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    • 5. 发明授权
    • Substituted-phenyl (N,N'-cycloalkyl/alkyl
carboxamide)-1H/3H-imidazo[4,5-b]pyridine compounds as PAF antagonists
    • 取代的苯基(N,N'-环烷基/烷基甲酰胺)-1H / 3H-咪唑并[4,5-b]吡啶化合物作为PAF拮抗剂
    • US5359073A
    • 1994-10-25
    • US981957
    • 1992-11-24
    • Richard M. WeierIsh K. KhannaMichael A. StealeyJanet A. JulienKirk T. Lentz
    • Richard M. WeierIsh K. KhannaMichael A. StealeyJanet A. JulienKirk T. Lentz
    • A61K31/435A61P9/14A61P11/00A61P29/00C07D471/04C07F7/18C07D471/06
    • C07F7/1856C07D471/04
    • A class of N,N'-cycloalkyl/alkyl benzamides of certain 1H-imidazo[4,5-b]pyridine and 3H-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 the formula: ##STR1## wherein each of X.sup.a and X.sup.b is independently selected from nitrogen atom and --CH--, with the proviso that when one of X.sup.a and X.sup.b is selected as nitrogen atom, then the other of X.sup.a and X.sup.b must be --CH--; wherein R.sup.1 is selected from hydrido, alkyl, hydroxyalkyl, alkoxyalkyl, phenyl, halophenyl, alkylsilyloxyalkyl, amino, monoalkylamino, dialkylamino, aminoalkyl, monoalkylaminoalkyl and dialkylaminoalkyl; wherein each of R.sup.5, R.sup.6, R.sup.7 and R.sup.8 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.sup.9 and R.sup.10 is independently selected from hydrido, alkyl, cycloalkyl, bicycloalkyl, heteroaryl, aryl, alkenyl and cycloalkenyl, and wherein any of said R.sup.9 and R.sup.10 substituents may be further substituted or a pharmaceutically-acceptable salt thereof.
    • 描述了某些1H-咪唑并[4,5-b]吡啶和3H-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,用于治疗心血管和免疫炎性相关病症介导 通过血小板激活因子(PAF)。 特别感兴趣的化合物是下式的化合物:其中Xa和Xb各自独立地选自氮原子和-CH-,条件是当Xa和Xb中的一个被选为氮原子时,则另一个 Xa和Xb必须是-CH-; 其中R 1选自氢,烷基,羟基烷基,烷氧基烷基,苯基,卤代苯基,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。 其中R5,R6,R7和R8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,羟基烷基,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各自独立地选自氢化,烷基,环烷基,双环烷基,杂芳基,芳基,烯基和环烯基,并且其中所述R9和R10取代基中的任一个可以被进一步取代或其药学上可接受的盐。
    • 10. 发明授权
    • N,N'-cycloalkyl/alkyl carboxamide 4H-imidazo-[4,5-b]pyridine compounds
as PAF antagonists
    • N,N'-环烷基/烷基甲酰胺4H-咪唑并[4,5-b]吡啶化合物作为PAF拮抗剂
    • US5262426A
    • 1993-11-16
    • US7461
    • 1993-01-22
    • Richard M. WeierIsh K. KhannaMichael A. StealeyJanet A. Julien
    • Richard M. WeierIsh K. KhannaMichael A. StealeyJanet A. Julien
    • A61K31/435A61P7/02C07D471/04C07F7/18
    • 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 the formula: ##STR1## wherein R.sup.1 is selected from hydrido, alkyl, hydroxyalkyl, alkoxyalkyl, phenyl, halophenyl, pyridinyl, alkylsilyloxyalkyl, amino, monoalkylamino, dialkylamino, aminoalkyl, monoalkylaminoalkyl and dialkylaminoalkyl; wherein each of R.sup.5, R.sup.6, R.sup.7 and R.sup.8 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.sup.9 and R.sup.10 is independently selected from hydrido, alkyl, cycloalkyl, bicycloalkyl, heterocyclic, heterocyclicalkyl, aryl, alkenyl and cycloalkenyl, and wherein any of said R.sup.9 and R.sup.10 substituents may be further substituted with one or 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化合物是下式的化合物:其中R 1选自氢,烷基, 其中R5,R6,R7和R8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,羟基烷基,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R9和R10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 支链低级烷基,低级烷氧基,氟,氯和溴; 或其药学上可接受的盐。