Search Results - "SPANKA, Carsten"

Discovery of 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), A Potent and Selective Inhibitor of the Fibroblast Growth Factor Receptor Family of Receptor Tyrosine Kinase by Guagnano, Vito, Furet, Pascal, Spanka, Carsten, Bordas, Vincent, Le Douget, Mickaël, Stamm, Christelle, Brueggen, Josef, Jensen, Michael R, Schnell, Christian, Schmid, Herbert, Wartmann, Markus, Berghausen, Joerg, Drueckes, Peter, Zimmerlin, Alfred, Bussiere, Dirksen, Murray, Jeremy, Graus Porta, Diana

“…A novel series of N-aryl-N′-pyrimidin-4-yl ureas has been optimized to afford potent and selective inhibitors of the fibroblast growth factor receptor tyrosine…”
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Design and Synthesis of Metabolically Stable tRNA Synthetase Inhibitors Derived from Cladosporin by Rusch, Marion, Thevenon, Arnaud, Hoepfner, Dominic, Aust, Thomas, Studer, Christian, Patoor, Maude, Rollin, Patrick, Livendahl, Madeleine, Ranieri, Beatrice, Schmitt, Esther, Spanka, Carsten, Gademann, Karl, Bouchez, Laure C.

“…Selective and specific inhibitors of Plasmodium falciparum lysyl‐tRNA synthetase represent promising therapeutic antimalarial avenues. Cladosporin was…”
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N-Sulfonylanthranilic Acid Derivatives as Allosteric Inhibitors of Dengue Viral RNA-Dependent RNA Polymerase by Yin, Zheng, Chen, Yen-Liang, Kondreddi, Ravinder Reddy, Chan, Wai Ling, Wang, Gang, Ng, Ru Hui, Lim, Joanne Y. H, Lee, Wan Yen, Jeyaraj, Duraiswamy A, Niyomrattanakit, Pornwaratt, Wen, Daying, Chao, Alex, Glickman, J. Fraser, Voshol, Hans, Mueller, Dieter, Spanka, Carsten, Dressler, Sigmar, Nilar, Shahul, Vasudevan, Subhash G, Shi, Pei-Yong, Keller, Thomas H

“…A novel class of compounds containing N-sulfonylanthranilic acid was found to specifically inhibit dengue viral polymerase. The structural requirements for…”
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Solid-Phase Rhodium Carbenoid Reactions:  An N−H Insertion Route to a Diverse Series of Oxazoles by Clapham, Bruce, Spanka, Carsten, Janda, Kim D

“…The solid-phase synthesis of a series of oxazoles is described. The key step in the construction of these molecules involves the rhodium-catalyzed…”
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A segmented flow platform for on-demand medicinal chemistry and compound synthesis in oscillating droplets by Hwang, Ye-Jin, Coley, Connor W, Abolhasani, Milad, Marzinzik, Andreas L, Koch, Guido, Spanka, Carsten, Lehmann, Hansjoerg, Jensen, Klavs F

“…We report an automated flow chemistry platform that can efficiently perform a wide range of chemistries, including single/multi-phase and single/multi-step,…”
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Oxysterols direct immune cell migration via EBI2 by Hannedouche, Sébastien, Zhang, Juan, Yi, Tangsheng, Shen, Weijun, Nguyen, Deborah, Pereira, João P., Guerini, Danilo, Baumgarten, Birgit U., Roggo, Silvio, Wen, Ben, Knochenmuss, Richard, Noël, Sophie, Gessier, Francois, Kelly, Lisa M., Vanek, Mirka, Laurent, Stephane, Preuss, Inga, Miault, Charlotte, Christen, Isabelle, Karuna, Ratna, Li, Wei, Koo, Dong-In, Suply, Thomas, Schmedt, Christian, Peters, Eric C., Falchetto, Rocco, Katopodis, Andreas, Spanka, Carsten, Roy, Marie-Odile, Detheux, Michel, Chen, Yu Alice, Schultz, Peter G., Cho, Charles Y., Seuwen, Klaus, Cyster, Jason G., Sailer, Andreas W.

