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2004
Pyrazole derivatives
R 0180
The Development of Novel Inhibitors of Tumor Necrosis Factor-α (TNF-α) ProBased on Substituted [5,5]-Bicyclic Pyrazolones. — A novel series of bi49- 111 duction
cyclic pyrazolones, e.g. compounds (X) and (XI), is prepared and tested for their inhibition of TNF-α production. Compounds (X) and (XI) possess low nanomolar activity
and show positive oral efficacy in the rat iodoacetate model for osteoarthritis. —
(LAUFERSWEILER*, M. J.; et al.; Bioorg. Med. Chem. Lett. 14 (2004) 16,
4267-4272; Procter & Gamble Pharm. Health Care Res. Cent., Mason, OH 45040,
USA; Eng.) — R. Staver
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