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：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：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：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：US09505866B2

公开(公告)日：2016-11-29

申请号：US14003153

申请日：2012-03-23

申请人： Kazuhiko Maeda ,  Takahiro Nakamura ,  Hironori Matsuyama

发明人： Kazuhiko Maeda ,  Takahiro Nakamura ,  Hironori Matsuyama

IPC分类号： C08L51/04 ,  C08F265/04 ,  C08L51/00

CPC分类号： C08F265/04 ,  C08L51/003 ,  C08L51/04 ,  C08L2205/02 ,  C08F212/08 ,  C08F220/44

摘要： An acrylic rubber graft copolymer is obtained by graft polymerizing a vinyl monomer in the presence of a rubbery polymer including acrylate ester monomer units and polyfunctional monomer units, wherein the total amount of the polyfunctional monomer units in the rubbery polymer is 0.3 to 3 parts by mass with respect to 100 parts by mass of the acrylate ester monomer units, and the polyfunctional monomer units include 30 to 95 mass % of polyfunctional monomer units having two unsaturated bonds and 5 to 70 mass % of polyfunctional monomer units having three unsaturated bonds with respect to 100 mass % of the total of the polyfunctional monomer units. A thermoplastic resin composition includes the acrylic rubber graft copolymer.

摘要翻译： 通过在包含丙烯酸酯单体单元和多官能单体单元的橡胶状聚合物存在下将乙烯基单体接枝聚合而得到丙烯酸系橡胶接枝共聚物，其中，橡胶状聚合物中的多官能单体单元的总量为0.3〜3质量份 相对于100质量份的丙烯酸酯单体单元，多官能单体单元包含30〜95质量％的具有2个不饱和键的多官能单体单元和5〜70质量％的具有3个不饱和键的多官能单体单元相对于 100质量％的多官能单体单元。 热塑性树脂组合物包括丙烯酸橡胶接枝共聚物。

公开(公告)号：US20130345362A1

公开(公告)日：2013-12-26

申请号：US14003153

申请日：2012-03-23

申请人： Kazuhiko Maeda ,  Takahiro Nakamura ,  Hironori Matsuyama

发明人： Kazuhiko Maeda ,  Takahiro Nakamura ,  Hironori Matsuyama

IPC分类号： C08F265/04 ,  C08L51/04

CPC分类号： C08F265/04 ,  C08L51/003 ,  C08L51/04 ,  C08L2205/02 ,  C08F212/08 ,  C08F220/44

摘要： [Object] To provide acrylic rubber graft copolymers capable of giving thermoplastic resin compositions exhibiting excellent impact resistance, rigidity and appearance, and to provide thermoplastic resin compositions including the acrylic rubber graft copolymers.[Solution] An acrylic rubber graft copolymer is obtained by graft polymerizing a vinyl monomer in the presence of a rubbery polymer including acrylate ester monomer units and polyfunctional monomer units, wherein the total amount of the polyfunctional monomer units in the rubbery polymer is 0.3 to 3 parts by mass with respect to 100 parts by mass of the acrylate ester monomer units, and the polyfunctional monomer units include 30 to 95 mass % of polyfunctional monomer units having two unsaturated bonds and 5 to 70 mass % of polyfunctional monomer units having three unsaturated bonds with respect to 100 mass % of the total of the polyfunctional monomer units. A thermoplastic resin composition includes the acrylic rubber graft copolymer.

摘要翻译： 提供能够提供耐冲击性，刚性和外观优异的热塑性树脂组合物的丙烯酸橡胶接枝共聚物，以及提供包含丙烯酸橡胶接枝共聚物的热塑性树脂组合物。 [溶液]丙烯酸橡胶接枝共聚物通过在包含丙烯酸酯单体单元和多官能单体单元的橡胶状聚合物存在下将乙烯基单体接枝聚合而获得，其中橡胶状聚合物中多官能单体单元的总量为0.3〜3 相对于100质量份丙烯酸酯单体单元为质量份，多官能单体单元包含30〜95质量％的具有2个不饱和键的多官能单体单元和5〜70质量％的具有3个不饱和键的多官能单体单元 相对于多官能单体单元的100质量％。 热塑性树脂组合物包括丙烯酸橡胶接枝共聚物。