Design, Synthesis, and Anti-inflammatory Properties of Orally Active 4-(Phenylamino)-pyrrolo[2,1-f][1,2,4]triazine p38α Mitogen-Activated Protein Kinase Inhibitors
Hynes, John, Dyckman, Alaric J, Lin, Shuqun, Wrobleski, Stephen T, Wu, Hong, Gillooly, Kathleen M, Kanner, Steven B, Lonial, Herinder, Loo, Derek, McIntyre, Kim W, Pitt, Sidney, Shen, Ding Ren, Shuster, David J, Yang, XiaoXia, Zhang, Rosemary, Behnia, Kamelia, Zhang, Hongjian, Marathe, Punit H, Doweyko, Arthur M, Tokarski, John S, Sack, John S, Pokross, Matthew, Kiefer, Susan E, Newitt, John A, Barrish, Joel C, Dodd, John, Schieven, Gary L, Leftheris, Katerina
Published in Journal of medicinal chemistry (10.01.2008)
Published in Journal of medicinal chemistry (10.01.2008)
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Utilization of a nitrogen–sulfur nonbonding interaction in the design of new 2-aminothiazol-5-yl-pyrimidines as p38α MAP kinase inhibitors
Lin, Shuqun, Wrobleski, Stephen T., Hynes, John, Pitt, Sidney, Zhang, Rosemary, Fan, Yi, Doweyko, Arthur M., Kish, Kevin F., Sack, John S., Malley, Mary F., Kiefer, Susan E., Newitt, John A., McKinnon, Murray, Trzaskos, James, Barrish, Joel C., Dodd, John H., Schieven, Gary L., Leftheris, Katerina
Published in Bioorganic & medicinal chemistry letters (01.10.2010)
Published in Bioorganic & medicinal chemistry letters (01.10.2010)
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Synthesis and SAR of new pyrrolo[2,1- f][1,2,4]triazines as potent p38α MAP kinase inhibitors
Wrobleski, Stephen T., Lin, Shuqun, Hynes, John, Wu, Hong, Pitt, Sidney, Shen, Ding Ren, Zhang, Rosemary, Gillooly, Kathleen M., Shuster, David J., McIntyre, Kim W., Doweyko, Arthur M., Kish, Kevin F., Tredup, Jeffrey A., Duke, Gerald J., Sack, John S., McKinnon, Murray, Dodd, John, Barrish, Joel C., Schieven, Gary L., Leftheris, Katerina
Published in Bioorganic & medicinal chemistry (15.04.2008)
Published in Bioorganic & medicinal chemistry (15.04.2008)
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Synthesis and SAR of p38α MAP kinase inhibitors based on heterobicyclic scaffolds
Murali Dhar, T.G., Wrobleski, Stephen T., Lin, Shuqun, Furch, Joseph A., Nirschl, David S., Fan, Yi, Todderud, Gordon, Pitt, Sidney, Doweyko, Arthur M., Sack, John S., Mathur, Arvind, McKinnon, Murray, Barrish, Joel C., Dodd, John H., Schieven, Gary L., Leftheris, Katerina
Published in Bioorganic & medicinal chemistry letters (15.09.2007)
Published in Bioorganic & medicinal chemistry letters (15.09.2007)
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The Discovery of Orally Active Triaminotriazine Aniline Amides as Inhibitors of p38 MAP Kinase
Leftheris, Katerina, Ahmed, Gulzar, Chan, Ran, Dyckman, Alaric J, Hussain, Zahid, Ho, Kan, Hynes, John, Letourneau, Jeffrey, Li, Wei, Lin, Shuqun, Metzger, Axel, Moriarty, Kevin J, Riviello, Chris, Shimshock, Yvonne, Wen, James, Wityak, John, Wrobleski, Stephen T, Wu, Hong, Wu, Junjun, Desai, Madhuri, Gillooly, Kathleen M, Lin, Tsung H, Loo, Derek, McIntyre, Kim W, Pitt, Sidney, Shen, Ding Ren, Shuster, David J, Zhang, Rosemary, Diller, David, Doweyko, Arthur, Sack, John, Baldwin, Jack, Barrish, Joel, Dodd, John, Henderson, Ian, Kanner, Steve, Schieven, Gary L, Webb, Maria
