1219956-75-8Relevant academic research and scientific papers
2-AMINOPYRAZINE DERIVATIVES AS CSF-1 R KINASE INHIBITORS
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Page/Page column 36; 37, (2014/01/17)
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, N-oxide, hydrate or solvate thereof: wherein:ring A, R1, R2, n, X, V, W, Z, ring B, [Linker] and R areas defined herein. The compounds are useful as inhibitorsof CSF-1R kinase. The compounds can thus be used in medicine.
Structure-based drug design enables conversion of a DFG-in binding CSF-1R kinase inhibitor to a DFG-out binding mode
Meyers, Marvin J.,Pelc, Matthew,Kamtekar, Satwik,Day, Jacqueline,Poda, Gennadiy I.,Hall, Molly K.,Michener, Marshall L.,Reitz, Beverly A.,Mathis, Karl J.,Pierce, Betsy S.,Parikh, Mihir D.,Mischke, Deborah A.,Long, Scott A.,Parlow, John J.,Anderson, David R.,Thorarensen, Atli
scheme or table, p. 1543 - 1547 (2010/06/21)
The work described herein demonstrates the utility of structure-based drug design (SBDD) in shifting the binding mode of an HTS hit from a DFG-in to a DFG-out binding mode resulting in a class of novel potent CSF-1R kinase inhibitors suitable for lead development.
