Search Results - "Springthorpe, Brian"

The influence of drug-like concepts on decision-making in medicinal chemistry by Leeson, Paul D, Springthorpe, Brian

“…The application of guidelines linked to the concept of drug-likeness, such as the 'rule of five', has gained wide acceptance as an approach to reduce attrition…”
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Which Hydroxy? Evidence for Species Differences in the Regioselectivity of Glucuronidation in Rat, Dog, and Human in Vitro Systems and Dog in Vivo by MARTIN, Iain J, LEWIS, Richard J, BERNSTEIN, Michael A, BEATTIE, Iain G, MARTIN, Craig A, RILEY, Robert J, SPRINGTHORPE, Brian

“…The glucuronidation of (1 S ,2 R ,3 R ,5 R )-3-(hydroxymethyl)-5-[7-{[(1 R ,2 S )-2-phenylcyclopropyl]amino}-5-(propylthio)-3 H -[1,2,3]triazolo[4,5- d…”
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Overcoming Undesirable hERG Potency of Chemokine Receptor Antagonists Using Baseline Lipophilicity Relationships by Shamovsky, Igor, Connolly, Stephen, David, Laurent, Ivanova, Svetlana, Nordén, Bo, Springthorpe, Brian, Urbahns, Klaus

“…The inhibition of the hERG channel by noncardiovascular drugs is a side effect that severely impedes the development of new medications. To increase hERG…”
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From ATP to AZD6140 : The discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosis by SPRINGTHORPE, Brian, BAILEY, Andrew, HUNT, Simon F, INCE, Francis, INGALL, Anthony H, KIRK, Ian P, LEESON, Paul D, LEFF, Paul, LEWIS, Richard J, MARTIN, Barrie P, MCGINNITY, Dermot F, MORTIMORE, Michael P, BARTON, Patrick, PAINE, Stuart W, PAIRAUDEAU, Garry, PATEL, Anil, RIGBY, Aaron J, RILEY, Robert J, TEOBALD, Barry J, TOMLINSON, Wendy, WEBBORN, Peter J. H, WILLIS, Paul A, BIRKINSHAW, Timothy N, BONNERT, Roger V, BROWN, Roger C, CHAPMAN, David, DIXON, John, GUILE, Simon D, HUMPHRIES, Robert G

“…Starting from adenosine triphosphate (ATP), the identification of a novel series of P2Y(12) receptor antagonists and exploitation of their SAR is described…”
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Scaffold-hopping with zwitterionic CCR3 antagonists: Identification and optimisation of a series with good potency and pharmacokinetics leading to the discovery of AZ12436092 by Bahl, Ash, Barton, Patrick, Bowers, Keith, Caffrey, Moya V., Denton, Rebecca, Gilmour, Peter, Hawley, Shaun, Linannen, Tero, Luckhurst, Christopher A., Mochel, Tobias, Perry, Matthew W.D., Riley, Robert J., Roe, Emma, Springthorpe, Brian, Stein, Linda, Webborn, Peter

“…The discovery and optimisation of a series of zwitterionic CCR3 antagonists is described. Optimisation of the structure led to AZ12436092, a compound with…”
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Discovery and evolution of phenoxypiperidine hydroxyamide dual CCR3/H1 antagonists. Part II: Optimising in vivo clearance by Furber, Mark, Alcaraz, Lilian, Luckhurst, Christopher, Bahl, Ash, Beaton, Haydn, Bowers, Keith, Collington, John, Denton, Rebecca, Donald, David, Kinchin, Elizabeth, MacDonald, Cathy, Rigby, Aaron, Riley, Rob, Soars, Matt, Springthorpe, Brian, Webborn, Peter

“…The second part of this communication focuses on the resolution of issues surrounding the series of hydroxyamide phenoxypiperidine CCR3/H1 dual antagonists…”
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Discovery and evolution of phenoxypiperidine hydroxyamide dual CCR3/H1 antagonists. Part I by Furber, Mark, Alcaraz, Lilian, Luckhurst, Christopher, Bahl, Ash, Beaton, Haydn, Bowers, Keith, Collington, John, Denton, Rebecca, Donald, David, Kinchin, Elizabeth, MacDonald, Cathy, Rigby, Aaron, Riley, Rob, Soars, Matt, Springthorpe, Brian, Webborn, Peter

“…The discovery of potent small molecule dual antagonists of the human CCR3 and H1 receptors is described for the treatment of allergic diseases, for example,…”
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The discovery of CCR3/H1 dual antagonists with reduced hERG risk by Bahl, Ash, Barton, Patrick, Bowers, Keith, Brough, Steven, Evans, Richard, Luckhurst, Christopher A., Mochel, Tobias, Perry, Matthew W.D., Rigby, Aaron, Riley, Robert J., Sanganee, Hitesh, Sisson, Adam, Springthorpe, Brian

“…A series of dual CCR3/H1 antagonists based on a bispiperidine scaffold were discovered. Introduction of an acidic group overcame hERG liability…”
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Drug disposition and cardiac toxicity: A litterature-based review by Hammond, Tim, Bowes, Joanne, Boyer, Scott, Burnham, Matthew B., Cook, David, Gavaghan, Glaire, Hance, Mark, Haywood, Martin, Matis, Sherri, Roberts, Stephanie, Springthorpe, Brian, Valentin, Jean-Pierre

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From ATP to AZD6140: The discovery of an orally active reversible P2Y 12 receptor antagonist for the prevention of thrombosis by Springthorpe, Brian, Bailey, Andrew, Barton, Patrick, Birkinshaw, Timothy N., Bonnert, Roger V., Brown, Roger C., Chapman, David, Dixon, John, Guile, Simon D., Humphries, Robert G., Hunt, Simon F., Ince, Francis, Ingall, Anthony H., Kirk, Ian P., Leeson, Paul D., Leff, Paul, Lewis, Richard J., Martin, Barrie P., McGinnity, Dermot F., Mortimore, Michael P., Paine, Stuart W., Pairaudeau, Garry, Patel, Anil, Rigby, Aaron J., Riley, Robert J., Teobald, Barry J., Tomlinson, Wendy, Webborn, Peter J.H., Willis, Paul A.

“…Starting with ATP, the identification of novel P2Y 12 receptor antagonists are described. The leading compound, 17 (AZD6140), is currently in a phase III…”
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