Heterocycles substituted pyridine derivatives and antifungal agent containing thereof
申请人:Tanaka Keigo
公开号:US20070105904A1
公开(公告)日:2007-05-10
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 R
1
represents a hydrogen atom, a halogen atom, an amino group, a 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 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 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, a halogen atom, 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 5- or 6-member non-aromatic heterocyclic group which may have 1 or 2 substituents; and R
4
represents a hydrogen atom or a halogen atom.
本发明的目的是提供一种具有优异的抗真菌效果、在物理性质、安全性和代谢稳定性方面优越的抗真菌剂。根据本发明,公开了以下式(I)所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C1-6烷氧基C1-6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中的一个是氮原子,另一个是氮原子或氧原子;环A表示一个5-或6-成员杂芳环或苯环,可以有一个卤素原子或1或2个C1-6烷基;Z表示单键、亚甲基、乙烯基、氧原子、硫原子、—CH2O—、—OCH2—、—NH—、—CH2NH—、—NHCH2—、—CH2S—或—SCH2—;R3表示氢原子、卤素原子、C1-6烷基、C3-8环烷基、C6-10芳基、5-或6-成员杂芳基或5-或6-成员非芳杂环基,可以有1或2个取代基;R4表示氢原子或卤素原子。