70593-57-6Relevant academic research and scientific papers
AMIDE-SUBSTITUTED HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF CONDITIONS RELATED TO THE MODULATION OF IL-12, IL-23 AND/OR IFN-ALPHA
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Page/Page column 257, (2020/05/29)
Compounds having the following formula I: or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-2
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.
Boron-Containing Small Molecules as Anti-Inflammatory Agents
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Paragraph 1173-1174, (2015/11/16)
Compounds and methods of treating anti-inflammatory conditions are disclosed.
NICOTINAMIDES AS JAK KINASE MODULATORS
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Page/Page column 55, (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.
4,6-DIAMINONICOTINAMIDE COMPOUND
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Page/Page column 41, (2011/09/20)
[Problem] The present invention provides a 4,6-diaminonicotinamide compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for treating diseases caused by undesirable and/or abnormal cytokine signal transduction. [Means for Solution] The present inventors have extensively studied compounds having a JAK3 inhibitory action, and as a result, they have found that a 4,6-diaminonicotinamide compound which is the compound of the present invention has an excellent JAK3 inhibitory action and is useful as an agent for preventing or treating diseases caused by undesirable and/or abnormal cytokine signal transduction, thereby completing the present invention.
INHIBITORS OF JAK
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Page/Page column 207, (2010/11/18)
The present invention is directed to compounds of formula (I) and tautomers and pharmaceutically acceptable salts thereof which are selective inhibitors of JAK. 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 activity, and methods to prevent or treat a number of conditions mediated at least in part by JAK activity.
PYRIDINE DERIVATIVES USEFUL AS INHIBITORS OF PKC-THETA
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Page/Page column 12; 13, (2008/06/13)
Disclosed are novel compounds of formula (I): wherein R1, R2 and R3 are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and type II diabetes. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
