Search Results - "Dudley, Danette"

Discovery of (S)‑1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl‑1H‑pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)‑one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development by Blake, James F, Burkard, Michael, Chan, Jocelyn, Chen, Huifen, Chou, Kang-Jye, Diaz, Dolores, Dudley, Danette A, Gaudino, John J, Gould, Stephen E, Grina, Jonas, Hunsaker, Thomas, Liu, Lichuan, Martinson, Matthew, Moreno, David, Mueller, Lars, Orr, Christine, Pacheco, Patricia, Qin, Ann, Rasor, Kevin, Ren, Li, Robarge, Kirk, Shahidi-Latham, Sheerin, Stults, Jeffrey, Sullivan, Francis, Wang, Weiru, Yin, Jianping, Zhou, Aihe, Belvin, Marcia, Merchant, Mark, Moffat, John, Schwarz, Jacob B

“…The extracellular signal-regulated kinases ERK1/2 represent an essential node within the RAS/RAF/MEK/ERK signaling cascade that is commonly activated by…”
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Discovery of a Series of Imidazo[4,5-b]pyridines with Dual Activity at Angiotensin II Type 1 Receptor and Peroxisome Proliferator-Activated Receptor-γ by Casimiro-Garcia, Agustin, Filzen, Gary F, Flynn, Declan, Bigge, Christopher F, Chen, Jing, Davis, Jo Ann, Dudley, Danette A, Edmunds, Jeremy J, Esmaeil, Nadia, Geyer, Andrew, Heemstra, Ronald J, Jalaie, Mehran, Ohren, Jeffrey F, Ostroski, Robert, Ellis, Teresa, Schaum, Robert P, Stoner, Chad

“…Mining of an in-house collection of angiotensin II type 1 receptor antagonists to identify compounds with activity at the peroxisome proliferator-activated…”
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Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2 by Blake, James F., Gaudino, John J., De Meese, Jason, Mohr, Peter, Chicarelli, Mark, Tian, Hongqi, Garrey, Rustam, Thomas, Allen, Siedem, Christopher S., Welch, Michael B., Kolakowski, Gabrielle, Kaus, Robert, Burkard, Michael, Martinson, Matthew, Chen, Huifen, Dean, Brian, Dudley, Danette A., Gould, Stephen E., Pacheco, Patricia, Shahidi-Latham, Sheerin, Wang, Weiru, West, Kristina, Yin, Jianping, Moffat, John, Schwarz, Jacob B.

“…[Display omitted] The discovery and optimization of a series of tetrahydropyridopyrimidine based extracellular signal-regulated kinase (Erks) inhibitors…”
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Design, Synthesis, and Biological Activity of Potent and Selective Inhibitors of Blood Coagulation Factor Xa by Willardsen, J. Adam, Dudley, Danette A, Cody, Wayne L, Chi, Liguo, McClanahan, Thomas B, Mertz, Thomas E, Potoczak, Ronald E, Narasimhan, Lakshmi S, Holland, Debra R, Rapundalo, Stephen T, Edmunds, Jeremy J

“…Factor Xa (FXa) has materialized as a key enzyme for the intervention of the blood coagulation cascade and for the development of new antithrombotic agents…”
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The Discovery of (2R,4R)-N-(4-chlorophenyl)-N- (2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl)-4-methoxypyrrolidine-1,2-dicarboxamide (PD 0348292), an Orally Efficacious Factor Xa Inhibitor by Kohrt, Jeffrey T., Bigge, Christopher F., Bryant, John W., Casimiro-Garcia, Agustin, Chi, Liguo, Cody, Wayne L., Dahring, Tawny, Dudley, Danette A., Filipski, Kevin J., Haarer, Staci, Heemstra, Ron, Janiczek, Nancy, Narasimhan, Lakshmi, McClanahan, Thomas, Peterson, J. Thomas, Sahasrabudhe, Vaisheli, Schaum, Robert, Van Huis, Chad A., Welch, Kathleen M., Zhang, Erli, Leadley, Robert J., Edmunds, Jeremy J.

