Zobrazeno 1 - 10
of 68
pro vyhledávání: '"Louis J. Lombardo"'
Autor:
Shiuhang Yip, Emily Luk, Anwar Murtaza, Yong Zhang, Michael A. Poss, Louis J. Lombardo, Nimmi Raghavan, Zheng Yang, James Kempson, Audris Huang, David R. Tortolani, Jesse Swanson, Xiaoping Hou, Joseph Pawluczyk, James Smalley, Honghe Wan, Karen E. Parrish, Robert M. Borzilleri, Ashok V. Purandare, Karen Augustine-Rauch, Andrew F. Donnell
Publikováno v:
Journal of Medicinal Chemistry. 64:15787-15798
Inhibition of TGFβ signaling in concert with a checkpoint blockade has been shown to provide improved and durable antitumor immune response in mouse models. However, on-target adverse cardiovascular effects have limited the clinical use of TGFβ rec
Autor:
Jianqing Li, Daniel Smith, John S. Tokarski, Lihong Cheng, John E. Macor, Javed Khan, Adriana Zupa-Fernandez, Anil Thankappan, Chunjian Liu, Charu Chaudhry, David S. Weinstein, Percy H. Carter, Kathleen M. Gillooly, Kim W. McIntyre, Yifan Zhang, Anjaneya Chimalakonda, Joann Strnad, James Lin, James R. Burke, David J. Shuster, Manoj Chiney, Paul A. Elzinga, Max Ruzanov, Louis J. Lombardo, Charles M. Langevine
Publikováno v:
Journal of Medicinal Chemistry. 64:677-694
A search for structurally diversified Tyk2 JH2 ligands from 6 (BMS-986165), a pyridazine carboxamide-derived Tyk2 JH2 ligand as a clinical Tyk2 inhibitor currently in late development for the treatment of psoriasis, began with a survey of six-membere
Autor:
Yanlei Zhang, Jeffrey Tredup, Mertzman Michael E, Nelly Aranibar, Kim W. McIntyre, Kathleen M. Gillooly, Jodi K. Muckelbauer, James R. Burke, Lihong Cheng, Joann Strnad, Celia D’Arienzo, Dawn Mulligan, Stephen T. Wrobleski, Charu Chaudhry, Adriana Zupa-Fernandez, Percy H. Carter, Dianlin Xie, Manoj Chiney, Elizabeth M. Heimrich, Moslin Ryan M, Christine Huang, Xiaoxia Yang, Shuqun Lin, David S. Weinstein, Tokarski John S, Chiehying Chang, Louis J. Lombardo, Huadong Sun, Steven H. Spergel
Publikováno v:
Journal of Medicinal Chemistry. 62:8953-8972
As a member of the Janus (JAK) family of nonreceptor tyrosine kinases, TYK2 plays an important role in mediating the signaling of pro-inflammatory cytokines including IL-12, IL-23, and type 1 interferons. The nicotinamide 4, identified by a SPA-based
Autor:
Charu Chaudhry, Percy H. Carter, Moslin Ryan M, Celia D’Arienzo, James Lin, Jodi K. Muckelbauer, Luisa Salter-Cid, Tracy L. Taylor, Kim W. McIntyre, Chunjian Liu, James R. Burke, Paul A. Elzinga, Hyunsoo Park, Kathleen M. Gillooly, Chiehying Chang, Dianlin Xie, Jing Chen, Lihong Cheng, David S. Weinstein, Cliff Chen, Jeffrey Tredup, Huadong Sun, Peng Li, Louis J. Lombardo, Adriana Zupa-Fernandez, Joann Strnad, John S. Tokarski, Dauh-Rurng Wu, Nelly Aranibar
Publikováno v:
ACS Medicinal Chemistry Letters. 10:383-388
In sharp contrast to a previously reported series of 6-anilino imidazopyridazine based Tyk2 JH2 ligands, 6-((2-oxo-N1-substituted-1,2-dihydropyridin-3-yl)amino)imidazo[1,2-b]pyridazine analogs were found to display dramatically improved metabolic sta
Autor:
Marta Dabros, Paul Levesque, Elizabeth M. Heimrich, Arvind Mathur, Percy H. Carter, Richard Rampulla, Anuradha Gupta, Lois D. Lehman-McKeeman, Huadong Sun, David Marcoux, Ding Ren Shen, Xiaoxia Yang, Xia D. Zhou, Hai-Yun Xiao, Dauh-Rurng Wu, Louis J. Lombardo, Hong Shi, Zheng Yang, Mary Ellen Cvijic, Alaric J. Dyckman, Kim W. McIntyre, Luisa Salter-Cid, Celia D’Arienzo, Anthony M. Marino, Bala Pragalathan, Georgia Cornelius, Jenny Xie, T. G. Murali Dhar, Tracy L. Taylor, Rochelle Thomas
Publikováno v:
MedChemComm. 8:725-729
Recently, our research group reported the identification of prodrug amino-alcohol 2 as a potent and efficacious S1P1 receptor modulator. This molecule is differentiated preclinically over the marketed drug fingolimod (Gilenya 1), whose active phospha
Autor:
