-
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。
-
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:US08524738B2
公开(公告)日:2013-09-03
申请号:US13463434
申请日:2012-05-03
申请人: Taro Kiyoto , Tadashi Tanaka , Yasuhiro Tsutsui , Junichi Ando , Mai Motono , Yasuko Kawaguchi , Toshiya Noguchi , Yasunobu Ushiki , Fumihito Ushiyama , Hiroki Urabe
发明人: Taro Kiyoto , Tadashi Tanaka , Yasuhiro Tsutsui , Junichi Ando , Mai Motono , Yasuko Kawaguchi , Toshiya Noguchi , Yasunobu Ushiki , Fumihito Ushiyama , Hiroki Urabe
IPC分类号: A61K31/47
CPC分类号: C07D405/14 , C07D215/227 , C07D401/06 , C07D401/14 , C07D405/12 , C07D409/14 , C07D413/14 , C07D471/04 , C07D491/04 , C07D495/04 , C07D513/04 , C07D519/00
摘要: A nitrogen-containing heterocyclic compound or pharmaceutically acceptable salt thereof represented by the general formula: which have a potent antibacterial activity and a high safety. Thus, the compounds are useful as antibacterial agents against gram-positive bacteria, gram-negative bacteria and drug resistant bacteria.
摘要翻译: 由通式表示的含氮杂环化合物或其药学上可接受的盐,其具有强的抗菌活性和高安全性。 因此,这些化合物可用作抗革兰氏阳性细菌,革兰氏阴性细菌和耐药细菌的抗菌剂。
-
公开(公告)号:US08329694B2
公开(公告)日:2012-12-11
申请号:US11993652
申请日:2006-06-22
申请人: Taro Kiyoto , Tadashi Tanaka , Yasuhiro Tsutsui , Junichi Ando , Mai Motono , Yasuko Kawaguchi , Toshiya Noguchi , Yasunobu Ushiki , Fumihito Ushiyama , Hiroki Urabe
发明人: Taro Kiyoto , Tadashi Tanaka , Yasuhiro Tsutsui , Junichi Ando , Mai Motono , Yasuko Kawaguchi , Toshiya Noguchi , Yasunobu Ushiki , Fumihito Ushiyama , Hiroki Urabe
IPC分类号: A61K31/495
CPC分类号: C07D405/14 , C07D215/227 , C07D401/06 , C07D401/14 , C07D405/12 , C07D409/14 , C07D413/14 , C07D471/04 , C07D491/04 , C07D495/04 , C07D513/04 , C07D519/00
摘要: A nitrogen-containing heterocyclic compound or pharmaceutically acceptable salt thereof represented by the general formula: which have a potent antibacterial activity and a high safety. Thus, the compounds are useful as antibacterial agents against gram-positive bacteria, gram-negative bacteria and drug resistant bacteria.
摘要翻译: 由通式表示的含氮杂环化合物或其药学上可接受的盐,其具有强的抗菌活性和高安全性。 因此,这些化合物可用作抗革兰氏阳性细菌,革兰氏阴性细菌和耐药细菌的抗菌剂。
-
公开(公告)号:US20120214990A1
公开(公告)日:2012-08-23
申请号:US13463434
申请日:2012-05-03
申请人: Taro KIYOTO , Tadashi Tanaka , Yasuhiro Tsutsui , Junichi Ando , Mai Motono , Yasuko Kawaguchi , Toshiya Noguchi , Yasunobu Ushiki , Fumihito Ushiyama , Hiroki Urabe
发明人: Taro KIYOTO , Tadashi Tanaka , Yasuhiro Tsutsui , Junichi Ando , Mai Motono , Yasuko Kawaguchi , Toshiya Noguchi , Yasunobu Ushiki , Fumihito Ushiyama , Hiroki Urabe
IPC分类号: C07D405/14 , C07D491/056 , C07D413/14 , C07D417/14 , C07D513/04 , C07D498/04 , C07D471/04 , C07D401/06 , C07D495/04 , C07D401/14 , C07D405/12 , C07D215/22 , C07D409/14 , C07D455/04
CPC分类号: C07D405/14 , C07D215/227 , C07D401/06 , C07D401/14 , C07D405/12 , C07D409/14 , C07D413/14 , C07D471/04 , C07D491/04 , C07D495/04 , C07D513/04 , C07D519/00
摘要: A nitrogen-containing heterocyclic compound or pharmaceutically acceptable salt thereof represented by the general formula: which have a potent antibacterial activity and a high safety. Thus, the compounds are useful as antibacterial agents against gram-positive bacteria, gram-negative bacteria and drug resistant bacteria.
