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pyridine derivatives substituted with a heterocycle ring and phosphonoxymethyl group and antifungal agents containing them

机译:被杂环和膦酰氧基甲基取代的吡啶衍生物和含有它们的抗真菌剂

摘要

The present invention provides antifungal agents that have excellent antifungal action, and is also excellent in terms of its properties, particularly its solubility in water and its safety. According to the present invention, disclosed are compounds represented by the following formula (I): (wherein R 1 represents a hydrogen atom, a halogen atom, an amino group, R 11 -NH-(wherein R 11 represents a C 1-6 alkyl group, a hydroxy C 1-6 alkyl group, a C 1-6 alkoxy C 1-6 alkyl group, or a C 1-6 alkoxycarbonyl C 1-6 alkyl group), R 12 -(CO)-NH- (wherein R 12 represents a C 1-6 alkyl group or a C 1-6 alkoxy C 1-6 alkyl group), a C 1-6 alkyl group, a hydroxy C 1-6 alkyl group, a cyano C 1-6 alkyl group, a C 1-6 alkoxy group, or a C 1-6 alkoxy C 1-6 alkyl group; R 2 represents a hydrogen atom, a C 1-6 alkyl group, an amino group, or a di-C 1-6 alkylamino group; one of X and Y represents a nitrogen atom, and the other represents a nitrogen atom or an oxygen atom; ring A represents a 5- or 6-member heteroaryl ring or a benzene ring, which may have one or two halogen atoms or C 1-6 alkyl groups; Z represents a single bond, a methylene group, an ethylene group, an oxygen atom, a sulfur atom, -CH 2 O- -OCH 2 -, -NH-, -CH 2 NH-, -NHCH 2 -, -CH 2 S-, or -SCH 2 -; R 3 represents a hydrogen atom or a halogen atom, or a C 1-6 alkyl group, a C 3 - 8 cycloalkyl group, a C 6-10 aryl group, a 5- or 6-member heteroaryl group, or a 5- or 6-member non-aromatic heterocyclic group, wherein these groups may have one or two substituents selected from a substituent group ±; and R 4 represents a hydrogen atom or a halogen atom; [substituent Group ±] a halogen atom, a cyano group, a C 1-6 alkyl group, a C 1-6 alkoxy group, a C 1-6 alkoxycarbonyl group, a C 3-8 cycloalkyl group, a C 2-6 alkenyl group, and a C 2-6 alkynyl group).
机译:本发明提供了具有优异的抗真菌作用的抗真菌剂,并且在其性质,特别是其在水中的溶解性及其安全性方面也优异。根据本发明,公开了由下式(I)表示的化合物:(其中R 1代表氢原子,卤素原子,氨基,R 11 -NH-(其中R 11代表C 1-6烷基,羟基C 1-6烷基,C 1-6烷氧基C 1-6烷基或C 1-6烷氧羰基C 1-6烷基),R 12-(CO)-NH-(其中R 12代表C 1-6烷基或C 1-6烷氧基) C 1-6烷基),C 1-6烷基,羟基C 1-6烷基,氰基C 1-6烷基,C 1-6烷氧基或C 1-6烷氧基C 1-6个烷基;R 2表示氢原子,C 1-6烷基,氨基或二-C 1-6烷基氨基。X和Y之一表示氮原子,另一个表示氮原子或氧原子。环A代表5或6元杂芳基环或苯环,其可具有一个或两个卤素原子或C 1-6烷基;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代表氢原子或卤素原子,或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元非芳族杂环基,其中这些基团可具有一个或两个选自取代基组±的取代基;或6元非芳族杂环基。和R 4表示氢原子或卤素原子。[取代基组±]卤素原子,氰基,C 1-6烷基,C 1-6烷氧基,C 1-6烷氧基羰基,C 3-8环烷基,C 2-6烯基和C 2-6炔基)。

著录项

  • 公开/公告号BRPI0821653A8

    专利类型

  • 公开/公告日2018-07-10

    原文格式PDF

  • 申请/专利权人 EISAI R&D MANAGEMENT CO. LTD.;

    申请/专利号BR2008PI21653

  • 发明设计人 MASAYUKI MATSUKURA;

    申请日2008-12-26

  • 分类号C07F9/6558;A61K31/661;A61P31/10;

  • 国家 BR

  • 入库时间 2022-08-21 12:53:20

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