The discovery of first-in-class drugs: origins and evolution von Eder, Jörg, Sedrani, Richard, Wiesmann, Christian

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Targeted inhibition of the COP9 signalosome for treatment of cancer von Schlierf, Anita, Altmann, Eva, Quancard, Jean, Jefferson, Anne B., Assenberg, René, Renatus, Martin, Jones, Matthew, Hassiepen, Ulrich, Schaefer, Michael, Kiffe, Michael, Weiss, Andreas, Wiesmann, Christian, Sedrani, Richard, Eder, Jörg, Martoglio, Bruno

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JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRASG12C for the Treatment of Solid Tumors von 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

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Derivation of Rapamycin: Adventures in Natural Product Chemistry von Cottens, Sylvain, Kallen, Jörg, Schuler, Walter, Sedrani, Richard

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JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRAS G12C for the Treatment of Solid Tumors von 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

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Direct Renin Inhibitors as a New Therapy for Hypertension von Webb, Randy L, Schiering, Nikolaus, Sedrani, Richard, Maibaum, Jürgen

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Discovery of 3-(1H-Indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione (AEB071), a Potent and Selective Inhibitor of Protein Kinase C Isotypes von Wagner, Jürgen, von Matt, Peter, Sedrani, Richard, Albert, Rainer, Cooke, Nigel, Ehrhardt, Claus, Geiser, Martin, Rummel, Gabriele, Stark, Wilhelm, Strauss, Andre, Cowan-Jacob, Sandra W, Beerli, Christian, Weckbecker, Gisbert, Evenou, Jean-Pierre, Zenke, Gerhard, Cottens, Sylvain

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Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes von Sutton, Jon M., Clark, David E., Dunsdon, Stephen J., Fenton, Garry, Fillmore, Amanda, Harris, Neil V., Higgs, Chris, Hurley, Chris A., Krintel, Sussie L., MacKenzie, Robert E., Duttaroy, Alokesh, Gangl, Eric, Maniara, Wiesia, Sedrani, Richard, Namoto, Kenji, Ostermann, Nils, Gerhartz, Bernd, Sirockin, Finton, Trappe, Jörg, Hassiepen, Ulrich, Baeschlin, Daniel K.

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Discovery of C-(1-aryl-cyclohexyl)-methylamines as selective, orally available inhibitors of dipeptidyl peptidase IV von Namoto, Kenji, Sirockin, Finton, Ostermann, Nils, Gessier, Francois, Flohr, Stefanie, Sedrani, Richard, Gerhartz, Bernd, Trappe, Jörg, Hassiepen, Ulrich, Duttaroy, Alokesh, Ferreira, Suzie, Sutton, Jon M., Clark, David E., Fenton, Garry, Beswick, Mandy, Baeschlin, Daniel K.

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Structure of Human Cyclophilin A in Complex with the Novel Immunosuppressant Sanglifehrin A at 1.6 Å Resolution von Kallen, Joerg, Sedrani, Richard, Zenke, Gerhard, Wagner, Juergen

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Small-molecule factor B inhibitor for the treatment of complement-mediated diseases von Schubart, Anna, Anderson, Karen, Mainolfi, Nello, Sellner, Holger, Ehara, Takeru, Adams, Christopher M., Sweeney, Aengus Mac, Liao, Sha-Mei, Crowley, Maura, Littlewood-Evans, Amanda, Sarret, Sophie, Wieczorek, Grazyna, Perrot, Ludovic, Dubost, Valérie, Flandre, Thierry, Zhang, Yuzhou, Smith, Richard J. H., Risitano, Antonio M., Karki, Rajeshri G., Zhang, Chun, Valeur, Eric, Sirockin, Finton, Gerhartz, Bernd, Erbel, Paulus, Hughes, Nicola, Smith, Thomas M., Cumin, Frederic, Argikar, Upendra A., Haraldsson, Börje, Mogi, Muneto, Sedrani, Richard, Wiesmann, Christian, Jaffee, Bruce, Maibaum, Jürgen, Flohr, Stefanie, Harrison, Richard, Eder, Jörg

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Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C von 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

