Search Results - "Holmes, Ian P."

Chemically Catalyzed Asymmetric Cyanohydrin Syntheses by Brunel, Jean-Michel, Holmes, Ian P.

“…Over the past two decades, significant advances have been made towards developing chemically catalyzed asymmetric cyanohydrin syntheses. Preparations that were…”
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Palladium‐Catalyzed Tandem Alkenyl and Aryl CN Bond Formation: A Cascade N‐Annulation Route to 1‐Functionalized Indoles by Willis, Michael C., Brace, Gareth N., Holmes, Ian P.

“…A single tandem operation allows rapid access to a variety of substituted N‐functionalized indoles. The nitrogen atom of the indole nucleus is incorporated…”
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Characterization of the Novel Broad-Spectrum Kinase Inhibitor CTx-0294885 As an Affinity Reagent for Mass Spectrometry-Based Kinome Profiling by Zhang, Luxi, Holmes, Ian P, Hochgräfe, Falko, Walker, Scott R, Ali, Naveid A, Humphrey, Emily S, Wu, Jianmin, de Silva, Melanie, Kersten, Wilhelmus J. A, Connor, Theresa, Falk, Hendrik, Allan, Lynda, Street, Ian P, Bentley, John D, Pilling, Patricia A, Monahan, Brendon J, Peat, Thomas S, Daly, Roger J

“…Kinase enrichment utilizing broad-spectrum kinase inhibitors enables the identification of large proportions of the expressed kinome by mass spectrometry…”
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2-(2-Haloalkenyl)-aryl Halides as Substrates for Palladium-Catalysed Tandem CN Bond Formation: Efficient Synthesis of 1-Substituted Indoles by Willis, Michael C., Brace, Gareth N., Findlay, Thomas J. K., Holmes, Ian P.

“…2‐(2‐Haloalkenyl)‐aryl halides, conveniently prepared in a single step from the corresponding o‐halobenzaldehydes, are combined with amines under Pd catalysis…”
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The asymmetric addition of trimethylsilylcyanide to aldehydes catalysed by anionic chiral nucleophiles. Part 1 by Holmes, Ian P, Kagan, Henri B

“…Trimethylsilylcyanide has been added to a number of aldehydes using a highly active chiral catalyst. This procedure gives the TMS ethers of the corresponding…”
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The asymmetric addition of trimethylsilylcyanide to aldehydes catalysed by anionic chiral nucleophiles. Part 2 by Holmes, Ian P, Kagan, Henri B

“…Studies have been carried out on the addition of trimethylsilylcyanide to aldehydes using highly active chiral lithium phenolate catalysts. The screening of a…”
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The identification of a series of novel, soluble non-peptidic neuropeptide Y Y2 receptor antagonists by Lunniss, Gillian E., Barnes, Ashley A., Barton, Nick, Biagetti, Matteo, Bianchi, Federica, Blowers, Stephen M., Caberlotto, Laura L., Emmons, Amanda, Holmes, Ian P., Montanari, Dino, Norris, Roz, Puckey, Gemma V., Walters, Dewi J., Watson, Steve P., Willis, John

“…The optimisation of diamide 1 to amine 2, a soluble and selective NPY Y2 receptor antagonist with enhanced CNS exposure is described. The identification and…”
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Dopamine D3 receptor antagonists: The quest for a potentially selective PET ligand. Part one: Lead identification by HOLMES, Ian P, MICHELI, Fabrizio, GAINES, Simon, LORTHIOIR, Olivier, WATSON, Steve P, DI FABIO, Romano, GENTILE, Gabriella, HEIDBREDER, Christian, SAVOIA, Chiara, WORBY, Angela

“…The synthesis and SAR of a new series of potent and selective dopamine D(3) receptor antagonists is reported…”
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The identification and optimisation of novel and selective diamide neuropeptide Y Y2 receptor antagonists by Lunniss, Gillian E., Barnes, Ashley A., Barton, Nick, Biagetti, Matteo, Bianchi, Federica, Blowers, Stephen M., Caberlotto, Laura, Emmons, Amanda, Holmes, Ian P., Montanari, Dino, Norris, Ros, Walters, Dewi J., Watson, Steve P.

“…Identification of novel small molecule NPY Y2 antagonist 3 and optimisation through to 36 is described. A novel small molecule NPY Y2 antagonist (3) identified…”
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The identification of β-hydroxy carboxylic acids as selective MMP-12 inhibitors by Holmes, Ian P., Gaines, Simon, Watson, Steve P., Lorthioir, Olivier, Walker, Adam, Baddeley, Suzanne J., Herbert, Shane, Egan, Danielle, Convery, Máire A., Singh, Onkar M.P., Gross, Jeffrey W., Strelow, John M., Smith, Robert H., Amour, Augustin J., Brown, David, Martin, Stephen L.

