| 摘要 |
The invention relates to catechol carboxylic acid derivatives of the formula <IMAGE> I wherein, R1 is <IMAGE> acetyl, hydrogen, hydroxy or alkanoyloxy, R2 is <IMAGE> hydroxy, hydrogen or alkanoyloxy, wherein R is hydrogen, lower alkyl or -(CH2)n-N-(lower alkyl)2, R3 is hydrogen, lower alkyl or amino, R4 is hydrogen, lower alkyl, halogen or amino A is <IMAGE> A' wherein, R5 is hydrogen or acyl, R6 is hydrogen, halogen, lower alkyl, aryl or cycloalkyl, and R7 and R8, independently, are hydrogen, lower alkyl or halogen, or A is <IMAGE> A'' wherein, R5 is hydrogen or acyl, R9 is hydrogen, lower alkyl, R10 is hydrogen, lower alkyl or halogen, R11 is hydrogen, lower alkyl, cycloalkyl or halogen, m is 0 or 1, n is an integer of 2-10, provided, that no more than one of R1 or R2 can be hydroxy, alkanoyloxy or <IMAGE> and when R is hydrogen, salts thereof with pharmaceutically acceptable bases or when R is -(CH2)n-N-(lower alkyl)2, salts thereof with pharmaceutically acceptable acids. The compounds of formula I are useful as agents for the treatment of inflammatory diseases such as arthritis, inflammatory bowel disease such as colitis, cardiovascular diseases such as myocardial ischemia, skin diseases such as psoriasis by topical administration, and bronchopulmonary diseases such as asthma.
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