Search Results - "OLIVIERI, Philip R"

Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo Activity by Schenkel, Laurie B, Olivieri, Philip R, Boezio, Alessandro A, Deak, Holly L, Emkey, Renee, Graceffa, Russell F, Gunaydin, Hakan, Guzman-Perez, Angel, Lee, Josie H, Teffera, Yohannes, Wang, Weiya, Youngblood, Beth D, Yu, Violeta L, Zhang, Maosheng, Gavva, Narender R, Lehto, Sonya G, Geuns-Meyer, Stephanie

“…There has been significant interest in developing a transient receptor potential A1 (TRPA1) antagonist for the treatment of pain due to a wealth of data…”
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Synthesis of 4-Substituted Chlorophthalazines, Dihydrobenzoazepinediones, 2-Pyrazolylbenzoic Acid, and 2-Pyrazolylbenzohydrazide via 3-Substituted 3-Hydroxyisoindolin-1-ones by Nguyen, Hanh Nho, Cee, Victor J, Deak, Holly L, Du, Bingfan, Faber, Kathleen Panter, Gunaydin, Hakan, Hodous, Brian L, Hollis, Steven L, Krolikowski, Paul H, Olivieri, Philip R, Patel, Vinod F, Romero, Karina, Schenkel, Laurie B, Geuns-Meyer, Stephanie D

“…Herein we describe a general three-step synthesis of 4-substituted chlorophthalazines in good overall yields. In the key step, N,N-dimethylaminophthalimide…”
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Evolution of a Highly Selective and Potent 2-(Pyridin-2-yl)-1,3,5-triazine Tie-2 Kinase Inhibitor by Hodous, Brian L, Geuns-Meyer, Stephanie D, Hughes, Paul E, Albrecht, Brian K, Bellon, Steve, Bready, James, Caenepeel, Sean, Cee, Victor J, Chaffee, Stuart C, Coxon, Angela, Emery, Maurice, Fretland, Jenne, Gallant, Paul, Gu, Yan, Hoffman, Doug, Johnson, Rebecca E, Kendall, Richard, Kim, Joseph L, Long, Alexander M, Morrison, Michael, Olivieri, Philip R, Patel, Vinod F, Polverino, Anthony, Rose, Paul, Tempest, Paul, Wang, Ling, Whittington, Douglas A, Zhao, Huilin

“…Inhibition of angiogenesis is a promising and clinically validated approach for limiting tumor growth and survival. The receptor tyrosine kinase Tie-2 is…”
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Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors by Hodous, Brian L., Geuns-Meyer, Stephanie D., Hughes, Paul E., Albrecht, Brian K., Bellon, Steve, Caenepeel, Sean, Cee, Victor J., Chaffee, Stuart C., Emery, Maurice, Fretland, Jenne, Gallant, Paul, Gu, Yan, Johnson, Rebecca E., Kim, Joseph L., Long, Alexander M., Morrison, Michael, Olivieri, Philip R., Patel, Vinod F., Polverino, Anthony, Rose, Paul, Wang, Ling, Zhao, Huilin

“…A novel class of selective Tie-2 inhibitors was derived from a multi-kinase inhibitor 1. By reversing the amide connectivity and incorporating aminotriazine or…”
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Preclinical Evaluation of AMG 900, a Novel Potent and Highly Selective Pan-Aurora Kinase Inhibitor with Activity in Taxane-Resistant Tumor Cell Lines by PAYTON, Marc, BUSH, Tammy L, NHO NGUYEN, Hanh, OLIVIERI, Philip R, ROMERO, Karina, SCHENKEL, Laurie B, BAK, Annette, STANTON, Mary, DUSSAULT, Isabelle, PATEL, Vinod F, GEUNS-MEYER, Stephanie, RADINSKY, Robert, CHUNG, Grace, KENDALL, Richard L, ZIEGLER, Beth, EDEN, Patrick, MCELROY, Patricia, ROSS, Sandra, CEE, Victor J, DEAK, Holly L, HODOUS, Brian L