摘要翻译: 由通式表示的含氮杂环化合物或其药学上可接受的盐,其具有强的抗菌活性和高安全性。 因此,这些化合物可用作抗革兰氏阳性细菌,革兰氏阴性细菌和耐药细菌的抗菌剂。
-
公开(公告)号:US20100168418A1
公开(公告)日:2010-07-01
申请号:US11993652
申请日:2006-06-22
申请人: Taro Kiyoto , Tadashi Tanaka , Yasuhiro Tsutsui , Junichi Ando , Mai Motono , Yasuko Kawaguchi , Toshiya Noguchi , Yasunobu Ushiki , Fumihito Ushiyama , Hiroki Urabe
发明人: Taro Kiyoto , Tadashi Tanaka , Yasuhiro Tsutsui , Junichi Ando , Mai Motono , Yasuko Kawaguchi , Toshiya Noguchi , Yasunobu Ushiki , Fumihito Ushiyama , Hiroki Urabe
IPC分类号: C07D513/06 , C07D401/06 , C07D405/14 , C07D493/04 , C07D409/14
CPC分类号: C07D405/14 , C07D215/227 , C07D401/06 , C07D401/14 , C07D405/12 , C07D409/14 , C07D413/14 , C07D471/04 , C07D491/04 , C07D495/04 , C07D513/04 , C07D519/00
摘要: A nitrogen-containing heterocyclic compound represented by the general formula: wherein the dashed line represents a single bond or a double bond; R1, R2, R3, R4 and R5 independently represent a hydrogen atom, halogen atom, a lower alkyl, aryl, lower alkoxy or monocyclic heterocyclic group which may be substituted or the like; R6 represents a lower alkyl, aryl, monocyclic heterocyclic, bicyclic heterocyclic or tricyclic heterocyclic group which may be substituted; X1 represents a lower alkylene group or the like; X2 represents a lower alkylene, lower alkenylene or lower alkynylene group which may be substituted; X3 represents an oxygen atom, sulfur atom, a sulfinyl group, sulfonyl group or the like; Y1 represents a bivalent cyclic group, containing a nitrogen, which may be substituted or the like; and Z1 represents a nitrogen atom, a carbon atom which may be substituted or the like, or a salt thereof. The compound or salt has a potent antibacterial activity and a high safety, and is therefore useful as an excellent antibacterial agent.
摘要翻译: 由以下通式表示的含氮杂环化合物:其中虚线表示单键或双键; R1,R2,R3,R4和R5独立地表示氢原子,卤原子,可被取代的低级烷基,芳基,低级烷氧基或单环杂环基等; R6代表可被取代的低级烷基,芳基,单环杂环,双环杂环或三环杂环基; X1表示低级亚烷基等; X2表示可以被取代的低级亚烷基,低级亚烯基或低级亚烷基; X3表示氧原子,硫原子,亚磺酰基,磺酰基等; Y1表示含有氮的二价环状基团,其可以被取代等; Z1表示氮原子,可以被取代的碳原子等,或其盐。 该化合物或盐具有有效的抗菌活性和高安全性,因此可用作优异的抗菌剂。
-
公开(公告)号:US08367831B2
公开(公告)日:2013-02-05
申请号:US13468140
申请日:2012-05-10
申请人: Taro Kiyoto , Junichi Ando , Tadashi Tanaka , Yasuhiro Tsutsui , Mai Yokotani , Toshiya Noguchi , Fumihito Ushiyama , Hiroki Urabe , Hiromasa Horikiri
发明人: Taro Kiyoto , Junichi Ando , Tadashi Tanaka , Yasuhiro Tsutsui , Mai Yokotani , Toshiya Noguchi , Fumihito Ushiyama , Hiroki Urabe , Hiromasa Horikiri
IPC分类号: C07D471/04
CPC分类号: C07D471/04 , C07D491/056 , C07D519/00 , Y02P20/55
摘要: Disclosed is a compound represented by the general formula: wherein R1 represents an aryl or heterocyclic group which may be substituted or the like; X1 represents a C2-C4 alkylene group or the like; X2, X3 and X5 independently represent NH, a bond or the like; X4 represents a lower alkylene group, a bond or the like; Y1 represents a bivalent alicyclic hydrocarbon residue which may be substituted or a bivalent alicyclic amine residue which may be substituted; and Z1, Z2, Z3, Z4, Z5 and Z6 independently represent a nitrogen atom, a group represented by the formula: CH, or the like, provided that at least one of Z3, Z4, Z5 and Z6 represents a nitrogen atom, or a salt thereof, which is useful as an antibacterial agent.
