| abstract |
The following describes that prodrugs of COX-2 inhibitors of Formula I, or pharmaceutically acceptable salts thereof, are useful for treating inflammation and inflammation related disorders.n n n Formula In n n n n n n n Wherein A is a ring substituent selected from partially unsaturated heterocyclyl, heteroaryl, cycloalkenyl and aryl, A is alkylcarbonyl, formyl, halo, alkyl, haloalkyl, oxo, cyano, nitro, Carboxyl, alkoxy, aminocarbonyl, alkoxycarbonyl, carboxyalkyl, cyanoalkyl, hydroxyalkyl, haloalkylsulfonyloxy, alkoxyalkyloxyalkyl, carboxyalkoxyalkyl, cycloalkylalkyl, alkenyl, alkynyl, hetero Cyclyloxy, alkylthio, cycloalkyl, aryl, heterocyclyl, cycloalkenyl, aralkyl, heterocyclylalkyl, alkylthioalkyl, arylcarbonyl, aralkylcarbonyl, arkenyl, alkoxyalkyl, arylthioalkyl , Aryloxyalkyl, aralkylthioalkyl, aralkyloxy, alkoxycarbonylalkyl, aminocarbonylalkyl, alkylaminocarbonyl, N-arylaminocarbonyl, N-alkyl-N-arylaminocarbonyl, alkylami Carbonylalkyl, 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, aralkyloxy, arylthio, aralkylthio, alkylsulfinyl, alkylsulfonyl, Optionally substituted at a position substitutable with one or more radicals selected from aminosulfonyl, alkylaminosulfonyl, N-arylaminosulfonyl, arylsulfonyl and N-alkyl-N-arylaminosulfonyl; R 1 is selected from heterocyclyl, cycloalkyl, cycloalkenyl and aryl, R 1 is alkyl, haloalkyl, cyano, carboxyl, alkoxycarbonyl, hydroxyl, hydroxyalkyl, haloalkoxy, amino, alkyl Optionally substituted at a position substitutable with one or more radicals selected from amino, arylamino, nitro, alkoxyalkyl, alkylsulfinyl, halo, alkoxy and alkylthio; R 2 is selected from hydrido and alkoxycarbonylalkyl; R 3 is selected from alkyl, carboxyalkyl, acyl, alkoxycarbonyl, heteroarylcarbonyl, alkoxycarbonylalkylcarbonyl, alkoxycarbonylcarbonyl, amino acid residues and alkylcarbonylaminoalkylcarbonyl; Provided that A is not tetrazolium or pyridinium; And A is not indanone when R 3 is alkyl or carboxyalkyl. |