607721-72-2Relevant academic research and scientific papers
The development of monocyclic pyrazolone based cytokine synthesis inhibitors
Golebiowski, Adam,Townes, Jennifer A.,Laufersweiler, Matthew J.,Brugel, Todd A.,Clark, Michael P.,Clark, Cynthia M.,Djung, Jane F.,Laughlin, Steven K.,Sabat, Mark P.,Bookland, Roger G.,VanRens, John C.,De, Biswanath,Hsieh, Lily C.,Janusz, Michael J.,Walter, Richard L.,Webster, Mark E.,Mekel, Marlene J.
, p. 2285 - 2289 (2007/10/03)
4-Aryl-5-pyrimidyl based cytokine synthesis inhibitors that contain a novel monocyclic, pyrazolone heterocyclic core are described. Many of these inhibitors showed low nanomolar activity against LPS-induced TNF-α production. One of the compounds (6e) was found to be efficacious in the rat iodoacetate (RIA) in vivo model of osteoarthritis. The X-ray crystal structure of a pyrazolone inhibitor cocrystallized with mutated p38 (mp38) is presented.
1,2-dihydropyrazol-3-ones which controls inflammatory cytokines
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Page 26; 25-26, (2010/02/05)
The present invention relates to compounds which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, or enantiomeric and diasteriomeric forms or pharmaceutically acceptable salts thereof, have the formula: wherein R is an ether or amino unit, R1 is substituted phenyl, each R2 and R3 unit is independently selected from the group consisting of: a) hydrogen; and b) substituted or unsubstituted C1-C10 hydrocarbyl selected from the group consisting of: i) C1-C10 linear, branched or cyclic alkyl; ii) C1-C10 aryl; iii) C1-C10 heterocyclic; iv) C1-C10 heteroaryl.
