S
Stuart L. Wells
Researcher at AstraZeneca
Publications - 11
Citations - 637
Stuart L. Wells is an academic researcher from AstraZeneca. The author has contributed to research in topics: Amination & DMPU. The author has an hindex of 7, co-authored 11 publications receiving 521 citations.
Papers
More filters
Journal ArticleDOI
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
M. Raymond V. Finlay,Mark J. Anderton,Susan Ashton,Peter Ballard,Paul A. Bethel,Matthew R. Box,Robert Hugh Bradbury,Simon J. Brown,Sam Butterworth,Andrew D. Campbell,Christopher G. Chorley,Nicola Colclough,Darren Cross,Gordon S. Currie,Matthew Grist,Lorraine A. Hassall,George B. Hill,Daniel S. James,Michael James,Paul D. Kemmitt,Teresa Klinowska,Gillian M. Lamont,Scott G. Lamont,Nathaniel G. Martin,Heather L. McFarland,Martine J. Mellor,Jonathon P. Orme,David Perkins,Paula Perkins,Graham Richmond,Peter D. Smith,Richard A. Ward,Michael J. Waring,David Whittaker,Stuart L. Wells,Gail L. Wrigley +35 more
TL;DR: Following observations of significant tumor inhibition in preclinical models, the clinical candidate AZD9291 was administered clinically to patients with T790M positive EGFR-TKI resistant NSCLC and early efficacy has been observed, accompanied by an encouraging safety profile.
Journal ArticleDOI
Dipeptidyl nitrile inhibitors of Cathepsin L.
Nabil Asaad,Paul A. Bethel,Michelle Coulson,Jack E. Dawson,Susannah J. Ford,Stefan Gerhardt,Matthew Grist,Gordon A. Hamlin,Michael James,Emma V. Jones,Galith Karoutchi,Peter W. Kenny,Andrew David Morley,Keith Oldham,Neil Rankine,David Ryan,Stuart L. Wells,Linda J. Wood,Martin Augustin,Stephan Krapp,Hannes Simader,Stefan Steinbacher +21 more
TL;DR: A series of potentCathepsin L inhibitors with good selectivity with respect to other cysteine Cathepsins is described and SAR is discussed with reference to the crystal structure of a protein-ligand complex.
Journal ArticleDOI
Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer
Robert Hugh Bradbury,David G. Acton,Nicola Broadbent,A. Nigel Brooks,Carr Gregory Richard,Glenn Hatter,Barry R. Hayter,Hill Kathryn Jane,Nicholas J. Howe,Rhys D.O. Jones,David A. Jude,Scott G. Lamont,Sarah A. Loddick,Heather L. McFarland,Zaieda Parveen,Alfred A. Rabow,Gorkhn Sharma-Singh,Natalie Stratton,Andrew G. Thomason,Dawn Trueman,Graeme Walker,Stuart L. Wells,Joanne Wilson,J. Matthew Wood +23 more
TL;DR: Clinical candidate 6-(4-{4-[2-acetylpiperazin-1-yl)-3-(trifluoromethyl)-7,8-dihydro[1,2,4]triazolo[4,3-b]pyridazine (12), designated AZD3514, that is being evaluated in a Phase I clinical trial in patients with castrate-resistant prostate cancer.
Journal ArticleDOI
Balancing hERG affinity and absorption in the discovery of AZD5672, an orally active CCR5 antagonist for the treatment of rheumatoid arthritis
John G. Cumming,Howard Tucker,John Oldfield,Colin Fielding,Adrian John Highton,Alan Wellington Faull,Martin Wild,Dearg S. Brown,Stuart L. Wells,John S. Shaw +9 more
TL;DR: Modifications to a series of potent and selective substituted 1-(3,3-diphenylpropyl)-piperidine phenylacetamide CCR5 antagonists explored with the aim of reducing affinity at the hERG cardiac ion channel led to the identification of clinical compound AZD5672 which retained excellent potency while reducing hERG affinity.
Journal ArticleDOI
A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis.
Dearg S. Brown,Andrew J. Belfield,Brown George Robert,Douglas Campbell,Alan J. Foubister,David J. Masters,Kurt Gordon Pike,Wendy L. Snelson,Stuart L. Wells +8 more
TL;DR: The rational analogue design, synthesis and structure-activity relationship of this series of bis-amide inhibitors is reported and the activity in vivo and pharmacokinetic properties are exemplified for the more potent analogues.