| 摘要 |
PURPOSE:To provide partly new esculetin derivatives effective for suppressing the destruction of articular cartilage, having low toxicity and useful as a cartilage-protection agent for the treatment of rheumatoid arthritis, arthrosis deformans, scapulohumeral periarthritis, etc. CONSTITUTION:A cartilage-protection agent containing a compound expressed by formula I (R<1> and R<2> are H, 2-25C saturated or unsaturated aliphatic acyl or benzoyl; R<3> is H or alkyl). The compounds of formula II (R<11> and R<12> are H, pivaloyl, capryloyl, lauroyl, palmitoyl, stearoyl, linoleoyl, docosahexaenoyl or benzoyl; R<13> is H or methyl) (e.g. escu1etin-6-monopivalate) are new compounds in the compounds of formula I. Various carboxylic acid mono or diesters of esculetin or 4-alkylesculetin can be produced e.g. by reacting esculetin or 4-alkylesculetin with various carboxylic acids in the presence of an acid catalyst.
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