Published in Journal of medicinal chemistry (02.12.2004)
Published in Journal of medicinal chemistry (02.12.2004)
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Rational Design and Synthesis of an Orally Active Indolopyridone as a Novel Conformationally Constrained Cannabinoid Ligand Possessing Antiinflammatory Properties
Wrobleski, Stephen T, Chen, Ping, Hynes, John, Lin, Shuqun, Norris, Derek J, Pandit, Chennagiri R, Spergel, Steven, Wu, Hong, Tokarski, John S, Chen, Xiaorong, Gillooly, Kathleen M, Kiener, Peter A, McIntyre, Kim W, Patil-koota, Vina, Shuster, David J, Turk, Lori A, Yang, Guchen, Leftheris, Katerina
Published in Journal of medicinal chemistry (22.05.2003)
Published in Journal of medicinal chemistry (22.05.2003)
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Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains
Zhao, Chen, Sham, Hing L., Sun, Minghua, Stoll, Vincent S., Stewart, Kent D., Lin, Shuqun, Mo, Hongmei, Vasavanonda, Sudthida, Saldivar, Ayda, Park, Chang, McDonald, Edith J., Marsh, Kennan C., Klein, Larry L., Kempf, Dale J., Norbeck, Daniel W.
Published in Bioorganic & medicinal chemistry letters (15.12.2005)
Published in Bioorganic & medicinal chemistry letters (15.12.2005)
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Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165
Wrobleski, Stephen T, Moslin, Ryan, Lin, Shuqun, Zhang, Yanlei, Spergel, Steven, Kempson, James, Tokarski, John S, Strnad, Joann, Zupa-Fernandez, Adriana, Cheng, Lihong, Shuster, David, Gillooly, Kathleen, Yang, Xiaoxia, Heimrich, Elizabeth, McIntyre, Kim W, Chaudhry, Charu, Khan, Javed, Ruzanov, Max, Tredup, Jeffrey, Mulligan, Dawn, Xie, Dianlin, Sun, Huadong, Huang, Christine, D’Arienzo, Celia, Aranibar, Nelly, Chiney, Manoj, Chimalakonda, Anjaneya, Pitts, William J, Lombardo, Louis, Carter, Percy H, Burke, James R, Weinstein, David S
Published in Journal of medicinal chemistry (24.10.2019)
Published in Journal of medicinal chemistry (24.10.2019)
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A Novel, Picomolar Inhibitor of Human Immunodeficiency Virus Type 1 Protease
Sham, Hing L, Zhao, Chen, Stewart, Kent D, Betebenner, David A, Lin, Shuqun, Park, Chang H, Kong, Xiang-P, Rosenbrook, William, Herrin, Thomas, Madigan, Darold, Vasavanonda, Suthida, Lyons, Nicholas, Molla, Akhter, Saldivar, Ayda, Marsh, Kennan C, McDonald, Edith, Wideburg, Norman E, Denissen, Jon F, Robins, Terrel, Kempf, Dale J, Plattner, Jacob J, Norbeck, Daniel W
Published in Journal of medicinal chemistry (19.01.1996)
Published in Journal of medicinal chemistry (19.01.1996)
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Discovery and structure-based design of 4,6-diaminonicotinamides as potent and selective IRAK4 inhibitors
Bhide, Rajeev S., Keon, Alec, Weigelt, Carolyn, Sack, John S., Schmidt, Robert J., Lin, Shuqun, Xiao, Hai-Yun, Spergel, Steven H., Kempson, James, Pitts, William J., Carman, Julie, Poss, Michael A.
