| 摘要 |
The COX-2 inhibitor precursors are successfully used in the treatment of inflammations and conditions caused by them. They have the formula where A is optionally substituted in a position in which it can be substituted with one or more radicals selected amongst alkylcarbonyl, formyl, halo, alkyl, haloalkyl, oxo, cyano, nitro, carboxy, alkoxy, aminocarbonyl, alkoxycarbonyl, carboxyalkyl, cyanoalkyl, hydroxyalkyl, haloalkylsulphonyloxy, alkoxyalkyloxyalkyl, carboxyalkoxyalkyl, cycloalkylalkyl, alkenyl, alkynyl, heterocyclyloxy, alkylthio, cycloalkyl, aryl, heterocyclyl, cycloalkenyl, aralkyl, heterocyclylalkyl, alkylthioalkyl, arylcarbonyl, aralkylcarbonyl, aralkenyl, alkoxyalkyl, arylthioalkyl, aryloxyalkyl, aralkylthioalkyl, aralkoxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, alkylaminocarbonyl, N-arylaminocarbonyl, N-alkyl.N-arylaminocarbonyl, alkylaminocarbonylalkyl, alkylamino, N-arylamino, N-aralkylamino, N-alkyl-N-aralkylamino, N-alkyl-N-arylamino, aminoalkyl, alkylaminoalkyl, N-arylaminoalkyl, N-aralkylaminoalkyl, N-alkyl-N-aralkylaminoalkyl, N-alkyl-N-arylaminoalkyl, aryloxy, aralcoxy, aralkylthio, alkylsulphanyl, alkylsulphonyl, aminosulphonyl, alkylaminosulphonyl, N-arylaminosulphonyl, arylsulphonyl and N-alkyl-N-arylaminosulphonyl, R1 is selected amongst heterocaclyl, cycloalkyl, cycloalkyenyl and aryl, R1 optionally being substituted in a position where it can be substituted by one or more radical selected amongst alkyl, haloalkyl, cyano, carboxy, alkoxycarbonyl, hadroxy, hydroxyalkyl, haloalkoxy, amino, alkylamino, arylamino, nitro, alkoxyalkyl, alkylsulphonyl, halo, alkoxy and alkylthio. R being selected between hydrido and alkoxycarbonylalkyl, and R2 being selected amongst hydrido and alkoxycarbonylalkyl and R2 is selected amongst alkyl, carboxyalkyl,acyl, alkoxycarbonyl, heteroarylcarbonyl, alkoxycarbonylalkylcarbonyl, alkoxycarbonylcarbonyl, resude from amino acid and alkylcarbonylaminoalkylcarbonyl, A should not be tetrazole or pyridine radical and A should not be indanone when R3 is alkyl or carboxyalkyl or its pharmaceutically acceptable salt.
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