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    • 6. 发明申请
    • 1,2-SUBSTITUTED IMIDAZOLYL COMPOUNDS FOR THE TREATMENT OF INFLAMMATION
    • 用于治疗炎症的1,2-取代的咪唑啉化合物
    • WO1996003388A1
    • 1996-02-08
    • PCT/US1995009506
    • 1995-07-27
    • G.D. SEARLE & CO.KHANNA, Ish, K.WEIER, Richard, M.COLLINS, Paul, W.YU, YiXU, XiangdongHUFF, Renee, M.PARTIS, Richard, A.KOSZYK, Francis, J.
    • G.D. SEARLE & CO.
    • C07D233/54
    • 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 (II), wherein R is a radical selected from hydrido, alkyl, haloalkyl, aralkyl, heterocycloalkyl, acyl, cyano, alkoxy, alkylthio, alkylthioalkyl, alkylsulfonyl, cycloalkyloxy, cycloalkyloxyalkyle, cycloalkylthio, cycloalkylthioalkyl, cycloalkylsulfonyl, cyanoalkyl, cycloalkylsulfonylalkyl, haloalkylsulfonyl, azidoalkyl, arylsulfonyl, halo, hydroxyalkyl, alkoxyalkyl, arylthio, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, aryloxy, heterocycloalkylcarbonyl, alkylaminoalkyl, N-arylaminoalkyl, N-alkyl-N-arylaminoalkyl, carboxyalkyl, alkoxycarbonylalkyl, alkoxycarbonyl, haloalkylcarbonyl, aminocarbonyl, alkylaminocarbonylalkyl, aralkylthio, heteroarylalcoxyalkyl, heteroaryloxyalkyl, aralkoxy, heteroarylthioalkyl, heteroaralkoxy, heteroaralkylthio, heteroarylalkylthioalkyl, heteroaryloxy, heteroarylthio, arylthioalkyl, aryloxyalkyl, aralkylthioalkyl, aralkoxyalkyl, aryl and heteroaryl, wherein the aryl and heteroaryl radicals are optionally substitued at a substitutable position with one or more radicals selected from halo, alkylthio, alkylsufinyl, alkyl, cyano, haloalkyl, hydroxyl, alkoxy, hydroxyalkyl and haloalkoxy; wherein R is a radical selected from alkyl and amino; and wherein R is one or more radicals selected from hydrido, halo, alkyl, haloalkyl, alkoxy, amino, haloalkoxy, cyano, carboxyl, hydroxyl, hydroxyalkyl, alkoxyalkyl, alkylamino, nitro and alkylthio.
    • 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(II)定义,其中R 3是选自氢,烷基,卤代烷基,芳烷基,杂环烷基,酰基,氰基,烷氧基,烷硫基,烷硫基烷基,烷基磺酰基,环烷氧基,环烷氧基烯烃, 环烷基硫代烷基,环烷基磺酰基,氰基烷基,环烷基磺酰基烷基,卤代烷基磺酰基,叠氮基烷基,芳基磺酰基,卤素,羟基烷基,烷氧基烷基,芳硫基,烷基羰基,芳基羰基,芳烷基羰基,芳氧基,杂环烷基羰基,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,氨基羰基,烷基氨基羰基烷基,芳烷硫基,杂芳基烷氧基烷基,杂芳氧基烷基,芳烷氧基,杂芳硫基烷基,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,芳烷硫基烷基,芳烷氧基烷基,芳基和杂芳基,其中芳基和杂芳基是优选的 在一个可取代位置被一个或多个选自卤素,烷硫基,烷基亚磺酰基,烷基,氰基,卤代烷基,羟基,烷氧基,羟基烷基和卤代烷氧基的基团取代; 其中R 7是选自烷基和氨基的基团; 其中R 8是选自氢,卤代,烷基,卤代烷基,烷氧基,氨基,卤代烷氧基,氰基,羧基,羟基,羟基烷基,烷氧基烷基,烷基氨基,硝基和烷硫基中的一个或多个基团。