Search Results - "Jean-Marc Plancher"

Systematic Investigation of Halogen Bonding in Protein-Ligand Interactions by Hardegger, Leo A., Kuhn, Bernd, Spinnler, Beat, Anselm, Lilli, Ecabert, Robert, Stihle, Martine, Gsell, Bernard, Thoma, Ralf, Diez, Joachim, Benz, Jörg, Plancher, Jean-Marc, Hartmann, Guido, Banner, David W., Haap, Wolfgang, Diederich, François

“…Halogen bonding triggers activity: Increasing binding affinity was observed for a series of covalent human Cathepsin L inhibitors by exchanging an aryl ring H…”
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Evaluation of tert-Butyl Isosteres: Case Studies of Physicochemical and Pharmacokinetic Properties, Efficacies, and Activities by Westphal, Matthias V., Wolfstädter, Bernd T., Plancher, Jean-Marc, Gatfield, John, Carreira, Erick M.

“…The tert‐butyl group is a common motif in medicinal chemistry. Its incorporation into bioactive compounds is often accompanied by unwanted property modulation,…”
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Formation of α-SF5-Enolate Enables Preparation of 3-SF5-Quinolin-2-ones, 3-SF5-Quinolines, and 3-SF5-Pyridin-2-ones: Evaluation of their Physicochemical Properties by Joliton, Adrien, Plancher, Jean-Marc, Carreira, Erick M.

“…This study describes, for the first time, the generation of a SF5‐substituted ester enolate from benzyl SF5‐acetate under soft enolization conditions, which in…”
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Synthesis and Stability of Oxetane Analogs of Thalidomide and Lenalidomide by Burkhard, Johannes A, Wuitschik, Georg, Plancher, Jean-Marc, Rogers-Evans, Mark, Carreira, Erick M

“…Oxetanes are used in drug discovery to enable physicochemical and metabolic property enhancement for the structures to which they are grafted. An imide CO to…”
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Halogen Bonding at the Active Sites of Human Cathepsin L and MEK1 Kinase: Efficient Interactions in Different Environments by Hardegger, Leo A., Kuhn, Bernd, Spinnler, Beat, Anselm, Lilli, Ecabert, Robert, Stihle, Martine, Gsell, Bernard, Thoma, Ralf, Diez, Joachim, Benz, Jörg, Plancher, Jean-Marc, Hartmann, Guido, Isshiki, Yoshiaki, Morikami, Kenji, Shimma, Nobuo, Haap, Wolfgang, Banner, David W., Diederich, François

“…In two series of small‐molecule ligands, one inhibiting human cathepsin L (hcatL) and the other MEK1 kinase, biological affinities were found to strongly…”
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Adventures in drug-like chemistry space: from oxetanes to spiroazetidines and beyond by Rogers-Evans, Mark, Knust, Henner, Plancher, Jean-Marc, Carreira, Erick M, Wuitschik, George, Burkhard, Johannes, Li, Dong B, Guérot, Carine

“…Recently we have documented research efforts aimed at new classes of oxetanes as well as spiroheteroalicyclic ring systems (which we have termed 'Compact…”
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Gene expression-based in vivo and in vitro prediction of liver toxicity allows compound selection at an early stage of drug development by Roth, Adrian, Boess, Franziska, Landes, Christian, Steiner, Guido, Freichel, Christian, Plancher, Jean-Marc, Raab, Susanne, de Vera Mudry, Cristina, Weiser, Thomas, Suter, Laura

“…We have analyzed gene expression and histopathology of rat liver treated with a histamine‐3 receptor inverse agonist under development for the treatment of…”
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Mild and chemoselective catalytic deprotection of ketals and acetals using cerium(IV) ammonium nitrate by Ates, Ali, Gautier, Arnaud, Leroy, Bernard, Plancher, Jean-Marc, Quesnel, Yannick, Vanherck, Jean-Christophe, Markó, István E

“…Cerium(IV) ammonium nitrate (CAN) is a powerful, though mild, reagent for the efficient and selective removal of a range of ketals and acetals. This novel…”
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Small-Molecule Lead-Finding Trends across the Roche and Genentech Research Organizations by Dragovich, Peter S, Haap, Wolfgang, Mulvihill, Melinda M, Plancher, Jean-Marc, Stepan, Antonia F

“…The origin of small-molecule leads that were pursued across the independent research organizations Roche and Genentech from 2009 to 2020 is described. The…”
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Cerium(IV)-Catalyzed Deprotection of Acetals and Ketals under Mildly Basic Conditions by Markó, István E., Ates, Ali, Gautier, Arnaud, Leroy, Bernard, Plancher, Jean-Marc, Quesnel, Yannick, Vanherck, Jean-Christophe

“…Smooth and quantitative deprotection of a wide range of acetals and ketals [Eq. (a); R, R1=alkyl, aryl, H] under neutral to mildly basic conditions was…”
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Chemoproteomic discovery of a covalent allosteric inhibitor of WRN helicase by Baltgalvis, Kristen A., Lamb, Kelsey N., Symons, Kent T., Wu, Chu-Chiao, Hoffman, Melissa A., Snead, Aaron N., Song, Xiaodan, Glaza, Thomas, Kikuchi, Shota, Green, Jason C., Rogness, Donald C., Lam, Betty, Rodriguez-Aguirre, Maria E., Woody, David R., Eissler, Christie L., Rodiles, Socorro, Negron, Seth M., Bernard, Steffen M., Tran, Eileen, Pollock, Jonathan, Tabatabaei, Ali, Contreras, Victor, Williams, Heather N., Pastuszka, Martha K., Sigler, John J., Pettazzoni, Piergiorgio, Rudolph, Markus G., Classen, Moritz, Brugger, Doris, Claiborne, Christopher, Plancher, Jean-Marc, Cuartas, Isabel, Seoane, Joan, Burgess, Laurence E., Abraham, Robert T., Weinstein, David S., Simon, Gabriel M., Patricelli, Matthew P., Kinsella, Todd M.

