公开(公告)号：EP2678349B1

公开(公告)日：2016-01-13

申请号：EP12749570.3

申请日：2012-02-20

申请人： Taisho Pharmaceutical Co., Ltd. ,  Meiji Seika Pharma Co., Ltd.

发明人： SUGIMOTO, Tomohiro ,  SASAMOTO, Naoki ,  KUROSAKA, Jun ,  HAYASHI, Masato ,  YAMAMOTO, Kanako ,  KASHIMURA, Masato ,  USHIKI, Yasunobu ,  OGITA, Haruhisa ,  MIURA, Tomoaki ,  KANEMOTO, Kenichi ,  KUMURA, Kou ,  YOSHIDA, Satoshi ,  TAMURA, Keiji ,  SHITARA, Eiki

IPC分类号： C07H17/08 ,  A61K31/7048 ,  A61P31/04

CPC分类号： C07H17/08

公开(公告)号：EP2678349A1

公开(公告)日：2014-01-01

申请号：EP12749570.3

申请日：2012-02-20

申请人： Taisho Pharmaceutical Co., Ltd. ,  Meiji Seika Pharma Co., Ltd.

发明人： SUGIMOTO, Tomohiro ,  SASAMOTO, Naoki ,  KUROSAKA, Jun ,  HAYASHI, Masato ,  YAMAMOTO, Kanako ,  KASHIMURA, Masato ,  USHIKI, Yasunobu ,  OGITA, Haruhisa ,  MIURA, Tomoaki ,  KANEMOTO, Kenichi ,  KUMURA, Kou ,  YOSHIDA, Satoshi ,  TAMURA, Keiji ,  SHITARA, Eiki

IPC分类号： C07H17/08 ,  A61K31/7048 ,  A61P31/04

CPC分类号： C07H17/08

摘要： A macrolide compound represented by the formula (I) effective against erythromycin resistant bacteria (for example, resistant pneumococci, streptococci and mycoplasmas).

公开(公告)号：EP2738163B1

公开(公告)日：2016-01-20

申请号：EP12819674.8

申请日：2012-07-27

申请人： Taisho Pharmaceutical Co., Ltd. ,  Toyama Chemical Co., Ltd.

发明人： TANIKAWA, Tetsuya ,  USHIKI, Yasunobu ,  USHIYAMA, Fumihito ,  YAMAGUCHI, Toru ,  ONO, Naoya ,  YAMAMOTO, Keiko ,  TSURUTA, Risa ,  TSUTSUI, Yasuhiro ,  FUJINO, Noritomo ,  MORI, Ayumu

IPC分类号： C07D277/28 ,  A61K31/426 ,  A61K31/427 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61P17/00 ,  A61P31/10 ,  C07D277/20 ,  C07D277/30 ,  C07D277/34 ,  C07D277/48 ,  C07D277/56 ,  C07D285/08 ,  C07D417/04 ,  C07D417/12

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

公开(公告)号：EP2738163A1

公开(公告)日：2014-06-04

申请号：EP12819674.8

申请日：2012-07-27

申请人： Taisho Pharmaceutical Co., Ltd. ,  Toyama Chemical Co., Ltd.

发明人： TANIKAWA, Tetsuya ,  USHIKI, Yasunobu ,  USHIYAMA, Fumihito ,  YAMAGUCHI, Toru ,  ONO, Naoya ,  YAMAMOTO, Keiko ,  TSURUTA, Risa ,  TSUTSUI, Yasuhiro ,  FUJINO, Noritomo ,  MORI, Ayumu

IPC分类号： C07D277/28 ,  A61K31/426 ,  A61K31/427 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61P17/00 ,  A61P31/10 ,  C07D277/20 ,  C07D277/30 ,  C07D277/34 ,  C07D277/48 ,  C07D277/56 ,  C07D285/08 ,  C07D417/04

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 A 1 represents a nitrogen atom or a group represented by formula CR 6 ; A 2 and A 3 are the same as or different from each other and independently represent a nitrogen atom or a group represented by formula CH; R 1 represents an aryl group which may be substituted by 1 to 5 substituents independently selected from a substituent group (2) or the like; R 2 and R 3 are the same as or different from each other and independently represent a hydrogen atom, a halogen atom, a C 1-6 alkyl group, a C 1-6 haloalkyl group or a C 1-6 alkoxy group; and R 4 and R 5 are the same as or different from each other and independently represent a hydrogen atom, a C 1-6 haloalkyl group, a C 1-6 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，可用作药剂。 由式（I）表示的化合物（其中A 1表示氮原子或由式CR 6表示的基团; A 2和A 3彼此相同或不同，并且独立地表示氮原子或由 式CH; R 1表示可以被1至5个独立地选自取代基（2）等取代基的取代基取代的芳基; R 2和R 3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，C 1-6卤代烷基，C 1-6烷基等）或其盐可用作抗真菌剂。

公开(公告)号：EP3173408B1

公开(公告)日：2018-11-21

申请号：EP15825310.4

申请日：2015-07-24

申请人： Taisho Pharmaceutical Co., Ltd.

