Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors
Hynes, John, Wu, Hong, Kempson, James, Duan, James J.-W., Lu, Zhonghui, Jiang, Bin, Stachura, Sylwia, Tokarski, John S., Sack, John S., Khan, Javed A., Lippy, Jonathan S., Zhang, Rosemary F., Pitt, Sidney, Shen, Guoxiang, Gillooly, Kate, McIntyre, Kim, Carter, Percy H., Barrish, Joel C., Nadler, Steven G., Salter-Cid, Luisa M., Fura, Aberra, Schieven, Gary L., Pitts, William J., Wrobleski, Stephen T.
Published in Bioorganic & medicinal chemistry letters (15.07.2017)
Published in Bioorganic & medicinal chemistry letters (15.07.2017)
Get full text
Journal Article
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)
Get full text
Journal Article
Discovery of a JAK1/3 Inhibitor and Use of a Prodrug To Demonstrate Efficacy in a Model of Rheumatoid Arthritis
Spergel, Steven H, Mertzman, Michael E, Kempson, James, Guo, Junqing, Stachura, Sylwia, Haque, Lauren, Lippy, Jonathan S, Zhang, Rosemary F, Galella, Michael, Pitt, Sidney, Shen, Guoxiang, Fura, Aberra, Gillooly, Kathleen, McIntyre, Kim W, Tang, Vicky, Tokarski, John, Sack, John S, Khan, Javed, Carter, Percy H, Barrish, Joel C, Nadler, Steven G, Salter-Cid, Luisa M, Schieven, Gary L, Wrobleski, Stephen T, Pitts, William J
Published in ACS medicinal chemistry letters (14.03.2019)
Published in ACS medicinal chemistry letters (14.03.2019)
Get full text
Journal Article
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)
Get full text
Journal Article
Benzothiazole based inhibitors of p38α MAP kinase
Liu, Chunjian, Lin, James, Pitt, Sidney, Zhang, Rosemary F., Sack, John S., Kiefer, Susan E., Kish, Kevin, Doweyko, Arthur M., Zhang, Hongjian, Marathe, Punit H., Trzaskos, James, Mckinnon, Murray, Dodd, John H., Barrish, Joel C., Schieven, Gary L., Leftheris, Katerina
Published in Bioorganic & medicinal chemistry (15.03.2008)
Published in Bioorganic & medicinal chemistry (15.03.2008)
Get full text
Journal Article
5-Cyanopyrimidine Derivatives as a Novel Class of Potent, Selective, and Orally Active Inhibitors of p38α MAP Kinase
Liu, Chunjian, Wrobleski, Stephen T, Lin, James, Ahmed, Gulzar, Metzger, Axel, Wityak, John, Gillooly, Kathleen M, Shuster, David J, McIntyre, Kim W, Pitt, Sidney, Shen, Ding Ren, Zhang, Rosemary F, Zhang, Hongjian, Doweyko, Arthur M, Diller, David, Henderson, Ian, Barrish, Joel C, Dodd, John H, Schieven, Gary L, Leftheris, Katerina
Published in Journal of medicinal chemistry (06.10.2005)
Published in Journal of medicinal chemistry (06.10.2005)
Get full text
Journal Article
Dasatinib, a small-molecule protein tyrosine kinase inhibitor, inhibits T-cell activation and proliferation
Schade, Andrew E., Schieven, Gary L., Townsend, Robert, Jankowska, Anna M., Susulic, Vojkan, Zhang, Rosemary, Szpurka, Hadrian, Maciejewski, Jaroslaw P.
