503071-67-8Relevant articles and documents
Convergent synthesis of 2,3-bisarylpyrazolones through cyclization of bisacylated pyrazolidines and hydrazines
Brugel, Todd A.,Hudlicky, Tomas,Clark, Michael P.,Golebiowski, Adam,Sabat, Mark,Endoma, Mary Ann A.,Bui, Vu,Adams, David,Laufersweiler, Matthew J.,Maier, Jennifer A.,Bookland, Roger G.,De, Biswanath
, p. 3195 - 3198 (2007/10/03)
Cyclization of various bisacylated hydrazines and pyrazolidines using DBU or sodium hydride leads to the formation of various mono-, bi- and tricyclic pyrazolone scaffolds in 41-98% yield. The convergent nature by which the precyclization intermediates are constructed allows for rapid derivatization about the pyrazolone core.
The development of new isoxazolone based inhibitors of tumor necrosis factor-alpha (TNF-α) production
Laughlin, Steven K.,Clark, Michael P.,Djung, Jane F.,Golebiowski, Adam,Brugel, Todd A.,Sabat, Mark,Bookland, Roger G.,Laufersweiler, Matthew J.,VanRens, John C.,Townes, Jennifer A.,De, Biswanath,Hsieh, Lily C.,Xu, Susan C.,Walter, Richard L.,Mekel, Marlene J.,Janusz, Michael J.
, p. 2399 - 2403 (2007/10/03)
4-Aryl-3-pyridyl and 4-aryl-3-pyrimidinyl based tumor necrosis factor-alpha (TNF-α) inhibitors, which contain a novel isoxazolone five-membered heterocyclic core are described. Many showed sub-micromolar activity against lipopolysaccharide-induced TNF-α production.
6,7-dihydro-5H-pyrazolo[1,2-a]pyrazol-1-ones which control inflammatory cytokines
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, (2008/06/13)
The present invention relates to compounds which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: wherein R1 is substituted aryl; R4 is substituted or unsubstituted aryl or heteroaryl.
