Zobrazeno 1 - 2
of 2
pro vyhledávání: '"Suzanne Elaine Keeling"'
Autor:
Lisa E. Ranshaw, Tracy Jane Shipley, Suzanne Elaine Keeling, Colin David Eldred, Nicola Mary Aston, B. Judkins, Ed Robinson, Kam Gohil, Naimisha Trivedi, Christopher James Lunniss, Andy Craven
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:137-140
Species specific conversion of the lead PDE4 inhibitor 1 to the quinolone 3 was identified as the major route of metabolism in the cynomolgus monkey. Modification of the template to give the cinnoline 9 retained potency and selectivity, and greatly i
Autor:
Fiona S. Lucas, Anthony William James Cooper, Ed Robinson, Ian Robert Baldwin, Charlotte J. Hardy, Giovanni Vitulli, Suzanne Elaine Keeling, Daniel Thomas, Joelle Le, Christopher James Lunniss, Sarah Smith, Zoe Alicia Harrison, Angela M. Deakin, Augustin Amour, Stefano Livia, Stephen Barry Guntrip, Yoshiaki Washio, Leigh M. Felton, Katherine Louise Jones, Nigel J. Parr, Kenneth David Down, Paul Jones, J. Nicole Hamblin, Paul Rowland
Publikováno v:
Journal of medicinal chemistry. 58(18)
Optimization of lead compound 1, through extensive use of structure-based design and a focus on PI3Kδ potency, isoform selectivity, and inhaled PK properties, led to the discovery of clinical candidates 2 (GSK2269557) and 3 (GSK2292767) for the trea