Search Results - "Young, Erick R.R."

Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: Part 2, optimization for blood pressure reduction in spontaneously hypertensive rats by GINN, John D, BOSANAC, Todd, SCHLYER, Sabine, SMITH, James D, TURNER, Michael R, WU, Frank, YOUNG, Erick R. R, CHEN, Rhonda, CYWIN, Charles, HICKEY, Eugene, KASHEM, Mohammed, KERR, Steven, KUGLER, Stanley, XIANG LI, PROKOPOWICZ, Anthony

“…Phenylglycine substituted isoquinolones 1 and 2 have previously been described as potent dual ROCK1/ROCK2 inhibitors. Here we describe the further SAR of this…”
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Novel cross-talk within the IKK family controls innate immunity by Clark, Kristopher, Peggie, Mark, Plater, Lorna, Sorcek, Ronald J, Young, Erick R R, Madwed, Jeffrey B, Hough, Joanne, McIver, Edward G, Cohen, Philip

“…Members of the IKK {IκB [inhibitor of NF-κB (nuclear factor κB)] kinase} family play a central role in innate immunity by inducing NF-κB- and IRF [IFN…”
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Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: Part 3, aryl substituted pyrrolidines by Bosanac, Todd, Hickey, Eugene R., Ginn, John, Kashem, Mohammed, Kerr, Steven, Kugler, Stanley, Li, Xiang, Olague, Alan, Schlyer, Sabine, Young, Erick R.R.

“…The discovery and SAR of a series of β-aryl substituted pyrrolidine 2H-isoquinolin-1-one inhibitors of Rho-kinase (ROCK) derived from 2 is herein described…”
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Discovery of potent and selective PKC-θ inhibitors by Cywin, Charles L., Dahmann, Georg, Prokopowicz, Anthony S., Young, Erick R.R., Magolda, Ronald L., Cardozo, Mario G., Cogan, Derek A., DiSalvo, Darren, Ginn, John D., Kashem, Mohammed A., Wolak, John P., Homon, Carol A., Farrell, Thomas M., Grbic, Heather, Hu, Hanbo, Kaplita, Paul V., Liu, Lisa H., Spero, Denice M., Jeanfavre, Deborah D., O’Shea, Kathy M., White, Della M., Woska, Joseph R., Brown, Maryanne L.

“…An uHTS campaign was performed to identify selective inhibitors of PKC-θ. Initial triaging of the hit set based on selectivity and historical analysis led to…”
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Substituted 2 H-isoquinolin-1-ones as potent Rho-kinase inhibitors: Part 2, optimization for blood pressure reduction in spontaneously hypertensive rats by Ginn, John D., Bosanac, Todd, Chen, Rhonda, Cywin, Charles, Hickey, Eugene, Kashem, Mohammed, Kerr, Steven, Kugler, Stanley, Li, Xiang, Prokopowicz, Anthony, Schlyer, Sabine, Smith, James D., Turner, Michael R., Wu, Frank, Young, Erick R.R.

“…Phenylglycine substituted isoquinolones 1 and 2 have previously been described as potent dual ROCK1/ROCK2 inhibitors. Here we describe the further SAR of this…”
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BI 5700, a Selective Chemical Inhibitor of IκB Kinase 2, Specifically Suppresses Epithelial-Mesenchymal Transition and Metastasis in Mouse Models of Tumor Progression by Huber, Margit A, Maier, Harald J, Alacakaptan, Memetcan, Wiedemann, Eva, Braunger, Jürgen, Boehmelt, Guido, Madwed, Jeffrey B, Young, Erick R R, Marshall, Daniel R, Pehamberger, Hubert, Wirth, Thomas, Kraut, Norbert, Beug, Hartmut

“…Increasing evidence suggests that processes termed epithelial-mesenchymal transitions (EMTs) play a key role in therapeutic resistance, tumor recurrence, and…”
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Identification of a novel class of succinyl-nitrile-based Cathepsin S inhibitors by Bekkali, Younes, Thomson, David S., Betageri, Raj, Emmanuel, Michel J., Hao, Ming-Hong, Hickey, Eugene, Liu, Weimin, Patel, Usha, Ward, Yancey D., Young, Erick R.R., Nelson, Richard, Kukulka, Alison, Brown, Maryanne L., Crane, Kathy, White, Della, Freeman, Dorothy M., Labadia, Mark E., Wildeson, Jessi, Spero, Denice M.

“…The synthesis and SAR of the first succinyl-nitrile-based compounds as Cathepsin S inhibitors are described. The synthesis and in vitro activities of a series…”
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A Practical Synthesis of Pyrene-4,5-dione by Young, Erick R. R, Funk, Raymond L

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Vinyl and Alkynyl Pyrimidines as Michael Acceptors:  An Approach to a Cylindrospermopsin Substructure by Djung, Jane F, Hart, David J, Young, Erick R. R

“…Vinyl pyrimidine 9 and alkynyl pyrimidine 24 undergo base-mediated intramolecular conjugate addition reactions in which a carbamate and a urea, respectively,…”
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