“…EBI2 receptors revealed as oxysterols The EBI2 receptor (Epstein–Barr virus-induced gene 2, also known as GPR183) was recently shown to be linked to autoimmune…”
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Discovery of Amino Alcohols as Highly Potent, Selective, and Orally Efficacious Inhibitors of Leukotriene A4 Hydrolase by Thoma, Gebhard, Markert, Christian, Lueoend, Rainer, Miltz, Wolfgang, Spanka, Carsten, Bollbuck, Birgit, Wolf, Romain M., Srinivas, Honnappa, Penno, Carlos A., Kiffe, Michael, Gajewska, Monika, Bednarczyk, Dallas, Wieczorek, Grazyna, Evans, Amanda, Beerli, Christian, Röhn, Till A.

“…The discovery of chiral amino alcohols derived from our previously disclosed clinical LTA4H inhibitor LYS006 is described. In a biochemical assay, their…”
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Developing soluble polymers for high-throughput synthetic chemistry by Spanka, Carsten, Wentworth, Jr, Paul, Janda, Kim D

“…Soluble polymers have emerged as viable alternatives to resin supports across the broad spectrum of high-throughput organic chemistry. As the application of…”
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Piperidyl amides as novel, potent and orally active mGlu5 receptor antagonists with anxiolytic-like activity by Spanka, Carsten, Glatthar, Ralf, Desrayaud, Sandrine, Fendt, Markus, Orain, David, Troxler, Thomas, Vranesic, Ivo

“…Novel mGluR5 antagonists have been developed. SAR studies and lead optimizations are described, which result in compound 16m with high efficacy in animal…”
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The discovery of potent, orally bioavailable pyrazolo and triazolopyrimidine CXCR2 receptor antagonists by Porter, David W, Bradley, Michelle, Brown, Zarin, Canova, Riccardo, Charlton, Steven, Cox, Brian, Hunt, Peter, Kolarik, David, Lewis, Sarah, O'Connor, Des, Reilly, John, Spanka, Carsten, Tedaldi, Lauren, Watson, Simon J, Wermuth, Roland, Press, Neil J

“…A hit-to-lead optimisation programme was carried out on the Novartis archive screening hit, pyrazolopyrimidine…”
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Stabilizing Inactive Conformations of MALT1 as an Effective Approach to Inhibit Its Protease Activity by Hughes, Nicola, Erbel, Paul, Bornancin, Frédéric, Wiesmann, Christian, Schiering, Nikolaus, Villard, Frédéric, Decock, Arnaud, Rubi, Bertran, Melkko, Samu, Spanka, Carsten, Buschmann, Nicole, Pissot‐Soldermann, Carole, Simic, Oliver, Beerli, René, Sorge, Mickael, Tintelnot‐Blomley, Marina, Beltz, Karen, Régnier, Catherine H., Quancard, Jean, Schlapbach, Achim, Langlois, Jean‐Baptiste, Renatus, Martin

“…The paracaspase MALT1 (mucosa associated lymphoid tissue lymphoma translocated gene 1) plays an important role in various immune pathways and is proposed as a…”
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Abstract B246: NVP-BGJ398: A potent and selective inhibitor of the fibroblast growth factor receptor family by Guagnano, Vito, Porta, Diana Graus, Bordas, Vincent, Douget, Mickael Le, Stamm, Christelle, Furet, Pascal, Spanka, Carsten, Wartmann, Markus, Schmid, Herbert, Brueggen, Josef, Drueckes, Peter, Bussiere, Dirksen, Abrams, Tinya, Rendahl, Katherine, Bernard-Pierrot, Isabelle, Radvanyi, Francois

