Search Results - "Warrellow, Graham"

Racemic and chiral sulfoxides as potential prodrugs of the COX-2 inhibitors Vioxx ® and Arcoxia by Caturla, Francisco, Amat, Mercè, Reinoso, Raquel F., Córdoba, Mónica, Warrellow, Graham

“…The enantiomeric synthesis and profiling of sulfoxide-based rofecoxib and etoricoxib (Merck) prodrugs are reported. The preparation of the sulfoxide analogues…”
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Squaric acid derivatives as VLA-4 integrin antagonists by PORTER, John R, ARCHIBALD, Sarah C, WARRELLOW, Graham J, ALEXANDER, Rikki P, LANGHAM, Barry, CHILDS, Kirstie, CRITCHLEY, David, HEAD, John C, LINSLEY, Janeen M, PARTON, Ted A. H, ROBINSON, Martyn K, SHOCK, Anthony, TAYLOR, Richard J

“…SAR studies aimed at improving the rate of clearance by the incorporation of a 3,4-diamino-3-cyclobutene-1,2-dione group as an amino acid isostere in a series…”
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Discovery and evaluation of N-(triazin-1,3,5-yl) phenylalanine derivatives as VLA-4 integrin antagonists by Porter, John R., Archibald, Sarah C., Brown, Julien A., Childs, Kirstie, Critchley, David, Head, John C., Hutchinson, Brian, Parton, Ted A.H., Robinson, Martyn K., Shock, Anthony, Warrellow, Graham J., Zomaya, Alex

“…SAR studies aimed at improving the rate of clearance of a series of VLA-4 integrin antagonists by the introduction of a 1,3,5-triazine as an amide isostere are…”
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PDE 4 inhibitors: the use of molecular cloning in the design and development of novel drugs by Hughes, Bernadette, Owens, Ray, Perry, Martin, Warrellow, Graham, Allen, Rodger

“…Phosphodiesterase 4 (PDE 4) enzymes are the principal phosphodiesterases responsible for the hydrolysis of cAMP in pro-inflammatory leukocytes. The functional…”
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Dehydrophenylalanine derivatives as VLA-4 integrin antagonists by Porter, John R., Archibald, Sarah C., Brown, Julien A., Childs, Kirstie, Critchley, David, Head, John C., Parton, Ted A.H., Robinson, Martyn K., Shock, Anthony, Taylor, Richard J., Warrellow, Graham J.

“…We describe a series of dehydrophenylalanine derivatives where the Z isomers are potent VLA-4 antagonists but are subject to rapid biliary clearance and the E…”
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N-(Pyrimidin-4-yl) and N-(Pyridin-2-yl) phenylalanine derivatives as VLA-4 integrin antagonists by Porter, John R., Archibald, Sarah C., Brown, Julien A., Childs, Kirstie, Critchley, David, Head, John C., Hutchinson, Brian, Parton, Ted A.H., Robinson, Martyn K., Shock, Anthony, Warrellow, Graham J., Zomaya, Alex

“…The SAR studies to optimise both potency and rate of clearance in the rat for a series of pyrimidine and pyridine based VLA-4 antagonists are described. A…”
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Interview with Graham Warrellow by Isaac Bruce by Warrellow, Graham

“…Following his academic studies at the University of Surrey (UK), Graham Warrellow entered the pharmaceutical industry to pursue a career at the forefront of…”
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Discovery and evaluation of potent, cysteine-based α4β1 integrin antagonists by Archibald, Sarah C, Head, John C, Linsley, Janeen M, Porter, John R, Robinson, Martyn K, Shock, Anthony, Warrellow, Graham J

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Investigation of the in Vitro Metabolism Profile of a Phosphodiesterase-IV Inhibitor, CDP-840: Leading to Structural Optimization by Li, C, Chauret, N, Trimble, L A, Nicoll-Griffith, D A, Silva, J M, MacDonald, D, Perrier, H, Yergey, J A, Parton, T, Alexander, R P, Warrellow, G J

“…CDP-840 is a selective and potent phosphodiesterase type IV inhibitor, whose in vitro metabolism profile was first investigated using liver microsomes from…”
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Racemic and chiral sulfoxides as potential prodrugs of 4-pyrone COX-2 inhibitors by Caturla, Francisco, Amat, Mercè, Reinoso, Raquel F., Calaf, Elena, Warrellow, Graham

“…The enantiomeric synthesis and profiling of sulfoxide-based prodrugs of potent COX-2 inhibitors discovered at Almirall are reported. The preparation of the…”
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Discovery and Characterization of 4‘-(2-Furyl)-N-pyridin-3-yl-4,5‘-bipyrimidin-2‘-amine (LAS38096), a Potent, Selective, and Efficacious A2B Adenosine Receptor Antagonist by Vidal, Bernat, Nueda, Arsenio, Esteve, Cristina, Domenech, Teresa, Benito, Sonia, Reinoso, Raquel F, Pont, Mercè, Calbet, Marta, López, Rosa, Cadavid, María Isabel, Loza, María Isabel, Cárdenas, Álvaro, Godessart, Núria, Beleta, Jorge, Warrellow, Graham, Ryder, Hamish

