The 7 TM G-Protein-Coupled Receptor Target Family
Jacoby, Edgar, Bouhelal, Rochdi, Gerspacher, Marc, Seuwen, Klaus
Published in ChemMedChem (11.08.2006)
Published in ChemMedChem (11.08.2006)
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Stereoselective Preparation of N-[(R,R)-(E)-1-(3,4-dichlorobenzyl)-3- (2-oxoazepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamide, a Potent and Orally Active Dual Neurokinin NK1/NK2 Receptor Antagonist
Gerspacher, Marc, Lewis, Christine, Ball, Howard A, Howes, Colin, Subramanian, Natarajan, Ryffel, Karin, Fozard, John R
Published in Journal of medicinal chemistry (31.07.2003)
Published in Journal of medicinal chemistry (31.07.2003)
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Journal Article
JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRASG12C for the Treatment of Solid Tumors
Lorthiois, Edwige, Gerspacher, Marc, Beyer, Kim S., Vaupel, Andrea, Leblanc, Catherine, Stringer, Rowan, Weiss, Andreas, Wilcken, Rainer, Guthy, Daniel A., Lingel, Andreas, Bomio-Confaglia, Claudio, Machauer, Rainer, Rigollier, Pascal, Ottl, Johannes, Arz, Dorothee, Bernet, Pascal, Desjonqueres, Gaëlle, Dussauge, Solene, Kazic-Legueux, Malika, Lozac’h, Marie-Anne, Mura, Christophe, Sorge, Mickaël, Todorov, Milen, Warin, Nicolas, Zink, Florence, Voshol, Hans, Zecri, Frederic J., Sedrani, Richard C., Ostermann, Nils, Brachmann, Saskia M., Cotesta, Simona
Published in Journal of medicinal chemistry (22.12.2022)
Published in Journal of medicinal chemistry (22.12.2022)
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Journal Article
Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C
Weiss, Andreas, Lorthiois, Edwige, Barys, Louise, Beyer, Kim S, Bomio-Confaglia, Claudio, Burks, Heather, Chen, Xueying, Cui, Xiaoming, de Kanter, Ruben, Dharmarajan, Lekshmi, Fedele, Carmine, Gerspacher, Marc, Guthy, Daniel Alexander, Head, Victoria, Jaeger, Ashley, Núñez, Eloísa Jiménez, Kearns, Jeffrey D, Leblanc, Catherine, Maira, Sauveur-Michel, Murphy, Jason, Oakman, Helen, Ostermann, Nils, Ottl, Johannes, Rigollier, Pascal, Roman, Danielle, Schnell, Christian, Sedrani, Richard, Shimizu, Toshio, Stringer, Rowan, Vaupel, Andrea, Voshol, Hans, Wessels, Peter, Widmer, Toni, Wilcken, Rainer, Xu, Kun, Zecri, Frederic, Farago, Anna F, Cotesta, Simona, Brachmann, Saskia M
Published in Cancer discovery (02.06.2022)
Published in Cancer discovery (02.06.2022)
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Design and Biochemical Characterization of Peptidic Inhibitors of the Myb/p300 Interaction
Jones, Matthew, Grosche, Philipp, Floersheimer, Andreas, André, Jérome, Gattlen, Raphael, Oser, Dieter, Tinchant, Juliette, Wille, Roman, Chie-Leon, Barbara, Gerspacher, Marc, Ertl, Peter, Ostermann, Nils, Altmann, Eva, Manchado, Eusebio, Vorherr, Thomas, Chène, Patrick
Published in Biochemistry (Easton) (04.04.2023)
Published in Biochemistry (Easton) (04.04.2023)
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Abstract P124: JDQ443, a covalent irreversible inhibitor of KRAS G12C, exhibits a novel binding mode and demonstrates potent anti-tumor activity and favorable pharmacokinetic properties in preclinical models
Brachmann, Saskia M., Weiss, Andreas, Guthy, Daniel A., Beyer, Kim, Voshol, Johannes, Maira, Michel, Prahallad, Anirudh, Porta, Diana Graus, Schnell, Christian, Ostermann, Nils, Vaupel, Andrea, Gerspacher, Marc, Leblanc, Catherine, Erdmann, Dirk, Sterker, Dario, Kerr, Grainne, Jerome, Giovannoni, Head, Victoria, Stringer, Rowan, De Kanter, Ruben, Jeff, Kearns, Roman, Danielle, Widmer, Toni, Wessels, Peter, Nunez, Eloisa Jimenez, Sedrani, Richard, Zecri, Frederic, Hofmann, Francesco, Engleman, Jeff, Lorthiois, Edwige, Cotesta, Simona
