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公开(公告)号：EP2528897B9
公开(公告)日：2015-09-09
申请号：EP11705048.4
申请日：2011-01-28
发明人： TAKASU, Hideki , FUJITA, Shigekazu , OHTSUKA, Shinya , HIROSE, Toshiyuki , SATO, Yosuke , YAMADA, Satoshi , MIYAJIMA, Keisuke , SAKAI, Koji , KOJIMA, Yutaka , SEKIGUCHI, Kazuo , YANAGIHARA, Yasuo , SUZUKI, Takashi , TANAKA, Hideo , SUGIYAMA, Kazuhisa , OKUNO, Mitsuhiro , SUMIDA, Takumi
IPC分类号： C07D213/69 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , A61K31/44 , A61K31/4439 , A61K31/4545 , A61K31/4725 , A61K31/443 , A61K31/496 , A61P35/00
CPC分类号： C07D213/69 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12
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公开(公告)号：EP2089373A1
公开(公告)日：2009-08-19
申请号：EP07829383.4
申请日：2007-10-02
发明人： SEKIGUCHI, Kazuo , SUZUKI, Takashi , OHBUCHI, Yutaka , OKUNO, Mitsuhiro , OHI, Naoto , OHNISHI, Kenji , MOTOYAMA, Masaaki , YOSHIDA, Kenji , KODAMA, Takeshi , SUGIYAMA, Kazuhisa , AKAMATSU, Seiji , KIYONO, Kunihiko , YANAGIHARA, Yasuo , WATANABE, Takashi , HAYASHI, Kazuhiko , TANAKA, Hideo , SUMIDA, Takumi
IPC分类号： C07D317/58 , C07D405/12
CPC分类号： C07D401/12 , C07D213/38 , C07D401/04 , C07D405/12 , C07D405/14
摘要： An object of the present invention is to provide a STAT3/5 activation inhibitor. The present invention provides a STAT3/5 activation inhibitor containing an aromatic compound represented by the general formula or a salt thereof as an active ingredient: wherein X1 represents a nitrogen atom or a group -CH=, R1 represents a group -Z-R6, in which Z represents a group -CO-, a group -CH(OH)- or the like, R6 represents a 5-to 15-membered monocyclic, dicyclic or tricyclic saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms, R2 represents a hydrogen atom or a halogen atom, Y represents a group -O-, a group -CO-, a group -CH(OH)-or a lower alkylene group, and A represents a group wherein R3 represents a hydrogen atom, a lower alkoxy group or the like, p represents 1 or 2, R4 represents an imidazolyl lower alkyl group or the like.
摘要翻译： 本发明的目的是提供一种STAT3 / 5激活抑制剂。 本发明提供含有通式表示的芳香族化合物或其盐作为有效成分的STAT3 / 5活化抑制剂，式中，X1表示氮原子或基团-CH =，R1表示基团-Z-R6， 其中Z表示基团-CO-，基团-CH（OH） - 等，R 6表示具有1至4个氮原子的5至15元单环，二环或三环饱和或不饱和杂环基团，氧原子 或硫原子，R 2表示氢原子或卤素原子，Y表示基团-O-，基团-CO-，基团-CH（OH） - 或低级亚烷基，并且A表示其中R 3表示 氢原子，低级烷氧基等，p表示1或2，R4表示咪唑基低级烷基等。
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公开(公告)号：EP1019501A1
公开(公告)日：2000-07-19
申请号：EP98907199.8
申请日：1998-03-12
发明人： YAMADA, Satoshi , KINOSHITA, Naosumi , YASUMURA, Koichi , EDAMATSU, Koji , NAGAHAMA, Takao , ISHIKAWA, Shintaro , YAMAUCHI, Takeshi , KISHI, Kazumasa , SUGIYAMA, Kazuhisa
IPC分类号： C12N15/12
CPC分类号： C07D487/04
摘要： The present invention provides a novel pyrimidine derivative represented by general formula (1), wherein R, R?4 and R8¿ are the same as defined in the specification, or pharmaceutically acceptable salt thereof, which possesses an excellent activity for inhibiting the formation of NO (nitrogen oxide) in vivo.
