Michael Bryan Roe
Ferring Pharmaceuticals
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Publication
Featured researches published by Michael Bryan Roe.
Bioorganic & Medicinal Chemistry Letters | 1999
Michael Bryan Roe; Adrian John Folkes; Philip Anthony Ashworth; Julie Elizabeth Brumwell; Lal Chima; Sukhjit Hunjan; Ian Andrew Pretswell; Wendy Dangerfield; Hamish Ryder; Peter Charlton
We have synthesised and evaluated a series of anthranilamide based modulators of P-glycoprotein. These studies have identified XR9576(2), a potent inhibitor of P-glycoprotein in vitro and in vivo. The general synthesis and the SAR of these compounds are described.
Bioorganic & Medicinal Chemistry Letters | 2001
Adrian Folkes; Michael Bryan Roe; Sukhjit Sohal; Julian Golec; Richard Faint; Teresa Brooks; Peter Charlton
We have synthesized and evaluated a series of diketopiperazine-based inhibitors of PAI-1. These studies resulted in the identification of 34 which inhibited PAI-1 in vitro with an IC(50)=0.2 microM. The synthesis and SAR of these compounds are described.
Journal of Medicinal Chemistry | 2008
Christopher M. Yea; Christine Elizabeth Allan; Doreen Mary Ashworth; James Barnett; Andy J. Baxter; Janice D. Broadbridge; Richard Jeremy Franklin; Sally L. Hampton; Peter Hudson; John Horton; Paul D. Jenkins; Andy M. Penson; Gary Robert William Pitt; Pierre Riviere; Peter A. Robson; David Philip Rooker; Graeme Semple; Andrew Sheppard; Robert Haigh; Michael Bryan Roe
Vasopressin (AVP) is a hormone that stimulates an increase in water permeability through activation of V2 receptors in the kidney. The analogue of AVP, desmopressin, has proven an effective drug for diseases where a reduction of urine output is desired. However, its peptidic nature limits its bioavailability. We report herein the discovery of potent, nonpeptidic, benzylurea derived agonists of the vasopressin V2 receptor. We describe substitutions on the benzyl group to give improvements in potency and subsequent modifications to the urea end group to provide improvements in solubility and increased oral efficacy in a rat model of diuresis. The lead compound 20e (VA106483) is reported for the first time and has been selected for clinical development.
Tetrahedron | 2002
Nicolas Willand; Jurgen Joossens; Jean-Claude Gesquière; André Tartar; D.Michael Evans; Michael Bryan Roe
DPP-IV inhibitors have been suggested as potential new treatments for type-II diabetes and 2-cyanopyrrolidides have been reported as potent DPP-IV inhibitors. Alternative synthetic approaches to one such compound, NVP-DPP728, are investigated here. One strategy is based in solution phase and is amenable to scale-up. The other is based on solid phase and is appropriate for the rapid analoging of the structural series.
Bioorganic & Medicinal Chemistry Letters | 2004
Gary Robert William Pitt; Andrzej Roman Batt; Robert Haigh; Andrew Penson; Peter A. Robson; David Philip Rooker; André Tartar; Julie E. Trim; Christopher M. Yea; Michael Bryan Roe
Archive | 1997
Hamish Ryder; Philip Anthony Ashworth; Michael Bryan Roe; Julie Elizabeth Brumwell; Sukhjit Hunjan; Adrian Folkes; Jason Terry Sanderson; Susannah Williams; Levi Michael Maximen
Archive | 2003
Michael Bryan Roe; Andrzej Roman Batt; David Michael Evans; Gary Robert William Pitt; David Philip Rooker
Archive | 2004
Peter Hudson; Gary Robert William Pitt; David Philip Rooker; Andrzej Roman Batt; Celine Marguerite Simone Heeney; Michael Bryan Roe
Drugs of The Future | 2006
Doreen Mary Ashworth; Andrzej Roman Batt; Andrew John Baxter; Pierre Broqua; Robert Haigh; Peter Hudson; Celine Marguerite Simone Heeney; Régent Laporte; Andrew Penson; Gary Robert William Pitt; Peter A. Robson; David Philip Rooker; André Tartar; Chris Yea; Michael Bryan Roe
Archive | 2004
Peter Hudson; Andrzej Roman Batt; Celine Marguerite Simone Heeney; Andrew John Baxter; Michael Bryan Roe; Peter A. Robson