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    Heterocycles substituted pyridine derivatives and antifungal agent containing thereof
    8.
    发明授权
    Heterocycles substituted pyridine derivatives and antifungal agent containing thereof 有权
    杂环取代的吡啶衍生物和含有它的抗真菌剂

    公开(公告)号：US08153662B2

    公开(公告)日：2012-04-10

    申请号：US12704643

    申请日：2010-02-12

    申请人： Keigo Tanaka ,  Satoshi Inoue ,  Norio Murai ,  Masayuki Matsukura ,  Kazutaka Nakamoto ,  Shuji Shirotori ,  Shinya Abe

    发明人： Keigo Tanaka ,  Satoshi Inoue ,  Norio Murai ,  Masayuki Matsukura ,  Kazutaka Nakamoto ,  Shuji Shirotori ,  Shinya Abe

    IPC分类号： A61K31/42 ,  A61K31/443 ,  C07D413/14

    CPC分类号： A01N43/56 ,  A01N43/80 ,  C07D401/04 ,  C07D401/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14

    摘要： An object of the present invention is to provide an antifungal agent which has excellent antifungal effects and is superior in terms of its physical properties, safety and metabolic stability. According to the present invention, there is disclosed a compound represented by the following formula (I), or a salt thereof: wherein R1 represents a hydrogen atom, a halogen atom, an amino group, a C1-6 alkyl group, a C1-6 alkoxy group or a C1-6 alkoxy C1-6 alkyl group; R2 represents a hydrogen atom, a C1-6 alkyl group, an amino group or a di C1-6 alkylamino group; one of X and Y is a nitrogen atom while the other is a nitrogen atom or an oxygen atom; ring A represents a 5- or 6-member heteroaryl ring or a benzene ring which may have a halogen atom, or 1 or 2 C1-6 alkyl groups; Z represents a single bond, a methylene group, an ethylene group, an oxygen atom, a sulfur atom, —CH2O—, —OCH2—, —NH—, —CH2NH—, —NHCH2—, —CH2S—, or —SCH2—; R3 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group, a C3-8 cycloalkyl group, a C6-10 aryl group, a 5- or 6-member heteroaryl group, or 5- or 6-member non-aromatic heterocyclic group which may have 1 or 2 substituents; and R4 represents a hydrogen atom or a halogen atom.

    摘要翻译： 本发明的目的是提供一种具有优异的抗真菌作用并且在其物理性质，安全性和代谢稳定性方面优异的抗真菌剂。 根据本发明，公开了由下式（I）表示的化合物或其盐：其中R1表示氢原子，卤素原子，氨基，C1-6烷基，C1- 6烷氧基或C 1-6烷氧基C 1-6烷基; R2表示氢原子，C1-6烷基，氨基或二C1-6烷基氨基; X和Y之一是氮原子，而另一个是氮原子或氧原子; 环A表示可以具有卤素原子或1或2个C 1-6烷基的5或6元杂芳基环或苯环; Z表示单键，亚甲基，亚乙基，氧原子，硫原子，-CH 2 O - ， - OCH 2 - ， - NH - ， - CH 2 NH - ， - NHCH 2 - ， - CH 2 S-或-SCH 2 - ; R 3表示氢原子，卤素原子，C 1-6烷基，C 3-8环烷基，C 6-10芳基，5-或6-元杂芳基，或5-或6-元非 - 可以具有1或2个取代基的芳族杂环基; R4表示氢原子或卤素原子。