Search Results - "Taylor, Roger J."

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 of Icenticaftor (QBW251), a Cystic Fibrosis Transmembrane Conductance Regulator Potentiator with Clinical Efficacy in Cystic Fibrosis and Chronic Obstructive Pulmonary Disease by Grand, Darren Le, Gosling, Martin, Baettig, Urs, Bahra, Parmjit, Bala, Kamlesh, Brocklehurst, Cara, Budd, Emma, Butler, Rebecca, Cheung, Atwood K, Choudhury, Hedaythul, Collingwood, Stephen P, Cox, Brian, Danahay, Henry, Edwards, Lee, Everatt, Brian, Glaenzel, Ulrike, Glotin, Anne-Lise, Groot-Kormelink, Paul, Hall, Edward, Hatto, Julia, Howsham, Catherine, Hughes, Glyn, King, Anna, Koehler, Julia, Kulkarni, Swarupa, Lightfoot, Megan, Nicholls, Ian, Page, Christopher, Pergl-Wilson, Giles, Popa, Mariana Oana, Robinson, Richard, Rowlands, David, Sharp, Tom, Spendiff, Matthew, Stanley, Emily, Steward, Oliver, Taylor, Roger J, Tranter, Pamela, Wagner, Trixie, Watson, Hazel, Williams, Gareth, Wright, Penny, Young, Alice, Sandham, David A

“…Mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) ion channel are established as the primary causative factor in the devastating lung…”
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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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A new orally bioavailable dual adenosine A2B/A3 receptor antagonist with therapeutic potential by PRESS, Neil J, TAYLOR, Roger J, HATTO, Julia D. I, KEENAN, Mark, MERCER, Mark K, PRESS, Nicola E, SAHRI, Helene, TUFFNELL, Andrew R, TWEED, Morris, FOZARD, John R, FULLERTON, Joseph D, TRANTER, Pamela, MCCARTHY, Clive, KELLER, Thomas H, BROWN, Lyndon, CHEUNG, Robert, CHRISTIE, Julie, HABERTHUER, Sandra

“…The synthesis and SAR of 5-heterocycle-substituted aminothiazole adenosine receptor antagonists is described. Several compounds show high affinity and…”
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A convergent synthesis of the renin inhibitor CGP60536B by Sandham, David A, Taylor, Roger J, Carey, John S, Fässler, Alexander

“…Pseudoephedrine serves as a dual purpose chiral auxiliary and protecting group in the synthesis of the novel orally active renin inhibitor CGP60536B…”
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Phospho-transfer catalysis: On the asymmetric hydrophosphonylation of aldehydes by Davies, Stephen R, C. Mitchell, Michael, Cain, Christopher P, Devitt, Paul G, Taylor, Roger J, Kee, Terence P

“…We report here a precise, in situ 31P{ 1H}-NMR method of assaying enantiopurity of α-hydroxyphosphonate esters, the products of the carbonyl…”
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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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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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A new orally bioavailable dual adenosine A 2B/A 3 receptor antagonist with therapeutic potential by Press, Neil J., Taylor, Roger J., Fullerton, Joseph D., Tranter, Pamela, McCarthy, Clive, Keller, Thomas H., Brown, Lyndon, Cheung, Robert, Christie, Julie, Haberthuer, Sandra, Hatto, Julia D.I., Keenan, Mark, Mercer, Mark K., Press, Nicola E., Sahri, Helene, Tuffnell, Andrew R., Tweed, Morris, Fozard, John R.

“…The synthesis and SAR of novel aminothiazoles as adenosine receptor antagonists is described, culminating in the synthesis of a potent and orally bioavailable…”
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On the hydrolysis of dimethyl-H-phosphonate. An 18O-labelling and 31P-NMR study by Mitchell, Michael C., Taylor, Roger J., Kee, Terence P.

“…Quantitative 31P-NMR examination of the hydrolysis of dimethyl-H-phosphonate using 18O-enriched water under base-catalysed conditions supports a mechanism…”
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Phospho-transfer catalysis by Davies, Stephen R, C. Mitchell, Michael, Cain, Christopher P, Devitt, Paul G, Taylor, Roger J, Kee, Terence P

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Accurate in situ 31P{1H} assay of enantiopurity in α-hydroxyphosphonate esters using a diazaphospholidine derivatizing agent by Devitt, Paul G., Mitchell, Michael C., Weetman, John M., Taylor, Roger J., Kee, Terence P.

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Accurate in situ31P{ 1H} assay of enantiopurity in α-hydroxyphosphonate esters using a diazaphospholidine derivatizing agent by Devitt, Paul G., Mitchell, Michael C., Weetman, John M., Taylor, Roger J., Kee, Terence P.

“…A rapid, convenient and efficient in situ assay of enantiomeric excess in α-hydroxyphosphonate esters is reported exploiting 31P{ 1H} NMR analysis of the…”
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