“…Herein, we report the discovery of novel, proline‐based factor Xa inhibitors containing a neutral P1 chlorophenyl pharmacophore. Through the additional…”
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Exploration of 4,4-disubstituted pyrrolidine-1,2-dicarboxamides as potent, orally active Factor Xa inhibitors with extended duration of action by Van Huis, Chad A., Casimiro-Garcia, Agustin, Bigge, Christopher F., Cody, Wayne L., Dudley, Danette A., Filipski, Kevin J., Heemstra, Ronald J., Kohrt, Jeffrey T., Leadley, Robert J., Narasimhan, Lakshmi S., McClanahan, Thomas, Mochalkin, Igor, Pamment, Michael, Thomas Peterson, J., Sahasrabudhe, Vaishali, Schaum, Robert P., Edmunds, Jeremy J.

“…With the intent to improve upon the projected human half-life of the previously disclosed Factor Xa inhibitor 5, a series of 4,4-disubstituted…”
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The discovery of fluoropyridine-based inhibitors of the factor VIIa/TF complex—Part 2 by Kohrt, Jeffrey T., Filipski, Kevin J., Cody, Wayne L., Cai, Cuiman, Dudley, Danette A., Van Huis, Chad A., Willardsen, J. Adam, Narasimhan, Lakshmi S., Zhang, Erli, Rapundalo, Stephen T., Saiya-Cork, Kamlai, Leadley, Robert J., Edmunds, Jeremy J.

“…The activated factor VII/tissue factor complex (FVIIa/TF) is known to play a key role in the formation of blood clots. Inhibition of this complex may lead to…”
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The discovery of fluoropyridine-based inhibitors of the Factor VIIa/TF complex by Kohrt, Jeffrey T., Filipski, Kevin J., Cody, Wayne L., Cai, Cuiman, Dudley, Danette A., Van Huis, Chad A., Willardsen, J. Adam, Rapundalo, Stephen T., Saiya-Cork, Kamlai, Leadley, Robert J., Narasimhan, Lakshmi, Zhang, Erli, Whitlow, Marc, Adler, Marc, McLean, Kirk, Chou, Yuo-Ling, McKnight, Cecile, Arnaiz, Damian O., Shaw, Kenneth J., Light, David R., Edmunds, Jeremy J.

“…The activated Factor VII/tissue factor complex (FVIIa/TF) plays a key role in the formation of blood clots. Inhibition of this complex may lead to new…”
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Structure-based Drug Design of Pyrrolidine-1, 2-dicarboxamides as a Novel Series of Orally Bioavailable Factor Xa Inhibitors by Van Huis, Chad A., Bigge, Christopher F., Casimiro-Garcia, Agustin, Cody, Wayne L., Dudley, Danette A., Filipski, Kevin J., Heemstra, Ronald J., Kohrt, Jeffrey T., Narasimhan, Lakshmi S., Schaum, Robert P., Zhang, Erli, Bryant, John W., Haarer, Staci, Janiczek, Nancy, Leadley Jr, Robert J., McClanahan, Thomas, Thomas Peterson, J., Welch, Kathleen M., Edmunds, Jeremy J.

“…A novel series of pyrrolidine‐1,2‐dicarboxamides was discovered as factor Xa inhibitors using structure‐based drug design. This series consisted of a neutral…”
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Discovery of 2‑{3-[2-(1-Isopropyl-3-methyl‑1H‑1,2–4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2‑d][1,4]oxazepin-9-yl]‑1H‑pyrazol-1-yl}-2-methylpropanamide (GDC-0032): A β‑Sparing Phosphoinositide 3‑Kinase Inhibitor with High Unbound Exposure and Robust in Vivo Antitumor Activity by Ndubaku, Chudi O, Heffron, Timothy P, Staben, Steven T, Baumgardner, Matthew, Blaquiere, Nicole, Bradley, Erin, Bull, Richard, Do, Steven, Dotson, Jennafer, Dudley, Danette, Edgar, Kyle A, Friedman, Lori S, Goldsmith, Richard, Heald, Robert A, Kolesnikov, Aleksandr, Lee, Leslie, Lewis, Cristina, Nannini, Michelle, Nonomiya, Jim, Pang, Jodie, Price, Steve, Prior, Wei Wei, Salphati, Laurent, Sideris, Steve, Wallin, Jeffery J, Wang, Lan, Wei, BinQing, Sampath, Deepak, Olivero, Alan G

