Publications by authors named "Geoffrey Stemp"

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Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
Romano Di Fabio, Annalisa Pellacani, Stefania Faedo, Adelheid Roth, Laura Piccoli, Geoffrey Stemp

Bioorg Med Chem Lett· September 2011

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The discovery and optimisation of benzazepine sulfonamide and sulfones as potent agonists of the motilin receptor.
James M Bailey, Jackie S Scott, Jonathan B Basilla, Victoria J Bolton, Izzy Boyfield, Geoffrey Stemp

Bioorg Med Chem Lett· November 2009

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Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate.
Susan M Westaway, Samantha L Brown, Stephen C M Fell, Christopher N Johnson, David T MacPherson, Geoffrey Stemp

J Med Chem· February 2009

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Identification of small molecule agonists of the motilin receptor.
Tom D Heightman, Elizabeth Conway, David F Corbett, Gregor J Macdonald, Geoffrey Stemp

Bioorg Med Chem Lett· December 2008

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The discovery of biaryl carboxamides as novel small molecule agonists of the motilin receptor.
Susan M Westaway, Samantha L Brown, Elizabeth Conway, Tom D Heightman, Christopher N Johnson, Geoffrey Stemp

Bioorg Med Chem Lett· December 2008

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Tricyclic azepine derivatives as selective brain penetrant 5-HT6 receptor antagonists.
Giancarlo Trani, Stuart M Baddeley, Michael A Briggs, Tsu T Chuang, Nigel J Deeks, Geoffrey Stemp

Bioorg Med Chem Lett· October 2008

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Design and synthesis of 6-phenylnicotinamide derivatives as antagonists of TRPV1.
Susan M Westaway, Mervyn Thompson, Harshad K Rami, Geoffrey Stemp, Leontine S Trouw

Bioorg Med Chem Lett· October 2008

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BACE-1 inhibitors part 2: identification of hydroxy ethylamines (HEAs) with reduced peptidic character.
Brian Clarke, Emmanuel Demont, Colin Dingwall, Rachel Dunsdon, Andrew Faller, Geoffrey Stemp

Bioorg Med Chem Lett· February 2008

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BACE-1 inhibitors part 1: identification of novel hydroxy ethylamines (HEAs).
Brian Clarke, Emmanuel Demont, Colin Dingwall, Rachel Dunsdon, Andrew Faller, Geoffrey Stemp

Bioorg Med Chem Lett· February 2008

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BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells.
Paul Beswick, Nicolas Charrier, Brian Clarke, Emmanuel Demont, Colin Dingwall, Geoffrey Stemp

Bioorg Med Chem Lett· February 2008

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Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands.
Simon E Ward, Christopher N Johnson, Peter J Lovell, Claire M Scott, Paul W Smith, Geoffrey Stemp

Bioorg Med Chem Lett· September 2007

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Translational sciences-turning drug-like molecules into medicines.
Phil Jeffrey, Eric Karran, Alan Palmer, Geoffrey Stemp

Drug News Perspect· December 2006

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A concise, convergent total synthesis of monocerin.
John H Cassidy, Christopher N Farthing, Stephen P Marsden, Anders Pedersen, Mark Slater, Geoffrey Stemp

Org Biomol Chem· November 2006

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N-Tetrahydroquinolinyl, N-quinolinyl and N-isoquinolinyl biaryl carboxamides as antagonists of TRPV1.
Susan M Westaway, Ying-Kit Chung, John B Davis, Vicky Holland, Jeffrey C Jerman, Geoffrey Stemp

Bioorg Med Chem Lett· September 2006

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SAR of biphenyl carboxamide ligands of the human melanin-concentrating hormone receptor 1 (MCH R1): discovery of antagonist SB-568849.
David R Witty, John H Bateson, Guillaume J Hervieu, Phillip Jeffrey, Christopher N Johnson, Geoffrey Stemp

Bioorg Med Chem Lett· September 2006

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Discovery of potent and stable conformationally constrained analogues of the MCH R1 antagonist SB-568849.
David R Witty, John Bateson, Guillaume J Hervieu, Kamal Al-Barazanji, Phillip Jeffrey, Geoffrey Stemp

Bioorg Med Chem Lett· September 2006

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Discovery of SB-705498: a potent, selective and orally bioavailable TRPV1 antagonist suitable for clinical development.
Harshad K Rami, Mervyn Thompson, Geoffrey Stemp, Steve Fell, Jeffrey C Jerman

Bioorg Med Chem Lett· June 2006

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Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT6 receptor antagonists.
Mahmood Ahmed, Michael A Briggs, Steven M Bromidge, Tania Buck, Lorraine Campbell, Geoffrey Stemp

Bioorg Med Chem Lett· November 2005

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3,4-Dihydro-2H-benzoxazinones are 5-HT(1A) receptor antagonists with potent 5-HT reuptake inhibitory activity.
Peter J Atkinson, Steven M Bromidge, Mark S Duxon, Laramie M Gaster, Michael S Hadley, Geoffrey Stemp

Bioorg Med Chem Lett· February 2005

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Design and synthesis of trans-3-(2-(4-((3-(3-(5-methyl-1,2,4-oxadiazolyl))- phenyl)carboxamido)cyclohexyl)ethyl)-7-methylsulfonyl-2,3,4,5-tetrahydro-1H-3-benzazepine (SB-414796): a potent and selective dopamine D3 receptor antagonist.
Gregor J Macdonald, Clive L Branch, Michael S Hadley, Christopher N Johnson, David J Nash, Geoffrey Stemp

J Med Chem· November 2003

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The design of 8,8-dimethyl[1,6]naphthyridines as potential anticonvulsant agents.
Nigel E Austin, Michael S Hadley, John D Harling, Frank P Harrington, Gregor J Macdonald, Geoffrey Stemp

Bioorg Med Chem Lett· May 2003

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Dopamine D3 receptor antagonism inhibits cocaine-seeking and cocaine-enhanced brain reward in rats.
Stanislav R Vorel, Charles R Ashby, Mousumi Paul, Xinhe Liu, Robert Hayes, Geoffrey Stemp

J Neurosci· November 2002

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Directed dihydroxylation of cyclic allylic alcohols and trichloroacetamides using OsO4/TMEDA.
Timothy J Donohoe, Kevin Blades, Peter R Moore, Michael J Waring, Jon J G Winter, Geoffrey Stemp

J Org Chem· November 2002

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Directed Dihydroxylation of Allylic Trichloroacetamides.
Timothy J. Donohoe, Kevin Blades, Madeleine Helliwell, Peter R. Moore, Jonathan J. G. Winter, Geoffrey Stemp

J Org Chem· April 1999

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