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4.发明公开
公开(公告)号：EP0638075A1
公开(公告)日：1995-02-15
申请号：EP94907081.0
申请日：1994-02-21
发明人： YASUMURA, Koichi , MIYAJIMA, Keisuke , NAGAHAMA, Takao , ISHIKAWA, Shintaro , NAKAGAWA Yuko , SUGIYAMA, Kazuhisa
IPC分类号： C07D233 , A61K31 , A61P3 , A61P43 , C07D277 , C07D401 , C07D403 , C07D409 , C07D417 , C07D487
CPC分类号： C07D403/06 , C07D233/88 , C07D277/50 , C07D277/54 , C07D277/82 , C07D409/12 , C07D417/04 , C07D417/06 , C07D417/12 , C07D487/04
摘要： A compound represented by formula (I) is disclosed, wherein the all symbols are defined in the disclosure. A process for producing the compound, and a method for treating diseases caused by a Maillard reaction in living body using the compound are also disclosed.
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公开(公告)号：EP2528897B1
公开(公告)日：2014-10-15
申请号：EP11705048.4
申请日：2011-01-28
发明人： TAKASU, Hideki , FUJITA, Shigekazu , OHTSUKA, Shinya , HIROSE, Toshiyuki , SATO, Yosuke , YAMADA, Satoshi , MIYAJIMA, Keisuke , SAKAI, Koji , KOJIMA, Yutaka , SEKIGUCHI, Kazuo , YANAGIHARA, Yasuo , SUZUKI, Takashi , TANAKA, Hideo , SUGIYAMA, Kazuhisa , OKUNO, Mitsuhiro , SUMIDA, Takumi
IPC分类号： C07D213/69 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , A61K31/44 , A61K31/4439 , A61K31/4545 , A61K31/4725 , A61K31/443 , A61K31/496 , A61P35/00
CPC分类号： C07D213/69 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12
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公开(公告)号：EP2528897A1
公开(公告)日：2012-12-05
申请号：EP11705048.4
申请日：2011-01-28
发明人： TAKASU, Hideki , FUJITA, Shigekazu , OHTSUKA, Shinya , HIROSE, Toshiyuki , SATO, Yosuke , YAMADA, Satoshi , MIYAJIMA, Keisuke , SAKAI, Koji , KOJIMA, Yutaka , SEKIGUCHI, Kazuo , YANAGIHARA, Yasuo , SUZUKI, Takashi , TANAKA, Hideo , SUGIYAMA, Kazuhisa , OKUNO, Mitsuhiro , SUMIDA, Takumi
IPC分类号： C07D213/69 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , A61K31/44 , A61K31/4439 , A61K31/4545 , A61K31/4725 , A61K31/443 , A61K31/496 , A61P35/00
CPC分类号： C07D213/69 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： The present invention provides a novel compound having an excellent antitumor effect. The compound of the present invention is represented by the following general formula (1) wherein R1 and R2 are aryl or the like; A is lower alkylene; Ring X is optionally substituted arylene; E is bond or lower alkenylene; Ring Y is optionally substituted heterocycloalkylene containing one or more nitrogen atoms, one of which is attached to the adjacent carbonyl group; G is —NH-G2-, —N(lower alkyl)-G2-, —NH—CH2-G2-, —N(lower alkyl)-CH2-G2- or —CH2-G2-, [wherein G2 binds to R2, G2-R2 is bond-R2, phenylene-G3-R2, phenylene-G4-O—R2, phenylene-G5-NH—R2, phenylene-G6-N(lower alkyl)-R2 or quinolinediyl-O—R2, the phenylene of said phenylene-containing groups being optionally substituted with one or more substituents; G3-R2 is —O-lower alkylene-R2 or the like; G4-O— is lower alkylene-O— or the like; G5 is lower alkylene; G6 is lower alkylene].
