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公开(公告)号:US4948808A
公开(公告)日:1990-08-14
申请号:US225278
申请日:1988-07-28
申请人: Shigeru Souda , Naoyuki Shimomura , Norihiro Ueda , Shuhei Miyazawa , Takashi Yamanaka , Kaname Miyamoto , Ieharu Hishinuma , Junichi Nagakawa , Naoko Nagaoka , Hidetoshi Kawashima , Tsutomu Kawata , Junsaku Nagaoka , Tsuneo Wakabayashi
发明人: Shigeru Souda , Naoyuki Shimomura , Norihiro Ueda , Shuhei Miyazawa , Takashi Yamanaka , Kaname Miyamoto , Ieharu Hishinuma , Junichi Nagakawa , Naoko Nagaoka , Hidetoshi Kawashima , Tsutomu Kawata , Junsaku Nagaoka , Tsuneo Wakabayashi
IPC分类号: A61K31/235 , A61K31/245 , A61K31/40 , A61K31/4015 , A61K31/403 , A61K31/4035 , A61K31/42 , A61K31/421 , A61K31/445 , A61P1/00 , A61P7/02 , A61P7/04 , A61P43/00 , C07C67/00 , C07C313/00 , C07C319/20 , C07C323/20 , C07D207/40 , C07D207/404 , C07D207/408 , C07D209/48 , C07D209/76 , C07D211/76 , C07D211/88 , C07D263/44
CPC分类号: C07D207/404 , C07C323/20 , C07D209/48 , C07D263/44
摘要: A guanidinobenzoic ester derivative having the formula is novel and effective to inhibit enzymes such as trypsin, plasmin and thrombin, being useful for treatment of the pancreatitis and hemorrhagic disease and thrombosis. ##STR1## wherein X represents a group of the formula: ##STR2## in which Y is a group of the formula: --(CH.sub.2).sub.m--, m being an integer of 2 or 3, ##STR3## or a group of the formula:--ORin which R is a hydrogen atom or a lower alkyl group, and n represents an integer of 1 to 5.
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公开(公告)号:US5075335A
公开(公告)日:1991-12-24
申请号:US495444
申请日:1990-03-16
申请人: Shigeru Souda , Naoyuki Shimomura , Norihiro Ueda , Shuhei Miyazawa , Takashi Yamanaka , Kaname Miyamoto , Ieharu Hishinuma , Junichi Nagakawa , Naoko Nagaoka , Hidetoshi Kawashima , Tsutomu Kawata , Junsaku Nagaoka , Tsuneo Wakabayashi
发明人: Shigeru Souda , Naoyuki Shimomura , Norihiro Ueda , Shuhei Miyazawa , Takashi Yamanaka , Kaname Miyamoto , Ieharu Hishinuma , Junichi Nagakawa , Naoko Nagaoka , Hidetoshi Kawashima , Tsutomu Kawata , Junsaku Nagaoka , Tsuneo Wakabayashi
IPC分类号: A61K31/235 , A61K31/245 , A61K31/40 , A61K31/4015 , A61K31/403 , A61K31/4035 , A61K31/42 , A61K31/421 , A61K31/445 , A61P1/00 , A61P7/02 , A61P7/04 , A61P43/00 , C07C67/00 , C07C313/00 , C07C319/20 , C07C323/20 , C07D207/40 , C07D207/404 , C07D207/408 , C07D209/48 , C07D209/76 , C07D211/76 , C07D211/88 , C07D263/44
CPC分类号: C07D207/404 , C07C323/20 , C07D209/48 , C07D263/44
摘要: A guanidinobenzoic ester derivative having the formula is novel and effective to inhibit enzymes such as trypsin, plasmin and thrombin, being useful for treatment of the pancreatitis and hemorrhagic disease and thrombosis. ##STR1## wherein X represents a group of the formula: ##STR2## in which Y is a group of the formula: --(CH.sub.2).sub.m --, m being an integer of 2 or 3, ##STR3## or a group of the formula:--ORin which R is a hydrogen atom or a lower alkyl group, and n represents an integer of 1 to 5.