Published in Bioorganic & medicinal chemistry letters (01.11.2017)
Published in Bioorganic & medicinal chemistry letters (01.11.2017)
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Discovery of highly potent, selective, covalent inhibitors of JAK3
Kempson, James, Ovalle, Damaso, Guo, Junqing, Wrobleski, Stephen T., Lin, Shuqun, Spergel, Steven H., Duan, James J.-W., Jiang, Bin, Lu, Zhonghui, Das, Jagabandhu, Yang, Bingwei V., Hynes, John, Wu, Hong, Tokarski, John, Sack, John S., Khan, Javed, Schieven, Gary, Blatt, Yuval, Chaudhry, Charu, Salter-Cid, Luisa M., Fura, Aberra, Barrish, Joel C., Carter, Percy H., Pitts, William J.
Published in Bioorganic & medicinal chemistry letters (15.10.2017)
Published in Bioorganic & medicinal chemistry letters (15.10.2017)
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Novel advances in biotransformation and bioactivation research - 2020 year in review
Khojasteh, S. Cyrus, Argikar, Upendra A., Driscoll, James P., Heck, Carley J. S., King, Lloyd, Jackson, Klarissa D., Jian, Wenying, Kalgutkar, Amit S., Miller, Grover P., Kramlinger, Valerie, Rietjens, Ivonne M. C. M., Teitelbaum, Aaron M., Wang, Kai, Wei, Cong
Published in Drug metabolism reviews (03.07.2021)
Published in Drug metabolism reviews (03.07.2021)
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Discovery of ((4-(5-(CyclopropylcarbamoyI)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38a MAP Kinase Inhibitor
Liu, Chunjian, Lin, James, Hynes, John, Wu, Hong, Wrobleski, Stephen T., Lin, Shuqun, Dhar, T. G. Murali, Vrudhula, Vivekananda M., Sun, Jung-Hui, Chao, Sam, Zhao, Rulin, Wang, Bei, Chen, Bang-Chi, Everlof, Gerry, Gesenberg, Christoph, Zhang, Hongjian, Marathe, Punit H., McIntyre, Kim W., Taylor, Tracy L., Gillooly, Kathleen, Shuster, David J., McKinnon, Murray, Dodd, John H., Barrish, Joel C., Schieven, Gary L., Leftheris, Katerina
Published in Journal of medicinal chemistry (08.10.2015)
Published in Journal of medicinal chemistry (08.10.2015)
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Discovery of 4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a Clinical p38α MAP Kinase Inhibitor for the Treatment of Inflammatory Diseases
Liu, Chunjian, Lin, James, Wrobleski, Stephen T, Lin, Shuqun, Hynes, John, Wu, Hong, Dyckman, Alaric J, Li, Tianle, Wityak, John, Gillooly, Kathleen M, Pitt, Sidney, Shen, Ding Ren, Zhang, Rosemary F, McIntyre, Kim W, Salter-Cid, Luisa, Shuster, David J, Zhang, Hongjian, Marathe, Punit H, Doweyko, Arthur M, Sack, John S, Kiefer, Susan E, Kish, Kevin F, Newitt, John A, McKinnon, Murray, Dodd, John H, Barrish, Joel C, Schieven, Gary L, Leftheris, Katerina
Published in Journal of medicinal chemistry (23.09.2010)
Published in Journal of medicinal chemistry (23.09.2010)
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Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors
Duan, James J. -W., Lu, Zhonghui, Jiang, Bin, Yang, Bingwei V., Doweyko, Lidia M., Nirschl, David S., Haque, Lauren E., Lin, Shuqun, Brown, Gregory, Hynes, John, Tokarski, John S., Sack, John S., Khan, Javed, Lippy, Jonathan S., Zhang, Rosemary F., Pitt, Sidney, Shen, Guoxiang, Pitts, William J., Carter, Percy H., Barrish, Joel C., Nadler, Steven G., Salter-Cid, Luisa M., McKinnon, Murray, Fura, Aberra, Schieven, Gary L., Wrobleski, Stephen T.
