Katharine L. Turner
Novartis
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Publication
Featured researches published by Katharine L. Turner.
Bioorganic & Medicinal Chemistry Letters | 2009
David Andrew Sandham; Claire Adcock; Kamlesh Bala; Lucy Barker; Zarin Brown; Gerald Dubois; David C. Budd; Brian Cox; Robin Alec Fairhurst; Markus Furegati; Catherine Leblanc; Jodie Manini; Rachael Profit; John Reilly; Rowan Stringer; Alfred Schmidt; Katharine L. Turner; Simon James Watson; Jennifer Willis; Gareth Williams; Caroline Wilson
High throughput screening identified a 7-azaindole-3-acetic acid scaffold as a novel CRTh2 receptor antagonist chemotype, which could be optimised to furnish a highly selective compound with good functional potency for inhibition of human eosinophil shape change in whole blood and oral bioavailability in the rat.
Bioorganic & Medicinal Chemistry | 2013
David Andrew Sandham; Nicola Arnold; Heinrich Aschauer; Kamlesh Bala; Lucy Barker; Lyndon Nigel Brown; Zarin Brown; David C. Budd; Brian Cox; Cerys Docx; Gerald Dubois; Nicholas Duggan; Karen England; Brian Everatt; Marcus Furegati; Edward Charles Hall; Frank Kalthoff; Anna King; Catherine Leblanc; Jodie Manini; Josef G. Meingassner; Rachael Profit; Alfred Schmidt; Jennifer Simmons; Bindi Sohal; Rowan Stringer; Matthew Thomas; Katharine L. Turner; Christoph Walker; Simon James Watson
Optimization of a 7-azaindole-3-acetic acid CRTh2 receptor antagonist chemotype derived from high throughput screening furnished a highly selective compound NVP-QAV680 with low nM functional potency for inhibition of CRTh2 driven human eosinophil and Th2 lymphocyte activation in vitro. The molecule exhibited good oral bioavailability in the rat, combined with efficacy in rodent CRTh2-dependent mechanistic and allergic disease models and was suitable for clinical development.
Bioorganic & Medicinal Chemistry Letters | 2002
Ruth Arnold; David Beer; Gurdip Bhalay; Urs Baettig; Stephen Paul Collingwood; Sarah Craig; Nicholas James Devereux; Andrew Dunstan; Angela Glen; Sylvie Gomez; Sandra Haberthuer; Trevor Howe; Stephen Jelfs; Heinz E. Moser; Reto Naef; Paul Leslie Nicklin; David Andrew Sandham; Rowan Stringer; Katharine L. Turner; Simon James Watson; Mauro Zurini
In clinical studies, several inhibitors of phosphodiesterase 5 (PDE5) have demonstrated utility in the treatment of erectile dysfunction. We describe herein a series of 8-aryl xanthine derivatives which function as potent PDE5 inhibitors with, in many cases, high levels of selectivity versus other PDE isoforms.
ACS Medicinal Chemistry Letters | 2017
David Andrew Sandham; Lucy Barker; Lyndon Nigel Brown; Zarin Brown; David C. Budd; Steven J. Charlton; Devnandan Chatterjee; Brian Cox; Gerald Dubois; Nicholas Duggan; Edward Charles Hall; Julia Hatto; Janet Maas; Jodie Manini; Rachael Profit; Darren M. Riddy; Catherine Ritchie; Bindi Sohal; Duncan Shaw; Rowan Stringer; David A. Sykes; Matthew Bm Thomas; Katharine L. Turner; Simon James Watson; Ryan West; Elisabeth Willard; Gareth Williams; Jennifer Willis
Further optimization of an initial DP2 receptor antagonist clinical candidate NVP-QAV680 led to the discovery of a follow-up molecule 2-(2-methyl-1-(4-(methylsulfonyl)-2-(trifluoromethyl)benzyl)-1H-pyrrolo[2,3-b]pyridin-3-yl)acetic acid (compound 11, NVP-QAW039, fevipiprant), which exhibits improved potency on human eosinophils and Th2 cells, together with a longer receptor residence time, and is currently in clinical trials for severe asthma.
ACS Medicinal Chemistry Letters | 2017
David Andrew Sandham; Lucy Barker; Lyndon Nigel Brown; Zarin Brown; David C. Budd; Steven J. Charlton; Devnandan Chatterjee; Brian Cox; Gerald Dubois; Nicholas Duggan; Edward Charles Hall; Julia Hatto; Catherine Leblanc; Janet Maas; Jodie Manini; Rachael Profit; Darren M. Riddy; Catherine Ritchie; Bindi Sohal; Duncan Shaw; Rowan Stringer; David A. Sykes; Matthew Thomas; Katharine L. Turner; Simon James Watson; Ryan West; Elisabeth Willard; Gareth Williams; Jennifer Willis
[This corrects the article DOI: 10.1021/acsmedchemlett.7b00157.].
Archive | 2004
Robin Alec Fairhurst; David Andrew Sandham; David Beattie; Ian Bruce; Bernard Cuenoud; Reamonn Madden; Neil John Press; Roger John Taylor; Katharine L. Turner; Simon James Watson
Bioorganic & Medicinal Chemistry | 2004
David Andrew Sandham; Lucy Barker; David Beattie; David Beer; Louise Bidlake; David Bentley; Keith Butler; Sarah Craig; David Farr; Claire Ffoulkes-Jones; John R. Fozard; Sandra Haberthuer; Colin Howes; Deborah Hynx; Sarah Jeffers; Thomas H. Keller; Paul Kirkham; Janet Maas; Lazzaro Mazzoni; Andrew Nicholls; Gaynor Elizabeth Pilgrim; Elisabeth Schaebulin; Gillian Spooner; Rowan Stringer; Pamela Tranter; Katharine L. Turner; Morris Tweed; Christoph Walker; Simon James Watson; Bernard Cuenoud
Archive | 2005
David Andrew Sandham; Katharine L. Turner; Catherine Leblanc
Bioorganic & Medicinal Chemistry Letters | 2007
David Andrew Sandham; Clive Aldcroft; Urs Baettig; Lucy Barker; David Beer; Gurdip Bhalay; Zarin Brown; Gerald Dubois; David C. Budd; Louise Bidlake; Emma Michelle Campbell; Brian Cox; Brian Everatt; David Bryan Harrison; Catherine Leblanc; Jodie Manini; Rachael Profit; Rowan Stringer; Katy S Thompson; Katharine L. Turner; Morris Tweed; Christopher Walker; Simon James Watson; Steven Whitebread; Jennifer Willis; Gareth Williams; Caroline Wilson
Bioorganic & Medicinal Chemistry Letters | 2012
David Beattie; David Beer; Michelle Bradley; Ian Bruce; Steven J. Charlton; Bernard Cuenoud; Robin Alec Fairhurst; David Farr; John R. Fozard; Diana Janus; Elizabeth M. Rosethorne; David Andrew Sandham; David A. Sykes; Alexandre Trifilieff; Katharine L. Turner; Elke Wissler
