Judy Hayler
Novartis
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Publication
Featured researches published by Judy Hayler.
Bioorganic & Medicinal Chemistry Letters | 2012
Ian Bruce; Mohammed Akhlaq; Graham Charles Bloomfield; Emma Budd; Brian Cox; Bernard Cuenoud; Peter Finan; Peter Gedeck; Julia Hatto; Judy Hayler; Denise Head; Thomas H. Keller; Louise Kirman; Catherine Leblanc; Darren Le Grand; Clive Mccarthy; Desmond O’Connor; Charles Owen; Mrinalini Sachin Oza; Gaynor Elizabeth Pilgrim; Nicola Press; Lilya Sviridenko; Lewis Whitehead
Using a parallel synthesis approach to target a non-conserved region of the PI3K catalytic domain a pan-PI3K inhibitor 1 was elaborated to provide alpha, delta and gamma isoform selective Class I PI3K inhibitors 21, 24, 26 and 27. The compounds had good cellular activity and were selective against protein kinases and other members of the PI3K superfamily including mTOR and DNA-PK.
Bioorganic & Medicinal Chemistry Letters | 2000
Judy Hayler; Peter Kane; Darren Mark Legrand; Florence Lugrin; Keith Menear; Richard Price; Mark C. Allen; Xiao-Ling Fan Cockcroft; John Ambler; Keith Butler; Karren Dunnet; Andrew Mitchelson; Mark Talbot; Morris Tweed; Nicholas Wills
The further optimisation of the novel lead compound CGH752 (Fig. 1) is described. By introducing various substituents into the 6-position of the 3,3-dimethyltetrahydroquinoline (DMTHQS) ring we have been able to favourably affect the in vitro and in vivo activity, and the pharmacokinetics of such compounds. One of the inhibitors synthesised (CGH1484) is bioavailable and shows efficacy in animal models of thrombosis.
Tetrahedron Letters | 1999
Christine Bailey; Emma Baker; Judy Hayler; Peter Kane
The application of 4-methoxybenzyl-4-nitrophenylcarbonate as a reagent for the N-protection of amidinonaphthol has been demonstrated. The facile introduction of the 4-methoxybenzyloxycarbonyl group and the mildness of the deprotection conditions make this reagent well suited for the multiparallel solution phase synthesis of substituted benzamidines.
Bioorganic & Medicinal Chemistry Letters | 1999
John Ambler; Emma Baker; Dave Bentley; Lyndon Nigel Brown; Keith Butler; Paul Butler; Dave Farr; Karen Dunnet; Darren Le Grand; Judy Hayler; Diana Janus; Darryl Brynley Jones; Keith Menear; Mark Mercer; Garrick Smith; Mark Talbot; Morris Tweed
The application of selection criteria, based on potency and physicochemical parameters, to a candidate library of thrombin inhibitors is described. The utility of the approach is exemplified by the discovery of a potent, selective and bioavailable thrombin inhibitor 62.
Bioorganic & Medicinal Chemistry Letters | 1999
John Ambler; Lyndon Nigel Brown; Xiao-Ling Fan Cockcroft; Markus Grütter; Judy Hayler; Diana Janus; Darryl Brynley Jones; Peter Kane; Keith Menear; John P. Priestle; Garrick Smith; Mark Talbot; Clive Victor Walker; Bernard Wathey
The optimisation of the P2 pharmacophore in a series of thrombin inhibitors is described. The interaction of a number of piperidine P2 functionalities with lysine 60G of thrombin is explored with reference to the crystal structure of inhibitor enzyme complexes. A primary ion-dipole interaction between the terminal P2 side chain group and lysine 60G is evoked to explain the SAR in this series.
Archive | 2004
Ian Bruce; Bernard Cuenoud; Thomas H. Keller; Gaynor Elizabeth Pilgrim; Nicola Press; Grand Darren Mark Le; Cathy Ritchie; Barbara Valade; Judy Hayler; Emma Budd
Archive | 2000
Stephen Paul Collingwood; Judy Hayler; Darren Le Grand; Henri Mattes; Keith Menear; Clive Victor Walker; Xiao-Ling Fan Cockcroft
Archive | 2003
Ian Bruce; Peter Finan; Catherine Leblanc; Clive Mccarthy; Lewis Whitehead; Nicola Press; Graham Charles Bloomfield; Judy Hayler; Louise Kirman; Mrinalini Sachin Oza; Lena Shukla
Archive | 2007
Ian Bruce; Judy Hayler; Graham Charles Bloomfield; Lee Edwards; Brian Cox; Catherine Howsham
Organic Letters | 2007
Alan C. Spivey; Lena Shukla; Judy Hayler