发明人： KURODA, Shoichi ,  KAWABE, Kenichi ,  USHIKI, Yasunobu ,  OHTA, Hiroshi ,  UNEUCHI, Fumito ,  SHIBATA, Tsuyoshi ,  TABUSE, Hideaki ,  MUNETOMO, Eiji ,  CHONAN, Sumi

IPC分类号： C07D401/10 ,  C07D401/14 ,  C07D403/14 ,  C07D405/10 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  A61K31/4725 ,  A61P1/10 ,  A61P13/12 ,  A61P19/00 ,  A61P43/00

CPC分类号： C07D417/10 ,  A61K31/4725 ,  C07D401/10 ,  C07D401/14 ,  C07D403/14 ,  C07D405/10 ,  C07D413/10 ,  C07D413/14

摘要： The present invention provides a compound represented by the following formula [1] or a pharmaceutically acceptable salt thereof which has an excellent NHE3 inhibitory effect: €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ[Formula 15]€ƒ€ƒ€ƒ€ƒ€ƒA-Y [1] wherein A represents a structure represented by the following formula [2]: wherein R 11 and R 12 each represent a halogen atom or the like, R 2 represents C 1-6 alkyl or the like, ring E represents triazole, tetrazole, pyrimidine, or the like, R 31 and R 32 each represent a hydrogen atom, C 1-6 alkyl, C 1-6 alkoxy, or the like, and W represents a single bond, the formula -NH-, the formula -O-, or the formula -CONH-, and Y represents a hydrogen atom or a structure represented by the following formula [3']:

公开(公告)号：EP3173408A1

公开(公告)日：2017-05-31

申请号：EP15825310.4

申请日：2015-07-24

申请人： Taisho Pharmaceutical Co., Ltd.

发明人： KURODA, Shoichi ,  KAWABE, Kenichi ,  USHIKI, Yasunobu ,  OHTA, Hiroshi ,  UNEUCHI, Fumito ,  SHIBATA, Tsuyoshi ,  TABUSE, Hideaki ,  MUNETOMO, Eiji ,  CHONAN, Sumi

IPC分类号： C07D401/10 ,  A61K31/4725 ,  A61P1/10 ,  A61P43/00 ,  C07D401/14 ,  C07D403/14 ,  C07D405/10 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10

CPC分类号： C07D417/10 ,  A61K31/4725 ,  C07D401/10 ,  C07D401/14 ,  C07D403/14 ,  C07D405/10 ,  C07D413/10 ,  C07D413/14

摘要： The present invention provides a compound represented by the following formula [1] or a pharmaceutically acceptable salt thereof which has an excellent NHE3 inhibitory effect:

        [Formula 15]     A-Y [1]

wherein
A represents a structure represented by the following formula [2]:

wherein
R 11 and R 12 each represent a halogen atom or the like,
R 2 represents C 1-6 alkyl or the like,
ring E represents triazole, tetrazole, pyrimidine, or the like,
R 31 and R 32 each represent a hydrogen atom, C 1-6 alkyl, C 1-6 alkoxy, or the like, and
W represents a single bond, the formula -NH-, the formula -O-, or the formula -CONH-, and

Y represents a hydrogen atom or a structure represented by the following formula [3']:

摘要翻译： 本发明提供由下式[1]表示的化合物或其药学上可接受的盐，其具有优异的NHE3抑制作用：€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ[15式] ƒ€ƒ€ƒA-Y [1]其中A表示由下式[2]表示的结构：其中R 11和R 12各自表示卤素原子等，R 2表示C 1-6烷基 环E表示三唑，四唑，嘧啶等，R 31和R 32各自表示氢原子，C 1-6烷基，C 1-6烷氧基等，W表示单键 ，式-NH-，式-O-或式-CONH-，Y表示氢原子或由下式[3']表示的结构：

公开(公告)号：EP1900732A1

公开(公告)日：2008-03-19

申请号：EP06767173.5

申请日：2006-06-22

申请人： TOYAMA CHEMICAL CO., LTD. ,  TAISHO PHARMACEUTICAL CO., LTD

发明人： KIYOTO, Taro ,  TANAKA, Tadashi ,  TSUTSUI, Yasuhiro ,  ANDO, Junichi ,  MOTONO, Mai ,  KAWAGUCHI, Yasuko ,  NOGUCHI, Toshiya ,  USHIKI, Yasunobu ,  USHIYAMA, Fumihito ,  URABE, Hiroki

IPC分类号： C07D401/06 ,  A61K31/4709 ,  A61K31/496 ,  A61P31/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D491/056

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; R 1 , R 2 , R 3 , R 4 and R 5 independently represent a hydrogen atom, halogen atom, a lower alkyl, aryl, lower alkoxy or monocyclic heterocyclic group which may be substituted or the like; R 6 represents a lower alkyl, aryl, monocyclic heterocyclic, bicyclic heterocyclic or tricyclic heterocyclic group which may be substituted; X 1 represents a lower alkylene group or the like; X 2 represents a lower alkylene, lower alkenylene or lower alkynylene group which may be substituted; X 3 represents an oxygen atom, sulfur atom, a sulfinyl group, sulfonyl group or the like; Y 1 represents a bivalent cyclic group, containing a nitrogen, which may be substituted or the like; and Z 1 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： 一种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; R 1，R 2，R 3，R 4和R 5独立地表示可以被取代的氢原子，卤素原子，低级烷基，芳基，低级烷氧基或单环杂环基等。 R 6表示可以被取代的低级烷基，芳基，单环杂环，双环杂环或三环杂环基; X 1表示低级亚烷基等; X 2表示可以被取代的低级亚烷基，低级亚烯基或低级亚烷基; X 3表示氧原子，硫原子，亚磺酰基，磺酰基等; Y 1表示可以被取代的氮的二价环状基团， Z 1表示氮原子，可被取代的碳原子等，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。