公开(公告)号：US20120322807A1

公开(公告)日：2012-12-20

申请号：US13526283

申请日：2012-06-18

申请人： Kazuo Sekiguchi ,  Takashi Suzuki ,  Yutaka Ohbuchi ,  Mitsuhiro Okuno ,  Naoto Ohi ,  Kenji Ohnishi ,  Masaaki Motoyama ,  Kenji Yoshida ,  Takeshi Kodama ,  Kazuhisa Sugiyama ,  Seiji Akamatsu ,  Kunihiko Kiyono ,  Yasuo Yanagihara ,  Takashi Watanabe ,  Kazuhiko Hayashi ,  Hideo Tanaka ,  Takumi Sumida

发明人： Kazuo Sekiguchi ,  Takashi Suzuki ,  Yutaka Ohbuchi ,  Mitsuhiro Okuno ,  Naoto Ohi ,  Kenji Ohnishi ,  Masaaki Motoyama ,  Kenji Yoshida ,  Takeshi Kodama ,  Kazuhisa Sugiyama ,  Seiji Akamatsu ,  Kunihiko Kiyono ,  Yasuo Yanagihara ,  Takashi Watanabe ,  Kazuhiko Hayashi ,  Hideo Tanaka ,  Takumi Sumida

IPC分类号： A61K31/496 ,  A61P37/08

CPC分类号： C07D401/12 ,  C07D213/38 ,  C07D401/04 ,  C07D405/12 ,  C07D405/14

摘要： 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

摘要翻译： 本发明提供含有由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，其中X1表示氮原子或-CH =，R1表示-Z-R6基团， 其中Z表示-CO-基团，-CH（OH） - 基等，R6表示具有1-4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，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，A表示基团

公开(公告)号：US08263599B2

公开(公告)日：2012-09-11

申请号：US12311500

申请日：2007-10-02

申请人： Kazuo Sekiguchi ,  Takashi Suzuki ,  Yutaka Ohbuchi ,  Mitsuhiro Okuno ,  Naoto Ohi ,  Kenji Ohnishi ,  Masaaki Motoyama ,  Kenji Yoshida ,  Takeshi Kodama ,  Kazuhisa Sugiyama ,  Seiji Akamatsu ,  Kunihiko Kiyono ,  Yasuo Yanagihara ,  Takashi Watanabe ,  Kazuhiko Hayashi ,  Hideo Tanaka ,  Takumi Sumida

发明人： Kazuo Sekiguchi ,  Takashi Suzuki ,  Yutaka Ohbuchi ,  Mitsuhiro Okuno ,  Naoto Ohi ,  Kenji Ohnishi ,  Masaaki Motoyama ,  Kenji Yoshida ,  Takeshi Kodama ,  Kazuhisa Sugiyama ,  Seiji Akamatsu ,  Kunihiko Kiyono ,  Yasuo Yanagihara ,  Takashi Watanabe ,  Kazuhiko Hayashi ,  Hideo Tanaka ,  Takumi Sumida

IPC分类号： A61K31/497

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所示的芳香族化合物或其盐作为活性成分的STAT3 / 5活化抑制剂，其中，X1表示氮原子或-CH =，R1表示-Z-R6基， 其中Z表示-CO-基团，-CH（OH） - 基等，R6表示具有1-4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，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，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。

公开(公告)号：US20100210661A1

公开(公告)日：2010-08-19

申请号：US12311500

申请日：2007-10-02

申请人： Kazuo Sekiguchi ,  Takashi Suzuki ,  Yutaka Ohbuchi ,  Mitsuhiro Okuno ,  Naoto Ohi ,  Kenji Ohnishi ,  Masaaki Motoyama ,  Kenji Yoshida ,  Takeshi Kodama ,  Kazuhisa Sugiyama ,  Seiji Akamatsu ,  Kunihiko Kiyono ,  Yasuo Yanagihara ,  Takashi Watanabe ,  Kazuhiko Hayashi ,  Hideo Tanaka ,  Takumi Sumida

发明人： Kazuo Sekiguchi ,  Takashi Suzuki ,  Yutaka Ohbuchi ,  Mitsuhiro Okuno ,  Naoto Ohi ,  Kenji Ohnishi ,  Masaaki Motoyama ,  Kenji Yoshida ,  Takeshi Kodama ,  Kazuhisa Sugiyama ,  Seiji Akamatsu ,  Kunihiko Kiyono ,  Yasuo Yanagihara ,  Takashi Watanabe ,  Kazuhiko Hayashi ,  Hideo Tanaka ,  Takumi Sumida

