Výsledky vyhledávání - "Michael Dennis Lowe"

Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design

Autor: Lori Krim Gavrin, David Hepworth, Jennifer R. Thomason, Iain Kilty, Joel Adam Goldberg, Christoph W. Zapf, Vikram R. Rao, Brian P. Boscoe, Akshay Patny, Peter T. Symanowicz, Marina W.H. Shen, Kevin J. Curran, Elizabeth Murphy, Martin Hegen, Fabien Vincent, Richard Vargas, Satwik Kamtekar, Heidi M. Morgan, Heidi R. Hope, Richard K. Frisbie, Jeanne S. Chang, Ken Dower, Susan E. Drozda, Strohbach Joseph Walter, Mathias John Paul, David R. Anderson, Jacqueline E. Day, Stephen W. Wright, Ivan J. Samardjiev, Seungil Han, Julia H Shin, Frank Lovering, Andrea G Bree, Arthur Lee, Holly H. Soutter, Joanne Brodfuehrer, John David Trzupek, Brian Samas, Christoph Martin Dehnhardt, Michael Dennis Lowe, Catherine M. Ambler, Seung Won Chung, Eddine Saiah, Nikolaos Papaioannou, Pierce Betsy S, Jiangli Yan, Katherine L. Lee, Lih-Ling Lin, Chulho Choi

Publikováno v: Journal of Medicinal Chemistry. 60:5521-5542

Through fragment-based drug design focused on engaging the active site of IRAK4 and leveraging three-dimensional topology in a ligand-efficient manner, a micromolar hit identified from a screen of a Pfizer fragment library was optimized to afford IRA

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::54d71e108dde9e50f577dacbc8e3364e
https://doi.org/10.1021/acs.jmedchem.7b00231

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Discovery of 2-[1-(4-Chlorophenyl)cyclopropyl]-3-hydroxy-8-(trifluoromethyl)quinoline-4-carboxylic Acid (PSI-421), a P-Selectin Inhibitor with Improved Pharmacokinetic Properties and Oral Efficacy in Models of Vascular Injury

Autor: Steve Tam, Qin Wang, Adrian Huang, Desiree H.H. Tsao, Natalia Sushkova, Michael Dennis Lowe, Gray D. Shaw, Patricia W. Bedard, Li Di, Boris Tchernychev, James C. Keith, Neelu Kaila, Robert G. Schaub, Kristin Janz, Valerie Clerin, Alessandro Moretto

Publikováno v: Journal of Medicinal Chemistry. 53:6003-6017

Previously, we reported the discovery of PSI-697 (1a), a C-2 benzyl substituted quinoline salicylic acid-based P-selectin inhibitor. It is active in a variety of animal models of cardiovascular disease. Compound 1a has also been shown to be well tole

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::037abec3fb0ac922950e891045ae2fb2
https://doi.org/10.1021/jm9013696

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