1227862-57-8Relevant articles and documents
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.
, p. 4908 - 4913 (2017/09/27)
The identification of small molecule inhibitors of IRAK4 for the treatment of autoimmune diseases has been an area of intense research. We discovered novel 4,6-diaminonicotinamides which potently inhibit IRAK4. Optimization efforts were aided by X-ray crystal structures of inhibitors bound to IRAK4. Structure activity relationship (SAR) studies led to the identification of compound 29 which exhibited sub-micromolar potency in a LTA stimulated cellular assay.
NICOTINAMIDES AS JAK KINASE MODULATORS
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Page/Page column 47, (2012/05/07)
The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.