“…A new class of selective MMP-12 inhibitors have been identified via high throughput screening. Crystallization with MMP-12 confirmed the mode of binding and…”
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The identification of a selective dopamine D2 partial agonist, D3 antagonist displaying high levels of brain exposure by HOLMES, Ian P, BLUNT, Richard J, HOWES, Claire M, MICHELI, Fabrizio, DI FABIO, Romano, DONATI, Daniele, TERRENI, Silvia, HAMPRECHT, Dieter, ARISTA, Luca, WORBY, Angela, WATSON, Steve P, LORTHIOIR, Olivier E, BLOWERS, Stephen M, GRIBBLE, Andy, PAYNE, Andrew H, STANSFIELD, Ian G, WOOD, Martyn, WOOLLARD, Patrick M, REAVILL, Charlie

“…The identification of a highly selective D(2) partial agonist, D(3) antagonist tool molecule which demonstrates high levels of brain exposure and selectivity…”
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A simple, user-friendly process for the homologation of aldehydes using tosylhydrazone salts by Aggarwal, Varinder K, de Vicente, Javier, Pelotier, Beatrice, Holmes, Ian P, Bonnert, Roger V

“…Aldehydes can be homologated to ketones in moderate to good yields using aryldiazomethanes generated in situ from tosylhydrazones. Chiral aldehydes can be…”
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Palladium-Catalyzed Tandem Alkenyl and Aryl CN Bond Formation: A Cascade N-Annulation Route to 1-Functionalized Indoles by Willis, Michael C., Brace, Gareth N., Holmes, Ian P.

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Chemisch katalysierte asymmetrische Cyanhydrinsynthesen by Brunel, Jean-Michel, Holmes, Ian P.

“…In den letzten 20 Jahren wurden bemerkenswerte Fortschritte bei der Entwicklung chemisch katalysierter asymmetrischer Cyanhydrinsynthesen erzielt. Klassische,…”
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Palladium-Catalyzed Tandem Alkenyl and Aryl CN Bond Formation: A Cascade N-Annulation Route to 1-Functionalized Indoles by Willis, Michael C., Brace, Gareth N., Holmes, Ian P.

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Abstract 5371: PRMT5 inhibitors as novel treatment for cancers by Falk, Hendrik, Foitzik, Richard C., Allan, Elizabeth, deSilva, Melanie, Yang, Hong, Bozikis, Ylva E., Nikac, Marica, Walker, Scott R., Camerino, Michelle A., Morrow, Ben J., Stupple, Alexandra E., Lagiakos, Rachel, Pinson, Jo-Anne, Lessene, Romina, Kersten, Wilhelmus JA, Ganame, Danny G., Holmes, Ian P., Lunniss, Gill E., Chung, Matthew, Hermans, Stefan J., Parker, Michael W., Thistlethwaite, Alison, White, Karen, Charman, Susan A., Monahan, Brendon J., Pilling, Patricia, Grusovin, Julian, Peat, Thomas S., Sonderegger, Stefan, Toulmin, Emma, Jane, Stephen M., Curtis, David J., Stupple, Paul A., Street, Ian P.

“…Increased expression or dysregulation of protein arginine methyltransferase 5 (PRMT5) activity is associated with poor prognosis in many cancers. Through…”
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Dopamine D 3 receptor antagonists: The quest for a potentially selective PET ligand. Part one: Lead identification by Holmes, Ian P., Micheli, Fabrizio, Gaines, Simon, Lorthioir, Olivier, Watson, Steve P., Fabio, Romano Di, Gentile, Gabriella, Heidbreder, Christian, Savoia, Chiara, Worby, Angela

“…The synthesis of a new class of potent and selective D 3 antagonists is reported. The synthesis and SAR of a new series of potent and selective dopamine D 3…”
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The identification of a selective dopamine D 2 partial agonist, D 3 antagonist displaying high levels of brain exposure by Holmes, Ian P., Blunt, Richard J., Lorthioir, Olivier E., Blowers, Stephen M., Gribble, Andy, Payne, Andrew H., Stansfield, Ian G., Wood, Martyn, Woollard, Patrick M., Reavill, Charlie, Howes, Claire M., Micheli, Fabrizio, Fabio, Romano Di, Donati, Daniele, Terreni, Silvia, Hamprecht, Dieter, Arista, Luca, Worby, Angela, Watson, Steve P.

“…The identification of a hitherto unprecedented pharmacology in a compound ( 3) displaying highly selective DA D2 partial agonism and DA D3 antagonism, but…”
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The identification of a selective dopamine D sub(2) partial agonist, D sub(3) antagonist displaying high levels of brain exposure by Holmes, Ian P, Blunt, Richard J, Lorthioir, Olivier E, Blowers, Stephen M, Gribble, Andy, Payne, Andrew H, Stansfield, Ian G, Wood, Martyn, Woollard, Patrick M, Reavill, Charlie, Howes, Claire M, Micheli, Fabrizio, Di Fabio, Romano, Donati, Daniele, Terreni, Silvia, Hamprecht, Dieter, Arista, Luca, Worby, Angela, Watson, Steve P

“…The identification of a highly selective D sub(2) partial agonist, D sub(3) antagonist tool molecule which demonstrates high levels of brain exposure and…”
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Palladium‐Catalyzed Tandem Alkenyl and Aryl CN Bond Formation: A Cascade N‐Annulation Route to 1‐Functionalized Indoles by Willis, Michael C., Brace, Gareth N., Holmes, Ian P.

“…In nur einer Stufe gewährt eine Tandemreaktion Zugang zu einer Vielfalt substituierter N‐funktionalisierter Indole. Das Stickstoffatom des Indolrings wird…”
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