摘要翻译: 公开了由以下通式表示的化合物:其中R1表示可被取代的芳基或杂环基等; X1表示C2-C4亚烷基等; X2,X3和X5独立地表示NH,键等; X 4表示低级亚烷基,键等; Y1表示可以被取代的二价脂环族烃残基或可以被取代的二价脂环族胺残基; 并且Z 1,Z 2,Z 3,Z 4,Z 5和Z 6独立地表示氮原子,由式CH表示的基团等,条件是Z 3,Z 4,Z 5和Z 6中的至少一个表示氮原子,或 其盐,其可用作抗菌剂。
-
8.
公开(公告)号:US20120226035A1
公开(公告)日:2012-09-06
申请号:US13468140
申请日:2012-05-10
申请人: Taro KIYOTO , Junichi Ando , Tadashi Tanaka , Yasuhiro Tsutsui , Mai Yokotani , Toshiya Noguchi , Fumihito Ushiyama , Hiroki Urabe , Hiromasa Horikiri
发明人: Taro KIYOTO , Junichi Ando , Tadashi Tanaka , Yasuhiro Tsutsui , Mai Yokotani , Toshiya Noguchi , Fumihito Ushiyama , Hiroki Urabe , Hiromasa Horikiri
IPC分类号: C07D471/04 , C07D491/052 , C07D498/04 , C07D491/056 , C07D513/04
CPC分类号: C07D471/04 , C07D491/056 , C07D519/00 , Y02P20/55
摘要: Disclosed is a compound represented by the general formula: wherein R1 represents an aryl or heterocyclic group which may be substituted or the like; X1 represents a C2-C4 alkylene group or the like; X2, X3 and X5 independently represent NH, a bond or the like; X4 represents a lower alkylene group, a bond or the like; Y1 represents a bivalent alicyclic hydrocarbon residue which may be substituted or a bivalent alicyclic amine residue which may be substituted; and Z1, Z2, Z3, Z4, Z5 and Z6 independently represent a nitrogen atom, a group represented by the formula: CH, or the like, provided that at least one of Z3, Z4, Z5 and Z6 represents a nitrogen atom, or a salt thereof, which is useful as an antibacterial agent.