“…Dysfunctional signaling through the phosphoinositide 3-kinase (PI3K)/AKT/mTOR pathway leads to uncontrolled tumor proliferation. In the course of the discovery…”
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Rational Design, Synthesis, and Biological Activity of Benzoxazinones as Novel Factor Xa Inhibitors by Dudley, Danette A, Bunker, Amy M, Chi, Liguo, Cody, Wayne L, Holland, Debra R, Ignasiak, Diane P, Janiczek-Dolphin, Nancy, McClanahan, Thomas B, Mertz, Thomas E, Narasimhan, Lakshmi S, Rapundalo, Stephen T, Trautschold, Julia A, Van Huis, Chad A, Edmunds, Jeremy J

“…Inappropriate thrombus formation within blood vessels is the leading cause of mortality in the industrialized world. Factor Xa (FXa) is a trypsin-like serine…”
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Structure-Guided Rescaffolding of Selective Antagonists of BCL-X L by Koehler, Michael F. T., Bergeron, Philippe, Choo, Edna F., Lau, Kevin, Ndubaku, Chudi, Dudley, Danette, Gibbons, Paul, Sleebs, Brad E., Rye, Carl S., Nikolakopoulos, George, Bui, Chinh, Kulasegaram, Sanji, Kersten, Wilhelmus J. A., Smith, Brian J., Czabotar, Peter E., Colman, Peter M., Huang, David C. S., Baell, Jonathan B., Watson, Keith G., Hasvold, Lisa, Tao, Zhi-Fu, Wang, Le, Souers, Andrew J., Elmore, Steven W., Flygare, John A., Fairbrother, Wayne J., Lessene, Guillaume

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Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase β isoform by Staben, Steven T., Ndubaku, Chudi, Blaquiere, Nicole, Belvin, Marcia, Bull, Richard J., Dudley, Danette, Edgar, Kyle, Gray, Daniel, Heald, Robert, Heffron, Timothy P., Jones, Graham E., Jones, Mark, Kolesnikov, Aleks, Lee, Leslie, Lesnick, John, Lewis, Cristina, Murray, Jeremy, McLean, Neville J., Nonomiya, Jim, Olivero, Alan G., Ord, Rachel, Pang, Jodie, Price, Stephen, Prior, Wei Wei, Rouge, Lionel, Salphati, Laurent, Sampath, Deepak, Wallin, Jeff, Wang, Lan, Wei, BinQing, Weismann, Christian, Wu, Ping

“…A series of suitable five-membered heterocyclic alternatives to thiophenes within a thienobenzoxepin class of PI3-kinase (PI3K) inhibitors was discovered…”
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Structure-Guided Rescaffolding of Selective Antagonists of BCL‑XL by Koehler, Michael F. T, Bergeron, Philippe, Choo, Edna F, Lau, Kevin, Ndubaku, Chudi, Dudley, Danette, Gibbons, Paul, Sleebs, Brad E, Rye, Carl S, Nikolakopoulos, George, Bui, Chinh, Kulasegaram, Sanji, Kersten, Wilhelmus J. A, Smith, Brian J, Czabotar, Peter E, Colman, Peter M, Huang, David C. S, Baell, Jonathan B, Watson, Keith G, Hasvold, Lisa, Tao, Zhi-Fu, Wang, Le, Souers, Andrew J, Elmore, Steven W, Flygare, John A, Fairbrother, Wayne J, Lessene, Guillaume

“…Because of the promise of BCL-2 antagonists in combating chronic lymphocytic leukemia (CLL) and non-Hodgkin’s lymphoma (NHL), interest in additional selective…”
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A versatile copper-catalyzed coupling reaction of pyridin-2(1 H)-ones with aryl halides by Filipski, Kevin J., Kohrt, Jeffrey T., Casimiro-Garcia, Agustin, Van Huis, Chad A., Dudley, Danette A., Cody, Wayne L., Bigge, Christopher F., Desiraju, Shrilakshmi, Sun, Shaoyi, Maiti, Samarendra N., Jaber, Mohamad R., Edmunds, Jeremy J.