Published in Blood (01.02.2008)
Published in Blood (01.02.2008)
Get full text
Journal Article
Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3‑Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders
Liu, Qingjie, Shi, Qing, Marcoux, David, Batt, Douglas G, Cornelius, Lyndon, Qin, Lan-Ying, Ruan, Zheming, Neels, James, Beaudoin-Bertrand, Myra, Srivastava, Anurag S, Li, Ling, Cherney, Robert J, Gong, Hua, Watterson, Scott H, Weigelt, Carolyn, Gillooly, Kathleen M, McIntyre, Kim W, Xie, Jenny H, Obermeier, Mary T, Fura, Aberra, Sleczka, Bogdan, Stefanski, Kevin, Fancher, R. M, Padmanabhan, Shweta, RP, Thatipamula, Kundu, Ipsit, Rajareddy, Kallem, Smith, Rodney, Hennan, James K, Xing, Dezhi, Fan, Jingsong, Levesque, Paul C, Ruan, Qian, Pitt, Sidney, Zhang, Rosemary, Pedicord, Donna, Pan, Jie, Yarde, Melissa, Lu, Hao, Lippy, Jonathan, Goldstine, Christine, Skala, Stacey, Rampulla, Richard A, Mathur, Arvind, Gupta, Anuradha, Arunachalam, Pirama Nayagam, Sack, John S, Muckelbauer, Jodi K, Cvijic, Mary Ellen, Salter-Cid, Luisa M, Bhide, Rajeev S, Poss, Michael A, Hynes, John, Carter, Percy H, Macor, John E, Ruepp, Stefan, Schieven, Gary L, Tino, Joseph A
Published in Journal of medicinal chemistry (22.06.2017)
Published in Journal of medicinal chemistry (22.06.2017)
Get full text
Journal Article
Development of a Human Whole Blood Screening Platform to Monitor JAK/STAT Signaling Using High-Throughput Flow Cytometry
Fereshteh, Mark P, Li, Xin, Li, Sha, Fan, Yi, Zhang, Rosemary, Farr, Glen A, Kolodin, Garrett, Lippy, Jonathan, Naglich, Joseph G, Schieven, Gary, Schweizer, Liang, Zhang, Litao
Published in Journal of biomolecular screening (01.09.2016)
Published in Journal of biomolecular screening (01.09.2016)
Get full text
Journal Article
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)
Get full text
Journal Article
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)
Get full text
Journal Article
The identification of novel p38I- isoform selective kinase inhibitors having an unprecedented p38I- binding mode
Wrobleski, Stephen, Lin, Shuqun, Dhar, T G, Dyckman, Alaric, Li, Tianle, Pitt, Sidney, Zhang, Rosemary, Fan, Yi, Doweyko, Arthur, Tokarski, John, Kish, Kevin, Kiefer, Susan, Sack, John, Newitt, John, Witmer, Mark, McKinnon, Murray, Barrish, Joel, Dodd, John, Schieven, Gary, Leftheris, Katerina
Published in Bioorganic & medicinal chemistry letters (01.07.2013)
Published in Bioorganic & medicinal chemistry letters (01.07.2013)
Get full text
Journal Article
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)
Get full text
Journal Article
Pyrazolo-pyrimidines: A novel heterocyclic scaffold for potent and selective p38α inhibitors
Das, Jagabandhu, Moquin, Robert V., Pitt, Sidney, Zhang, Rosemary, Shen, Ding Ren, McIntyre, Kim W., Gillooly, Kathleen, Doweyko, Arthur M., Sack, John S., Zhang, Hongjian, Kiefer, Susan E., Kish, Kevin, McKinnon, Murray, Barrish, Joel C., Dodd, John H., Schieven, Gary L., Leftheris, Katerina
Published in Bioorganic & medicinal chemistry (15.04.2008)
Published in Bioorganic & medicinal chemistry (15.04.2008)
Get full text
Journal Article
Discovery of 4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a Clinical p38[alpha] MAP Kinase Inhibitor for the Treatment of Inflammatory Diseases
Liu, Chunjian, Lin, James, Wrobleski, Stephen T., Lin, Shuqun, Hynes, Jr., 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 (20.11.2013)
Published in Journal of medicinal chemistry (20.11.2013)
Get full text
Journal Article
5-Amino-pyrazoles as potent and selective p38α inhibitors
Das, Jagabandhu, Moquin, Robert V., Dyckman, Alaric J., Li, Tianle, Pitt, Sidney, Zhang, Rosemary, Shen, Ding Ren, McIntyre, Kim W., Gillooly, Kathleen, Doweyko, Arthur M., Newitt, John A., Sack, John S., Zhang, Hongjian, Kiefer, Susan E., Kish, Kevin, McKinnon, Murray, Barrish, Joel C., Dodd, John H., Schieven, Gary L., Leftheris, Katerina
Published in Bioorganic & medicinal chemistry letters (01.12.2010)
Published in Bioorganic & medicinal chemistry letters (01.12.2010)
Get full text
Journal Article
Discovery of pyrrolo[2,1- f][1,2,4]triazine C6-ketones as potent, orally active p38α MAP kinase inhibitors
Dyckman, Alaric J., Li, Tianle, Pitt, Sidney, Zhang, Rosemary, Shen, Ding Ren, McIntyre, Kim W., Gillooly, Kathleen M., Shuster, David J., Doweyko, Arthur M., Sack, John S., Kish, Kevin, Kiefer, Susan E., Newitt, John A., Zhang, Hongjian, Marathe, Punit H., McKinnon, Murray, Barrish, Joel C., Dodd, John H., Schieven, Gary L., Leftheris, Katerina
Published in Bioorganic & medicinal chemistry letters (01.08.2011)
Published in Bioorganic & medicinal chemistry letters (01.08.2011)
Get full text
Journal Article
Dasatinib Once-Daily Dose Regimen Provides Robust Anti-Leukemic Activity While Avoiding Suppression of T Cell Activation
Schieven, Gary L, Zhang, Rosemary, Pitt, Sidney, McGlinchey, Kelly, Menard, Krista, Smykla, Richard, Susulic, Vojkan, Wen, Mei-Li, Wiebesiek, Amy, Townsend, Robert, Lee, Francis Y.
Published in Blood (20.11.2009)
Published in Blood (20.11.2009)
Get full text
Journal Article
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)
Get full text
Journal Article