| abstract |
Highly water soluble phenylpyridazine derivatives of formula (1) with high oral absorbability are described wherein: R1 is optionally substituted alkyl, or alkenyl R2 and R3 are each independently hydrogen or an alkyl, hydroxyalkyl, dihydroxyalkyl or alkynyl, or R2 and R3 are fused together with the adjacent nitrogen atom to form an optionally substituted, nitrogen-containing, saturated heterocyclic group; X, Y and Z each independently hydrogen or halogen, optionally substituted alkyl, alkoxy, alkylthio, alkylsulfinyl or alkylsulfonyl, or optionally substituted aryl; and n is 1 to 5; with the proviso that R2 and R3 are not hydrogen or the same C1-C3 alkyl groups at the same time when R1 is a benzyl group or a C1-C3 alkyl group. Pharmaceutical compositions comprising the compounds are useful for the prevention or treatment of diseases caused by stimulation of interleukin-1beta production, immune system diseases, inflammatory diseases, ischemic diseases, osteoporosis, ichorremia, rheumatism, arthritis and inflammatory colitis. |