Zobrazeno 1 - 10
of 13
pro vyhledávání: '"Lyndon Nigel Brown"'
Autor:
Nicola Arnold, Julie Christie, Sandra Haberthuer, Roger J. Taylor, Alastair Denholm, Mark Keenan, Julia Hatto, Mark Mercer, Lyndon Nigel Brown, Clive Mccarthy, Neil John Press, Helen Oakman, Andrew R. Tuffnell, Morris Tweed, Alexandre Trifilieff, Robert Cheung, Joseph D. Fullerton, Thomas H. Keller, David Beer, Helene Sahri, Pamela Tranter
Publikováno v:
Journal of Medicinal Chemistry. 58:6747-6752
Herein we describe the optimization of a series of PDE4 inhibitors, with special focus on solubility and pharamcokinetics, to clinical compound 2, 4-(8-(3-fluorophenyl)-1,7-naphthyridin-6-yl)transcyclohexanecarboxylic acid. Although compound 2 produc
Autor:
Catherine Ritchie, Lucy Barker, Matthew Bm Thomas, Jodie Manini, Elisabeth Willard, Jennifer Willis, Zarin Brown, Edward Charles Hall, Gareth Williams, Ryan West, Steven J. Charlton, David Andrew Sandham, Lyndon Nigel Brown, Simon J. Watson, Janet Maas, Devnandan Chatterjee, David A. Sykes, Nicholas Duggan, Katharine L. Turner, Gerald Dubois, David C. Budd, Bindi Sohal, Rowan Stringer, Rachael Profit, Darren Riddy, Duncan Shaw, Julia Hatto, Brian Cox
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,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e65a3f67567222f76078480d2373e99e
https://europepmc.org/articles/PMC5430394/
https://europepmc.org/articles/PMC5430394/
Autor:
John R. Fozard, Martin Gosling, David Farr, Lynne Jordan, David A. Sykes, Darryl Brynley Jones, David Beattie, Joe Fullerton, Lyndon Nigel Brown, Julia Hatto, Rachel Profit, Mark Mercer, Diana Janus, Christine Lewis, Helen Oakman, Robin Alec Fairhurst, Friedrich Schuerch, Michelle Bradley, Nicola Arnold, Roger J. Taylor, Janet Maas, Steven J. Charlton, Andrew Brearley, Andrew R. Tuffnell, Alexandre Trifilieff, Clive Mccarthy, Neil John Press
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:4341-4347
The optimisation of two series of 4-hydroxybenzothiazolone derived β2-adrenoceptor agonists, bearing α-substituted cyclopentyl and β-phenethyl amino-substituents, as inhaled long-acting bronchodilators is described. Analogues were selected for syn
Autor:
Brian Cox, David C. Budd, Anna King, Gareth Williams, Nicholas Duggan, Rowan Stringer, Marcus Furegati, Alfred Schmidt, Josef G. Meingassner, Kamlesh Bala, Brian Everatt, Katharine L. Turner, Jennifer Simmons, Cerys Docx, Catherine Leblanc, Gerald Dubois, Frank Kalthoff, Caroline Wilson, Lucy Barker, Karen England, Nicola Arnold, John Westwick, Edward Charles Hall, Bindi Sohal, Jennifer Willis, Heinrich Aschauer, David Andrew Sandham, Rachael Profit, Zarin Brown, Lyndon Nigel Brown, Simon J. Watson, Jodie Manini, Christoph Walker, Matthew Thomas
Publikováno v:
Bioorganic & Medicinal Chemistry. 21:6582-6591
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
Autor:
Helene Sahri, Julie Christie, Neil John Press, Mark Keenan, Sandra Haberthuer, Morris Tweed, Andrew R. Tuffnell, Mark Mercer, Joseph D. Fullerton, John R. Fozard, Thomas H. Keller, Nicola Elaine Press, Lyndon Nigel Brown, Roger J. Taylor, Clive Mccarthy, Julia Hatto, Robert Cheung, Pamela Tranter
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:3081-3085
The synthesis and SAR of 5-heterocycle-substituted aminothiazole adenosine receptor antagonists is described. Several compounds show high affinity and selectivity for the A2B and A3 receptors. One compound (5f) shows good ADME properties in the rat a
Autor:
Jennifer Willis, Devnandan Chatterjee, Elisabeth Willard, Gareth Williams, Zarin Brown, Duncan Shaw, Ryan West, Edward Charles Hall, David Andrew Sandham, Bindi Sohal, Julia Hatto, Steven J. Charlton, Lucy Barker, Gerald Dubois, Janet Maas, Jodie Manini, Rowan Stringer, Nicholas Duggan, Catherine Ritchie, David C. Budd, Katharine L. Turner, Brian Cox, Catherine Leblanc, Lyndon Nigel Brown, Simon J. Watson, David A. Sykes, Matthew Thomas, Darren Riddy, Rachael Profit
Publikováno v:
ACS Medicinal Chemistry Letters. 8:987-987
Autor:
Darryl Brynley Jones, Karen Dunnet, John Ambler, Lyndon Nigel Brown, Diana Janus, Garrick Smith, Dave Bentley, Mark Mercer, Keith Menear, Dave Farr, K D Butler, Paul Butler, Morris Tweed, Emma Baker, Mark Talbot, Darren Le Grand, Judy Hayler
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:737-742
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 th
Autor:
Sandra Haberthuer, Trixie Wagner, Lyndon Nigel Brown, Julia Hatto, Nicola Arnold, Clive Mccarthy, Julie Christie, John R. Fozard, Helene Sahri, Helen Oakman, Thomas H. Keller, Roger J. Taylor, Robert Cheung, Mark Keenan, Neil John Press, Joseph D. Fullerton, Andrew R. Tuffnell, Alexandre Trifilieff, John W. Tyler, David Beer, Alastair Denholm, Morris Tweed, Mark Mercer, Pamela Tranter
Publikováno v:
Journal of medicinal chemistry. 55(17)
The solubility-driven optimization of a series of 1,7-napthyridine phosphodiesterase-4 inhibitors is described. Directed structural changes resulted in increased aqueous solubility, enabling superior pharmacokinetic properties with retention of PDE4
Publikováno v:
Journal of Polymer Science Part A: Polymer Chemistry. 28:2651-2663
Des nanoparticules stabilisees steriquement en solution aqueuse de dimensions et de polydispersite definies sont preparees par desolvatation d'un copolymere greffe methacrylate de 2-aminoethyle/ethylene oxyde. La temperature de desolvatation influenc
Autor:
Peter D. Kane, Andrew Mitchelson, Colin Dell, Lyndon Nigel Brown, Sheila Garman, Morris Tweed, Alex Furzer, Garrick Smith, Mark Talbot, Clive Victor Walker, John Ambler, Diana Janus, Urs Baettig, Derek E. Brundish, Nicholas Wills, Xiaoling Cockcroft
Publikováno v:
Bioorganicmedicinal chemistry letters. 10(14)
A series of monocyclic and bicyclic amino acids have been synthesised and incorporated into thrombin inhibitors based on CGH728, an analogue of the Mitsubishi compound MD805. Benzthiazolylalanine (Bta) was found to be a good non-polar substitute for