Published in Bioorganic & medicinal chemistry letters (15.12.2014)
Published in Bioorganic & medicinal chemistry letters (15.12.2014)
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Journal Article
Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor
Liu, Chunjian, Lin, James, Hynes, John, Wu, Hong, Wrobleski, Stephen T, Lin, Shuqun, Dhar, T G Murali, Vrudhula, Vivekananda M, Sun, Jung-Hui, Chao, Sam, Zhao, Rulin, Wang, Bei, Chen, Bang-Chi, Everlof, Gerry, Gesenberg, Christoph, Zhang, Hongjian, Marathe, Punit H, McIntyre, Kim W, Taylor, Tracy L, Gillooly, Kathleen, Shuster, David J, McKinnon, Murray, Dodd, John H, Barrish, Joel C, Schieven, Gary L, Leftheris, Katerina
Published in Journal of medicinal chemistry (08.10.2015)
Published in Journal of medicinal chemistry (08.10.2015)
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Journal Article
Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2‑f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor
Liu, Chunjian, Lin, James, Hynes, John, Wu, Hong, Wrobleski, Stephen T., Lin, Shuqun, Dhar, T. G. Murali, Vrudhula, Vivekananda M., Sun, Jung-Hui, Chao, Sam, Zhao, Rulin, Wang, Bei, Chen, Bang-Chi, Everlof, Gerry, Gesenberg, Christoph, Zhang, Hongjian, Marathe, Punit H., McIntyre, Kim W., Taylor, Tracy L., Gillooly, Kathleen, Shuster, David J., McKinnon, Murray, Dodd, John H., Barrish, Joel C., Schieven, Gary L., Leftheris, Katerina
Published in Journal of medicinal chemistry (08.10.2015)
Published in Journal of medicinal chemistry (08.10.2015)
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Novel Azacyclic Ureas That Are Potent Inhibitors of HIV-1 Protease
Sham, Hing L., Zhao, Chen, Marsh, Kennan C., Betebenner, David A., Lin, Shuqun, Jr, William Rosenbrook, Herrin, Thomas, Li, Leping, Madigan, Darold, Vasavanonda, Suthida, Molla, Akhter, Saldivar, Ayda, McDonald, Edith, Wideburg, Norman E., Kempf, Dale, Norbeck, Daniel W., Plattner, Jacob J.
Published in Biochemical and biophysical research communications (14.08.1996)
Published in Biochemical and biophysical research communications (14.08.1996)
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AMIDE-SUBSTITUTED HETEROCYCLIC COMPOUNDS USEFUL AS MODULATORS OF IL-12, IL-23 AND/OR IFNα RESPONSES
STEPHEN T WROBLESKI, DAVID S WEINSTEIN, RYAN M MOSLIN, DOUGLAS G BATT, STEVEN H SPERGEL, AMIT KUMAR, JOHN S TOKARSKI, LIN SHUQUN, LIU CHUNJIAN, ZHANG YANLEI
Year of Publication 09.01.2020
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Year of Publication 09.01.2020
Patent
The identification of novel p38α isoform selective kinase inhibitors having an unprecedented p38α binding mode
Wrobleski, Stephen T., Lin, Shuqun, Murali Dhar, T.G., Dyckman, Alaric J., Li, Tianle, Pitt, Sidney, Zhang, Rosemary, Fan, Yi, Doweyko, Arthur M., Tokarski, John S., Kish, Kevin F., Kiefer, Susan E., Sack, John S., Newitt, John A., Witmer, Mark R., McKinnon, Murray, Barrish, Joel C., Dodd, John H., Schieven, Gary L., Leftheris, Katerina
Published in Bioorganic & medicinal chemistry letters (15.07.2013)
Published in Bioorganic & medicinal chemistry letters (15.07.2013)
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