“…A novel series of N-heteroaryl 4‘-(2-furyl)-4,5‘-bipyrimidin-2‘-amines has been identified as potent and selective A2B adenosine receptor antagonists. In…”
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Synthesis and .alpha.2-adrenoceptor antagonist activity of some disulfonamidobenzoquinolizines by Ward, Terence J, Warrellow, Graham J, Stirrup, John A, Lattimer, Norman, Rhodes, Keith F

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Racemic and chiral sulfoxides as potential prodrugs of the COX-2 inhibitors Vioxx super([registered]) and Arcoxia super([registered]) by Caturla, Francisco, Amat, Merce, Reinoso, Raquel F, Cordoba, Monica, Warrellow, Graham

“…The preparation of the sulfoxide analogues 2 and 4, and their enantiomeric pure forms is discussed as well as their potential to act as prodrugs to the potent…”
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Synthesis and Structure−Activity Relationships of Novel Histamine H 1 Antagonists:  Indolylpiperidinyl Benzoic Acid Derivatives by Fonquerna, Silvia, Miralpeix, Montse, Pagès, Lluís, Puig, Carles, Cardús, Arantxa, Antón, Francisca, Cárdenas, Álvaro, Vilella, Dolors, Aparici, Mónica, Calaf, Elena, Prieto, José, Gras, Jordi, Huerta, Josep M., Warrellow, Graham, Beleta, Jorge, Ryder, Hamish

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Synthesis and structure-activity relationships of piperidinylpyrrolopyridine derivatives as potent and selective H1 antagonists by FONQUERNA, Silvia, MIRALPEIX, Montse, BELETA, Jorge, RYDER, Hamish, PAGES, Lluis, PUIG, Caries, CARDUS, Arantxa, ANTON, Francisca, VILELLA, Dolors, APARICI, Monica, PRIETO, José, WARRELLOW, Graham

“…The synthesis and structure-activity relationships of piperidinylpyrrolopyridines as potent and selective H(1) antagonists are discussed. It was found that the…”
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Discovery and Characterization of 4‘-(2-Furyl)- N -pyridin-3-yl-4,5‘-bipyrimidin-2‘-amine (LAS38096), a Potent, Selective, and Efficacious A 2B Adenosine Receptor Antagonist by Vidal, Bernat, Nueda, Arsenio, Esteve, Cristina, Domenech, Teresa, Benito, Sonia, Reinoso, Raquel F., Pont, Mercè, Calbet, Marta, López, Rosa, Cadavid, María Isabel, Loza, María Isabel, Cárdenas, Álvaro, Godessart, Núria, Beleta, Jorge, Warrellow, Graham, Ryder, Hamish

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Synthesis and structure–activity relationships of piperidinylpyrrolopyridine derivatives as potent and selective H 1 antagonists by Fonquerna, Silvia, Miralpeix, Montse, Pagès, Lluís, Puig, Carles, Cardús, Arantxa, Antón, Francisca, Vilella, Dolors, Aparici, Mónica, Prieto, José, Warrellow, Graham, Beleta, Jorge, Ryder, Hamish

“…[Display omitted] The synthesis and structure–activity relationships of piperidinylpyrrolopyridines as potent and selective H 1 antagonists are discussed. It…”
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Discovery and evaluation of potent, tyrosine-based α4β1 integrin antagonists by Archibald, Sarah C., Head, John C., Gozzard, Neil, Howat, David W., Parton, Ted A.H., Porter, John R., Robinson, Martyn K., Shock, Anthony, Warrellow, Graham J., Abraham, William M.

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Synthesis and Structure−Activity Relationships of Novel Histamine H1 Antagonists:  Indolylpiperidinyl Benzoic Acid Derivatives by Fonquerna, Silvia, Miralpeix, Montse, Pagès, Lluís, Puig, Carles, Cardús, Arantxa, Antón, Francisca, Cárdenas, Álvaro, Vilella, Dolors, Aparici, Mónica, Calaf, Elena, Prieto, José, Gras, Jordi, Huerta, Josep M, Warrellow, Graham, Beleta, Jorge, Ryder, Hamish

“…A series of indolylpiperidinyl derivatives were prepared and evaluated for their activity as histamine H1 antagonists. Structure−activity relationship studies…”
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Pharmacological characterization of the neonatally sensitized rabbit model and effects of a novel phosphodiesterase (PDE) 4 inhibitor by Gozzard, Neil, Hughes, Bernadette, Warrellow, Graham, Higgs, Gerry

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