503071-70-3Relevant 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 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.
Isoxazolone compounds useful in treating diseases associated with unwanted cytokine activity
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, (2008/06/13)
Isoxazolone compounds having the generic structure: are used to treat disease associated with unwanted cytokine activity, including rheumatoid arthritis, osteoarthritis, diabetes, HIV/AIDS, inflammatory bowel disease, Crohn's disease, ulcerative colitis,