Search Results - "Stobie, Alan"

Design and synthesis of morpholine derivatives. SAR for dual serotonin & noradrenaline reuptake inhibition by Fish, Paul V., Deur, Christopher, Gan, Xinmin, Greene, Keri, Hoople, David, Mackenny, Malcolm, Para, Kimberly S., Reeves, Keith, Ryckmans, Thomas, Stiff, Cory, Stobie, Alan, Wakenhut, Florian, Whitlock, Gavin A.

“…Morpholine derivatives 5, 8– 23 are inhibitors of monoamine reuptake. Target compounds were prepared using a highly specific enzyme-catalysed resolution of…”
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Discovery of PF-184563, a potent and selective V1a antagonist for the treatment of dysmenorrhoea. The influence of compound flexibility on microsomal stability by Johnson, Patrick S., Ryckmans, Thomas, Bryans, Justin, Beal, Dave M., Dack, Kevin N., Feeder, Neil, Harrison, Anthony, Lewis, Mark, Mason, Helen J., Mills, James, Newman, Julie, Pasquinet, Christelle, Rawson, Dave J., Roberts, Lee R., Russell, Rachel, Spark, Deborah, Stobie, Alan, Underwood, Toby J., Ward, Robin, Wheeler, Simon

“…The V1a receptor has emerged as an attractive target for a range of indications including Raynaud’s disease and dysmenorrhoea. As part of an effort to discover…”
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Novel 2-imidazoles as potent, selective and CNS penetrant α1A adrenoceptor partial agonists by ROBERTS, Lee R, BRYANS, Justin, CONLON, Kelly, MCMURRAY, Gordon, STOBIE, Alan, WHITLOCK, Gavin A

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Pyridyl-phenyl ether monoamine reuptake inhibitors: Impact of lipophilicity on dual SNRI pharmacology and off-target promiscuity by Whitlock, Gavin A., Fish, Paul V., Fray, M. Jonathan, Stobie, Alan, Wakenhut, Florian

“…A novel series of pyridyl-phenyl ethers are disclosed, which possess potent dual 5-HT and NA reuptake pharmacology with good selectivity over dopamine reuptake…”
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Potent and selective α1A adrenoceptor partial agonists—Novel imidazole frameworks by Whitlock, Gavin A., Brennan, Paul E., Roberts, Lee R., Stobie, Alan

“…Novel imidazole frameworks have been identified as potent and selective α1A partial agonists with good CNS drug-like properties. Novel imidazole frameworks…”
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[4-(Phenoxy)pyridin-3-yl]methylamines: A new class of selective noradrenaline reuptake inhibitors by Fish, Paul V., Ryckmans, Thomas, Stobie, Alan, Wakenhut, Florian

“…Pyridinyl phenyl ethers are disclosed as a new series of selective noradrenaline reuptake inhibitors (NRI). Structure–activity relationships established that…”
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Design, synthesis and evaluation of N-[(3 S)-pyrrolidin-3-yl]benzamides as selective noradrenaline reuptake inhibitors: CNS penetration in a more polar template by Fish, Paul V., Wakenhut, Florian, Ryckmans, Thomas, Stobie, Alan

“…Derivatives of N-[(3 S)-pyrrolidin-3-yl]benzamides are disclosed as a new series of noradrenaline reuptake inhibitors (NRI). Benzamide 11e was identified as a…”
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4-Piperidines and 3-pyrrolidines as dual serotonin and noradrenaline reuptake inhibitors: Design, synthesis and structure–activity relationships by Fish, Paul V., Andrews, Mark D., Jonathan Fray, M., Stobie, Alan, Wakenhut, Florian, Whitlock, Gavin A.

“…[(Aryloxy)(pyridinyl)methyl]piperidine and pyrrolidine derivatives 5– 9 are inhibitors of monoamine reuptake. Structure–activity relationships established that…”
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Potent and selective alpha 1A adrenoceptor partial agonists-Novel imidazole frameworks by Whitlock, Gavin A, Brennan, Paul E, Roberts, Lee R, Stobie, Alan

“…Novel imidazole frameworks have been identified as potent partial agonists of the alpha 1A adrenergic receptor, with good selectivity over the alpha 1B, alpha…”
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Novel 2-imidazoles as potent, selective and CNS penetrant alpha sub(1A) adrenoceptor partial agonists by Roberts, Lee R, Bryans, Justin, Conlon, Kelly, McMurray, Gordon, Stobie, Alan, Whitlock, Gavin A

“…A novel series of central nervous system (CNS) penetrant indane 2- imidazoles have been identified as potent, partial agonists of the alpha sub(1A) adrenergic…”
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Novel 2-imidazoles as potent and selective α1A adrenoceptor partial agonists by WHITLOCK, Gavin A, CONLON, Kelly, MCMURRAY, Gordon, ROBERTS, Lee R, STOBIE, Alan, THURLOW, Richard J

