| 摘要 |
Prodrugs of COX-2 inhibitors with formula (I) are described as useful in treatment of inflammation and disturbances connected with inflammations, where A is a ring substituent, selected among partly unsaturated heterocyclyl, heteroaryl, cycloalkenyl and aryl, where A is substituted, if requested, on a position which can be substituted with one or several rests, selected among the following, such as alkylcarbonyl, formyl, halo, alkyl, haloalkyl, oxo, cyano, nitro, carboxy, alkoxy, aminocarbonyl, alkoxycarbonyl, carboxyalkyl, cyanoalkyl, hydroxyalkyl, haloalkylsulphonyloxy, alkoxyalkyloxyalkyl, carboxyalkoxyalkyl, cycloalkylalkyl, alkenyl, alkinyl, heterocyclyloxi, alkyltio, cycloalkyl, aryl, heterocyclyl, cycloalkenyl, aralkyl, heterocyclylalkyl, alkyltioalkyl, arylcarbonyl, aralkylcarbonyl, aralkenyl, alkoxyalkyl, aryltioalkyl, aryloxyalkyl, aralkyltioalkyl, 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, aryloxy, aralkoxy, aryltio, aralkyltio, alkylsulphynyl, alkylsulphonyl, aminosulphonyl, alkylaminosulphonyl, N- arylaminosulphonyl, arylsulphonyl and N-alkyl-N-arylaminosulphonyl; where R1 is selected among heterocyclyl, cycloalkyl, cycloalkenyl and aryl, where R1 is substituted, if requested, on a position which can be substituted with one or several rests, selected among alkyl, haloalkyl, cyano, carboxyl, alkoxycarbonyl, hydroxyl, hydroxyalkyl, haloalkoxy, amino, alkylamino, arylamino, nitro, alkoxyalkyl, alkylsulphynyl, halo, alkoxy and alkyltio; where R2 is selected between hydrido and alkoxycarbonylalkyl; and where R3 is selected among alkyl, carboxyalkyl, acyl, alkoxycarbonyl, heteroarylcarbonyl, alkoxycarbonylalkylcarbonyl, alkoxycarbonylcarbonyl, amino acid rest and alkylcarbonylaminoalkylcarbonyl; under the condition that A is not tetrazolium or pyridinium; and further under the condition that A is not indanon, when R3 is alkyl or carboxyalkyl; or its pharmaceutically acceptable salt. |
