219838-93-4Relevant academic research and scientific papers
SAR of 2,6-diamino-3,5-difluoropyridinyl substituted heterocycles as novel p38MAP kinase inhibitors.
Revesz, Laszlo,Di Padova, Franco E,Buhl, Thomas,Feifel, Roland,Gram, Hermann,Hiestand, Peter,Manning, Ute,Wolf, Romain,Zimmerlin, Alfred G
, p. 2109 - 2112 (2007/10/03)
2,6-Diamino-3,5-difluoropyridinyl substituted pyridinylimidazoles, -pyrroles, -oxazoles, -thiazoles and -triazoles have been identified as novel p38alpha inhibitors. Pyridinylimidazole 11 potently inhibited LPS-induced TNFalpha in mice, showed good efficacy in the established rat adjuvant (ED(50): 10 mg/kg po b.i.d.) and collagen induced arthritis (ED(50): 5 mg/kg po b.i.d.) with disease modifying properties based on histological analysis of the joints.
2-substituted 4,5-diaryl imidazoles
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, (2008/06/13)
Novel 2-substituted 4,5-diaryl imidazoles are provided, in particular compounds of Formula I wherein R1, R2, R3 and R4 are as defined, in free or pharmaceutically-acceptable acid addition salt or physiologically-cleavable ester form, which have p38 MAP kinase (Mitogen Activated Protein Kinase) inhibiting activity. The compounds are used as pharmaceuticals for treating TNFα and IL-1 mediated diseases such as rheumatoid arthritis and diseases of bone metabolism, e.g. osteoporosis.
