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    • 1. 发明授权
    • Purine derivatives having phosphodiesterase IV inhibition activity
    • 具有磷酸二酯酶IV抑制活性的嘌呤衍生物
    • US06294541B1
    • 2001-09-25
    • US09418330
    • 1999-10-14
    • David J. CavallaMark ChasinPeter HoferAndre GehrigPeter Wintergerst
    • David J. CavallaMark ChasinPeter HoferAndre GehrigPeter Wintergerst
    • C07D27320
    • C07D473/24C07D473/18C07D473/20C07D473/30C07D473/34
    • A compound of the formula: wherein R3 represent a C1-8 alkyl which is unbranched or branched and unsubstituted or substituted with OH, alkoxy, CO2H, ═NOH, ═NOCONH2, or ═O; C3-8 cycloalkyl which is unsubstituted or substituted with OH, alkoxy, CO2H, ═NOH, ═NOCONH2, or ═O; C4-8 cycloalkylalkyl wherein the cycloalkyl portion is unsubstituted or substituted with OH, alkoxy, CO2H, ═NOH, ═NOCONH2, or ═O; aryl which is unsubstituted or substituted with Cl, NH2, alkylamino, dialkylamino, amido, C1-C8 alkylamido, C1-C3 dialkylamido, OH, alkoxy, HC═NOH, HC═NOCONH2, C1-C3 alkyl, phenyl or benzyl; aralkyl (C1-4); heterocyclyl; heterocyclylalkyl (C1-C4); and heteroaryl; R8 represents H or a C1-8 alkyl which is unbranched or branched and unsubstituted or substituted with OH, alkoxy, CO2H, ═NOH, ═NOCONH2, or ═O; C3-8 cycloalkyl which is unsubstituted or substituted with OH, alkoxy, CO2H, ═NOH, ═NOCONH2, or ═O; C4-8 cycloalkylalkyl wherein the cycloalkyl portion is unsubstituted or substituted with OH, alkoxy, CO2H, ═NOH, ═NOCONH2, or ═O; aryl which is unsubstituted or substituted with Cl, NH2, alkylamino, dialkylamino, amido, C1-C8 alkylamido, C1-C3 dialkylamido, OH, alkoxy, HC═NOH, HC═NOCONH2, C1-C3 alkyl, phenyl or benzyl; aralkyl (C1-4); heterocyclyl; heterocyclylalkyl (C1-C4); and heteroaryl.
    • 下式的化合物:其中R 3表示未支链或未支化或被OH,烷氧基,CO 2 H,= NOH,= NOCONH 2或= O取代的C 1-8烷基; 未取代或被OH,烷氧基,CO 2 H,= NOH,= NOCONH 2或= O取代的C 3-8环烷基; C4-8环烷基烷基,其中环烷基部分未被取代或被OH,烷氧基,CO 2 H,= NOH,= NOCONH 2或= O取代; 未取代或被Cl,NH 2,烷基氨基,二烷基氨基,酰氨基,C 1 -C 8烷基酰氨基,C 1 -C 3二烷基氨基,OH,烷氧基,HC = NOH,HC = NOCONH 2,C 1 -C 3烷基,苯基或苄基取代的芳基; 芳烷基(C1-4); 杂环基 杂环基烷基(C1-C4); R 8表示H或未分支或未被取代或被OH,烷氧基,CO 2 H,= NOH,= NOCONH 2或= O取代的C 1-8烷基; 未取代或被OH,烷氧基,CO 2 H,= NOH,= NOCONH 2或= O取代的C 3-8环烷基; C4-8环烷基烷基,其中环烷基部分未被取代或被OH,烷氧基,CO 2 H,= NOH,= NOCONH 2或= O取代; 未取代或被Cl,NH 2,烷基氨基,二烷基氨基,酰氨基,C 1 -C 8烷基酰氨基,C 1 -C 3二烷基氨基,OH,烷氧基,HC = NOH,HC = NOCONH 2,C 1 -C 3烷基,苯基或苄基取代的芳基; 芳烷基(C1-4); 杂环基 杂环基烷基(C1-C4); 和杂芳基。