| 摘要 |
PURPOSE: Provided is a pharmaceutical composition which is useful in the treatment of degenerative diseases such as emphysema, rheumatoid arthritis, pancreatitis, cystic fibrosis, chronic bronchitis, adult respiratory distress syndrome, inflammatory bowel disease, psoriasis, bullous pemphigoid and alpha-1-antitrypsin deficiency. CONSTITUTION: The pharmaceutical composition comprises a proteolytic enzyme inhibiting concentration of a compound represented by the formula 1 or a pharmaceutically acceptable addition salt thereof in a pharmaceutical carrier. In the formula I, R1 is hydrogen, halo, unsubstituted or substituted alkyl, alkenyl, alkynyl, cyano, amino, alkylamino, alkoxy, benzyloxy, alkoxycarbonyl or phenyl; R2 is selected from one to three substituents at any or all of the 5-, 6- and 7-positions and is hydrogen, unsubstituted or substituted alkyl, cycloalkyl, formyl, cyano, carboxy, carbonyl, B=N, pyrrolyl, amino, nitro, hydroxy, carbonyloxy, alkoxy, cycloalkoxy, alkylenoxy, methylenedioxy, alkylphosphonyloxy, thio, sulfinyl, sulfonyl or halo, R3 is hydrogen, alkyl or phenyl; X is hydrogen, nitro, halo, unsubstituted or substituted alkyl, phenyl, carbonyl, formyl, alkanoyl, carboxy, cyano, B=N, hydroxy, alkoxy, phenyloxy, alkylthio, phenylthio, alkylsulfonyl, B=N is unsubstituted or substituted amino or N-containing heterocyclic group; and -Y- is the remaining atoms of a monocyclic or bicyclic, substituted or unsubstituted carbocyclic or heterocyclic ring system.
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