PURPOSE: To obtain a new compound exhibiting an interleukin-1 inhibitory activity and useful as an interleukin-1 inhibitor.
CONSTITUTION: A compound of formula I (R1 is a lower alkyl), formula II (R2 is hydroxymethyl or carboxyl), formula III (R3 is a lower alkoxycarbonyl or hydroxymethyl; R4 and R5 are each a lower alkoxy) or formula IV, e.g. 1,2,3,4,4a,5,8,9,10,10a-decahydro-1,4a-dimethyl-7-(1-methyl ester)-5,8-dioxo-1- phenanthrenecarboxylic acid. The compound of formula I can be synthesized by reacting a compound of formula V with diethyl phosphorocyanidate, triethyleneamine and proline methyl ester in a solvent (e.g. DMF) at 0 to 30°C. Interleukin-1 is an important biological substance inducing and transferring systemic biological reactions against infection or inflammation and the compounds of formula I to IV are useful especially for improvement of chronic inflammation.
SHISHIDO KOZO
SHIBUYA MASAYUKI
GOTO KIYOTO
ONO YUKIHISA
OTSUKA PHARMA FACTORY INC
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