Antitumor Activity of Osimertinib, an Irreversible Mutant-Selective EGFR Tyrosine Kinase Inhibitor, in NSCLC Harboring EGFR Exon 20 Insertions von Floc'h, Nicolas, Martin, Matthew J, Riess, Jonathan W, Orme, Jonathan P, Staniszewska, Anna D, Ménard, Ludovic, Cuomo, Maria Emanuela, O'Neill, Daniel J, Ward, Richard A, Finlay, M Raymond V, McKerrecher, Darren, Cheng, Mingshan, Vang, Daniel P, Burich, Rebekah A, Keck, James G, Gandara, David R, Mack, Philip C, Cross, Darren A E

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Use of Small-Molecule Crystal Structures To Address Solubility in a Novel Series of G Protein Coupled Receptor 119 Agonists: Optimization of a Lead and in Vivo Evaluation von Scott, James S, Birch, Alan M, Brocklehurst, Katy J, Broo, Anders, Brown, Hayley S, Butlin, Roger J, Clarke, David S, Davidsson, Öjvind, Ertan, Anne, Goldberg, Kristin, Groombridge, Sam D, Hudson, Julian A, Laber, David, Leach, Andrew G, MacFaul, Philip A, McKerrecher, Darren, Pickup, Adrian, Schofield, Paul, Svensson, Per H, Sörme, Pernilla, Teague, Joanne

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Challenges and Opportunities in Cancer Drug Resistance von Ward, Richard A, Fawell, Stephen, Floc’h, Nicolas, Flemington, Vikki, McKerrecher, Darren, Smith, Paul D

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The First Example of Simple Oxidative Addition of an Aryl Chloride to a Discrete Palladium N-Heterocyclic Carbene Amination Precatalyst von Caddick, Stephen, Cloke, F. Geoffrey N, Hitchcock, Peter B, Leonard, John, Lewis, Alexandra K. de K, McKerrecher, Darren, Titcomb, Lisa R

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Potent and Selective Inhibitors of the Epidermal Growth Factor Receptor to Overcome C797S-Mediated Resistance von Finlay, M. Raymond V, Barton, Peter, Bickerton, Sue, Bista, Michal, Colclough, Nicola, Cross, Darren A. E, Evans, Laura, Floc’h, Nicolas, Gregson, Clare, Guérot, Carine M, Hargreaves, David, Kang, Xiaoming, Lenz, Eva M, Li, Xu, Liu, Yi, Lorthioir, Olivier, Martin, Matthew J, McKerrecher, Darren, McWhirter, Claire, O’Neill, Daniel, Orme, Jonathan P, Mosallanejad, Arash, Rahi, Amar, Smith, Paul D, Talbot, Verity, Ward, Richard A, Wrigley, Gail, Wylot, Marta, Xue, Lin, Yao, Tieguang, Ye, Yang, Zhao, Xiliang

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Abstract 4451: Evaluation of the therapeutic potential of phosphine oxide pyrazole inhibitors in tumors harboring EGFR C797S mutation von Floch, Nicolas, Finlay, M. Raymond V., Bianco, Ambra, Bickerton, Sue, Colclough, Nicola, Cross, Darren A., Cuomo, Emanuela M., Guerot, Carine M., Hargreaves, David, Martin, Matthew J., McKerrecher, Darren, O’Neill, Daniel J., Orme, Jonathan P., Rahi, Amar, Smith, Paul D., Ward, Richard A.

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Abstract 4813: Comparative activity profiling of tyrosine kinase inhibitors (TKIs) against exon 20 insertions and the wild-type form of epidermal growth factor receptor (EGFR) von Ward, Richard A., Bianco, Ambra, Colclough, Nicola, Cross, Darren, Cuomo, Emanuela M., Finlay, M. Raymond V., Fitzek, Martina, Floc’h, Nicolas, Gagrica, Sladjana, Hammond, Beverley, Martin, Matthew J., McKerrecher, Darren, O’Neill, Daniel J., Orme, Jonathan P., Smith, Paul D., Staniszewska, Anna D., Urosevic, Jelena, Whalley, Nicky, Yates, James W.

