Verity Margaret Sabin

George M. Buckley; Richard Fosbeary; Joanne L. Fraser; Lewis Gowers; Alicia P. Higueruelo; Lynwen James; Kerry Jenkins; Stephen R. Mack; Trevor Morgan; David M. Parry; William R. Pitt; Oliver Rausch; Marianna Dilani Richard; Verity Margaret Sabin

Following the identification of a potent IRAK inhibitor through routine project cross screening, a novel class of IRAK-4 inhibitor was established. The SAR of imidazo[1,2-a]pyridino-pyridines and benzimidazolo-pyridines was explored.

George M. Buckley; Thomas A. Ceska; Joanne L. Fraser; Lewis Gowers; Colin R. Groom; Alicia P. Higueruelo; Kerry Jenkins; Stephen R. Mack; Trevor Morgan; David M. Parry; William R. Pitt; Oliver Rausch; Marianna Dilani Richard; Verity Margaret Sabin

A potent IRAK-4 inhibitor was identified through routine project cross screening. The binding mode was inferred using a combination of in silico docking into an IRAK-4 homology model, surrogate crystal structure analysis and chemical analogue SAR.

George M. Buckley; Lewis Gowers; Alicia P. Higueruelo; Kerry Jenkins; Stephen R. Mack; Trevor Morgan; David M. Parry; William R. Pitt; Oliver Rausch; Marianna Dilani Richard; Verity Margaret Sabin; Joanne L. Fraser

The synthesis and profile of a series of amides are described. Some of these compounds were potent IRAK-4 inhibitors and two examples were evaluated in vivo.

Nicolas Briet; Michael H. Brookes; Richard John Davenport; Frances Celia Anne Galvin; Philip J. Gilbert; Stephen R. Mack; Verity Margaret Sabin

A series of novel substituted isoquinolones have been synthesised. This has been achieved by two routes, either Curtius rearrangment of cinnamic acids or via an isoquinoline N-oxide.

M. Motasim Billah; Nicola Cooper; Francis M. Cuss; Richard John Davenport; Hazel Joan Dyke; Robert W. Egan; Ashit K. Ganguly; Lewis Gowers; Duncan Hannah; Alan Findlay Haughan; Hannah Jayne Kendall; Christopher Lowe; Michael Minnicozzi; John Gary Montana; Robert J. Naylor; Janet Oxford; Joanna C. Peake; John J. Piwinski; Karen Ann Runcie; Verity Margaret Sabin; Andrew Sharpe; Neng-Yang Shih; Julie B.H. Warneck

The syntheses and pharmacological profiles of some 2-trifluoromethyl-8-methoxyquinoline-5-carboxamides are described. SCH351591 is a potent selective inhibitor of phosphodiesterase type 4 (PDE4).

M. Motasim Billah; George M. Buckley; Nicola Cooper; Hazel Joan Dyke; Robert W. Egan; Ashit K. Ganguly; Lewis Gowers; Alan Findlay Haughan; Hannah Jayne Kendall; Christopher Lowe; Michael Minnicozzi; John Gary Montana; Janet Oxford; Joanna C. Peake; C.Louise Picken; John J. Piwinski; Robert J. Naylor; Verity Margaret Sabin; Neng-Yang Shih; Julie B.H. Warneck

The synthesis and pharmacological profile of a novel series of 2-substituted 8-methoxyquinolines is described. The 2-trifluoromethyl compound was found to be a potent inhibitor of phosphodiesterase type 4 (PDE4).

Benjamin Perry; Rikki Peter Alexander; Gavin Bennett; George M. Buckley; Tom Ceska; Tom Crabbe; Verity Q Dale; Lewis Gowers; Helen Tracey Horsley; Lynwen James; Kerry Jenkins; Karen Viviane Lucile Crépy; Claire Louise Kulisa; Helen Lightfoot; Chris Lock; Stephen R. Mack; Trevor Morgan; Anne-Lise Nicolas; Will R. Pitt; Verity Margaret Sabin; Sara Wright

The SAR and pharmacokinetic profiles of a series of multi-isoform PI3K inhibitors based on a 3,4-dihydro-2H-benzo[1,4]oxazine scaffold are disclosed.

Eileen Mary Seward; Christopher John Swain; Kevin John Merchant; Simon Neil Owen; Verity Margaret Sabin; Margaret A. Cascieri; Sharon Sadowski; Catherine D. Strader; Raymond Baker

Abstract A series of 3-benzyloxy-derivatives of CP-96,345 has been evaluated and found to have significant affinity for the human NK1 receptor. 3,5-Disubstitution of the benzyl ether has been identified to be essential for high affinity.

George M. Buckley; Nicola Cooper; Richard John Davenport; Hazel Joan Dyke; Fiona P. Galleway; Lewis Gowers; Alan Findlay Haughan; Hannah Jayne Kendall; Christopher Lowe; John Gary Montana; Janet Oxford; Joanna C. Peake; C.Louise Picken; Marianna Dilani Richard; Verity Margaret Sabin; Andrew Sharpe; Julie B.H. Warneck

The synthesis and pharmacological profile of a novel series of 7-methoxy-furo[2,3-c]pyridine-4-carboxamides is described. Some of these compounds were found to be potent inhibitors of phosphodiesterase type 4 (PDE4).

George M. Buckley; Nicola Cooper; Hazel Joan Dyke; Fiona P. Galleway; Lewis Gowers; Joanna C Gregory; Duncan R Hannah; Alan Findlay Haughan; Paul G. Hellewell; Hannah Jayne Kendall; Christopher Lowe; Robert James Maxey; John Gary Montana; Robert J. Naylor; C.Louise Picken; Karen Ann Runcie; Verity Margaret Sabin; Bishwa R Tuladhar; Julie B.H. Warneck

The synthesis and pharmacological profile of a novel series of 7-methoxybenzofuran-4-carboxamides is described. Some of these compounds were found to be potent inhibitors of phosphodiesterase type 4 (PDE4).