“…In mammalian cells, the aurora kinases (aurora-A, -B, and -C) play essential roles in regulating cell division. The expression of aurora-A and -B is elevated…”
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Discovery of N‑(4-(3-(2-Aminopyrimidin-4-yl)pyridin-2-yloxy)phenyl)-4-(4-methylthiophen-2-yl)phthalazin-1-amine (AMG 900), A Highly Selective, Orally Bioavailable Inhibitor of Aurora Kinases with Activity against Multidrug-Resistant Cancer Cell Lines by Geuns-Meyer, Stephanie, Cee, Victor J, Deak, Holly L, Du, Bingfan, Hodous, Brian L, Nguyen, Hanh Nho, Olivieri, Philip R, Schenkel, Laurie B, Vaida, Karina R, Andrews, Paul, Bak, Annette, Be, Xuhai, Beltran, Pedro J, Bush, Tammy L, Chaves, Mary K, Chung, Grace, Dai, Yang, Eden, Patrick, Hanestad, Kelly, Huang, Liyue, Lin, Min-Hwa Jasmine, Tang, Jin, Ziegler, Beth, Radinsky, Robert, Kendall, Richard, Patel, Vinod F, Payton, Marc

“…Efforts to improve upon the physical properties and metabolic stability of Aurora kinase inhibitor 14a revealed that potency against multidrug-resistant cell…”
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Discovery of a Potent, Selective, and Orally Bioavailable Pyridinyl-Pyrimidine Phthalazine Aurora Kinase Inhibitor by Cee, Victor J, Schenkel, Laurie B, Hodous, Brian L, Deak, Holly L, Nguyen, Hanh N, Olivieri, Philip R, Romero, Karina, Bak, Annette, Be, Xuhai, Bellon, Steve, Bush, Tammy L, Cheng, Alan C, Chung, Grace, Coats, Steve, Eden, Patrick M, Hanestad, Kelly, Gallant, Paul L, Gu, Yan, Huang, Xin, Kendall, Richard L, Lin, Min-Hwa Jasmine, Morrison, Michael J, Patel, Vinod F, Radinsky, Robert, Rose, Paul E, Ross, Sandra, Sun, Ji-Rong, Tang, Jin, Zhao, Huilin, Payton, Marc, Geuns-Meyer, Stephanie D

“…The discovery of aurora kinases as essential regulators of cell division has led to intense interest in identifying small molecule aurora kinase inhibitors for…”
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Pyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase by Cee, Victor J., Cheng, Alan C., Romero, Karina, Bellon, Steve, Mohr, Christopher, Whittington, Douglas A., Bak, Annette, Bready, James, Caenepeel, Sean, Coxon, Angela, Deak, Holly L., Fretland, Jenne, Gu, Yan, Hodous, Brian L., Huang, Xin, Kim, Joseph L., Lin, Jasmine, Long, Alexander M., Nguyen, Hanh, Olivieri, Philip R., Patel, Vinod F., Wang, Ling, Zhou, Yihong, Hughes, Paul, Geuns-Meyer, Stephanie

“…The optimization of a nonselective scaffold into 15, a potent inhibitor of Tie-2 kinase with selectivity against VEGFR2 kinase, is reported. Selective small…”
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Alkynylpyrimidine Amide Derivatives as Potent, Selective, and Orally Active Inhibitors of Tie-2 Kinase by Cee, Victor J, Albrecht, Brian K, Geuns-Meyer, Stephanie, Hughes, Paul, Bellon, Steve, Bready, James, Caenepeel, Sean, Chaffee, Stuart C, Coxon, Angela, Emery, Maurice, Fretland, Jenne, Gallant, Paul, Gu, Yan, Hodous, Brian L, Hoffman, Doug, Johnson, Rebecca E, Kendall, Richard, Kim, Joseph L, Long, Alexander M, McGowan, David, Morrison, Michael, Olivieri, Philip R, Patel, Vinod F, Polverino, Anthony, Powers, David, Rose, Paul, Wang, Ling, Zhao, Huilin

“…The recognition that aberrant angiogenesis contributes to the pathology of inflammatory diseases, cancer, and myocardial ischemia has generated considerable…”
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Abstract 5776: Discovery of AMG 900, a highly selective, orally bioavailable inhibitor of aurora kinases with efficacy in preclinical antitumor models and activity against multidrug-resistant cells by Geuns-Meyer, Stephanie, Cee, Victor J., Deak, Holly L., Du, Bingfan, Hodous, Brian L., Nguyen, Hanh N., Olivieri, Philip R., Romero, Karina, Schenkel, Laurie B., Patel, Vinod F., Be, Xuhai, Bush, Tammy L., Chung, Grace, Eden, Patrick, Huang, Liyue, Kendall, Richard, Lin, Min-Hwa Jasmine, Radinsky, Robert, Ziegler, Beth, Payton, Marc

“…Abstract The aurora family of serine/threonine kinases (Aurora-A, -B, -C) regulate cell-cycle progression in mammalian cells. Whereas aurora kinase C function…”
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