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：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：US08551999B2

公开(公告)日：2013-10-08

申请号：US12740684

申请日：2008-10-29

申请人： Takumi Sumida ,  Fujio Tabusa ,  Kazuo Sekiguchi ,  Takeshi Kodama ,  Koichi Yasumura ,  Yutaka Kojima ,  Masaaki Motoyama ,  Keisuke Miyajima ,  Kenji Yoshida ,  Keizo Kan ,  Makoto Sakamoto ,  Hideki Takasu ,  Takashi Nakagawa ,  Naoto Ohi ,  Yasuo Harada ,  Norikazu Hashimoto ,  Hironori Matsuyama ,  Masatoshi Iida ,  Shigekazu Fujita ,  Tae Fukushima

发明人： Takumi Sumida ,  Fujio Tabusa ,  Kazuo Sekiguchi ,  Takeshi Kodama ,  Koichi Yasumura ,  Yutaka Kojima ,  Masaaki Motoyama ,  Keisuke Miyajima ,  Kenji Yoshida ,  Keizo Kan ,  Makoto Sakamoto ,  Hideki Takasu ,  Takashi Nakagawa ,  Naoto Ohi ,  Yasuo Harada ,  Norikazu Hashimoto ,  Hironori Matsuyama ,  Masatoshi Iida ,  Shigekazu Fujita ,  Tae Fukushima

IPC分类号： A61K31/496 ,  A61K31/454 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D417/14 ,  A61K31/506 ,  C07D403/12

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.

摘要翻译： 本发明提供由通式（1）表示的杂环化合物：其中R1为R5-Z1-基团等，Z1为低级亚烷基等，R5为通式所示的基团。 其中R 13为氢原子等，m为1至5的整数; R2是氢原子：Y是CH或N：A1是选自吲哚二基的杂环，其中杂环可以具有至少一个取代基：T是-CO-等：R3是 氢原子等：R4是任选被一个或多个羟基取代的低级烷基等：R 3和R 4与它们所键合的氮原子一起可以彼此结合形成5- 10元饱和杂环，其中杂环可以具有至少一个取代基。 本发明的杂环化合物具有抑制胶原蛋白的生成和/或治疗肿瘤的优异效果。

公开(公告)号：US20100261720A1

公开(公告)日：2010-10-14

申请号：US12740684

申请日：2008-10-29

申请人： Takumi Sumida ,  Fujio Tabusa ,  Kazuo Sekiguchi ,  Takeshi Kodama ,  Koichi Yasumura ,  Yutaka Kojima ,  Masaaki Motoyama ,  Keisuke Miyajima ,  Kenji Yoshida ,  Keizo Kan ,  Makoto Sakamoto ,  Hideki Takasu ,  Takashi Nakagawa ,  Naoto Ohi ,  Yasuo Harada ,  Norikazu Hashimoto ,  Hironori Matsuyama ,  Masatoshi Iida ,  Shigekazu Fujita ,  Tae Fukushima

发明人： Takumi Sumida ,  Fujio Tabusa ,  Kazuo Sekiguchi ,  Takeshi Kodama ,  Koichi Yasumura ,  Yutaka Kojima ,  Masaaki Motoyama ,  Keisuke Miyajima ,  Kenji Yoshida ,  Keizo Kan ,  Makoto Sakamoto ,  Hideki Takasu ,  Takashi Nakagawa ,  Naoto Ohi ,  Yasuo Harada ,  Norikazu Hashimoto ,  Hironori Matsuyama ,  Masatoshi Iida ,  Shigekazu Fujita ,  Tae Fukushima

IPC分类号： A61K31/5377 ,  C07D401/14 ,  C07D413/14 ,  A61K31/497 ,  C07D403/14 ,  A61P35/00 ,  A61P43/00

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.

摘要翻译： 本发明提供由通式（1）表示的杂环化合物：其中R1为R5-Z1-基团等，Z1为低级亚烷基等，R5为通式所示的基团。 其中R 13为氢原子等，m为1至5的整数; R2是氢原子：Y是CH或N：A1是选自吲哚二基的杂环，其中杂环可以具有至少一个取代基：T是-CO-等：R3是 氢原子等：R4是任选被一个或多个羟基取代的低级烷基等：R 3和R 4与它们所键合的氮原子一起可以彼此结合形成5- 10元饱和杂环，其中杂环可以具有至少一个取代基。 本发明的杂环化合物具有抑制胶原蛋白的生成和/或治疗肿瘤的优异效果。