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Circumventing Seizure Activity in a Series of G Protein Coupled Receptor 119 (GPR119) Agonists von Scott, James S, Bowker, Suzanne S, Brocklehurst, Katy J, Brown, Hayley S, Clarke, David S, Easter, Alison, Ertan, Anne, Goldberg, Kristin, Hudson, Julian A, Kavanagh, Stefan, Laber, David, Leach, Andrew G, MacFaul, Philip A, Martin, Elizabeth A, McKerrecher, Darren, Schofield, Paul, Svensson, Per H, Teague, Joanne

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Anti-tumor activity of osimertinib, an irreversible mutant-selective EGFR tyrosine kinase inhibitor, in NSCLC harboring EGFR Exon 20 Insertions von Floc’h, Nicolas, Martin, Matthew J., Riess, Jonathan W., Orme, Jonathan P., Staniszewska, Anna D., Menard, Ludovic, Cuomo, Maria Emanuela, O'Neill, Daniel J, Ward, Richard A., Finlay, M. Raymond V., McKerrecher, Darren, Cheng, Mingshan, Vang, Daniel P, Tsai, Rebekah A., Keck, James G., Gandara, David R., Mack, Philip C., Cross, Darren, AE

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Abstract 2079: Osimertinib, an irreversible mutant selective EGFR tyrosine kinase inhibitor, exerts anti tumor activity in NSCLC harbouring exon 20 insertion mutant-EGFR von Floc'h, Nicolas, Ashton, Susan, Bianco, Ambra, Colclough, Nicola, Cross, Darren AE, Cuomo, Maria Emanuela, Finlay, M. Raymond V., Martin, Matthew J, Menard, Ludovic, McKerrecher, Darren, O'Neill, Daniel J, Orme, Jonathan P, Staniszewska, Anna D, Ward, Richard A, Yates, James W T

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Antitumor activity of osimertinib in NSCLC harboring EGFR exon 20 insertions von Riess, Jonathan, Floch, Nicolas, Martin, Matthew, Orme, Jonathon, Staniszewska, Anna, Menard, Ludovic, Cuomo, Maria Emanuela, O'Neill, Daniel, Ward, Richard, Finlay, Raymond, McKerrecher, Darren, Cheng, Mingshan, Vang, Daniel, Tsai, Rebekah, Ye, Chunting, Keck, James G., Gandara, David R., Mack, Philip C., Cross, Darren

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A chemistry wiki to facilitate and enhance compound design in drug discovery von Robb, Graeme R., McKerrecher, Darren, Newcombe, Nicholas J., Waring, Mike J.

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Unexpected reactivity of two-coordinate palladium–carbene complexes; synthetic and catalytic implications von Titcomb, Lisa R., Caddick, Stephen, Cloke, F. Geoffrey N., Wilson, D. James, McKerrecher, Darren

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Matrix-based multiparameter optimisation of glucokinase activators: the discovery of AZD1092 von Waring, Michael J., Johnstone, Craig, McKerrecher, Darren, Pike, Kurt G., Robb, Graeme

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Design of a potent, soluble glucokinase activator with excellent in vivo efficacy von McKerrecher, Darren, Allen, Joanne V., Caulkett, Peter W.R., Donald, Craig S., Fenwick, Mark L., Grange, Emma, Johnson, Keith M., Johnstone, Craig, Jones, Clifford D., Pike, Kurt G., Rayner, John W., Walker, Rolf P.

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Conformational restriction in a series of GPR119 agonists: Differences in pharmacology between mouse and human von Scott, James S., Brocklehurst, Katy J., Brown, Hayley S., Clarke, David S., Coe, Helen, Groombridge, Sam D., Laber, David, MacFaul, Philip A., McKerrecher, Darren, Schofield, Paul

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Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life von Pike, Kurt G., Allen, Joanne V., Caulkett, Peter W.R., Clarke, David S., Donald, Craig S., Fenwick, Mark L., Johnson, Keith M., Johnstone, Craig, McKerrecher, Darren, Rayner, John W., Walker, Rolf P., Wilson, Ingrid

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Property based optimisation of glucokinase activators – discovery of the phase IIb clinical candidate AZD1656 von Waring, Michael J., Clarke, David S., Fenwick, Mark D., Godfrey, Linda, Groombridge, Sam D., Johnstone, Craig, McKerrecher, Darren, Pike, Kurt G., Rayner, John W., Robb, Graeme R., Wilson, Ingrid

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Dissociated non-steroidal glucocorticoid receptor modulators: an update on new compounds von Schäcke, Heike, Berger, Markus, Hansson, Thomas G, McKerrecher, Darren, Rehwinkel, Hartmut

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An improved synthesis of bis(1,3-di- N- tert-butylimidazol-2-ylidene)palladium(0) and its use in C–C and C–N coupling reactions von Caddick, Stephen, Cloke, F.Geoffrey N., Clentsmith, Guy K.B., Hitchcock, Peter B., McKerrecher, Darren, Titcomb, Lisa R., Williams, Meredith R.V.

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