IPC分类号： A61K31/496 ,  C07D401/14 ,  C07D405/10 ,  A61P3/04 ,  A61P25/28 ,  A61P3/10

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所示的芳香族化合物或其盐作为活性成分的STAT3 / 5活化抑制剂，其中，X1表示氮原子或-CH =，R1表示-Z-R6基， 其中Z表示-CO-基团，-CH（OH） - 基等，R6表示具有1-4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，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，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。

公开(公告)号：US20120238750A1

公开(公告)日：2012-09-20

申请号：US13409090

申请日：2012-02-29

申请人： Tae FUKUSHIMA ,  Shuji Matsumura ,  Noriaki Takemura ,  Hideaki Satou ,  Nobuaki Ito ,  Takuya Shitsuta ,  Hironori Tsutsui ,  Michinori Tanaka ,  Keizo Kan ,  Hitoshi Nagao ,  Kenji Watanabe ,  Kuninori Tai ,  Takashi Nakagawa ,  Hideki Takasu ,  Makoto Sakamoto ,  Keisuke Miyajima ,  Satoshi Yamada ,  Yutaka Kojima ,  Koichi Yasumura ,  Naoto Ohi ,  Mitsuhiro Okuno ,  Kazuhisa Sugiyama ,  Kunihiko Kiyono ,  Takashi Suzuki ,  Seiji Akamatsu ,  Takeshi Kodama ,  Yasuo Yanagihara ,  Takumi Sumida

发明人： Tae FUKUSHIMA ,  Shuji Matsumura ,  Noriaki Takemura ,  Hideaki Satou ,  Nobuaki Ito ,  Takuya Shitsuta ,  Hironori Tsutsui ,  Michinori Tanaka ,  Keizo Kan ,  Hitoshi Nagao ,  Kenji Watanabe ,  Kuninori Tai ,  Takashi Nakagawa ,  Hideki Takasu ,  Makoto Sakamoto ,  Keisuke Miyajima ,  Satoshi Yamada ,  Yutaka Kojima ,  Koichi Yasumura ,  Naoto Ohi ,  Mitsuhiro Okuno ,  Kazuhisa Sugiyama ,  Kunihiko Kiyono ,  Takashi Suzuki ,  Seiji Akamatsu ,  Takeshi Kodama ,  Yasuo Yanagihara ,  Takumi Sumida

IPC分类号： C07D401/12 ,  C07D413/14 ,  C07D211/46 ,  C07D295/155 ,  C07D405/14

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 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： 本发明的化合物由以下通式（1）表示：[其中X 1表示氮原子或-CH =; R1表示基团-Z-R6，其中Z表示基团-CO-，基团-CH（OH） - 等，R6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。

公开(公告)号：US08188277B2

公开(公告)日：2012-05-29

申请号：US11659689

申请日：2005-08-03

申请人： Tae Fukushima ,  Shuji Matsumura ,  Noriaki Takemura ,  Hideaki Satou ,  Nobuaki Ito ,  Takuya Shitsuta ,  Hironori Tsutsui ,  Michinori Tanaka ,  Keizo Kan ,  Hitoshi Nagao ,  Kenji Watanabe ,  Kuninori Tai ,  Takashi Nakagawa ,  Hideki Takasu ,  Makoto Sakamoto ,  Keisuke Miyajima ,  Satoshi Yamada ,  Yutaka Kojima ,  Koichi Yasumura ,  Naoto Ohi ,  Mitsuhiro Okuno ,  Kazuhisa Sugiyama ,  Kunihiko Kiyono ,  Takashi Suzuki ,  Seiji Akamatsu ,  Takeshi Kodama ,  Yasuo Yanagihara ,  Takumi Sumida

发明人： Tae Fukushima ,  Shuji Matsumura ,  Noriaki Takemura ,  Hideaki Satou ,  Nobuaki Ito ,  Takuya Shitsuta ,  Hironori Tsutsui ,  Michinori Tanaka ,  Keizo Kan ,  Hitoshi Nagao ,  Kenji Watanabe ,  Kuninori Tai ,  Takashi Nakagawa ,  Hideki Takasu ,  Makoto Sakamoto ,  Keisuke Miyajima ,  Satoshi Yamada ,  Yutaka Kojima ,  Koichi Yasumura ,  Naoto Ohi ,  Mitsuhiro Okuno ,  Kazuhisa Sugiyama ,  Kunihiko Kiyono ,  Takashi Suzuki ,  Seiji Akamatsu ,  Takeshi Kodama ,  Yasuo Yanagihara ,  Takumi Sumida

IPC分类号： C07D241/36 ,  C07D413/12 ,  C07D403/12 ,  C07D221/02 ,  C07D401/12 ,  C07D213/62 ,  A61K31/535 ,  A61K31/497 ,  A61K31/445

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，其具有优异的抑制胶原产生的效果和较少的副作用。 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-CH =; R1表示基团-Z-R6，其中Z表示基团-CO-，基团-CH（OH） - 等，R6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。

