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    • 9. 发明申请
    • Heterocyclo-substituted imidazoles for the treatment of inflammation
    • 杂环取代的咪唑用于治疗炎症
    • US20030036557A1
    • 2003-02-20
    • US10004944
    • 2001-12-05
    • G.D. Searle & Co.
    • Ish K. KhannaRichard M. WeierPaul W. CollinsYi YuXiangdong XuRichard A. PartisFrancis J. KoszykRenee M. Huff
    • A61K031/655A61K031/4178A61K031/417C07D43/02C07D233/54
    • C07D233/64C07D233/32C07D233/90C07D401/04C07D403/04C07D405/04C07D409/04C07D419/04
    • A class of imidazolyl compounds is described for use in treating inflammation. Compounds of particular interest are defined by Formula V: 1 wherein R3 is a radical selected from hydrido, alkyl, haloalkyl, aralkyl, heterocycloalkyl, heteroaralkyl, acyl, cyano, alkoxy, alkylthio, alkylthioalkyl, alkylsulfonyl, cycloalkylthio, cycloalkylthioalkyl, cycloalkylsulfonyl, cycloalkylsulfonylalkyl, haloalkylsulfonyl, arylsulfonyl, halo, hydroxyalkyl, alkoxyalkyl, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, heterocyclocarbonyl, cyanoalkyl, aminoalkyl, alkylaminoalkyl, N-arylaminoalkyl, N-alkyl-N-arylaminoalkyl, carboxyalkyl, alkoxycarbonylalkyl, alkoxycarbonyl, haloalkylcarbonyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, alkylaminocarbonylalkyl, heteroarylalkoxyalkyl, heteroaryloxyalkyl, heteroarylthioalkyl, aralkoxy, aralkylthio, heteroaralkoxy, heteroaralkylthio, heteroarylalkylthioalkyl, heteroaryloxy, heteroarylthio, arylthioalkyl, aryloxyalkyl, arylthio, aryloxy, aralkylthioalkyl, aralkoxyalkyl, aryl and heteroaryl; wherein R4 is a radical selected from hydrido, alkyl and halo; and wherein R13 and R14 are independently selected from aryl and heterocyclo, wherein R13 and R14 are optionally substituted at a substitutable position with one or more radicals independently selected from alkylsulfonyl, aminosulfonyl, halo, alkylthio, alkyl, cyano, carboxyl, alkoxycarbonyl, haloalkyl, hydroxyl, alkoxy, hydroxyalkyl, alkoxyalkyl, haloalkoxy, amino, alkylamino, arylamino and nitro; provided at least one of R13 and R14 is aryl substituted with alkylsulfonyl or aminosulfonyl; or a pharmaceutically-acceptable salt thereof.
    • 描述了一类咪唑基化合物用于治疗炎症。 特别感兴趣的化合物由式V定义:其中R3是选自氢,烷基,卤代烷基,芳烷基,杂环烷基,杂芳烷基,酰基,氰基,烷氧基,烷硫基,烷硫基烷基,烷基磺酰基,环烷硫基,环烷硫基烷基,环烷基磺酰基,环烷基磺酰基烷基,卤代烷基磺酰基 ,芳基磺酰基,卤素,羟基烷基,烷氧基烷基,烷基羰基,芳基羰基,芳烷基羰基,杂环羰基,氰基烷基,氨基烷基,烷基氨基烷基,N-芳基氨基烷基,N-烷基-N-芳基氨基烷基,羧基烷基,烷氧基羰基烷基,烷氧基羰基,卤代烷基羰基,羧基,氨基羰基,烷基氨基羰基,烷基氨基羰基烷基 杂芳基烷氧基,杂芳基硫基,杂芳烷氧基,杂芳烷硫基,杂芳基烷硫基烷基,杂芳氧基,杂芳硫基,芳硫基烷基,芳氧基烷基,芳硫基,芳氧基,芳烷硫基烷基,芳烷氧基烷基,芳基和杂芳基; 其中R4是选自氢,烷基和卤素的基团; 并且其中R 13和R 14独立地选自芳基和杂环,其中R 13和R 14在可取代的位置任选被一个或多个独立地选自烷基磺酰基,氨基磺酰基,卤素,烷硫基,烷基,氰基,羧基,烷氧基羰基,卤代烷基, 羟基,烷氧基,羟基烷基,烷氧基烷基,卤代烷氧基,氨基,烷基氨基,芳基氨基和硝基; 提供R13和R14中的至少一个是被烷基磺酰基或氨基磺酰基取代的芳基; 或其药学上可接受的盐。