ORGN 474 |
| Lawrence A. Black1, R. Athalye2, Anwer Basha2, Pramila A. Bhatia2, Jennifer J. Bouska2, Linda Chernesky2, John DeMattei2, Todd Gane2, Ahmed Hakeem2, Richard Harris2, Cathy Henry2, Peer B Jacobson3, Jianguo Ji2, Teodozyj Kolasa2, Michael E. Kort2, Daniel Larson2, Huaqing Liu2, Sandy Majest2, Kennan Marsh4, Catherine M. McCarty2, Merrill Nuss2, Meena V. Patel2, Daisy Pireh2, Marina Pliuschev2, James Ratajczyk2, Jeffrey J. Rohde2, Teresa Rosenberg2, Richard J. Sciotti2, S. Surapaneni2, Frank L. Wagenaar5, Michael R. Michaelides2, Andrew O. Stewart2, Michael J. Coghlan2, James Summers2, Clint D. W. Brooks2, George W. Carter2, and Randy L. Bell2. (1) Global Pharmaceutical Research and Development, Abbott Laboratories, R4MN, AP9A, 216, 100 Abbott Park Road, Abbott Park, IL 60064-6123, (2) Abbott Laboratories, (3) Metabolic Diseases Research, Abbott Laboratories, R47H, AP13, 100 Abbott Park Road, Abbott Park, IL 60064, (4) Exploratory Science, Abbott Laboratories, R4EK, AP9, 100 Abbott Park Rd., Abbott Park, IL 60064-6101, (5) Infectious Disease Research, Abbott Laboratories, D47N Bldg AP52N, 200 Abbott Park Rd, Abbott Park, IL 60064-6217 |
| Clinical experience with the three marketed selective COX-2 inhibitors, Celebrex® (celecoxib), Vioxx® (rofecoxib) and Bextra® (valdecoxib), has supported the hypothesis that these agents would effectively treat pain, inflammation, and fever with improved gastrointestinal safety relative to the older, non-selective NSAIDs. All three of these new drugs share a similar structural motif: a core heterocyclic ring substituted with a phenyl ring and a 4-(sulfonyl)phenyl ring on adjacent atoms. At Abbott, this structural motif was investigated employing 3(2H)-pyridazinone as the core heterocycle. This report describes the initial identification of the active regioisomers, and the ensuing SAR studies that culminated in the selection of ABT-963 for clinical investigation. |
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Technical Achievement in Organic Chemistry Awards
8:30 AM-11:25 AM, Wednesday, September 10, 2003 Sheraton New York -- Imperial Ballroom A, Oral
Division of Organic Chemistry |