Max Ruzanov, David J. Shuster, Manoj Chiney, Kim W. McIntyre, James R. Burke, Celia D’Arienzo, Nelly Aranibar, Elizabeth M. Heimrich, Louis J. Lombardo, Dianlin Xie, Moslin Ryan M, Joann Strnad, Anjaneya Chimalakonda, Lihong Cheng, James Kempson, Adriana Zupa-Fernandez, Javed Khan, Charu Chaudhry, Huadong Sun, Shuqun Lin, Percy H. Carter, Steven H. Spergel, Christine Huang, Dawn Mulligan, Stephen T. Wrobleski, Kathleen M. Gillooly, Yanlei Zhang, Jeffrey Tredup, David S. Weinstein, Tokarski John S, William J. Pitts, Xiaoxia Yang
Publikováno v:
Journal of medicinal chemistry. 62(20)
Small molecule JAK inhibitors have emerged as a major therapeutic advancement in treating autoimmune diseases. The discovery of isoform selective JAK inhibitors that traditionally target the catalytically active site of this kinase family has been a
Autor:
Chunjian, Liu, James, Lin, Ryan, Moslin, John S, Tokarski, Jodi, Muckelbauer, ChiehYing, Chang, Jeffrey, Tredup, Dianlin, Xie, Hyunsoo, Park, Peng, Li, Dauh-Rurng, Wu, Joann, Strnad, Adriana, Zupa-Fernandez, Lihong, Cheng, Charu, Chaudhry, Jing, Chen, Cliff, Chen, Huadong, Sun, Paul, Elzinga, Celia, D'arienzo, Kathleen, Gillooly, Tracy L, Taylor, Kim W, McIntyre, Luisa, Salter-Cid, Louis J, Lombardo, Percy H, Carter, Nelly, Aranibar, James R, Burke, David S, Weinstein
Publikováno v:
ACS medicinal chemistry letters. 10(3)
[Image: see text] In sharp contrast to a previously reported series of 6-anilino imidazopyridazine based Tyk2 JH2 ligands, 6-((2-oxo-N1-substituted-1,2-dihydropyridin-3-yl)amino)imidazo[1,2-b]pyridazine analogs were found to display dramatically impr
Autor:
Hart Amy C, Javed Khan, Grebinski James W, James Kempson, Jonathan Lippy, Gretchen M. Schroeder, Theresa M. McDevitt, Ashok V. Purandare, Ragini Vuppugalla, John S. Tokarski, George L. Trainor, Junqing Guo, Jennifer Inghrim, Matthew V. Lorenzi, Dan You, Honghe Wan, John S. Sack, William J. Pitts, Yueping Zhang, Louis J. Lombardo
Publikováno v:
ACS Medicinal Chemistry Letters. 6:845-849
Early hit to lead work on a pyrrolopyridine chemotype provided access to compounds with biochemical and cellular potency against Janus kinase 2 (JAK2). Structure-based drug design along the extended hinge region of JAK2 led to the identification of a
Autor:
Claude A. Quesnelle, Patrice Gill, Richard Rampulla, Ching Su, Gerry Everlof, George L. Trainor, Ke Chen, Vinod Arora, Richard A. Westhouse, Celia D’Arienzo, Andrew J. Tebben, Weifang Shan, John T. Hunt, Derek J. Norris, Louis J. Lombardo, Zheng Yang, Arvind Mathur, Mei-Li Wen, Yingru Zhang, Dauh-Rurng Wu, Wen-Ching Han, Krista Menard, Victor R. Guarino, Asoka Ranasinghe, Richard E. Olson, Ashvinikumar V. Gavai, Bruce S. Fischer, Phil S. Baran, Anne Rose, Lan Xiao, Ronald E. White, Mary Ellen Cvijic, Gregory D. Vite, Ding Ren Shen, Jere E. Meredith, Haiqing Wang, Francis Y. Lee, Aaron Balog
Publikováno v:
ACS Medicinal Chemistry Letters. 6:523-527
Structure-activity relationships in a series of (2-oxo-1,4-benzodiazepin-3-yl)-succinamides identified highly potent inhibitors of γ-secretase mediated signaling of Notch1/2/3/4 receptors. On the basis of its robust in vivo efficacy at tolerated dos
Autor:
Matthew V. Lorenzi, Xia Han, Honghe Wan, Kim W. McIntyre, Yifan Zhang, E Michaud, A Tefferi, Stuart Emanuel, Ragini Vuppugalla, Becky Penhallow, George L. Trainor, Y Blat, Animesh Pardanani, Tracy L. Taylor, Elizabeth Fitzpatrick, Petra Ross-Macdonald, Frank Lee, Louis J. Lombardo, Theresa M. McDevitt, Ashok V. Purandare, Marco M. Gottardis, Adrian Woolfson, H de Silva, Terra L. Lasho, Dan You, Stefan Ruepp, Jennifer Hosbach, Donna L. Pedicord, C Mulligan
Publikováno v:
Leukemia. 26:280-288
We report the characterization of BMS-911543, a potent and selective small-molecule inhibitor of the Janus kinase (JAK) family member, JAK2. Functionally, BMS-911543 displayed potent anti-proliferative and pharmacodynamic (PD) effects in cell lines d