Search Results - "OAKMAN, Helen"

Solubility-Driven Optimization of Phosphodiesterase‑4 Inhibitors Leading to a Clinical Candidate by Press, Neil J, Taylor, Roger J, Fullerton, Joseph D, Tranter, Pamela, McCarthy, Clive, Keller, Thomas H, Arnold, Nicola, Beer, David, Brown, Lyndon, Cheung, Robert, Christie, Julie, Denholm, Alastair, Haberthuer, Sandra, Hatto, Julia D. I, Keenan, Mark, Mercer, Mark K, Oakman, Helen, Sahri, Helene, Tuffnell, Andrew R, Tweed, Morris, Tyler, John W, Wagner, Trixie, Fozard, John R, Trifilieff, Alexandre

“…The solubility-driven optimization of a series of 1,7-napthyridine phosphodiesterase-4 inhibitors is described. Directed structural changes resulted in…”
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Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C by 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

“…Covalent inhibitors of KRASG12C have shown antitumor activity against advanced/metastatic KRASG12C-mutated cancers, though resistance emerges and additional…”
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Discovery and Optimization of 4-(8-(3-Fluorophenyl)-1,7-naphthyridin-6-yl)transcyclohexanecarboxylic Acid, an Improved PDE4 Inhibitor for the Treatment of Chronic Obstructive Pulmonary Disease (COPD) by Press, Neil J, Taylor, Roger J, Fullerton, Joseph D, Tranter, Pamela, McCarthy, Clive, Keller, Thomas H, Arnold, Nicola, Beer, David, Brown, Lyndon, Cheung, Robert, Christie, Julie, Denholm, Alastair, Haberthuer, Sandra, Hatto, Julia D I, Keenan, Mark, Mercer, Mark K, Oakman, Helen, Sahri, Helene, Tuffnell, Andrew R, Tweed, Morris, Trifilieff, Alexandre

“…Herein we describe the optimization of a series of PDE4 inhibitors, with special focus on solubility and pharamcokinetics, to clinical compound 2,…”
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Discovery and Optimization of 4‑(8-(3-Fluorophenyl)-1,7-naphthyridin-6-yl)­transcyclohexane­carboxylic Acid, an Improved PDE4 Inhibitor for the Treatment of Chronic Obstructive Pulmonary Disease (COPD) by Press, Neil J., Taylor, Roger J., Fullerton, Joseph D., Tranter, Pamela, McCarthy, Clive, Keller, Thomas H., Arnold, Nicola, Beer, David, Brown, Lyndon, Cheung, Robert, Christie, Julie, Denholm, Alastair, Haberthuer, Sandra, Hatto, Julia D. I., Keenan, Mark, Mercer, Mark K., Oakman, Helen, Sahri, Helene, Tuffnell, Andrew R., Tweed, Morris, Trifilieff, Alexandre

“…Herein we describe the optimization of a series of PDE4 inhibitors, with special focus on solubility and pharamcokinetics, to clinical compound 2,…”
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The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-acting β2-adrenoceptor agonist by Arnold, Nicola, Beattie, David, Bradley, Michelle, Brearley, Andrew, Brown, Lyndon, Charlton, Steven J., Fairhurst, Robin A., Farr, David, Fozard, John, Fullerton, Joe, Gosling, Martin, Hatto, Julia, Janus, Diana, Jones, Darryl, Jordan, Lynne, Lewis, Christine, Maas, Janet, McCarthy, Clive, Mercer, Mark, Oakman, Helen, Press, Neil, Profit, Rachel, Schuerch, Friedrich, Sykes, David, Taylor, Roger J., Trifilieff, Alexandre, Tuffnell, Andrew