Published in Molecular cancer therapeutics (01.12.2021)
Published in Molecular cancer therapeutics (01.12.2021)
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Journal Article
JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRAS G12C for the Treatment of Solid Tumors
Lorthiois, Edwige, Gerspacher, Marc, Beyer, Kim S, Vaupel, Andrea, Leblanc, Catherine, Stringer, Rowan, Weiss, Andreas, Wilcken, Rainer, Guthy, Daniel A, Lingel, Andreas, Bomio-Confaglia, Claudio, Machauer, Rainer, Rigollier, Pascal, Ottl, Johannes, Arz, Dorothee, Bernet, Pascal, Desjonqueres, Gaëlle, Dussauge, Solene, Kazic-Legueux, Malika, Lozac'h, Marie-Anne, Mura, Christophe, Sorge, Mickaël, Todorov, Milen, Warin, Nicolas, Zink, Florence, Voshol, Hans, Zecri, Frederic J, Sedrani, Richard C, Ostermann, Nils, Brachmann, Saskia M, Cotesta, Simona
Published in Journal of medicinal chemistry (22.12.2022)
Published in Journal of medicinal chemistry (22.12.2022)
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Synthesis and sar of a novel, potent and structurally simple LTD4 antagonist of the quinoline class
VON SPRECHER, A, GERSPACHER, M, BECK, A, KIMMEL, S, WIESTNER, H, ANDERSON, G. P, NIEDERHAUSER, U, SUBRAMANIAN, N, BRAY, M. A
Published in Bioorganic & medicinal chemistry letters (21.04.1998)
Published in Bioorganic & medicinal chemistry letters (21.04.1998)
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Discovery of a novel tricyclic 4H-thiazolo[5′,4′:4,5]pyrano[2,3-c]pyridine-2-amino scaffold and its application in a PI3Kα inhibitor with high PI3K isoform selectivity and potent cellular activity
Gerspacher, Marc, Fairhurst, Robin A., Mah, Robert, Roehn-Carnemolla, Esther, Furet, Pascal, Fritsch, Christine, Guthy, Daniel A.
Published in Bioorganic & medicinal chemistry letters (01.09.2015)
Published in Bioorganic & medicinal chemistry letters (01.09.2015)
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Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805
Baffert, Fabienne, Régnier, Catherine H, De Pover, Alain, Pissot-Soldermann, Carole, Tavares, Gisele A, Blasco, Francesca, Brueggen, Josef, Chène, Patrick, Drueckes, Peter, Erdmann, Dirk, Furet, Pascal, Gerspacher, Marc, Lang, Marc, Ledieu, David, Nolan, Lynda, Ruetz, Stephan, Trappe, Joerg, Vangrevelinghe, Eric, Wartmann, Markus, Wyder, Lorenza, Hofmann, Francesco, Radimerski, Thomas
Published in Molecular cancer therapeutics (01.07.2010)
Published in Molecular cancer therapeutics (01.07.2010)
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Journal Article
Design of two new chemotypes for inhibiting the Janus kinase 2 by scaffold morphing
Furet, Pascal, Gerspacher, Marc, Pissot-Soldermann, Carole
Published in Bioorganic & medicinal chemistry letters (15.03.2010)
Published in Bioorganic & medicinal chemistry letters (15.03.2010)
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Journal Article
Identification and optimisation of a 4′,5-bisthiazole series of selective phosphatidylinositol-3 kinase alpha inhibitors
Fairhurst, Robin A., Imbach-Weese, Patricia, Gerspacher, Marc, Caravatti, Giorgio, Furet, Pascal, Zoller, Thomas, Fritsch, Christine, Haasen, Dorothea, Trappe, Joerg, Guthy, Daniel A., Arz, Dorothee, Wirth, Jasmin
Published in Bioorganic & medicinal chemistry letters (01.09.2015)
Published in Bioorganic & medicinal chemistry letters (01.09.2015)
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Journal Article
PYRAZOLYL DERIVATIVES USEFUL AS ANTI-CANCER AGENTS
ANDREA VAUPEL, STEFAN STUTZ, MARC GERSPACHER, PASCAL RIGOLLIER, NICOLAS WARIN, SIMONA COTESTA, RAINER MACHAUER, MAH ROBERT, LIU BO, CHRISTOPHE MURA, RAINER WILCKEN, CATHERINE LEBLANC, NADINE SCHNEIDER, EDWIGE LILIANE JEANNE LORTHIOIS