公开(公告)号：US20100004438A1

公开(公告)日：2010-01-07

申请号：US12095930

申请日：2006-12-04

申请人： Hironori Matsuyama ,  Kenji Ohnishi ,  Takashi Nakagawa ,  Hideki Takasu ,  Makoto Sakamoto ,  Kumi Higuchi ,  Keisuke Miyajima ,  Satoshi Yamada ,  Masaaki Motoyama ,  Yutaka Kojima ,  Koichi Yasumura ,  Takeshi Kodama ,  Shun Otsuji ,  Keizo Kan ,  Takumi Sumida

发明人： Hironori Matsuyama ,  Kenji Ohnishi ,  Takashi Nakagawa ,  Hideki Takasu ,  Makoto Sakamoto ,  Kumi Higuchi ,  Keisuke Miyajima ,  Satoshi Yamada ,  Masaaki Motoyama ,  Yutaka Kojima ,  Koichi Yasumura ,  Takeshi Kodama ,  Shun Otsuji ,  Keizo Kan ,  Takumi Sumida

IPC分类号： C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D401/12 ,  C07D295/155 ,  C07D211/56 ,  C07D213/72

CPC分类号： A61K31/496 ,  A61K31/495

摘要： An object of the present invention is to provide a medicinal drug much improved in anti tumor activity and excellent in safety. According to the present invention, there is provided a medicinal drug containing a compound represented by the following general formula (1) or a salt thereof as an active ingredient: [Formula 1] 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 [Formula 2] 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： 本发明的目的在于提供一种抗肿瘤活性大大提高的安全性药物。 根据本发明，提供含有下述通式（1）表示的化合物或其盐作为有效成分的药物：[式1]其中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，R6表示5至15元单环，二环或三环饱和或不饱和杂环基 具有1至4个氮原子，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[式2]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：US08236826B2

公开(公告)日：2012-08-07

申请号：US12095930

申请日：2006-12-04

申请人： Hironori Matsuyama ,  Kenji Ohnishi ,  Takashi Nakagawa ,  Hideki Takasu ,  Makoto Sakamoto ,  Kumi Higuchi ,  Keisuke Miyajima ,  Satoshi Yamada ,  Masaaki Motoyama ,  Yutaka Kojima ,  Koichi Yasumura ,  Takeshi Kodama ,  Shun Otsuji ,  Keizo Kan ,  Takumi Sumida

发明人： Hironori Matsuyama ,  Kenji Ohnishi ,  Takashi Nakagawa ,  Hideki Takasu ,  Makoto Sakamoto ,  Kumi Higuchi ,  Keisuke Miyajima ,  Satoshi Yamada ,  Masaaki Motoyama ,  Yutaka Kojima ,  Koichi Yasumura ,  Takeshi Kodama ,  Shun Otsuji ,  Keizo Kan ,  Takumi Sumida

IPC分类号： A61K31/44

CPC分类号： A61K31/496 ,  A61K31/495

摘要： An object of the present invention is to provide a medicinal drug much improved in anti tumor activity and excellent in safety. According to the present invention, there is provided a medicinal drug containing a compound represented by the following general formula (1) or a salt thereof as an active ingredient: [Formula 1] 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 [Formula 2] 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： 本发明的目的在于提供一种抗肿瘤活性大大提高的安全性药物。 根据本发明，提供了含有下述通式（1）表示的化合物或其盐作为有效成分的药物：[式1]其中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，R6表示5至15元单环，二环或三环饱和或不饱和杂环基 具有1至4个氮原子，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[式2]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：US20050239319A1

公开(公告)日：2005-10-27

申请号：US11115508

申请日：2005-04-27

申请人： Hideki Takasu

发明人： Hideki Takasu

IPC分类号： H01R4/18 ,  H01R9/05 ,  H01R103/00 ,  H01R4/24

CPC分类号： H01R24/44 ,  H01R4/184 ,  H01R9/0518 ,  H01R2103/00

摘要： A coaxial connector, in which control of impedance is facilitated, and in which fluctuations in impedance are extremely small. The coaxial connector includes an inner contact, having a crimp connection portion which is crimped onto an inner conductor of a coaxial cable, an outer contact, which is crimped onto an outer conductor of the coaxial cable and an insulator (dielectric), which is provided between the inner contact and the outer contract. Concavities are formed in the outer surface of the dielectric at positions corresponding to the crimp connection portion of the inner contact The concavities control the characteristic impedance of the coaxial connector.

摘要翻译： 一种同轴连接器，其中阻抗的控制被促进，并且其中阻抗的波动非常小。 同轴连接器包括内接触件，其具有压接在同轴电缆的内导体上的压接连接部分，压接在同轴电缆的外导体上的外触点和绝缘体（电介质） 内部接触和外部合同之间。 在电介质的外表面形成凹部，该位置对应于内触头的压接连接部分。凹部控制同轴连接器的特性阻抗。