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公开(公告)号：EP1773797A2
公开(公告)日：2007-04-18
申请号：EP05780290.2
申请日：2005-08-03
发明人： FUKUSHIMA, Tae , MATSUMURA, Shuji, La Soreado 201 , TAKEMURA, Noriaki , SATOU, Hideaki , ITO, Nobuaki , SHITSUTA, Takuya , TSUTSUI, Hironori , TANAKA, Michinori , KAN, Keizo , NAGAO, Hitoshi , WATANABE, Kenji , TAI, Kuninori , NAKAGAWA, Takashi , TAKASU, Hideki , SAKAMOTO, Makoto , MIYAJIMA, Keisuke , YAMADA, Satoshi , KOJIMA, Yutaka , YASUMURA, Koichi , OHI, Naoto , OKUNO, Mitsuhiro , SUGIYAMA, Kazuhisa , KIYONO, Kunihiko , SUZUKI, Takashi , AKAMATSU, Seiji , KODAMA, Takeshi , YANAGIHARA, Yasuo , SUMIDA, Takumi
IPC分类号： C07D295/192 , C07D317/58 , C07D211/46 , C07D211/58 , C07D213/75
CPC分类号： C07C229/18 , C07C205/38 , C07C217/90 , C07C233/45 , C07C233/75 , C07C271/58 , C07C275/34 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07D211/46 , C07D211/58 , C07D211/62 , C07D211/70 , C07D213/75 , C07D239/42 , C07D241/20 , C07D295/185 , C07D295/192 , C07D317/58 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention provides a novel compound, which has an excellent effect of suppressing the generation of collagen and less side effects, with being excellent in terms of safety. The compound of the present invention is represented by the following general formula (1): [wherein X1 represents a nitrogen atom or a group -CH=; R1 represents a group -Z-R6, wherein Z represents a group -CO-, a group -CH(OH)-, or the like, and R6 represents a 5- to 15-membered monocyclic, dicyclic, or tricyclic, saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms, or sulfur atoms; R2 represents a hydrogen atom, a halogen atom or a lower alkylene group; Y represents a group -O-, a group -CO-, a group -CH(OH)-, a lower alkylene group, or the like; and (A) represents a group or the like, wherein R3 represents a hydrogen atom, a lower alkoxy group, or the like, p represents 1 or 2, and R4 represents an imidazolyl lower alkyl group or the like.
摘要翻译： 本发明提供了一种新颖的化合物，其在安全性方面优异，具有抑制胶原产生和副作用小的优异效果。 本发明的化合物由以下通式（1）表示：[其中X 1表示氮原子或基团-CH =; R 1表示基团-Z-R 6，其中Z表示-CO-基团，基团-CH（OH） - 等，R 6表示5至15元单环，双环或三环饱和或 具有1-4个氮原子的不饱和杂环基，氧原子或硫原子; R2表示氢原子，卤素原子或低级亚烷基; Y表示基团-O-，基团-CO-，基团-CH（OH） - ，低级亚烷基基团等; A表示基团等，其中R3表示氢原子，低级烷氧基等，p表示1或2，R4表示咪唑基低级烷基等。
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公开(公告)号：EP0638075B1
公开(公告)日：2002-01-16
申请号：EP94907081.7
申请日：1994-02-21
发明人： YASUMURA, Koichi , MIYAJIMA, Keisuke , NAGAHAMA, Takao , ISHIKAWA, Shintaro , NAKAGAWA Yuko , SUGIYAMA, Kazuhisa
IPC分类号： C07D277/54 , C07D233/88 , A61K31/425 , A61K31/415 , C07D277/50 , C07D233/96 , C07D277/82 , C07D417/12 , C07D417/04 , C07D487/04
CPC分类号： C07D403/06 , C07D233/88 , C07D277/50 , C07D277/54 , C07D277/82 , C07D409/12 , C07D417/04 , C07D417/06 , C07D417/12 , C07D487/04
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