C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 401/04 (2006.01) A61K 31/18 (2006.01) A61K 31/33 (2006.01) A61K 31/365 (2006.01) A61K 31/41 (2006.01) A61K 31/415 (2006.01) A61K 31/42 (2006.01) A61K 31/44 (2006.01) A61K 31/635 (2006.01) C07C 311/16 (2006.01) C07C 311/51 (2006.01) C07D 207/33 (2006.01) C07D 231/12 (2006.01) C07D 233/54 (2006.01) C07D 233/64 (2006.01) C07D 261/08 (2006.01) C07D 263/32 (2006.01) C07D 307/58 (2006.01) C07D 403/04 (2006.01) C07D 405/04 (2006.01) C07D 409/04 (2006.01) C07D 413/04 (2006.01) C07D 417/04 (2006.01) C07D 471/04
Patent
CA 2249009
Prodrugs of COX-2 inhibitors of formula (I) are described as being useful in treating inflammation and inflammation-related disorders wherein A is a ring substituent selected from partially unsaturated heterocyclyl, heteroaryl, cycloalkenyl and aryl, wherein A is optionally substituted at a substitutable position with one or more radicals selected from alkylcarbonyl, formyl, halo, alkyl, haloalkyl, oxo, cyano, nitro, carboxyl, alkoxy, aminocarbonyl, alkoxycarbonyl, carboxyalkyl, cyanoalkyl, hydroxyalkyl, haloalkylsulfonyloxy, 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, aralkoxy, arylthio, aralkylthio, alkylsulfinyl, alkylsulfonyl, aminosulfonyl, alkylaminosulfonyl, N-arylaminosulfonyl, arylsulfonyl, and N-alkyl-N- arylaminosulfonyl; wherein R1 is selected from heterocyclyl, cycloalkyl, cycloalkenyl and aryl, wherein R1 is optionally substituted at a substitutable position with one or more radicals selected from alkyl, haloalkyl, cyano, carboxyl, alkoxycarbonyl, hydroxyl, hydroxyalkyl, haloalkoxy, amino, alkylamino, arylamino, nitro, alkoxyalkyl, alkylsulfinyl, halo, alkoxy and alkylthio; wherein R2 is selected from hydrido and alkoxycarbonylalkyl; and wherein R3 is selected from alkyl, carboxyalkyl, acyl, alkoxycarbonyl, heteroarylcarbonyl, alkoxycarbonylalkylcarbonyl, alkoxycarbonylcarbonyl, amino acid residue, and alkylcarbonylaminoalkylcarbonyl; provided A is not tetrazolium, or pyridinum; and further provided A is not indanone when R3 is alkyl or carboxyalkyl; or a pharmaceutically-acceptable salt thereof.
La présente invention concerne des précurseurs, inhibiteurs du COX-2, représentés par la formule générale (I) et convenant en thérapie des inflammations et des troubles liés aux inflammations ou l'un de leurs sels galéniques. Dans cette formule générale (I), "A" est un substituant cyclique appartenant au groupe des hétérocyclyle, hétéroaryle, cycloalkényle et aryle, la substitution de "A" se faisant éventuellement en une position admettant la substitution, et ce, au moyen d'un ou plusieurs radicaux appartenant au groupe des alkylcarbonyl, formyl, halo, alkyl, haloalkyl, oxo, cyano, nitro, carboxyl, alcoxy, aminocarbonyl, alcoxycarbonyl, carboxyalkyl, cyanoalkyl, hydroxyalkyl, haloalkylsulfonyloxy, alcoxyalkyloxyalkyl, carboxyalcoxyalkyl, cycloalkylalkyl, alkényl, alkynyl, hétérocyclyloxy, alkylthio, cycloalkyl, aryl, hétérocyclyl, cycloalkényl, aralkyl, hétérocyclyalkyl, alkylthioalkyl, arylcarbonyl, aralkylcarbonyl, aralkényl, alcoxyalkyl, arylthioalkyl, aryloxyalkyl, aralkylthioalkyl, aralcoxyalkyl, alcoxycarbonylalkyl, 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, arylthio, aralkylthio, alkylsulfinyl,alkylsulfonyl, aminosulfonyl, alkylaminosulfonyl, N-aralkylaminosulfonyl, arylsulfonyl, et N-alkyl-N-arylaminosulfonyl; R?1¿ appartient au groupe des hétérocyclyle, cycloalkyle, cycloalkényle et aryle, R?1¿ étant éventuellement substitué, en une position admettant la substitution, au moyen d'un ou plusieurs radicaux appartenant au groupe des alkyl, haloalkyl, cyano, carboxyl, alcoxycarbonyl, hydroxyl, hydroxyalkyl, haloalcoxyn amino, alkylamino, arylamino, nitro, alcoxyalkyl, alkylsulfinyl, halo, alcoxy et alkylthio; R?2¿ appartient au groupe des hydrido et alcoxycarbonylalkyl; et R?3¿ appartient au groupe des alkyl, carboxyalkyl, acyl, alcoxycarbonyl, hétéroarylcarbonyl, alcoxycarbonylalkylcarbonyl, alcoxycarbonylcarbonyl, radical d'acide aminé et alkylcarbonylaminoalkylcarbonyl; "A" ne devant être ni tétrazolium ni pyridinium; en outre "A" ne peut être indanone lorsque R?3¿ est alkyl ou carboxyalkyl.
Bertenshaw Stephen
Brown David L.
Carter Jeffery S.
Graneto Matthew J.
Khanna Ish K.
G.d. Searle & Co.
Smart & Biggar
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