Year of Publication 23.04.2024
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Year of Publication 23.04.2024
Patent
Identification and optimisation of 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole and 4,5-dihydrothiazolo[4,5-h]quinazoline series of selective phosphatidylinositol-3 kinase alpha inhibitors
Fairhurst, Robin A., Gerspacher, Marc, Imbach-Weese, Patricia, Mah, Robert, Caravatti, Giorgio, Furet, Pascal, Fritsch, Christine, Schnell, Christian, Blanz, Joachim, Blasco, Francesca, Desrayaud, Sandrine, Guthy, Daniel A., Knapp, Mark, Arz, Dorothee, Wirth, Jasmin, Roehn-Carnemolla, Esther, Luu, Van Huy
Published in Bioorganic & medicinal chemistry letters (01.09.2015)
Published in Bioorganic & medicinal chemistry letters (01.09.2015)
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Journal Article
Abstract 4026: JDQ443, a covalent inhibitor of KRASG12C with a novel binding mode, shows broad antitumor activity in KRASG12C preclinical models as a single agent and in combination with inhibitors of SHP2, MEK or CDK4/6
Weiss, Andreas, Voshol, Hans, Porta, Diana Graus, Fedele, Carmine, Sterker, Dario, De Kanter, Ruben, Stringer, Rowan, Widmer, Toni, Loo, Alice, Guthy, Daniel A., Beyer, Kim S., Ostermann, Nils, LeBlanc, Catherine, Gerspacher, Marc, Vaupel, Andrea, Sedrani, Richard, Zecri, Frederic, Maria, Saveur-Michel, Hofmann, Francesco, Hammerman, Peter, Engelman, Jeff, Lorthiois, Edwige, Cotesta, Simona, Brachmann, Saskia M.
Published in Cancer research (Chicago, Ill.) (15.06.2022)
Published in Cancer research (Chicago, Ill.) (15.06.2022)
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1-Alkyl-4-phenyl-6-alkoxy-1H-quinazolin-2-ones: A Novel Series of Potent Calcium-Sensing Receptor Antagonists
Widler, Leo, Altmann, Eva, Beerli, René, Breitenstein, Werner, Bouhelal, Rochdi, Buhl, Thomas, Gamse, Rainer, Gerspacher, Marc, Halleux, Christine, John, Markus R, Lehmann, Hansjoerg, Kalb, Oskar, Kneissel, Michaela, Missbach, Martin, Müller, Irene R, Reidemeister, Sibylle, Renaud, Johanne, Taillardat, Agnes, Tommasi, Ruben, Weiler, Sven, Wolf, Romain M, Seuwen, Klaus
Published in Journal of medicinal chemistry (11.03.2010)
Published in Journal of medicinal chemistry (11.03.2010)
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Penta-substituted benzimidazoles as potent antagonists of the calcium-sensing receptor (CaSR-antagonists)
Gerspacher, Marc, Altmann, Eva, Beerli, René, Buhl, Thomas, Endres, Ralf, Gamse, Rainer, Kameni-Tcheudji, Jacques, Kneissel, Michaela, Krawinkler, Karl Heinz, Missbach, Martin, Schmidt, Alfred, Seuwen, Klaus, Weiler, Sven, Widler, Leo
Published in Bioorganic & medicinal chemistry letters (01.09.2010)
Published in Bioorganic & medicinal chemistry letters (01.09.2010)
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Journal Article
2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors
Gerspacher, Marc, Furet, Pascal, Pissot-Soldermann, Carole, Gaul, Christoph, Holzer, Philipp, Vangrevelinghe, Eric, Lang, Marc, Erdmann, Dirk, Radimerski, Thomas, Regnier, Catherine H., Chene, Patrick, Pover, Alain De, Hofmann, Francesco, Baffert, Fabienne, Buhl, Thomas, Aichholz, Reiner, Blasco, Francesca, Endres, Ralf, Trappe, Jörg, Drueckes, Peter
Published in Bioorganic & medicinal chemistry letters (01.03.2010)
Published in Bioorganic & medicinal chemistry letters (01.03.2010)
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Journal Article
Peptidoleukotriene Antagonists State of the Art
Andreas von Sprecher, Andreas Beck, Marc Gerspacher, Michael A. Bray
Published in Chimia (01.07.1992)
Published in Chimia (01.07.1992)
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