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公开(公告)号：EP2562155B1
公开(公告)日：2019-06-05
申请号：EP11772045.8
申请日：2011-04-20
发明人： TAKASHIMA, Hajime , TSURUTA, Risa , YABUUCHI, Tetsuya , OKA, Yusuke , URABE, Hiroki , SUGA, Yoichiro , TAKAHASHI, Masato , UNEUCHI, Fumito , KOTSUBO, Hironori , SHOJI, Muneo , KAWAGUCHI, Yasuko
IPC分类号： C07C259/06 , A61K31/166 , A61K31/337 , A61K31/341 , A61K31/343 , A61K31/351 , A61K31/357 , A61K31/36 , A61K31/381 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/402 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/4045 , A61K31/407 , A61K31/415 , A61K31/416
CPC分类号： C07C233/83 , C07C235/84 , C07C237/36 , C07C259/06 , C07C271/22 , C07C271/28 , C07C309/30 , C07C311/08 , C07C317/28 , C07C317/44 , C07C323/41 , C07C323/62 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/08 , C07D205/04 , C07D205/12 , C07D207/10 , C07D207/12 , C07D207/27 , C07D207/327 , C07D209/08 , C07D209/12 , C07D209/14 , C07D209/44 , C07D209/52 , C07D211/14 , C07D211/18 , C07D211/38 , C07D211/46 , C07D211/56 , C07D211/70 , C07D213/38 , C07D213/40 , C07D213/54 , C07D213/61 , C07D213/64 , C07D213/65 , C07D213/70 , C07D213/74 , C07D213/81 , C07D215/14 , C07D217/04 , C07D217/12 , C07D231/12 , C07D231/56 , C07D233/61 , C07D235/04 , C07D257/04 , C07D261/08 , C07D263/14 , C07D263/32 , C07D263/56 , C07D265/30 , C07D265/36 , C07D265/38 , C07D267/10 , C07D271/12 , C07D277/20 , C07D277/30 , C07D277/62 , C07D277/66 , C07D285/12 , C07D295/08 , C07D295/12 , C07D295/14 , C07D295/16 , C07D305/06 , C07D305/08 , C07D307/14 , C07D307/18 , C07D307/52 , C07D307/54 , C07D307/78 , C07D307/81 , C07D307/82 , C07D307/87 , C07D309/04 , C07D309/14 , C07D317/30 , C07D317/60 , C07D319/18 , C07D319/20 , C07D333/24 , C07D405/06 , C07D413/06 , C07D471/04 , C07D471/10 , C07D487/08 , C07D491/20 , C07D498/04 , C07D498/08 , C07F9/091
摘要： Provided is a novel compound which is useful as a pharmaceutical composition by inhibiting an LpxC activity, thereby exhibiting potent antimicrobial activity against gram-negative bacteria including Pseudomonas aeruginosa and its drug resistant bacteria. Provided is a hydroxamic acid derivative represented by the following general formula [1] or a pharmaceutically acceptable salt thereof:
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公开(公告)号：EP2562155B8
公开(公告)日：2019-07-17
申请号：EP11772045.8
申请日：2011-04-20
发明人： TAKASHIMA, Hajime , TSURUTA, Risa , YABUUCHI, Tetsuya , OKA, Yusuke , URABE, Hiroki , SUGA, Yoichiro , TAKAHASHI, Masato , UNEUCHI, Fumito , KOTSUBO, Hironori , SHOJI, Muneo , KAWAGUCHI, Yasuko
IPC分类号： C07C259/06 , A61K31/166 , A61K31/337 , A61K31/341 , A61K31/343 , A61K31/351 , A61K31/357 , A61K31/36 , A61K31/381 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/402 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/4045 , A61K31/407 , A61K31/415 , A61K31/416
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公开(公告)号：EP2562155A1
公开(公告)日：2013-02-27
申请号：EP11772045.8
申请日：2011-04-20
发明人： TAKASHIMA, Hajime , TSURUTA, Risa , YABUUCHI, Tetsuya , OKA, Yusuke , URABE, Hiroki , SUGA, Yoichiro , TAKAHASHI, Masato , UNEUCHI, Fumito , KOTSUBO, Hironori , SHOJI, Muneo , KAWAGUCHI, Yasuko
IPC分类号： C07C259/06 , A61K31/166 , A61K31/337 , A61K31/341 , A61K31/343 , A61K31/351 , A61K31/357 , A61K31/36 , A61K31/381 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/402 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/4045 , A61K31/407 , A61K31/415 , A61K31/416
CPC分类号： C07C233/83 , C07C235/84 , C07C237/36 , C07C259/06 , C07C271/22 , C07C271/28 , C07C309/30 , C07C311/08 , C07C317/28 , C07C317/44 , C07C323/41 , C07C323/62 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/08 , C07D205/04 , C07D205/12 , C07D207/10 , C07D207/12 , C07D207/27 , C07D207/327 , C07D209/08 , C07D209/12 , C07D209/14 , C07D209/44 , C07D209/52 , C07D211/14 , C07D211/18 , C07D211/38 , C07D211/46 , C07D211/56 , C07D211/70 , C07D213/38 , C07D213/40 , C07D213/54 , C07D213/61 , C07D213/64 , C07D213/65 , C07D213/70 , C07D213/74 , C07D213/81 , C07D215/14 , C07D217/04 , C07D217/12 , C07D231/12 , C07D231/56 , C07D233/61 , C07D235/04 , C07D257/04 , C07D261/08 , C07D263/14 , C07D263/32 , C07D263/56 , C07D265/30 , C07D265/36 , C07D265/38 , C07D267/10 , C07D271/12 , C07D277/20 , C07D277/30 , C07D277/62 , C07D277/66 , C07D285/12 , C07D295/08 , C07D295/12 , C07D295/14 , C07D295/16 , C07D305/06 , C07D305/08 , C07D307/14 , C07D307/18 , C07D307/52 , C07D307/54 , C07D307/78 , C07D307/81 , C07D307/82 , C07D307/87 , C07D309/04 , C07D309/14 , C07D317/30 , C07D317/60 , C07D319/18 , C07D319/20 , C07D333/24 , C07D405/06 , C07D413/06 , C07D471/04 , C07D471/10 , C07D487/08 , C07D491/20 , C07D498/04 , C07D498/08 , C07F9/091
摘要： Provided is a novel compound which is useful as a pharmaceutical composition by inhibiting an LpxC activity, thereby exhibiting potent antimicrobial activity against gram-negative bacteria including Pseudomonas aeruginosa and its drug resistant bacteria. Provided is a hydroxamic acid derivative represented by the following general formula [1] or a pharmaceutically acceptable salt thereof:
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公开(公告)号：EP4008405A1
公开(公告)日：2022-06-08
申请号：EP20847275.3
申请日：2020-07-29
发明人： KURODA, Shoichi , KOBAYASHI, Yuki , HATANAKA, Kanako , ITO, Yuji , UNEUCHI, Fumito , UEHARA, Yuko
IPC分类号： A61P43/00 , C07C275/18 , C07C275/26 , C07C307/06 , C07C311/51 , C07C317/32 , C07D207/16 , C07D211/26 , C07D211/66 , C07D235/08 , C07D257/04 , C07D305/08 , C07D309/14 , C07D319/18 , C07D335/02 , C07D471/04 , A61P17/00 , C07D209/08 , C07D209/14 , C07D209/44 , C07D213/40
摘要： The present invention provides a compound represented by formula [I] having an LPA1 receptor-antagonizing action, or a pharmaceutically acceptable salt thereof.
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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
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']:
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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
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：
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