Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders von Di Fabio, Romano, Pellacani, Annalisa, Faedo, Stefania, Roth, Adelheid, Piccoli, Laura, Gerrard, Philip, Porter, Rod A., Johnson, Christopher N., Thewlis, Kevin, Donati, Daniele, Stasi, Luigi, Spada, Simone, Stemp, Geoffrey, Nash, David, Branch, Clive, Kindon, Leanda, Massagrande, Mario, Poffe, Alessandro, Braggio, Simone, Chiarparin, Elisabetta, Marchioro, Carla, Ratti, Emiliangelo, Corsi, Mauro

Volltext

Directed Dihydroxylation of Cyclic Allylic Alcohols and Trichloroacetamides Using OsO4/TMEDA von Donohoe, Timothy J, Blades, Kevin, Moore, Peter R, Waring, Michael J, Winter, Jon J. G, Helliwell, Madeleine, Newcombe, Nicholas J, Stemp, Geoffrey

Volltext

BACE-1 inhibitors Part 1: Identification of novel hydroxy ethylamines (HEAs) von Clarke, Brian, Demont, Emmanuel, Dingwall, Colin, Dunsdon, Rachel, Faller, Andrew, Hawkins, Julie, Hussain, Ishrut, MacPherson, David, Maile, Graham, Matico, Rosalie, Milner, Peter, Mosley, Julie, Naylor, Alan, O’Brien, Alistair, Redshaw, Sally, Riddell, David, Rowland, Paul, Soleil, Virginie, Smith, Kathrine J., Stanway, Steven, Stemp, Geoffrey, Sweitzer, Sharon, Theobald, Pam, Vesey, David, Walter, Daryl S., Ward, John, Wayne, Gareth

Volltext

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 C... von Westaway, Susan M, Brown, Samantha L, Fell, Stephen C. M, Johnson, Christopher N, MacPherson, David T, Mitchell, Darren J, Myatt, James W, Stanway, Steven J, Seal, Jon T, Stemp, Geoffrey, Thompson, Mervyn, Lawless, Kirk, McKay, Fiona, Muir, Alison I, Barford, Jonathan M, Cluff, Chermaine, Mahmood, Sadhia R, Matthews, Kim L, Mohamed, Shiyam, Smith, Beverley, Stevens, Alexander J, Bolton, Victoria J, Jarvie, Emma M, Sanger, Gareth J

Volltext

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): ... von Macdonald, Gregor J, Branch, Clive L, Hadley, Michael S, Johnson, Christopher N, Nash, David J, Smith, Alexander B, Stemp, Geoffrey, Thewlis, Kevin M, Vong, Antonio K. K, Austin, Nigel E, Jeffrey, Phillip, Winborn, Kim Y, Boyfield, Izzy, Hagan, Jim J, Middlemiss, Derek N, Reavill, Charlie, Riley, Graham J, Watson, Jeannette M, Wood, Martyn, Parker, Steve G, Ashby, Charles R

Volltext

Discovery of SB-705498: A potent, selective and orally bioavailable TRPV1 antagonist suitable for clinical development von Rami, Harshad K., Thompson, Mervyn, Stemp, Geoffrey, Fell, Steve, Jerman, Jeffrey C., Stevens, Alexander J., Smart, Darren, Sargent, Becky, Sanderson, Dominic, Randall, Andrew D., Gunthorpe, Martin J., Davis, John B.

Volltext

Dopamine D3 Receptor Antagonism Inhibits Cocaine-Seeking and Cocaine-Enhanced Brain Reward in Rats von Vorel, Stanislav R, Ashby, Charles R., Jr, Paul, Mousumi, Liu, Xinhe, Hayes, Robert, Hagan, Jim J, Middlemiss, Derek N, Stemp, Geoffrey, Gardner, Eliot L

Volltext

A syn selective dihydroxylation of cyclic allylic trichloroacetamides using catalytic osmium tetroxide von Blades, Kevin, Donohoe, Timothy J, Winter, Jonathan J.G, Stemp, Geoffrey

Volltext

BACE-1 inhibitors part 2: Identification of hydroxy ethylamines (HEAs) with reduced peptidic character von Clarke, Brian, Demont, Emmanuel, Dingwall, Colin, Dunsdon, Rachel, Faller, Andrew, Hawkins, Julie, Hussain, Ishrut, MacPherson, David, Maile, Graham, Matico, Rosalie, Milner, Peter, Mosley, Julie, Naylor, Alan, O’Brien, Alistair, Redshaw, Sally, Riddell, David, Rowland, Paul, Soleil, Virginie, Smith, Kathrine J., Stanway, Steven, Stemp, Geoffrey, Sweitzer, Sharon, Theobald, Pam, Vesey, David, Walter, Daryl S., Ward, John, Wayne, Gareth

Volltext

BACE-1 inhibitors part 3: Identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells von Beswick, Paul, Charrier, Nicolas, Clarke, Brian, Demont, Emmanuel, Dingwall, Colin, Dunsdon, Rachel, Faller, Andrew, Gleave, Robert, Hawkins, Julie, Hussain, Ishrut, Johnson, Christopher N., MacPherson, David, Maile, Graham, Matico, Rosalie, Milner, Peter, Mosley, Julie, Naylor, Alan, O’Brien, Alistair, Redshaw, Sally, Riddell, David, Rowland, Paul, Skidmore, John, Soleil, Virginie, Smith, Kathrine J., Stanway, Steven, Stemp, Geoffrey, Stuart, Alistair, Sweitzer, Sharon, Theobald, Pam, Vesey, David, Walter, Daryl S., Ward, John, Wayne, Gareth

