发明公开
EP0892791A1 SUBSTITUTED BENZENESULFONAMIDE DERIVATIVES AS PRODRUGS OF COX-2 INHIBITORS
失效
替代苯甲酰胺衍生物ALS PRODROGEN VON COX-2 INHIBITOREN
- 专利标题: SUBSTITUTED BENZENESULFONAMIDE DERIVATIVES AS PRODRUGS OF COX-2 INHIBITORS
- 专利标题(中): 替代苯甲酰胺衍生物ALS PRODROGEN VON COX-2 INHIBITOREN
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申请号: EP97921092.0申请日: 1997-04-11
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公开(公告)号: EP0892791A1公开(公告)日: 1999-01-27
- 发明人: TALLEY, John, J. , MALECHA, James, W. , BERTENSHAW, Stephen , GRANETO, Matthew, J. , CARTER, Jeffery, S. , LI, Jinglin , NAGARAJAN, Srinivasan , BROWN, David, L. , ROGIER, Donald, J., Jr. , PENNING, Thomas, D. , KHANNA, Ish, K. , XU, Xiangdong , WEIER, Richard, M.
- 申请人: G.D. SEARLE & CO.
- 申请人地址: P.O. Box 5110 Chicago IL 60680-5110 US
- 专利权人: G.D. SEARLE & CO.
- 当前专利权人: G.D. SEARLE & CO.
- 当前专利权人地址: P.O. Box 5110 Chicago IL 60680-5110 US
- 代理机构: Beil, Hans Christoph, Dr., et al
- 优先权: US19960631514 19960412
- 国际公布: WO1997038986 19971023
- 主分类号: C07D
- IPC分类号: C07D ; C07D233 ; A61K31 ; A61P1 ; A61P3 ; A61P5 ; A61P7 ; A61P9 ; A61P11 ; A61P13 ; A61P15 ; A61P17 ; A61P19 ; A61P21 ; A61P25 ; A61P27 ; A61P29 ; A61P31 ; A61P35 ; A61P37 ; A61P43 ; C07C311 ; C07D207 ; C07D231 ; C07D261 ; C07D263 ; C07D307 ; C07D401 ; C07D417 ; C07D495
摘要:
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.
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