“…A robust method has been developed to couple a wide variety of pyridin-2-ones and aryl halides. This C–N bond forming reaction makes use of catalytic copper(I)…”
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Discovery of a Series of Imidazo[4,5-b]pyridines with Dual Activity at Angiotensin II Type 1 Receptor and Peroxisome Proliferator-Activated Receptor-[gamma] by Casimiro-Garcia, Agustin, Filzen, Gary F., Flynn, Declan, Bigge, Christopher F., Chen, Jing, Davis, Jo Ann, Dudley, Danette A., Edmunds, Jeremy J., Esmaeil, Nadia, Geyer, Andrew, Heemstra, Ronald J., Jalaie, Mehran, Ohren, Jeffrey F., Ostroski, Robert, Ellis, Teresa, Schaum, Robert P., Stoner, Chad

“…Mining of an in-house collection of angiotensin II type 1 receptor antagonists to identify compounds with activity at the peroxisome proliferator-activated…”
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Abstract DDT02-01: Discovery of GDC-0032: A beta-sparing PI3K inhibitor active against PIK3CA mutant tumors by Olivero, Alan G., Heffron, Timothy P., Baumgardner, Matthew, Belvin, Marcia, Ross, Leanne Berry, Blaquiere, Nicole, Bradley, Erin, Castanedo, Georgette, Derynck, Mika, Do, Steven, Dotson, Jennafer, Dudley, Danette, Edgar, Kyle, Folkes, Adrian, Francis, Ross, Gianetti, Tony, Goldsmith, Richard, Goldsmith, Paul, Guan, Jane, Harrison, Trevor, Heald, Robert, Hsu, Jerry, Jackson, Phillip, Jones, Graham, Kim, Amy, Kolesnikov, Aleks, Lackner, Mark, Lee, Leslie, Lesnick, John, Lewis, Cristina, Mamounas, Michael, McLean, Neville, Murray, Jeremy, Ndubaku, Chudi, Nonomiya, Jim, Pang, Jodie, Pegg, Neil, Prior, Wei Wei, Salphati, Laurent, Sampath, Deepack, Sideris, Stephen, Siu, Michael, Staben, Steven, Sutherlin, Daniel, Ultsch, Mark, Wallin, Jeff, Wang, Lan, Wiesmann, Christian, Zhang, Xiaolin, Friedman, Lori S.

“…Modifications of the phosphoinositide-3 kinase (PI3K)/Akt signaling pathway are frequent in cancer due to multiple mechanisms, including activating mutations…”
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The Discovery of (2R,4R)-N-(4-chlorophenyl)-N- (2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl)-4-methoxypyrrolid ine-1,2-dicarboxamide (PD 0348292), an Orally Efficacious Factor Xa Inhibitor by Kohrt, Jeffrey T, Bigge, Christopher F, Bryant, John W, Casimiro-Garcia, Agustin, Chi, Liguo, Cody, Wayne L, Dahring, Tawny, Dudley, Danette A, Filipski, Kevin J, Haarer, Staci, Heemstra, Ron, Janiczek, Nancy, Narasimhan, Lakshmi, McClanahan, Thomas, Peterson, JThomas, Sahasrabudhe, Vaisheli, Schaum, Robert, Van Huis, Chad A, Welch, Kathleen M, Zhang, Erli, Leadley, Robert J, Edmunds, Jeremy J

“…Herein, we report the discovery of novel, proline-based factor Xa inhibitors containing a neutral P1 chlorophenyl pharmacophore. Through the additional…”
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