“…WRN helicase is a promising target for treatment of cancers with microsatellite instability (MSI) due to its essential role in resolving deleterious…”
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Aminothiazole Derivatives as Neuropeptide Y5 Receptor Ligands: Finding the Balance between Affinity and Physicochemical Properties by Nettekoven, Matthias, Guba, Wolfgang, Neidhart, Werner, Mattei, Patrizio, Pflieger, Philippe, Plancher, Jean-Marc, Taylor, Sven

“…Potential appetite control: A straightforward parallel solution‐phase synthesis of novel thiazole derivatives with varying linker moieties gave access to a set…”
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Discovery of novel and orally active FXR agonists for the potential treatment of dyslipidemia & diabetes by Richter, Hans G.F., Benson, Gregory M., Blum, Denise, Chaput, Evelyne, Feng, Song, Gardes, Christophe, Grether, Uwe, Hartman, Peter, Kuhn, Bernd, Martin, Rainer E., Plancher, Jean-Marc, Rudolph, Markus G., Schuler, Franz, Taylor, Sven, Bleicher, Konrad H.

“…Herein we describe the synthesis and structure activity relationship of a new class of FXR agonists identified from a high-throughput screening campaign…”
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Histamine-3 Receptor Inverse Agonists for the Treatment of Obesity: Validation of the Target and Identification of Novel Series by Pascale David Pierson, Christoph Ullmer, Sven Taylor, Tadakatsu Takahashi, Franz Schuler, Monique Schmitt, Rosa María Rodríguez Sarmiento, Olivier Roche, Hans Richter, Susanne Raab, Jean-Marc Plancher, Matthias Nettekoven, Toshito Nakagawa, Peter Mohr, Jörg Huwyler, Cornelia Hertel, Silvia Gatti-Mac Arthur, Christian Freichel, Ruby Wiegand

“…Obesity is a major risk factor for the development of conditions such as hypertension, hyperglycemia, dyslipidemia, coronary artery disease and cancer. Several…”
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Identification of an N-oxide pyridine GW4064 analog as a potent FXR agonist by Feng, Song, Yang, Minmin, Zhang, Zhenshan, Wang, Zhanguo, Hong, Di, Richter, Hans, Benson, Gregory Martin, Bleicher, Konrad, Grether, Uwe, Martin, Rainer E., Plancher, Jean-Marc, Kuhn, Bernd, Rudolph, Markus Georg, Chen, Li

“…A series of 3-aryl heterocyclic isoxazole analogs were designed and synthesized, N-oxide pyridine analog ( 7b) was identified as a promising FXR agonist with…”
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Inside Cover: Evaluation of tert-Butyl Isosteres: Case Studies of Physicochemical and Pharmacokinetic Properties, Efficacies, and Activities (ChemMedChem 3/2015) by Westphal, Matthias V., Wolfstädter, Bernd T., Plancher, Jean-Marc, Gatfield, John, Carreira, Erick M.

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Selective naphthalene H3 receptor inverse agonists with reduced potential to induce phospholipidosis and their quinoline analogs by Rodríguez Sarmiento, Rosa María, Nettekoven, Matthias H., Taylor, Sven, Plancher, Jean-Marc, Richter, Hans, Roche, Olivier

“…We reported earlier the refinement of our initial five-point pharmacophore model for the Histamine 3 receptor (H3R), with a new acceptor feature important for…”
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Formation of α-SF5-Enolate Enables Preparation of 3-SF5-Quinolin-2-ones, 3-SF5-Quinolines, and 3-SF5-Pyridin-2-ones: Evaluation of their Physicochemical Properties by Joliton, Adrien, Plancher, Jean-Marc, Carreira, Erick M.

“…This study describes, for the first time, the generation of a SF5‐substituted ester enolate from benzyl SF5‐acetate under soft enolization conditions, which in…”
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5-Hydroxyindole-2-carboxylic Acid Amides: Novel Histamine-3 Receptor Inverse Agonists for the Treatment of Obesity by Pierson, Pascale David, Fettes, Alec, Freichel, Christian, Gatti-McArthur, Silvia, Hertel, Cornelia, Huwyler, Jörg, Mohr, Peter, Nakagawa, Toshito, Nettekoven, Matthias, Plancher, Jean-Marc, Raab, Susanne, Richter, Hans, Roche, Olivier, Rodríguez Sarmiento, Rosa María, Schmitt, Monique, Schuler, Franz, Takahashi, Tadakatsu, Taylor, Sven, Ullmer, Christoph, Wiegand, Ruby

“…Obesity is a major risk factor in the development of conditions such as hypertension, hyperglycemia, dyslipidemia, coronary artery disease, and cancer. Several…”
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5-HT2C Receptor Agonists for the Treatment of Obesity. Biological and Chemical Adventures by David Adams, Sven Taylor, Stephan Röver, Hans Richter, Jean-Marc Plancher, Jacques Mizrahi, Craig S. Malcolm, Antony R. Knight, Guy A. Kennett, Paul Hebeisen, Ian A. Cliffe, Anne Bourson, Caterina Bissantz, Jon M. Bentley, Mike J. Bickerdike, Agnès Bénardeau, Steven P. Vickers

“…Obesity is a major risk factor in the development of conditions such as hypertension, hyperglycemia, dyslipidemia, coronary artery disease and cancer. There is…”
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