摘要翻译: 公开了由以下通式表示的化合物:其中R1表示可被取代的芳基或杂环基等; X1表示C2-C4亚烷基等; X2,X3和X5独立地表示NH,键等; X 4表示低级亚烷基,键等; Y1表示可以被取代的二价脂环族烃残基或可以被取代的二价脂环族胺残基; 并且Z 1,Z 2,Z 3,Z 4,Z 5和Z 6独立地表示氮原子,由式CH表示的基团等,条件是Z 3,Z 4,Z 5和Z 6中的至少一个表示氮原子,或 其盐,其可用作抗菌剂。
-
公开(公告)号:US08211908B2
公开(公告)日:2012-07-03
申请号:US12302451
申请日:2007-05-24
申请人: Taro Kiyoto , Junichi Ando , Tadashi Tanaka , Yasuhiro Tsutsui , Mai Yokotani , Toshiya Noguchi , Fumihito Ushiyama , Hiroki Urabe , Hiromasa Horikiri
发明人: Taro Kiyoto , Junichi Ando , Tadashi Tanaka , Yasuhiro Tsutsui , Mai Yokotani , Toshiya Noguchi , Fumihito Ushiyama , Hiroki Urabe , Hiromasa Horikiri
IPC分类号: A61K31/4353 , C07D471/22
CPC分类号: C07D471/04 , C07D491/056 , C07D519/00 , Y02P20/55
摘要: Disclosed is a compound represented by the general formula: [wherein R1 represents an aryl or heterocyclic group which may be substituted or the like; X1 represents a C2-C4 alkylene group or the like; X2, X3 and X5 independently represent NH, a bond or the like; X4 represents a lower alkylene group, a bond or the like; Y1 represents a bivalent alicyclic hydrocarbon residue which may be substituted or a bivalent alicyclic amine residue which may be substituted; and Z1, Z2, Z3, Z4, Z5 and Z6 independently represent a nitrogen atom, a group represented by the formula: CH, or the like, provided that at least one of Z3, Z4, Z5 and Z6 represents a nitrogen atom] or a salt thereof, which is useful as an antibacterial agent.
摘要翻译: 公开了由以下通式表示的化合物:其中R 1表示可被取代的芳基或杂环基等; X1表示C2-C4亚烷基等; X2,X3和X5独立地表示NH,键等; X 4表示低级亚烷基,键等; Y1表示可以被取代的二价脂环族烃残基或可以被取代的二价脂环族胺残基; 并且Z 1,Z 2,Z 3,Z 4,Z 5和Z 6独立地表示氮原子,由式CH表示的基团等,条件是Z 3,Z 4,Z 5和Z 6中的至少一个表示氮原子]或 其盐,其可用作抗菌剂。
-
10.
公开(公告)号:US20090198063A1
公开(公告)日:2009-08-06
申请号:US12302451
申请日:2007-05-24
申请人: Taro Kiyoto , Junichi Ando , Tadashi Tanaka , Yasuhiro Tsutsui , Mai Yokotani , Toshiya Noguchi , Fumihito Ushiyama , Hiroki Urabe , Hiromasa Horikiri
发明人: Taro Kiyoto , Junichi Ando , Tadashi Tanaka , Yasuhiro Tsutsui , Mai Yokotani , Toshiya Noguchi , Fumihito Ushiyama , Hiroki Urabe , Hiromasa Horikiri
IPC分类号: A61K31/4375 , C07D471/04 , A61P31/04
CPC分类号: C07D471/04 , C07D491/056 , C07D519/00 , Y02P20/55
摘要: Disclosed is a compound represented by the general formula: [wherein R1 represents an aryl or heterocyclic group which may be substituted or the like; X1 represents a C2-C4 alkylene group or the like; X2, X3 and X5 independently represent NH, a bond or the like; X4 represents a lower alkylene group, a bond or the like; Y1 represents a bivalent alicyclic hydrocarbon residue which may be substituted or a bivalent alicyclic amine residue which may be substituted; and Z1, Z2, Z3, Z4, Z5 and Z6 independently represent a nitrogen atom, a group represented by the formula: CH, or the like, provided that at least one of Z3, Z4, Z5 and Z6 represents a nitrogen atom] or a salt thereof, which is useful as an antibacterial agent.
摘要翻译: 公开了由以下通式表示的化合物:其中R 1表示可被取代的芳基或杂环基等; X1表示C2-C4亚烷基等; X2,X3和X5独立地表示NH,键等; X 4表示低级亚烷基,键等; Y1表示可以被取代的二价脂环族烃残基或可以被取代的二价脂环族胺残基; 并且Z 1,Z 2,Z 3,Z 4,Z 5和Z 6独立地表示氮原子,由式CH表示的基团等,条件是Z 3,Z 4,Z 5和Z 6中的至少一个表示氮原子]或 其盐,其可用作抗菌剂。
-
-
-
-
-
-
-
-
-