PURPOSE: To obtain the subject new compound composed of a diaryl nitrogen- containing heterocyclic compound, having an interleukin-1 production-infhibitory effect and useful, e.g. for therapy and prevention of diseases caused by interleukin-1, e.g. chronic articular rheumatism, sepsis and asthma.
CONSTITUTION: A compound represented by formula I [Ar1 and Ar2 are each a (substituted) aryl, a (substituted) heteroaryl; R1 to R4 are each H, a (substituted) lower alkyl, a lower alkenyl, a (substituted) aryl, nitro, cyano, carbonyl, etc.; X is N or formula CR8 (R8 is H, a lower alkyl, a lower alkenyl, an aryl, a halogen, etc.)]. This compound can be synthesized by reacting a 1,2-diarylethane expressed by formula III with an aminoarylcarboxylic acid ester shown by formula II (R is a lower alkyl) in the presence of a Lewis acid to form a compound of formula IV, subsequently conducting a ring closure reaction thereof and then substituting the hydroxyl group of the reactional product.
KAJIYASHIKI TSUYOSHI
KAGEYU AKIRA
IDA HIROSHI
TAKAGI MICHIYO
ISHII TAKAHIRO
TAKASUGI YASUNORI
SHIONO MANZO
