Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Joseph D. Fullerton"'
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3f1713cba513710940b786b9defedf19
https://doi.org/10.1021/acs.jmedchem.5b00902
https://doi.org/10.1021/acs.jmedchem.5b00902
Autor:
Robin Alec Fairhurst, Joseph D. Fullerton, David Andrew Sandham, Heinz E. Moser, Mauro Zurini, Sandra Haberthuer, Darryl Brynley Jones, Mark Dodds, Julia Hatto, Gurdip Bhalay, Colin Howes, Paul Nicklin, Simon J. Watson, David Farr, Reto Naef, Irene Muller, Andrew Dunstan, Nichola J. Arnold, Nicholas James Devereux, Morris Tweed, Angela Glen, Katharine L. Turner, Beate Leuenberger, David Beer, Sylvie Gomez, Ruth Arnold, Thomas H. Keller, Stephen Paul Collingwood, Sarah Craig
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:2376-2379
Inhibitors of PDE5 are useful therapeutic agents for treatment of erectile dysfunction. A series of novel xanthine derivatives has been identified as potent inhibitors of PDE5, with good levels of selectivity against other PDE isoforms, including PDE
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1e21375e8e7ea71d3deb6323b8cc3fb4
https://doi.org/10.1016/j.bmcl.2006.11.019
https://doi.org/10.1016/j.bmcl.2006.11.019
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3947523839cef2983228f572e9013e7c
https://doi.org/10.1016/j.bmcl.2005.04.021
https://doi.org/10.1016/j.bmcl.2005.04.021
Autor:
Graham Arton Howarth, Talbot, Judy Hayler, Garrick Smith, Derek E. Brundish, Wakeford R, John Ambler, Mark C. Allen, Joseph D. Fullerton, Peter D. Kane, Christoph Walker, Sheila Garman, Donovan, Bull A, K D Butler, William Hoyle, Diana Janus, McDonnell M
Publikováno v:
Journal of Medicinal Chemistry. 42:4584-4603
Mitsubishi's MD-805, a potent and selective inhibitor of thrombin which contains four stereogenic centers, has been the starting point for an optimization program. A systematic synthetic study resulted in thrombin inhibitors achiral at P2 and P3 but
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6622861e59d1bf122b24db6df96f42fb
https://doi.org/10.1021/jm9811209
https://doi.org/10.1021/jm9811209
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::817ed3d0e78a77ec4c0cc42ee5087e6b
https://pubmed.ncbi.nlm.nih.gov/22889281
https://pubmed.ncbi.nlm.nih.gov/22889281
Publikováno v:
Journal of the Chemical Society, Perkin Transactions 1. :1759
N-Aryl 1-naphthyl nitroxides self-react in solution to give the corresponding secondary amines and N-aryl-1,4-naphthoquinone imines. When reaction at the 4-naphthyl position is hindered by substituents benzoquinone imines are also produced. N-Phenyl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c2fc1ce481e1eca36a47904223c45166
https://doi.org/10.1039/p19830001759
https://doi.org/10.1039/p19830001759
Publikováno v:
Journal of the Chemical Society, Perkin Transactions 1. :989
The syntheses are described of cyclo-{[D-Trp8,Gaba12]somatostatin-(5–12)-peptide}(77), and (79)–(82) labelled singly at positions 6, 7, 8, and 11 and doubly at residues 6 and 11 to specific radioactivities of between 4.8 and 22.4 Ci mmol–1. The
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::4704b35e4a90bda82693369eecb57f3e
https://doi.org/10.1039/p19860000989
https://doi.org/10.1039/p19860000989
Publikováno v:
Journal of the Chemical Society, Perkin Transactions 1. :2711
Comparison is made between products obtained by oxidation of N-phenyl-1-naphthylamines and 1-naphthyl phenyl nitroxides with peroxyl radicals. It is concluded that oxidation of the amines does not proceed to a considerable extent via the nitroxides.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1acfb06343ee3896c74ff51373a3206c
https://doi.org/10.1039/p19830002711
https://doi.org/10.1039/p19830002711
Publikováno v:
Journal of the Chemical Society, Perkin Transactions 2. :1481
The e.s.r. spectra of a series of naphth-1-yl phenyl nitroxides have been interpreted with the aid of complementary n.m.r. measurements. McLachlan MO calculations on naphth-1-yl phenyl nitroxide gives values for the naphthyl proton coupling constants
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ba8085d93ed88374ebe57ad147f65480
https://doi.org/10.1039/p29830001481
https://doi.org/10.1039/p29830001481
Publikováno v:
Journal of the Chemical Society, Perkin Transactions 2. :1477
Rate constants for the reaction of a series of N-phenylnaphth-1-ylamines and some related nitroxides and hydroxylamines with t-alkylperoxyl radicals have been measured using kinetic e.s.r. spectrometry and activation energies and A factors have been
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::979cdb71cb5dad6316dd5dc2d4dc5be4
https://doi.org/10.1039/p29830001477
https://doi.org/10.1039/p29830001477