| 摘要 |
PROBLEM TO BE SOLVED: To obtain new compounds, useful as an interleukin-1βinhibitor and effective in mitigating inflammations such as chronic articular rheumatism, osteoarthritis, etc. SOLUTION: The compounds are represented by formula I [R1 is a halogen, hydroxyl, a substitutable 1-6C alkoxy, etc.; R2 is a substitutable aryl; Ra and Rb are each H or a 1-6C alkyl; X is O, S or NR; R is H or a 1-6C alkyl; Y is (CH2 )m -Z-(CH2 )n ; Z is O, S, NH, etc.; (m) and (n) are each 0-2], e.g. 2- hydroxymethyl-5-(4-pyridyloxy)benzimidazole. The compounds represented by formula I (X is NR) are obtained by reacting a compound represented by the formula R2 -Y-H with 2-nitro-5-chloroaniline, providing a compound represented by formula II, then catalytically reducing the resultant compound and subsequently reacting the reduced compound with a compound represented by formula III in an acidic medium. At least one of the compounds represented by formula I can be contained as an active ingredient and formulated as a pharmaceutical preparation in a peroral, a parenteral (intravenous or subcutaneous) and an intranasal administration forms. The daily dose thereof is 0.1-100mg. |
