| 摘要 |
PURPOSE: To obtain a new pyridazine compound capable of inhibiting interleukin-1βprotease activity and useful for treating an inflammatory disease, an immune system disease or a cancer. CONSTITUTION: A compound of formula I [R1 is a halogen or an oxygen-bound leaving group; R2 is OR5 , N(R5 )R6 (R5 and R6 are each H, a lower alkyl, aryl, etc.); R3 is H or an alkyl; R4 is H, a (substituted) aryl, an alkyl, etc.; (m)=1-6; (n)=2-6], e.g. 3-chloro-4-carboxamido-6-(4-pyridyl)pyridazine. A compound of formula I is obtained as follows: a compound of formula II is made to react with a compound of formula III; the product is treated with hydrazine in ethanol for reduction to obtain a 6-aryl-3-hydroxypyridazine; this compound is saponified with an alkali aqueous solution followed by neutralization; the product is refluxed in the presence of POCl3 ; etc.
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