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    • 2. 发明申请
    • N,N'-CYCLOALKYL/ALKYL CARBOXAMIDE 4H-IMIDAZO[4,5-b]PYRIDINE COMPOUNDS AS PAF ANTAGONISTS
    • N,N'-环烷基/烷基羧酰胺4H-咪唑并[4,5-b]吡啶化合物作为PAF拮抗剂
    • WO1994017063A1
    • 1994-08-04
    • PCT/US1993010220
    • 1993-10-29
    • G.D. SEARLE & CO.WEIER, Richard, MathiasKHANNA, Ish, KumarSTEALEY, Michael, AllanJULIEN, Janet, Anne
    • G.D. SEARLE & CO.
    • C07D471/04
    • C07D471/04
    • A class of N,N'-cycloalkyl/alkyl benzamides of certain 4H-imidazo[4,5-b]pyridine compounds is described for treating cardiovascular and immuno-inflammatory related disorders mediated by platelet activating factor (PAF). Compounds of particular interest are those of formula (1) wherein R is selected from hydrido, alkyl, hydroxyalkyl, alkoxyalkyl, phenyl, halophenyl, pyridinyl, alkylsilyloxyalkyl, amino, monoalkylamino, dialkylamino, aminoalkyl, monoalkylaminoalkyl and dialkylaminoalkyl; wherein each of R , R , R and R is independently selected from hydrido, hydroxy, alkyl, alkoxy, fluoro, chloro, bromo, haloalkyl, alkylthio, alkoxyalkyl, hydroxyalkyl, alkylthioalkyl, cyano, amino, monoalkylamino and dialkylamino; wherein each of R and R is independently selected from hydrido, alkyl, cycloalkyl, bicycloalkyl, heterocyclic, heterocyclicalkyl, aryl, alkenyl and cycloalkenyl, and wherein any of said R and R substituents may be further substituted with one ore more groups selected from linear or branched lower alkyl, lower alkoxy, fluoro, chloro and bromo; or a pharmaceutically-acceptable salt thereof.
    • 描述了某些4H-咪唑并[4,5-b]吡啶化合物的一类N,N'-环烷基/烷基苯甲酰胺,用于治疗由血小板活化因子(PAF)介导的心血管和免疫炎性相关病症。 烷基,羟基烷基,烷氧基烷基,苯基,卤代苯基,吡啶基,烷基甲硅烷氧基烷基,氨基,单烷基氨基,二烷基氨基,氨基烷基,单烷基氨基烷基和二烷基氨基烷基的式(1)化合物,其中R 1选自氢, 其中R 5,R 6,R 7和R 8各自独立地选自氢,羟基,烷基,烷氧基,氟,氯,溴,卤代烷基,烷硫基,烷氧基烷基,羟烷基,烷硫基烷基, 氰基,氨基,单烷基氨基和二烷基氨基; 其中R 9和R 10各自独立地选自氢,烷基,环烷基,双环烷基,杂环,杂环烷基,芳基,烯基和环烯基,并且其中所述R 9和R 10取代基中的任何一个可以 进一步被一个或多个选自直链或支链的低级烷基,低级烷氧基,氟,氯和溴的基团取代; 或其药学上可接受的盐。