公开(公告)号：US20070270422A1

公开(公告)日：2007-11-22

申请号：US11659689

申请日：2005-08-03

申请人： Tae Fukushima ,  Shuji Matsumura ,  Noriaki Takemura ,  Hideaki Satou ,  Nobuaki Ito ,  Takuya Shitsuta ,  Hironori Tsutsui ,  Michinori Tanaka ,  Keizo Kan ,  Hitoshi Nagao ,  Kenji Watanabe ,  Kuninori Tai ,  Takashi Nakagawa ,  Hideki Takasu ,  Makoto Sakamoto ,  Keisuke Miyajima ,  Satoshi Yamada ,  Yutaka Kojima ,  Koichi Yasumura ,  Naoto Ohi ,  Mitsuhiro Okuno ,  Kazuhisa Sugiyama ,  Kunihiko Kiyono ,  Takashi Suzuki ,  Seiji Akamatsu ,  Takeshi Kodama ,  Yasuo Yanagihara ,  Takumi Sumida

发明人： Tae Fukushima ,  Shuji Matsumura ,  Noriaki Takemura ,  Hideaki Satou ,  Nobuaki Ito ,  Takuya Shitsuta ,  Hironori Tsutsui ,  Michinori Tanaka ,  Keizo Kan ,  Hitoshi Nagao ,  Kenji Watanabe ,  Kuninori Tai ,  Takashi Nakagawa ,  Hideki Takasu ,  Makoto Sakamoto ,  Keisuke Miyajima ,  Satoshi Yamada ,  Yutaka Kojima ,  Koichi Yasumura ,  Naoto Ohi ,  Mitsuhiro Okuno ,  Kazuhisa Sugiyama ,  Kunihiko Kiyono ,  Takashi Suzuki ,  Seiji Akamatsu ,  Takeshi Kodama ,  Yasuo Yanagihara ,  Takumi Sumida

IPC分类号： C07D401/14 ,  A61K31/165 ,  A61K31/167 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/4523 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5375 ,  A61K31/5377 ,  A61P11/00 ,  C07C233/00 ,  C07C233/92 ,  C07D211/00 ,  C07D211/40 ,  C07D211/56 ,  C07D241/04 ,  C07D413/14 ,  C07D413/02 ,  C07D241/36

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，其具有优异的抑制胶原产生的效果和较少的副作用。 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-ZR 6，其中Z表示-CO-基团，-CH（OH） - 基等基团，R“ 6表示具有1至4个氮原子，氧原子或硫原子的5至15元单环，二环或三环饱和或不饱和杂环基; R 2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R 3表示氢原子，低级烷氧基等，p表示1或2，R 4表示 咪唑基低级烷基等。

公开(公告)号：US08722663B2

公开(公告)日：2014-05-13

申请号：US13318053

申请日：2011-01-28

申请人： Hideki Takasu ,  Shigekazu Fujita ,  Shinya Ohtsuka ,  Toshiyuki Hirose ,  Yosuke Sato ,  Satoshi Yamada ,  Keisuke Miyajima ,  Koji Sakai ,  Yutaka Kojima ,  Kazuo Sekiguchi ,  Yasuo Yanagihara ,  Takashi Suzuki ,  Hideo Tanaka ,  Kazuhisa Sugiyama ,  Mitsuhiro Okuno ,  Takumi Sumida

发明人： Hideki Takasu ,  Shigekazu Fujita ,  Shinya Ohtsuka ,  Toshiyuki Hirose ,  Yosuke Sato ,  Satoshi Yamada ,  Keisuke Miyajima ,  Koji Sakai ,  Yutaka Kojima ,  Kazuo Sekiguchi ,  Yasuo Yanagihara ,  Takashi Suzuki ,  Hideo Tanaka ,  Kazuhisa Sugiyama ,  Mitsuhiro Okuno ,  Takumi Sumida

IPC分类号： A61K31/44 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/443 ,  A61K31/496 ,  A61K31/551 ,  A61K31/553 ,  C07D213/69 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12

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].

