Search Results - "Bethel, Paul A."

Structure- and Reactivity-Based Development of Covalent Inhibitors of the Activating and Gatekeeper Mutant Forms of the Epidermal Growth Factor Receptor (EGFR) by Ward, Richard A, Anderton, Mark J, Ashton, Susan, Bethel, Paul A, Box, Matthew, Butterworth, Sam, Colclough, Nicola, Chorley, Christopher G, Chuaqui, Claudio, Cross, Darren A. E, Dakin, Les A, Debreczeni, Judit É, Eberlein, Cath, Finlay, M. Raymond V, Hill, George B, Grist, Matthew, Klinowska, Teresa C. M, Lane, Clare, Martin, Scott, Orme, Jonathon P, Smith, Peter, Wang, Fengjiang, Waring, Michael J

“…A novel series of small-molecule inhibitors has been developed to target the double mutant form of the epidermal growth factor receptor (EGFR) tyrosine kinase,…”
Get full text

Discovery of a Potent and Selective EGFR Inhibitor (AZD9291) of Both Sensitizing and T790M Resistance Mutations That Spares the Wild Type Form of the Receptor by Finlay, M. Raymond V, Anderton, Mark, Ashton, Susan, Ballard, Peter, Bethel, Paul A, Box, Matthew R, Bradbury, Robert H, Brown, Simon J, Butterworth, Sam, Campbell, Andrew, Chorley, Christopher, Colclough, Nicola, Cross, Darren A. E, Currie, Gordon S, Grist, Matthew, Hassall, Lorraine, Hill, George B, James, Daniel, James, Michael, Kemmitt, Paul, Klinowska, Teresa, Lamont, Gillian, Lamont, Scott G, Martin, Nathaniel, McFarland, Heather L, Mellor, Martine J, Orme, Jonathon P, Perkins, David, Perkins, Paula, Richmond, Graham, Smith, Peter, Ward, Richard A, Waring, Michael J, Whittaker, David, Wells, Stuart, Wrigley, Gail L

“…Epidermal growth factor receptor (EGFR) inhibitors have been used clinically in the treatment of non-small-cell lung cancer (NSCLC) patients harboring…”
Get full text

Thermal Stability of 2‑Butynoic Acid (Tetrolic Acid) by Ashton, Hannah, Bethel, Paul A, Cantlie, Sarah-Kate, Churchill, Trevor, Cooper, Katie, Dobson, Benjamin, Golden, Michael, Hoyle, Mark

“…Work to assess the thermal properties of 2-butynoic acid (a precursor to acalabrutinib) has revealed the potential for thermal runaway on heating; testing…”
Get full text

Synthesis of a Protected keto-Lysidine Analogue via Improved Preparation of Arabino-isoCytosine Nucleosides by Sweeney, Joseph B, Bethel, Paul A, Gill, Duncan M, Ochocińska, Agata M, Walsh, Anthony E. J, Walton, Scarlett M

“…Anhydrouridines react with aliphatic amines to give N-alkyl isocytosines, but reported procedures often demand very long reaction times and can be low…”
Get full text

Optimized scale up of 3-pyrimidinylpyrazolo[1,5-a]pyridine via Suzuki coupling; a general method of accessing a range of 3-(hetero)arylpyrazolo[1,5-a]pyridines by Bethel, Paul A., Campbell, Andrew D., Goldberg, Frederick W., Kemmitt, Paul D., Lamont, Gillian M., Suleman, Abid

“…We have developed an improved synthesis of 3-(hetero)aryl pyrazolo[1,5-a]pyridines (such as 3-(2,5-dichloropyrimidin-4-yl)pyrazolo[1,5-a]pyridine (8)) via an…”
Get full text

Novel and Versatile Synthesis of Disubstituted 1,2-Dihydro-1,2,4-triazol-3-ones by Graham, Mark A, Bethel, Paul A, Burgess, Jonathan, Fairley, Gary, Glossop, Steve C, Greenwood, Ryan D. R, Jones, Clifford D, Lovell, Scott, Swallow, Steve

“…A novel method for the synthesis of a wide range of 1,5-disubstituted 1,2-dihydro-1,2,4-triazol-3-ones is described. The key step involves a reaction between a…”
Get full text

Dipeptidyl nitrile inhibitors of Cathepsin L by Asaad, Nabil, Bethel, Paul A., Coulson, Michelle D., Dawson, Jack E., Ford, Susannah J., Gerhardt, Stefan, Grist, Matthew, Hamlin, Gordon A., James, Michael J., Jones, Emma V., Karoutchi, Galith I., Kenny, Peter W., Morley, Andrew D., Oldham, Keith, Rankine, Neil, Ryan, David, Wells, Stuart L., Wood, Linda, Augustin, Martin, Krapp, Stephan, Simader, Hannes, Steinbacher, Stefan

“…A series of potent Cathepsin L inhibitors with good selectivity with respect to other cysteine Cathepsins is described and SAR is discussed with reference to…”
Get full text

Design of selective Cathepsin inhibitors by Bethel, Paul A., Gerhardt, Stefan, Jones, Emma V., Kenny, Peter W., Karoutchi, Galith I., Morley, Andrew D., Oldham, Keith, Rankine, Neil, Augustin, Martin, Krapp, Stephan, Simader, Hannes, Steinbacher, Stefan

“…A number of molecular recognition features have been exploited in structure-based design of selective Cathepsin inhibitors…”
Get full text

Preparation of differentially substituted 3,6-diaminopyridazines under mild conditions by Bethel, Paul A., Roberts, Bryan, Bailey, Andrew

“…Although desirable from a medicinal chemistry perspective, the differentially substituted 3,6-diaminopyridazine moiety is a highly challenging target using…”
Get full text

Development of Commercial Manufacturing Processes for Acalabrutinib by Bethel, Paul A., Chan, Lai Chun, Cooper, Katie, Ensor, Gareth J., Evarts, Jerry, Garrey, Rustam, Ford, J. Gair, Harding, Daniel, Hughes, Shaun, Jackson, Lucy, Golden, Michael, Millard, Kirsty, Phillips, Andrew, Robbins, Andrew, Short, David, Telford, Alex, Whittaker, David T. E.

“…The development of processes to produce the Bruton tyrosine kinase inhibitor, acalabrutinib 1, has resulted in improvements to the yield, cycle time, and…”
Get full text