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公开(公告)号:US4801603A
公开(公告)日:1989-01-31
申请号:US946458
申请日:1986-12-24
申请人: Shigeru Souda , Naoyuki Shimomura , Norihiro Ueda , Shuhei Miyazawa , Takashi Yamanaka , Kaname Miyamoto , Ieharu Hishinuma , Junichi Nagakawa , Naoko Nagaoka , Hidetoshi Kawashima , Tsutomu Kawata , Junsaku Nagaoka , Tsuneo Wakabayashi
发明人: Shigeru Souda , Naoyuki Shimomura , Norihiro Ueda , Shuhei Miyazawa , Takashi Yamanaka , Kaname Miyamoto , Ieharu Hishinuma , Junichi Nagakawa , Naoko Nagaoka , Hidetoshi Kawashima , Tsutomu Kawata , Junsaku Nagaoka , Tsuneo Wakabayashi
IPC分类号: A61K31/235 , A61K31/245 , A61K31/40 , A61K31/4015 , A61K31/403 , A61K31/4035 , A61K31/42 , A61K31/421 , A61K31/445 , A61P1/00 , A61P7/02 , A61P7/04 , A61P43/00 , C07C67/00 , C07C313/00 , C07C319/20 , C07C323/20 , C07D207/40 , C07D207/404 , C07D207/408 , C07D209/48 , C07D209/76 , C07D211/76 , C07D211/88 , C07D263/44
CPC分类号: C07D207/404 , C07C323/20 , C07D209/48 , C07D263/44
摘要: A guanidinobenzoic ester derivative having the formula is novel and effective to inhibit enzymes such as trypsin, plasmin and thrombin, being useful for treatment of the pancreatitis and hemorrhagic disease and thrombosis. ##STR1## wherein X represents a group of the formula: ##STR2## in which Y is a group of the formula: --(CH.sub.2).sub.m --, m being an integer of 2 or 3, ##STR3## or a group of the formula:--ORin which R is a hydrogen atom or a lower alkyl group, and n represents an integer of 1 to 5.
摘要翻译: 具有下式的胍基苯甲酸酯衍生物是新颖有效的抑制酶如胰蛋白酶,纤溶酶和凝血酶,可用于治疗胰腺炎和出血性疾病和血栓形成。 其中X表示下式的基团:其中Y是下式的基团: - (CH 2)m - ,m是2或3的整数,
或基团 其中R是氢原子或低级烷基,n表示1〜5的整数。 -
4.
公开(公告)号:US5162317A
公开(公告)日:1992-11-10
申请号:US445664
申请日:1989-12-05
申请人: Shigeru Souda , Shuhei Miyazawa , Norihiro Ueda , Katsuya Tagami , Seiichiro Nomoto , Makoto Okita , Naoyuki Shimomura , Toshihiko Kaneko , Masatoshi Fujimoto , Manabu Murakami , Kiyoshi Oketani , Hideaki Fujisaki , Hisashi Shibata , Tsuneo Wakabayashi
发明人: Shigeru Souda , Shuhei Miyazawa , Norihiro Ueda , Katsuya Tagami , Seiichiro Nomoto , Makoto Okita , Naoyuki Shimomura , Toshihiko Kaneko , Masatoshi Fujimoto , Manabu Murakami , Kiyoshi Oketani , Hideaki Fujisaki , Hisashi Shibata , Tsuneo Wakabayashi
IPC分类号: C07D401/04 , C07D401/14 , C07D413/14 , C07D417/14 , C07D513/14
CPC分类号: C07D401/04 , C07D401/14 , C07D413/14 , C07D417/14 , C07D513/14
摘要: A pyridinium salt useful as an antiulcer agent, defined by formula (I) is disclosed. It includes a sulphenamide compound and a pyridinium compound. J is benzimidazole, K is --S-- or --SSR-- and Z is hydroxy or alkoxy. ##STR1##
摘要翻译: PCT No.PCT / JP89 / 00482 Sec。 371日期1989年12月5日第 102(e)日期1989年12月5日PCT提交1989年5月11日PCT公布。 出版物WO89 / 10927 日本公报(公开)公开了用作抗溃疡剂的吡啶鎓盐。 它包括苯丙胺化合物和吡啶鎓化合物。 J为苯并咪唑,K为-S-或-SSR-,Z为羟基或烷氧基。 (一)
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公开(公告)号:US5840910A
公开(公告)日:1998-11-24
申请号:US354726
申请日:1994-12-06
申请人: Shigeru Souda , Norihiro Ueda , Shuhei Miyazawa , Katsuya Tagami , Seiichiro Nomoto , Makoto Okita , Naoyuki Shimomura , Toshihiko Kaneko , Masatoshi Fujimoto , Manabu Murakami , Kiyoshi Oketani , Hideaki Fujisaki , Hisashi Shibata , Tsuneo Wakabayashi
发明人: Shigeru Souda , Norihiro Ueda , Shuhei Miyazawa , Katsuya Tagami , Seiichiro Nomoto , Makoto Okita , Naoyuki Shimomura , Toshihiko Kaneko , Masatoshi Fujimoto , Manabu Murakami , Kiyoshi Oketani , Hideaki Fujisaki , Hisashi Shibata , Tsuneo Wakabayashi
IPC分类号: A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/54 , A61P1/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
CPC分类号: C07D401/12 , C07D401/14 , C07D405/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要: Pyridine derivatives useful for preventing or treating peptic ulcers, pharmaceutical preparations and methods of treating peptic ulcers are disclosed.
