookings, Daniel C., Carbery, Rachel J., Simorte, Jose Gascon, Hutchings, Martin C., Langham, Barry J., Lowe, Martin A., Allen, Rodger A., Fetterman, Joanne R., Turner, James, Meier, Christoph, Kennedy, Jeff, Merriman, Mark
Published in Bioorganic & medicinal chemistry letters (01.01.2012)
Published in Bioorganic & medicinal chemistry letters (01.01.2012)
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Journal Article
Palladium-Mediated Annulation of Vinyl Aziridines with Michael Acceptors: Stereocontrolled Synthesis of Substituted Pyrrolidines and Its Application in a Formal Synthesis of (-)-[alpha]-Kainic Acid
Lowe, Martin A, Ostovar, Mehrnoosh, Ferrini, Serena, Chen, C Chun, Lawrence, Paul G, Fontana, Francesco, Calabrese, Andrew A, Aggarwal, Varinder K
Published in Angewandte Chemie International Edition (04.07.2011)
Published in Angewandte Chemie International Edition (04.07.2011)
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Journal Article
Palladium-Mediated Annulation of Vinyl Aziridines with Michael Acceptors: Stereocontrolled Synthesis of Substituted Pyrrolidines and Its Application in a Formal Synthesis of (-)-[alpha]-Kainic Acid
Lowe, Martin A, Ostovar, Mehrnoosh, Ferrini, Serena, Chen, C Chun, Lawrence, Paul G, Fontana, Francesco, Calabrese, Andrew A, Aggarwal, Varinder K
Published in Angewandte Chemie (04.07.2011)
Published in Angewandte Chemie (04.07.2011)
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Journal Article
Palladium-Mediated Annulation of Vinyl Aziridines with Michael Acceptors: Stereocontrolled Synthesis of Substituted Pyrrolidines and Its Application in a Formal Synthesis of (−)-α-Kainic Acid
Lowe, Martin A., Ostovar, Mehrnoosh, Ferrini, Serena, Chen, C. Chun, Lawrence, Paul G., Fontana, Francesco, Calabrese, Andrew A., Aggarwal, Varinder K.
Published in Angewandte Chemie (04.07.2011)
Published in Angewandte Chemie (04.07.2011)
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Journal Article
Anti-malarial hexahydropyrimidine analogs
LOWE MARTIN ALEXANDER, MACCOSS MALCOLM, DE HARO GARCIA TERESA, TAYLOR RICHARD DAVID, ZHU ZHAONING
Year of Publication 18.03.2022
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Year of Publication 18.03.2022
Patent
ANTIMALARIAL HEXAHYDROPYRIMIDINE ANALOGUES
LOWE MARTIN ALEXANDER, MACCOSS MALCOLM, KING LLOYD MALCOLM, DE HARO GARCIA TERESA, TAYLOR RICHARD DAVID, ZHU ZHAONING
Year of Publication 13.11.2020
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Year of Publication 13.11.2020
Patent
FUSED PENTACYCLIC IMIDAZOLE DERIVATIVES AS MODULATORS OF TNF ACTIVITY
LOWE MARTIN ALEXANDER, DELIGNY MICHAEL LOUIS ROBERT, HEER JAG PAUL, LEPISSIER LUCE ELSA, KAYAERTS JEAN
Year of Publication 11.01.2019
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Year of Publication 11.01.2019
Patent
IMINOTHIADIAZINANE DIOXIDE DERIVATIVES AS PLASMEPSIN V INHIBITORS
LOWE MARTIN ALEXANDER, MACCOSS MALCOLM, DE HARO GARCIA TERESA, TAYLOR RICHARD DAVID, ZHU ZHAONING
Year of Publication 04.01.2019
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Year of Publication 04.01.2019
Patent
Iminotetrahydropyrimidinone derivatives as PLASMEPSIN V inhibitors
LOWE MARTIN ALEXANDER, MACCOSS MALCOLM, MORGAN TREVOR, DE HARO GARCIA TERESA, CHARLTON REBECCA LOUISE, TAYLOR RICHARD DAVID, ZHU ZHAONING
Year of Publication 17.07.2018
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Year of Publication 17.07.2018
Patent
Tetrahydroimidazopyridine derivatives as modulators of TNF activity
LOWE MARTIN ALEXANDER, PORTER JOHN ROBERT, JACKSON VICTORIA ELIZABETH, KROEPLIEN BORIS
Year of Publication 27.07.2016
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Year of Publication 27.07.2016
Patent
Purine derivatives as modulators of TNF activity
LOWE MARTIN ALEXANDER, PORTER JOHN ROBERT, JACKSON VICTORIA ELIZABETH, KROEPLIEN BORIS
Year of Publication 27.07.2016
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Year of Publication 27.07.2016
Patent
Fused imidazole and pyrazole derivatives as modulators of TNF activity
LOWE MARTIN ALEXANDER, PORTER JOHN ROBERT, JACKSON VICTORIA ELIZABETH, KROEPLIEN BORIS
Year of Publication 27.07.2016
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Year of Publication 27.07.2016
Patent
BENZOXAZINONE DERIVATIVES AND ANALOGUES THEREOF AS MODULATORS OF TNF ACTIVITY
JONES SEVERINE DANIELLE, LOWE MARTIN ALEXANDER, PORTER JOHN ROBERT, PALMER CHRISTOPHER FRANCIS, UDDIN MUHAMMED, LECOMTE FABIEN CLAUDE, NORMAN TIMOTHY JOHN, ZHU ZHAONING, LOKE PUI LENG, JOHNSON JAMES ANDREW, BRACE GARETH NEIL, SMYTH DONALD, TRANI GIANCARLO, CHOVATIA PRAFULKUMAR TULSHIBHAI, FOULKES GREGORY, MANDAL AJAY, PEREZ-FUERTES YOLANDA, KROEPLIEN BORIS
Year of Publication 03.04.2018
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Year of Publication 03.04.2018
Patent