“…The mammalian fibroblast growth factor/fibroblast growth factor receptor (FGF/FGFR) family comprises 22 FGF ligands, 18 of which exert their action through 4…”
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Oxysterols direct immune cell migration through EBI2 by Hannedouche, Sébastien, Zhang, Juan, Yi, Tangsheng, Shen, Weijun, Nguyen, Deborah, Pereira, João P., Guerini, Danilo, Baumgarten, Birgit U., Roggo, Silvio, Wen, Ben, Knochenmuss, Richard, Noël, Sophie, Gessier, Francois, Kelly, Lisa M., Vanek, Mirka, Laurent, Stephane, Preuss, Inga, Miault, Charlotte, Christen, Isabelle, Karuna, Ratna, Li, Wei, Koo, Dong-In, Suply, Thomas, Schmedt, Christian, Peters, Eric C., Falchetto, Rocco, Katopodis, Andreas, Spanka, Carsten, Roy, Marie-Odile, Detheux, Michel, Chen, Yu Alice, Schultz, Peter G., Cho, Charles Y., Seuwen, Klaus, Cyster, Jason G., Sailer, Andreas W.

“…Epstein-Barr virus (EBV)-induced gene 2 (EBI2, aka GPR183) is a G protein-coupled receptor that is required for humoral immune responses and polymorphisms in…”
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Application of Microgels as Polymer Supports for Organic Synthesis:  Preparation of a Small Phthalide Library, a Scavenger, and a Borohydride Reagent by Shimomura, Osamu, Clapham, Bruce, Spanka, Carsten, Mahajan, Suresh, Janda, Kim D

“…Microgel polymers containing a series of functional groups have been prepared. These microgels were composed of cross-linked poly(styrene) and were prepared by…”
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Preparation of New Microgel Polymers and Their Application as Supports in Organic Synthesis by Spanka, Carsten, Clapham, Bruce, Janda, Kim D

“…A series of soluble microgel polymers have been synthesized using solution-phase polymerization reactions. In a systematic manner, several variables such as…”
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A Tunable Hydrogel for Encapsulation and Controlled Release of Bioactive Proteins by Delgado, Mercedes, Spanka, Carsten, Kerwin, Lisa D, Wentworth, Paul, Janda, Kim D

“…A N,N-dimethylacrylamide-based hydrogel (2) with the new cross-linker (ethylenedioxy) bis[2,2‘-(N-acryloylamino)ethane] (1) has been prepared, and its…”
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N Sulfonylanthranilic Acid Derivatives as Allosteric Inhibitors of Dengue Viral RNA-Dependent RNA Polymerise by ZHENG YIN, CHEN, Yen-Liang, DAYING WEN, CHAO, Alex, FRASER GLICKMAN, J, VOSHOL, Hans, MUELLER, Dieter, SPANKA, Carsten, DRESSLER, Sigmar, NILAR, Shahul, VASUDEVAN, Subhash G, SHI, Pei-Yong, REDDY KONDREDDI, Ravinder, KELLER, Thomas H, WAI LING CHAN, GANG WANG, RU HUI NG, LIM, Joanne Y. H, WAN YEN LEE, JEYARAJ, Duraiswamy A, NIYOMRATTANAKIT, Pomwaratt

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Soluble polymer-supported methods for combinatorial and organic synthesis by Wentworth, Jr, Paul, Spanka, Carsten

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Improving the Oral Bioavailability of the Iron Chelator HBED by Breaking the Symmetry of the Intramolecular H-Bond Network by Faller, Bernard, Spanka, Carsten, Sergejew, Thomas, Tschinke, Vincenzo

“…Physicochemical analysis and Monte Carlo simulations were used to identify structural features which prevent oral absorption of HBED, a potent iron chelator…”
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A Parallel Approach to the Discovery of Carrier Delivery Vehicles To Enhance Antigen Immunogenicity by Delgado, Mercedes, Lee, Kyung Joo, Altobell, Spanka, Carsten, Wentworth, Paul, Janda, Kim D

“…As part of an ongoing effort to generate human and murine monoclonal antibodies against poorly immunogenic tumor-associated antigens we have merged the rapidly…”
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