摘要翻译: 公开了用于预防或治疗消化性溃疡的吡啶衍生物,药物制剂和治疗消化性溃疡的方法。
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公开(公告)号:US5239079A
公开(公告)日:1993-08-24
申请号:US928742
申请日:1992-08-13
申请人: Shigeru Souda , Shuhei Miyazawa , Norihiro Ueda , Katsuya Tagami , Seiichiro Nomoto , Makoto Okita , Naoyuki Shimomura , Toshihiko Kaneko , Masatoshi Fujimoto , Manabu Murakami , Kiyoshi Oketani , Hideaki Fujisaki , Hisashi Shibata , Tsuneo Wakabayashi
发明人: Shigeru Souda , Shuhei Miyazawa , Norihiro Ueda , Katsuya Tagami , Seiichiro Nomoto , Makoto Okita , Naoyuki Shimomura , Toshihiko Kaneko , Masatoshi Fujimoto , Manabu Murakami , Kiyoshi Oketani , Hideaki Fujisaki , Hisashi Shibata , Tsuneo Wakabayashi
IPC分类号: C07D401/04 , C07D401/14 , C07D413/14 , C07D417/14 , C07D513/14
CPC分类号: C07D401/04 , C07D401/14 , C07D413/14 , C07D417/14 , C07D513/14
摘要: A pyridinium salt is useful as an antiulcer and is defined by the following formula. It includes a sulphenamide compound and a pyridinium compound. J is benzoimidazole, K is --S-- or --SSR, Z is hydroxy or oxyalkyl. ##STR1##
摘要翻译: 吡啶鎓盐可用作抗溃疡剂并由下式定义。 它包括苯丙胺化合物和吡啶鎓化合物。 J为苯并咪唑,K为-S-或-SSR,Z为羟基或烷氧基。
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公开(公告)号:US5045552A
公开(公告)日:1991-09-03
申请号:US462328
申请日:1989-12-28
申请人: Shigeru Souda , Norihiro Ueda , Shuhei Miyazawa , Katsuya Tagami , Seiichiro Nomoto , Makoto Okita , Naoyuki Shimomura , Toshihiko Kaneko , Masatoshi Fujimoto , Manabu Murakami , Kiyoshi Oketani , Hideaki Fujisaki , Hisashi Shibata , Tsuneo Wakabayashi
发明人: Shigeru Souda , Norihiro Ueda , Shuhei Miyazawa , Katsuya Tagami , Seiichiro Nomoto , Makoto Okita , Naoyuki Shimomura , Toshihiko Kaneko , Masatoshi Fujimoto , Manabu Murakami , Kiyoshi Oketani , Hideaki Fujisaki , Hisashi Shibata , Tsuneo Wakabayashi
IPC分类号: A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/54 , A61P1/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
CPC分类号: C07D401/12 , C07D401/14 , C07D405/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要: Pyridine derivatives useful for preventing or treating peptic ulcers, pharmaceutical preparations and methods of treating peptic ulcers are described.
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公开(公告)号:US5998445A
公开(公告)日:1999-12-07
申请号:US679473
申请日:1996-07-09
申请人: Shigeru Souda , Norihiro Ueda , Shuhei Miyazawa , Katsuya Tagami , Seiichiro Nomoto , Makoto Okita , Naoyuki Shimomura , Toshihiko Kaneko , Masatoshi Fujimoto , Manabu Murakami , Kiyoshi Oketani , Hideaki Fujisaki , Hisashi Shibata , Tsuneo Wakabayashi
发明人: Shigeru Souda , Norihiro Ueda , Shuhei Miyazawa , Katsuya Tagami , Seiichiro Nomoto , Makoto Okita , Naoyuki Shimomura , Toshihiko Kaneko , Masatoshi Fujimoto , Manabu Murakami , Kiyoshi Oketani , Hideaki Fujisaki , Hisashi Shibata , Tsuneo Wakabayashi
IPC分类号: A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/54 , A61P1/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
CPC分类号: C07D401/12 , C07D401/14 , C07D405/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要: Pyridine derivatives useful for preventing or treating peptic ulcers, pharmaceutical preparations and methods of treating peptic ulcers are described.
