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公开(公告)号：EP2207773B1
公开(公告)日：2012-07-11
申请号：EP08845000.2
申请日：2008-10-29
发明人： SUMIDA, Takumi , TABUSA, Fujio , SEKIGUCHI, Kazuo , KODAMA, Takeshi , YASUMURA, Koichi , KOJIMA, Yutaka , MOTOYAMA, Masaaki , MIYAJIMA, Keisuke , YOSHIDA, Kenji , KAN, Keizo , SAKAMOTO, Makoto , TAKASU, Hideki , NAKAGAWA, Takashi , OHI, Naoto , HARADA, Yasuo , HASHIMOTO, Norikazu , MATSUYAMA, Hironori , IIDA, Masatoshi , FUJITA, Shigekazu , FUKUSHIMA, Tae
IPC分类号： C07D401/12 , C07D403/12 , A61K31/444 , A61K31/506 , A61P1/16
CPC分类号： C07D401/12 , C07D403/12
摘要： The present invention provides a heterocyclic compound represented by General Formula (1): wherein R1 is a group R5-Z1-, etc., Z1 is a lower alkylene group, etc., and R5 is a group represented by General Formula; wherein R13 is a hydrogen atom, etc., m is an integer from 1 to 5; R2 is a hydrogen atom: Y is CH or N: A1 is a heterocyclic ring selected from the group consisting of indolediyl groups, wherein the heterocyclic ring may have at least one substituent: T is a group -CO-, etc.: R3 is a hydrogen atom, etc.: R4 is a lower alkyl group optionally substituted by one or more hydroxy groups, etc.: R3 and R4, together with the nitrogen atom to which they bind, may bind to each other and form a 5- to 10-membered saturated heterocyclic ring, wherein the heterocyclic ring may have at least one substituent. The heterocyclic compound of the present invention has excellent effects of suppressing the production of collagen and/or treating tumors.
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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：EP2207773A2
公开(公告)日：2010-07-21
申请号：EP08845000.2
申请日：2008-10-29
发明人： SUMIDA, Takumi , TABUSA, Fujio , SEKIGUCHI, Kazuo , KODAMA, Takeshi , YASUMURA, Koichi , KOJIMA, Yutaka , MOTOYAMA, Masaaki , MIYAJIMA, Keisuke , YOSHIDA, Kenji , KAN, Keizo , SAKAMOTO, Makoto , TAKASU, Hideki , NAKAGAWA, Takashi , OHI, Naoto , HARADA, Yasuo , HASHIMOTO, Norikazu , MATSUYAMA, Hironori , IIDA, Masatoshi , FUJITA, Shigekazu , FUKUSHIMA, Tae
IPC分类号： C07D401/12 , C07D403/12 , A61K31/444 , A61K31/506 , A61P1/16
CPC分类号： C07D401/12 , C07D403/12
摘要： The present invention provides a heterocyclic compound represented by General Formula (1): wherein R1 is a group R5-Z1-, etc., Z1 is a lower alkylene group, etc., and R5 is a group represented by General Formula; wherein R13 is a hydrogen atom, etc., m is an integer from 1 to 5; R2 is a hydrogen atom: Y is CH or N: A1 is a heterocyclic ring selected from the group consisting of indolediyl groups, wherein the heterocyclic ring may have at least one substituent: T is a group -CO-, etc.: R3 is a hydrogen atom, etc.: R4 is a lower alkyl group optionally substituted by one or more hydroxy groups, etc.: R3 and R4, together with the nitrogen atom to which they bind, may bind to each other and form a 5- to 10-membered saturated heterocyclic ring, wherein the heterocyclic ring may have at least one substituent. The heterocyclic compound of the present invention has excellent effects of suppressing the production of collagen and/or treating tumors.
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