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    • 6. 发明授权
    • Immunosuppressive effects of pteridine derivatives
    • 蝶啶衍生物的免疫抑制作用
    • US07276506B2
    • 2007-10-02
    • US10651604
    • 2003-08-29
    • Mark Jozef Albert WaerPiet André Maurits Maria HerdewijnWolfgang Eugen Pfleiderer
    • Mark Jozef Albert WaerPiet André Maurits Maria HerdewijnWolfgang Eugen Pfleiderer
    • C07D475/04A61K31/4985
    • C07D475/10A61K31/519A61K31/5377A61K31/541A61K31/551A61K38/13C07D471/04C07D475/04C07D475/08A61K2300/00
    • This invention relates to a group of trisubstituted and tetrasubstituted pteridine derivatives, having the formula: wherein X represents an oxygen atom or a group with the formula NZ and wherein: R1 C1-7 alkyl or arylalkyl; Z is a group independently defined as R1 or the group NZ together with R1 is an optionally substituted heterocyclic group containing at least one nitrogen atom; R2 is amino or acylamino; R4 is an atom or a group selected from the group consisting of hydrogen; C1-7 alkyl; and C1-7 alkoxy; and R3 is an atom or a group selected from the group consisting of aryl optionally substituted with one or more substituents selected from the group consisting of halogen, C1-7 alkyl, and C1-7 alkoxy, their pharmaceutically acceptable salts, and enantiomers, possessing unexpectedly desirable pharmaceutical properties, in particular which are highly active immunosuppressive agents, and being useful in the treatment in transplant rejection, certain inflammatory diseases, cardiovascular disorders, allergic conditions, disorders of the central nervous system and cell proliferative disorders.
    • 本发明涉及一组具有下式的三取代和四取代蝶啶衍生物:其中X表示氧原子或式NZ的基团,其中:R 1 C 1-7 烷基或芳基烷基; Z是独立地定义为R 1或基团NZ与R 1一起为任选取代的含有至少一个氮原子的杂环基; R 2是氨基或酰氨基; R 4是选自氢的原子或基团; C 1-7烷基; 和C 1-7烷氧基; 并且R 3是选自以下的原子或基团:任选被一个或多个选自以下的取代基取代的芳基:卤素,C 1-7烷基 和C 1-7烷氧基,其药学上可接受的盐和对映异构体,具有意想不到的期望的药物性质,特别是高活性免疫抑制剂,并且可用于移植排斥反应中的某些炎症 疾病,心血管疾病,过敏性疾病,中枢神经系统疾病和细胞增殖性疾病。