摘要翻译: 描述了可用于预防或治疗消化性溃疡的吡啶衍生物,药物制剂和治疗消化性溃疡的方法。
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公开(公告)号:US5708013A
公开(公告)日:1998-01-13
申请号:US524109
申请日:1995-08-21
申请人: Shigeru Souda , Norihiro Ueda , Shuhei Miyazawa , Katsuya Tagami , Seiichiro Nomoto , Makoto Okita , Naoyuki Shimomura , Toshihiko Kaneko , Masatoshi Fujimoto , Manabu Murakami , Kiyoshi Oketani , Hideaki Fujisaki , Hisashi Shibata , Tsuneo Wakabayashi
发明人: Shigeru Souda , Norihiro Ueda , Shuhei Miyazawa , Katsuya Tagami , Seiichiro Nomoto , Makoto Okita , Naoyuki Shimomura , Toshihiko Kaneko , Masatoshi Fujimoto , Manabu Murakami , Kiyoshi Oketani , Hideaki Fujisaki , Hisashi Shibata , Tsuneo Wakabayashi
IPC分类号: C07D401/12 , A61K31/44
CPC分类号: C07D401/12
摘要: A pyridine compound having the formula is disclosed and useful to treat the peptic ulcer. ##STR1## wherein R.sup.1 and R.sup.2 which may be the same or different are each a hydrogen atom, a lower alkyl group, a lower alkoxy group, a halogenated lower alkyl group, or a halogen atom, R.sup.3 and R.sup.4 which may be the same or different are each a hydrogen atom or a lower alkyl group, X is a group represented by the formula --S--, a group represented by the formula ##STR2## or a group represented by the formula ##STR3## and n is an integer of 1 to 6, provided that R.sup.3 and R.sup.4 are not simultaneously hydrogen atoms when n is 1.
摘要翻译: 公开了具有下式的吡啶化合物,可用于治疗消化性溃疡。 其中可以相同或不同的R 1和R 2各自为氢原子,低级烷基,低级烷氧基,卤代低级烷基或卤素原子,可以相同的R 3和R 4, 不同的是氢原子或低级烷基,X是由式-S-表示的基团,即由式d表示的基团,当n为1时,R3和R4不同时为氢原子。
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公开(公告)号:US20090325228A1
公开(公告)日:2009-12-31
申请号:US12103600
申请日:2008-04-15
申请人: Kappei Tsukahara , Katsura Hata , Koji Sagane , Kazutaka Nakamoto , Mamiko Tsuchiya , Naoaki Watanabe , Fuminori Oba , Itaru Tsukada , Norihiro Ueda , Keigo Tanaka , Junko Kai
发明人: Kappei Tsukahara , Katsura Hata , Koji Sagane , Kazutaka Nakamoto , Mamiko Tsuchiya , Naoaki Watanabe , Fuminori Oba , Itaru Tsukada , Norihiro Ueda , Keigo Tanaka , Junko Kai
CPC分类号: C07K14/40 , A61K31/00 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/44 , A61K31/472 , A61K31/4725 , A61K31/5377 , A61K38/00 , C07D213/68 , C07D217/18 , C07D217/20 , C07K14/37 , C07K14/38 , C07K14/39 , C07K14/395 , C07K2319/02 , G01N2500/00 , Y10S435/911
摘要: A reporter system reflecting the transport process that transports GPI-anchored proteins to the cell wall was constructed and compounds inhibiting this process were discovered. Further, genes conferring resistance to the above compounds were identified and methods of screening for compounds that inhibit the activity of the proteins encoded by these genes were developed. Therefore, through the novel compounds, the present invention showed that antifungal agents having a novel mechanism, i.e. inhibiting the process that transports GPI-anchored proteins to the cell wall, could be achieved.
摘要翻译: 构建了将GPI锚定蛋白转运至细胞壁的运输过程的记录系统,发现了抑制该过程的化合物。 此外,鉴定了赋予对上述化合物的抗性的基因,并开发了筛选抑制由这些基因编码的蛋白质的活性的化合物的方法。 因此,通过本发明,可以实现具有新机理的抗真菌剂,即抑制将GPI锚定蛋白转运到细胞壁的过程。
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