Volltext

Design and synthesis of 6-phenylnicotinamide derivatives as antagonists of TRPV1 von Westaway, Susan M., Thompson, Mervyn, Rami, Harshad K., Stemp, Geoffrey, Trouw, Leontine S., Mitchell, Darren J., Seal, Jon T., Medhurst, Stephen J., Lappin, Sarah C., Biggs, James, Wright, James, Arpino, Sandra, Jerman, Jeffrey C., Cryan, Jennifer E., Holland, Vicky, Winborn, Kim Y., Coleman, Tanya, Stevens, Alexander J., Davis, John B., Gunthorpe, Martin J.

Volltext

Design and Synthesis of trans - N -[4-[2-(6-Cyano-1,2,3,4-tetrahydroisoquinolin-2- yl)ethyl]cyclohexyl]-4-quinolinecarboxamide (SB-277011):  A Potent and Selective Dopamine D 3 Rec... von Stemp, Geoffrey, Ashmeade, Tracey, Branch, Clive L., Hadley, Michael S., Hunter, A. Jacqueline, Johnson, Christopher N., Nash, David J., Thewlis, Kevin M., Vong, Antonio K. K., Austin, Nigel E., Jeffrey, Phillip, Avenell, Kim Y., Boyfield, Izzy, Hagan, Jim J., Middlemiss, Derek N., Reavill, Charlie, Riley, Graham J., Routledge, Carole, Wood, Martyn

Volltext

Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT6 receptor antagonists von AHMED, Mahmood, BRIGGS, Michael A, JOHNSON, Christopher N, MEDHURST, Andrew D, MITCHELL, Darren J, MOSS, Stephen F, POWLES, Jenifer, SEAL, Jon T, STEAN, Tania O, STEMP, Geoffrey, THOMPSON, Mervyn, TRAIL, Brenda, BROMIDGE, Steven M, UPTON, Neil, WINBORN, Kim, WITTY, David R, BUCK, Tania, CAMPBELL, Lorraine, DEEKS, Nigel J, GARNER, Ashley, GORDON, Laurie, HAMPRECHT, Dieter W, HOLLAND, Vicky

Volltext

3,4-Dihydro-2H-benzoxazinones are 5-HT1A receptor antagonists with potent 5-HT reuptake inhibitory activity von ATKINSON, Peter J, BROMIDGE, Steven M, RAMI, Harshad K, RILEY, Graham J, SCOTT, Claire M, SHAW, Tracey E, STARR, Kathryn R, STEMP, Geoffrey, THEWLIS, Kevin M, THOMAS, David R, THOMPSON, Mervyn, VONG, Antonio K. K, DUXON, Mark S, WATSON, Jeannette M, GASTER, Laramie M, HADLEY, Michael S, HAMMOND, Beverley, JOHNSON, Christopher N, MIDDLEMISS, Derek N, NORTH, Stephanie E, PRICE, Gary W

Volltext

Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT 6 receptor antagonists von Ahmed, Mahmood, Briggs, Michael A., Bromidge, Steven M., Buck, Tania, Campbell, Lorraine, Deeks, Nigel J., Garner, Ashley, Gordon, Laurie, Hamprecht, Dieter W., Holland, Vicky, Johnson, Christopher N., Medhurst, Andrew D., Mitchell, Darren J., Moss, Stephen F., Powles, Jenifer, Seal, Jon T., Stean, Tania O., Stemp, Geoffrey, Thompson, Mervyn, Trail, Brenda, Upton, Neil, Winborn, Kim, Witty, David R.

Volltext

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

Volltext

Palladium(0)-Catalysed Arylations using Pyrrole and Indole 2-Boronic Acids von Johnson, Christopher N., Stemp, Geoffrey, Anand, Neel, Stephen, Susanna C., Gallagher, Timothy

Volltext

Hydrogen bonding control in the oxidative cyclisation of 1,5-dienes von Donohoe, Timothy J, Winter, Jonathan J.G, Helliwell, Madeleine, Stemp, Geoffrey

Volltext

Identification of small molecule agonists of the motilin receptor von Heightman, Tom D., Conway, Elizabeth, Corbett, David F., Macdonald, Gregor J., Stemp, Geoffrey, Westaway, Susan M., Celestini, Paolo, Gagliardi, Stefania, Riccaboni, Mauro, Ronzoni, Silvano, Vaidya, Kalindi, Butler, Sharon, McKay, Fiona, Muir, Alison, Powney, Ben, Winborn, Kim, Wise, Alan, Jarvie, Emma M., Sanger, Gareth J.

Volltext

SAR of biphenyl carboxamide ligands of the human melanin-concentrating hormone receptor 1 (MCH R1): Discovery of antagonist SB-568849 von Witty, David R., Bateson, John H., Hervieu, Guillaume J., Jeffrey, Phillip, Johnson, Christopher N., Muir, Alison I., O’Hanlon, Peter J., Stemp, Geoffrey, Stevens, Alex J., Thewlis, Kevin M., Wilson, Shelagh, Winborn, Kim Y.

Volltext