Zobrazeno 1 - 4
of 4
pro vyhledávání: '"Rosemary Z. Sasse"'
Autor:
Robert J. H. Austin, Christopher Patten, Eugene L. Stewart, Simon Taylor, Peter Brown, Christopher M. Yates, Davina C. Angell, Jason A. Holt, Rosemary Z. Sasse, Iain Uings, Ryan P. Trump, Jodi M. Maglich
Publikováno v:
Journal of Medicinal Chemistry. 53:4531-4544
Glucocorticoid receptor (GR) agonists have been used for more than half a century as the most effective treatment of acute and chronic inflammatory conditions despite serious side effects that accompany their extended use that include glucose intoler
Autor:
Gerard Martin Paul Giblin, Beverley Smith, Alan Naylor, James R. Musgrave, Adrian Hall, Rosemary Z. Sasse, Ishrut Hussain, Richard L. Elliott
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:1306-1311
This Letter details the SAR of a novel series of piperidine-derived gamma-secretase modulators. Compound 10h was found to be a potent modulator in vitro, which on further profiling, was found to decrease Abeta42, increase Abeta38 and have no effect o
Autor:
Simon J. F. Macdonald, Graham I. Somers, Natalie Rayner, Tony W. J. Cooper, Iain Mcfarlane Mclay, James Michael Woolven, Simon Taylor, Rosemary Z. Sasse, Gordon G. Weingarten, Diane Mary Coe, Heather A. Barnett, Tracy Jane Shipley, Iain Uings, Phil A. Skone, Torquil I. Jack, Haydn Terence Jones
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:158-162
Aryl aminopyrazole amides capped with N-alkylbenzamides 13-16 are selective glucocorticoid receptor agonists. 2,6-Disubstituted benzamides have prednisolone-like potency or better in vitro. Good oral exposure was demonstrated in the rat, with compoun
Autor:
Paul W. Smith, Poonam Shah, William Cairns, Mythily Vimal, Matilde Caivano, David Brown, Nicolas Bertheleme, Stephen P. Watson, Joseph Rimland, Iain Uings, Rosemary Z. Sasse, Pier D’Alessandro, Ryan P. Trump, Dino Montanari, David Standing, David N. Smith, David W. Gray, Sheraz Gul, Suchete S. Hunjan, Angela Dunne
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(7)
The identification of novel, potent, non-steroidal/small molecule functional GR antagonist GSK1564023A selective over PR is described. Associated structure–activity relationships and the process of optimisation of an initial HTS hit are also descri