摘要翻译： 本发明提供具有优异抗肿瘤效果的新型化合物。 本发明的化合物由以下通式（1）表示，其中R 1和R 2是芳基等; A是低级亚烷基; 环X是任选取代的亚芳基; E是键或低级亚烯基; 环Y是含有一个或多个氮原子的任选取代的杂环亚烷基，其中一个氮原子连接到相邻的羰基上; G是-NH-G2-，-N（低级烷基）-G2-，-NH-CH2-G2-，-N（低级烷基）-CH2-G2-或-CH2-G2-，其中G2与R2结合 ，G2-R2是键-R2，亚苯基-G3-R2，亚苯基-G4-O-R2，亚苯基-G5-NH-R2，亚苯基-G6-N（低级烷基）-R2或喹啉二基-O-R2， 所述含亚苯基的亚苯基任选被一个或多个取代基取代; G3-R2是-O-低级亚烷基-R2等; G4-O-是低级亚烷基-O-等; G5为低级亚烷基; G6为低级亚烷基]。

公开(公告)号：US20120283242A1

公开(公告)日：2012-11-08

申请号：US13318053

申请日：2011-01-28

申请人： Hideki Takasu ,  Shigekazu Fujita ,  Shinya Ohtsuka ,  Toshiyuki Hirose ,  Yosuke Sato ,  Satoshi Yamada ,  Keisuke Miyajima ,  Koji Sakai ,  Yutaka Kojima ,  Kazuo Sekiguchi ,  Yasuo Yanagihara ,  Takashi Suzuki ,  Hideo Tanaka ,  Kazuhisa Sugiyama ,  Mitsuhiro Okuno ,  Takumi Sumida

发明人： Hideki Takasu ,  Shigekazu Fujita ,  Shinya Ohtsuka ,  Toshiyuki Hirose ,  Yosuke Sato ,  Satoshi Yamada ,  Keisuke Miyajima ,  Koji Sakai ,  Yutaka Kojima ,  Kazuo Sekiguchi ,  Yasuo Yanagihara ,  Takashi Suzuki ,  Hideo Tanaka ,  Kazuhisa Sugiyama ,  Mitsuhiro Okuno ,  Takumi Sumida

IPC分类号： A61K31/496 ,  C07D401/14 ,  C07D405/14 ,  A61K31/551 ,  A61P35/00 ,  A61K31/4545 ,  C07D413/14 ,  C07D413/12 ,  A61K31/553 ,  C07D401/12 ,  C07D417/14

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].

摘要翻译： 本发明提供具有优异抗肿瘤效果的新型化合物。 本发明的化合物由以下通式（1）表示，其中R 1和R 2是芳基等; A是低级亚烷基; 环X是任选取代的亚芳基; E是键或低级亚烯基; 环Y是含有一个或多个氮原子的任选取代的杂环亚烷基，其中一个氮原子连接到相邻的羰基上; G是-NH-G2-，-N（低级烷基）-G2-，-NH-CH2-G2-，-N（低级烷基）-CH2-G2-或-CH2-G2-，其中G2与R2结合 ，G2-R2是键-R2，亚苯基-G3-R2，亚苯基-G4-O-R2，亚苯基-G5-NH-R2，亚苯基-G6-N（低级烷基）-R2或喹啉二基-O-R2， 所述含亚苯基的亚苯基任选被一个或多个取代基取代; G3-R2是-O-低级亚烷基-R2等; G4-O-是低级亚烷基-O-等; G5为低级亚烷基; G6为低级亚烷基]。

公开(公告)号：US20210157818A1

公开(公告)日：2021-05-27

申请号：US16951954

申请日：2020-11-18

申请人： Takashi Suzuki

发明人： Takashi Suzuki

IPC分类号： G06F16/25 ,  G06F16/23 ,  H03M7/30

摘要： A computerized method of compressing symbolic information organized into a plurality of documents, each document having a plurality of symbols, includes: (i) automatically identifying a plurality of sequential and non-sequential symbol pairs in an input document; (ii) counting the number of appearances of each unique symbol pair; and (iii) producing a compressed document that includes a replacement symbol at each position associated with one of the plurality of symbol pairs, at least one of which corresponds to a non-sequential symbol pair. For each non-sequential pair the compressed document includes corresponding indicia indicating a distance between locations of the non-sequential symbols of the pair in the input document. In some instances the plurality of symbol pairs includes only those pairs of non-sequential symbols for which the distance between locations of the non-sequential symbols of the pair in the input document is less than a numeric distance cap.

公开(公告)号：US10387377B2

公开(公告)日：2019-08-20

申请号：US15600495

申请日：2017-05-19

申请人： Takashi Suzuki

发明人： Takashi Suzuki

IPC分类号： G06F16/00 ,  G06F16/174 ,  G06F16/22 ,  G06F16/951 ,  H03M7/30

摘要： A computerized method and apparatus compresses symbolic information, such as text. Symbolic information is compressed by recursively identifying pairs of symbols (e.g., pairs of words or characters) and replacing each pair with a respective replacement symbol. The number of times each symbol pair appears in the uncompressed text is counted, and pairs are only replaced if they appear more than a threshold number of times. In recursive passes, each replaced pair can include a previously substituted replacement symbol. The method and apparatus can achieve high compression especially for large datasets. Metadata, such as the number of times each pair appears, generated during compression of the documents can be used to analyze the documents and find similarities between two documents.