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公开(公告)号：US5422360A
公开(公告)日：1995-06-06
申请号：US95994
申请日：1993-07-23
IPC分类号： C07D233/88 , C07D233/96 , C07D277/20 , C07D277/54 , C07D487/04 , C07D513/04 , A61K31/415 , C07D233/70
CPC分类号： C07D277/20 , C07D233/88 , C07D233/96 , C07D277/54 , C07D487/04 , C07D513/04
摘要： A novel Maillard reaction inhibitor containing at least one compound represented by formula (1) and the salts thereof; methods for producing the compounds of formula (1) and the salts thereof; a composition for inhibiting the Maillard reaction in living body comprising at least one compound of formula (1) and the salts thereof; and a method for inhibiting the Maillard reaction in living body by administration of a compound of formula (1') or a salt thereof are disclosed.
摘要翻译： 一种含有至少一种式（1）表示的化合物及其盐的新颖的美拉德反应抑制剂; 制备式（1）化合物及其盐的方法; 用于抑制活体中美拉德反应的组合物，其包含至少一种式（1）化合物及其盐; 公开了通过给予式（1'）化合物或其盐抑制活体中美拉德反应的方法。
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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。
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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。
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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。
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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。
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公开(公告)号：US5677322A
公开(公告)日：1997-10-14
申请号：US325233
申请日：1994-10-21
申请人： Koichi Yasumura , Keisuke Miyajima , Takao Nagahama , Shintaro Ishikawa , Yuko Nakagawa , Kazuhisa Sugiyama
发明人： Koichi Yasumura , Keisuke Miyajima , Takao Nagahama , Shintaro Ishikawa , Yuko Nakagawa , Kazuhisa Sugiyama
IPC分类号： C07D233/44 , A61K31/415 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/47 , A61P3/08 , A61P3/10 , A61P43/00 , C07D233/88 , C07D277/20 , C07D277/50 , C07D277/54 , C07D277/82 , C07D401/04 , C07D403/06 , C07D409/04 , C07D409/12 , C07D417/04 , C07D417/06 , C07D417/12 , C07D487/04 , C07D487/08
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 the following formula is disclosed: ##STR1## 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.
摘要翻译： PCT No.PCT / JP94 / 00260 Sec。 371日期：1994年10月21日 102（e）日期1994年10月21日PCT 1994年2月21日PCT PCT。 第WO94 / 19335号公报 1994年9月1日公开了下列化学式表示的化合物：其中全部符号在本公开内容中定义。 还公开了一种制备该化合物的方法以及使用该化合物治疗由生物体中的美拉德反应引起的疾病的方法。
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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。
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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。
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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。
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公开(公告)号：US06197774B1
公开(公告)日：2001-03-06
申请号：US09380742
申请日：1999-09-13
申请人： Satoshi Yamada , Naosumi Kinoshita , Koichi Yasumura , Kouji Edamatsu , Takao Nagahama , Shintaro Ishikawa , Takeshi Yamauchi , Kazumasa Kishi , Kazuhisa Sugiyama
发明人： Satoshi Yamada , Naosumi Kinoshita , Koichi Yasumura , Kouji Edamatsu , Takao Nagahama , Shintaro Ishikawa , Takeshi Yamauchi , Kazumasa Kishi , Kazuhisa Sugiyama
IPC分类号： C07D48704
CPC分类号： C07D487/04
摘要： The present invention provides a novel pyrimidine derivative represented by the general formula (1): (wherein R, R4 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.
摘要翻译： 本发明提供由通式（1）表示的新型嘧啶衍生物（其中R，R 4和R 8与说明书中定义的相同）或其药学上可接受的盐，其具有优异的抑制NO形成的活性 （氮氧化物）。
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