公开(公告)号：US20140155597A1

公开(公告)日：2014-06-05

申请号：US14235686

申请日：2012-07-27

申请人： Tetsuya Tanikawa ,  Yasunobu Ushiki ,  Fumihito Ushiyama ,  Toru Yamaguchi ,  Naoya Ono ,  Keiko Yamamoto ,  Risa Tsuruta ,  Yasuhiro Tsutsui ,  Noritomo Fujino ,  Ayumu Mori

发明人： Tetsuya Tanikawa ,  Yasunobu Ushiki ,  Fumihito Ushiyama ,  Toru Yamaguchi ,  Naoya Ono ,  Keiko Yamamoto ,  Risa Tsuruta ,  Yasuhiro Tsutsui ,  Noritomo Fujino ,  Ayumu Mori

IPC分类号： C07D417/12 ,  C07D285/08 ,  C07D277/56 ,  C07D417/04 ,  C07D277/28

CPC分类号： C07D417/12 ,  C07D277/20 ,  C07D277/28 ,  C07D277/30 ,  C07D277/34 ,  C07D277/48 ,  C07D277/56 ,  C07D285/08 ,  C07D417/04

摘要： The purpose of the present invention is to provide a novel compound which has an anti-fungal activity on pathogenic fungi including fungi belonging to the genus Candida, the genus Aspergillus and the genus Trichophyton and is useful as a medicinal agent. A compound represented by formula (I) (wherein A1 represents a nitrogen atom or a group represented by formula CR6; A2 and A3 are the same as or different from each other and independently represent a nitrogen atom or a group represented by formula CH; R1 represents an aryl group which may be substituted by 1 to 5 substituents independently selected from a substituent group (2) or the like; R2 and R3 are the same as or different from each other and independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group, a C1-6 haloalkyl group or a C1-6 alkoxy group; and R4 and R5 are the same as or different from each other and independently represent a hydrogen atom, a C1-6 haloalkyl group, a C1-6 alkyl group or the like) or a salt thereof is useful as an anti-fungal agent.

摘要翻译： 本发明的目的是提供一种对致病真菌具有抗真菌活性的新型化合物，其包括属于假丝酵母属，曲霉属和毛癣菌属的真菌，并且可用作药剂。 由式（I）表示的化合物（其中，A1表示氮原子或式CR6表示的基团; A2和A3彼此相同或不同，独立地表示氮原子或式CH表示的基团; R1 表示可以被1〜5个独立地选自取代基（2）等的取代基取代的芳基; R2和R3彼此相同或不同，独立地表示氢原子，卤素原子， C 1-6烷基，C 1-6卤代烷基或C 1-6烷氧基; R 4和R 5相同或不同，独立地表示氢原子，C1-6卤代烷基，C1- 6烷基等）或其盐可用作抗真菌剂。

公开(公告)号：US09045466B2

公开(公告)日：2015-06-02

申请号：US14235686

申请日：2012-07-27

申请人： Tetsuya Tanikawa ,  Yasunobu Ushiki ,  Fumihito Ushiyama ,  Toru Yamaguchi ,  Naoya Ono ,  Keiko Yamamoto ,  Risa Tsuruta ,  Yasuhiro Tsutsui ,  Noritomo Fujino ,  Ayumu Mori

发明人： Tetsuya Tanikawa ,  Yasunobu Ushiki ,  Fumihito Ushiyama ,  Toru Yamaguchi ,  Naoya Ono ,  Keiko Yamamoto ,  Risa Tsuruta ,  Yasuhiro Tsutsui ,  Noritomo Fujino ,  Ayumu Mori

IPC分类号： C07D417/12 ,  C07D417/04 ,  C07D277/20 ,  C07D277/28 ,  C07D277/30 ,  C07D277/34 ,  C07D277/48 ,  C07D277/56 ,  C07D285/08

CPC分类号： C07D417/12 ,  C07D277/20 ,  C07D277/28 ,  C07D277/30 ,  C07D277/34 ,  C07D277/48 ,  C07D277/56 ,  C07D285/08 ,  C07D417/04

摘要： An amidine compound represented by formula (I) (wherein A1 represents a nitrogen atom or a group represented by formula CR6; A2 and A3 are the same as or different from each other and independently represent a nitrogen atom or a group represented by formula CH; R1 represents an aryl group which may be substituted by 1 to 5 substituents independently selected from a substituent group (2) or the like; R2 and R3 are the same as or different from each other and independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group, a C1-6 haloalkyl group or a C1-6 alkoxy group; and R4 and R5 are the same as or different from each other and independently represent a hydrogen atom, a C1-6 haloalkyl group, a C1-6 alkyl group or the like) or a salt thereof. The compound is useful as an anti-fungal agent.

摘要翻译： 由式（I）表示的脒化合物（其中A1表示氮原子或式CR6表示的基团; A2和A3彼此相同或不同，并且独立地表示氮原子或由式CH表示的基团; R1表示可以被1〜5个独立地选自取代基（2）等的取代基取代的芳基; R2和R3彼此相同或不同，独立地表示氢原子，卤素原子， C 1-6烷基，C 1-6卤代烷基或C 1-6烷氧基; R 4和R 5彼此相同或不同，独立地表示氢原子，C1-6卤代烷基，C1 -6烷基等）或其盐。 该化合物可用作抗真菌剂。