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Discovery of 4-((2 S ,4 S )-4-Ethoxy-1-((5-methoxy-7-methyl-1 H -indol-4-yl)methyl)piperidin-2-yl)benzoic Acid (LNP023), a Factor B Inhibitor Specifically Designed To Be Applicable... von Mainolfi, Nello, Ehara, Takeru, Karki, Rajeshri G, Anderson, Karen, Mac Sweeney, Aengus, Liao, Sha-Mei, Argikar, Upendra A, Jendza, Keith, Zhang, Chun, Powers, James, Klosowski, Daniel W, Crowley, Maura, Kawanami, Toshio, Ding, Jian, April, Myriam, Forster, Cornelia, Serrano-Wu, Michael, Capparelli, Michael, Ramqaj, Rrezarta, Solovay, Catherine, Cumin, Frederic, Smith, Thomas M, Ferrara, Luciana, Lee, Wendy, Long, Debby, Prentiss, Melissa, De Erkenez, Andrea, Yang, Louis, Liu, Fang, Sellner, Holger, Sirockin, Finton, Valeur, Eric, Erbel, Paulus, Ostermeier, Daniela, Ramage, Paul, Gerhartz, Bernd, Schubart, Anna, Flohr, Stefanie, Gradoux, Nathalie, Feifel, Roland, Vogg, Barbara, Wiesmann, Christian, Maibaum, Jürgen, Eder, Jörg, Sedrani, Richard, Harrison, Richard A, Mogi, Muneto, Jaffee, Bruce D, Adams, Christopher M

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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 prope... von 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

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Structure-Based Design and Preclinical Characterization of Selective and Orally Bioavailable Factor XIa Inhibitors: Demonstrating the Power of an Integrated S1 Protease Family Appr... von Lorthiois, Edwige, Roache, James, Barnes-Seeman, David, Altmann, Eva, Hassiepen, Ulrich, Turner, Gordon, Duvadie, Rohit, Hornak, Viktor, Karki, Rajeshri G, Schiering, Nikolaus, Weihofen, Wilhelm A, Perruccio, Francesca, Calhoun, Amy, Fazal, Tanzina, Dedic, Darija, Durand, Corinne, Dussauge, Solene, Fettis, Kamal, Tritsch, Fabien, Dentel, Celine, Druet, Adelaide, Liu, Donglei, Kirman, Louise, Lachal, Julie, Namoto, Kenji, Bevan, Douglas, Mo, Rose, Monnet, Gabriela, Muller, Lionel, Zessis, Richard, Huang, Xueming, Lindsley, Loren, Currie, Treeve, Chiu, Yu-Hsin, Fridrich, Cary, Delgado, Peter, Wang, Shuangxi, Hollis-Symynkywicz, Micah, Berghausen, Joerg, Williams, Eric, Liu, Hong, Liang, Guiqing, Kim, Hyungchul, Hoffmann, Peter, Hein, Andreas, Ramage, Paul, D’Arcy, Allan, Harlfinger, Stefanie, Renatus, Martin, Ruedisser, Simon, Feldman, David, Elliott, Jason, Sedrani, Richard, Maibaum, Juergen, Adams, Christopher M

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Dynamic conformational equilibria in the active states of KRAS and NRAS von Rennella, Enrico, Henry, Chrystèle, Dickson, Callum J, Georgescauld, Florian, Wales, Thomas E, Erdmann, Dirk, Cotesta, Simona, Maira, Michel, Sedrani, Richard, Brachmann, Saskia M, Ostermann, Nils, Engen, John R, Kay, Lewis E, Beyer, Kim S, Wilcken, Rainer, Jahnke, Wolfgang

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Structure–Activity Relationship and Pharmacokinetic Studies of Sotrastaurin (AEB071), a Promising Novel Medicine for Prevention of Graft Rejection and Treatment of Psoriasis von Wagner, Jürgen, von Matt, Peter, Faller, Bernard, Cooke, Nigel G, Albert, Rainer, Sedrani, Richard, Wiegand, Hansjörg, Jean, Christian, Beerli, Christian, Weckbecker, Gisbert, Evenou, Jean-Pierre, Zenke, Gerhard, Cottens, Sylvain

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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 combinatio... von 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.

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A Novel Class of Oral Direct Renin Inhibitors: Highly Potent 3,5-Disubstituted Piperidines Bearing a Tricyclic P 3 – P 1 Pharmacophore von Ostermann, Nils, Ruedisser, Simon, Ehrhardt, Claus, Breitenstein, Werner, Marzinzik, Andreas, Jacoby, Edgar, Vangrevelinghe, Eric, Ottl, Johannes, Klumpp, Martin, Hartwieg, J. Constanze D., Cumin, Frederic, Hassiepen, Ulrich, Trappe, Jörg, Sedrani, Richard, Geisse, Sabine, Gerhartz, Bernd, Richert, Paul, Francotte, Eric, Wagner, Trixie, Krömer, Markus, Kosaka, Takatoshi, Webb, Randy L., Rigel, Dean F., Maibaum, Jürgen, Baeschlin, Daniel K.

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SDZ RAD, a new rapamycin derivative : Pharmacological properties in vitro and in vivo von SCHULER, W, SEDRANI, R, COTTENS, S, HÄBERLIN, B, SCHULZ, M, SCHUURMAN, H.-J, ZENKE, G, ZERWES, H.-G, SCHREIER, M. H

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