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Novel Selective Inhibitors of Neutral Endopeptidase for the Treatment of Female Sexual Arousal Disorder. Synthesis and Activity of Functionalized Glutaramides by Pryde, David C, Maw, Graham N, Planken, Simon, Platts, Michelle Y, Sanderson, Vivienne, Corless, Martin, Stobie, Alan, Barber, Christopher G, Russell, Rachel, Foster, Laura, Barker, Laura, Wayman, Christopher, Van Der Graaf, Piet, Stacey, Peter, Morren, Debbie, Kohl, Christopher, Beaumont, Kevin, Coggon, Sara, Tute, Michael

“…Female sexual arousal disorder (FSAD) is a highly prevalent sexual disorder affecting up to 40% of women. We describe herein our efforts to identify a…”
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Novel 2-imidazoles as potent and selective alpha sub(1A) adrenoceptor partial agonists by Whitlock, Gavin A, Conlon, Kelly, McMurray, Gordon, Roberts, Lee R, Stobie, Alan, Thurlow, Richard J

“…Novel 2-imidazoles have been identified as potent partial agonists of the alpha sub(1A) adrenergic receptor, with good selectivity over the alpha sub(1B),…”
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N-Benzyl- N-(tetrahydro-2 H-pyran-4-yl)pyrrolidin-3-amines as selective dual serotonin/noradrenaline reuptake inhibitors by Fish, Paul V., Fray, M. Jonathan, Stobie, Alan, Wakenhut, Florian, Whitlock, Gavin A.

“…A series of amino-pyrrolidines with potent dual 5-HT/NA reuptake inhibition, good metabolic stability and weak CYP2D6 inhibition is described. A series of…”
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N-[(3 S)-Pyrrolidin-3-yl]benzamides as novel dual serotonin and noradrenaline reuptake inhibitors: Impact of small structural modifications on P-gp recognition and CNS penetration by Wakenhut, Florian, Allan, Gill A., Fish, Paul V., Jonathan Fray, M., Harrison, Anthony C., McCoy, Rachel, Phillips, Stephen C., Stobie, Alan, Westbrook, Dominique, Westbrook, Simon L., Whitlock, Gavin A.

“…The structure–activity relationship and the synthesis of novel N-[(3 S)-pyrrolidin-3-yl]benzamides as dual serotonin and noradrenaline monoamine reuptake…”
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N-Benzyl- N-(pyrrolidin-3-yl)carboxamides as a new class of selective dual serotonin/noradrenaline reuptake inhibitors by Wakenhut, Florian, Fish, Paul V., Fray, M. Jonathan, Gurrell, Ian, Mills, James E., Stobie, Alan, Whitlock, Gavin A.

“…The structure–activity relationship and the synthesis of novel N-benzyl- N-(pyrrolidin-3-yl)carboxamides as dual serotonin (5-HT) and noradrenaline (NA)…”
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Structure–activity relationships of N-substituted piperazine amine reuptake inhibitors by Jonathan Fray, M., Bish, Gerwyn, Fish, Paul V., Stobie, Alan, Wakenhut, Florian, Whitlock, Gavin A.

“…The synthesis and structure–activity relationships are described for 26 variously N-substituted piperazines as dual serotonin/noradrenaline reuptake…”
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Novel 2-imidazoles as potent and selective α 1A adrenoceptor partial agonists by Whitlock, Gavin A., Conlon, Kelly, McMurray, Gordon, Roberts, Lee R., Stobie, Alan, Thurlow, Richard J.

“…A series of novel 2-imidazoles is described, which combine potent and selective α 1A partial agonist pharmacology with good drug-like properties. Novel…”
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Novel 2-imidazoles as potent, selective and CNS penetrant α 1A adrenoceptor partial agonists by Roberts, Lee R., Bryans, Justin, Conlon, Kelly, McMurray, Gordon, Stobie, Alan, Whitlock, Gavin A.

“…A series of novel 2-imidazoles is described, which combine potent and selective α 1A partial agonist pharmacology with good CNS penetration. A novel series of…”
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Designing rapid onset selective serotonin re-uptake inhibitors. Part 3: Site-directed metabolism as a strategy to avoid active circulating metabolites: Structure–activity relationships of (thioalkyl)phenoxy benzylamines by Middleton, Donald S., Andrews, Mark, Glossop, Paul, Gymer, Geoffrey, Hepworth, David, Jessiman, Alan, Johnson, Patrick S., MacKenny, Malcolm, Stobie, Alan, Tang, Kim, Morgan, Paul, Jones, Barry

“…A series of thio-alkyl containing diphenylethers were designed and evaluated, as a strategy to competitively direct metabolism away from unwanted amine…”
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