“…The optimisation of two series of 4-hydroxybenzothiazolone derived β2-adrenoceptor agonists, bearing α-substituted cyclopentyl and β-phenethyl…”
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A physical properties based approach for the exploration of a 4-hydroxybenzothiazolone series of β2-adrenoceptor agonists as inhaled long-acting bronchodilators by BEATTIE, David, BRADLEY, Michelle, LEWIS, Christine, MCCARTHY, Clive, OAKMAN, Helen, STRINGER, Rowan, TAYLOR, Roger J, TUFFNELL, Andrew, BREARLEY, Andrew, CHARLTON, Steven J, CUENOUD, Bernard M, FAIRHURST, Robin A, GEDECK, Peter, GOSLING, Martin, JANUS, Diana, JONES, Darryl

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Synthesis and evaluation of two series of 4'-aza-carbocyclic nucleosides as adenosine A2A receptor agonists by BEATTIE, David, BREARLEY, Andrew, NANSON, Lana, NEEF, James, OAKMAN, Helen, SPOONER, Gillian, TAYLOR, Roger J, TURNER, Robert J, WEST, Ryan, WOODWARD, Hannah, BROWN, Zarin, CHARLTON, Steven J, COX, Brian, FAIRHURST, Robin A, FOZARD, John R, GEDECK, Peter, KIRKHAM, Paul, MEJA, Koremu

“…The synthesis of two series of 4'-aza-carbocyclic nucleosides are described in which the 4'-substituent is either a reversed amide, relative to the carboxamide…”
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Synthesis and evaluation of two series of 4'-aza-carbocyclic nucleosides as adenosine A sub(2A) receptor agonists by Beattie, David, Brearley, Andrew, Brown, Zarin, Charlton, Steven J, Cox, Brian, Fairhurst, Robin A, Fozard, John R, Gedeck, Peter, Kirkham, Paul, Meja, Koremu, Nanson, Lana, Neef, James, Oakman, Helen, Spooner, Gillian, Taylor, Roger J, Turner, Robert J, West, Ryan, Woodward, Hannah

“…The synthesis of two series of 4'-aza-carbocyclic nucleosides are described in which the 4'-substituent is either a reversed amide, relative to the carboxamide…”
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Synthesis and evaluation of two series of 4′-aza-carbocyclic nucleosides as adenosine A 2A receptor agonists by Beattie, David, Brearley, Andrew, Brown, Zarin, Charlton, Steven J., Cox, Brian, Fairhurst, Robin A., Fozard, John R., Gedeck, Peter, Kirkham, Paul, Meja, Koremu, Nanson, Lana, Neef, James, Oakman, Helen, Spooner, Gillian, Taylor, Roger J., Turner, Robert J., West, Ryan, Woodward, Hannah

“…Two series of 4′-aza-carbocyclic nucleosides are described as adenosine A 2A receptor agonists. The synthesis of two series of 4′-aza-carbocyclic nucleosides…”
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A physical properties based approach for the exploration of a 4-hydroxybenzothiazolone series of β 2-adrenoceptor agonists as inhaled long-acting bronchodilators by Beattie, David, Bradley, Michelle, Brearley, Andrew, Charlton, Steven J., Cuenoud, Bernard M., Fairhurst, Robin A., Gedeck, Peter, Gosling, Martin, Janus, Diana, Jones, Darryl, Lewis, Christine, McCarthy, Clive, Oakman, Helen, Stringer, Rowan, Taylor, Roger J., Tuffnell, Andrew

“…The chiral synthesis of a 4-hydroxybenzothiazolone based series of β 2-adrenoceptor agonists is described. Using this methodology a library of N-substituted…”
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A physical properties based approach for the exploration of a 4-hydroxybenzothiazolone series of beta2-adrenoceptor agonists as inhaled long-acting bronchodilators by Beattie, David, Bradley, Michelle, Brearley, Andrew, Charlton, Steven J, Cuenoud, Bernard M, Fairhurst, Robin A, Gedeck, Peter, Gosling, Martin, Janus, Diana, Jones, Darryl, Lewis, Christine, McCarthy, Clive, Oakman, Helen, Stringer, Rowan, Taylor, Roger J, Tuffnell, Andrew

“…The chiral synthesis of a 4-hydroxybenzothiazolone based series of beta(2)-adrenoceptor agonists is described. Using this methodology a library of…”
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