公开(公告)号：US07897387B2

公开(公告)日：2011-03-01

申请号：US12060793

申请日：2008-04-01

申请人： Kappei Tsukahara ,  Katsura Hata ,  Koji Sagane ,  Kazutaka Nakamoto ,  Mamiko Tsuchiya ,  Naoaki Watanabe ,  Fuminori Ohba ,  Itaru Tsukada ,  Norihiro Ueda ,  Keigo Tanaka ,  Junko Kai

发明人： Kappei Tsukahara ,  Katsura Hata ,  Koji Sagane ,  Kazutaka Nakamoto ,  Mamiko Tsuchiya ,  Naoaki Watanabe ,  Fuminori Ohba ,  Itaru Tsukada ,  Norihiro Ueda ,  Keigo Tanaka ,  Junko Kai

IPC分类号： C12N15/80 ,  A61K36/06 ,  A61K38/00

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。

公开(公告)号：US07375204B2

公开(公告)日：2008-05-20

申请号：US11409530

申请日：2006-04-21

申请人： Kappei Tsukahara ,  Katsura Hata ,  Koji Sagane ,  Kazutaka Nakamoto ,  Mamiko Tsuchiya ,  Naoaki Watanabe ,  Fuminori Ohba ,  Itaru Tsukada ,  Norihiro Ueda ,  Keigo Tanaka ,  Junko Kai

发明人： Kappei Tsukahara ,  Katsura Hata ,  Koji Sagane ,  Kazutaka Nakamoto ,  Mamiko Tsuchiya ,  Naoaki Watanabe ,  Fuminori Ohba ,  Itaru Tsukada ,  Norihiro Ueda ,  Keigo Tanaka ,  Junko Kai

IPC分类号： C07H21/04 ,  A61K38/00

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, fungal 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. These genes encode proteins participating in fungal cell wall synthesis. 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真菌基因，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。 这些基因编码参与真菌细胞壁合成的蛋白质。 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。

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。

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。

公开(公告)号：US5610320A

公开(公告)日：1997-03-11

申请号：US450138

申请日：1995-05-26

申请人： Hiroshi Yoshino ,  Norihiro Ueda ,  Hirovuki Sugumi ,  Jun Niijima ,  Yoshihiko Kotake ,  Toshimi Okada ,  Nozomu Koyanagi ,  Tatsuo Watanabe ,  Makoto Asada ,  Kentaro Yoshimatsu ,  Atsumi Iijima ,  Takeshi Nagasu ,  Kappei Tsukahara ,  Kyosuke Kitoh

发明人： Hiroshi Yoshino ,  Norihiro Ueda ,  Hirovuki Sugumi ,  Jun Niijima ,  Yoshihiko Kotake ,  Toshimi Okada ,  Nozomu Koyanagi ,  Tatsuo Watanabe ,  Makoto Asada ,  Kentaro Yoshimatsu ,  Atsumi Iijima ,  Takeshi Nagasu ,  Kappei Tsukahara ,  Kyosuke Kitoh

IPC分类号： C07C311/48 ,  A61K31/18 ,  A61P35/00 ,  C07C311/21 ,  C07C311/29 ,  C07C311/44 ,  C07D213/74 ,  C07D213/76 ,  C07D213/81 ,  C07D213/82 ,  C07D239/42 ,  C07D239/48 ,  C07D239/50 ,  C07D239/69 ,  C07D307/68 ,  C07D333/38 ,  C07F9/58 ,  C07H15/203 ,  C07H15/26 ,  C07D307/02 ,  C07D333/02 ,  C07C311/15

CPC分类号： C07D213/74 ,  C07C311/21 ,  C07C311/29 ,  C07C311/44 ,  C07D213/76 ,  C07D213/81 ,  C07D213/82 ,  C07D239/42 ,  C07D239/48 ,  C07D239/50 ,  C07D307/68 ,  C07D333/38 ,  C07F9/588 ,  C07H15/203 ,  C07H15/26

摘要： Sulfonamide compounds of the formula or pharmacologically acceptable salts thereof: ##STR1## wherein: R.sup.1 is a hydrogen atom, halogen atom, lower alkyl group, lower alkoxy group, hydroxyl group, nitro group, phenoxy group, cyano group, acetyl group, amino group or a protected amino group; R.sup.2 and R.sup.3 may be the same or different from each other and each is a hydrogen atom, halogen atom, lower alkyl group or lower alkoxy group; R.sup.4 and R.sup.7 may be the same or different from each other and each is a hydrogen atom or a lower alkyl group; R.sup.5 and R.sup.6 may be the same or different from each other and each is a hydrogen atom, halogen atom, lower alkoxy group, amino group or amino group substituted with a lower alkyl or a phenyl group; A is .dbd.CH--; B is .dbd.CH--; and E is selected from the group consisting of ##STR2## in which Q is an oxygen atom or a sulfur atom; and R.sup.11 is a hydrogen atom, a lower alkyl group, an amino group which may be substituted with a lower alkyl group, a lower alkoxy group, a 2-thienyl group, a 2-furyl group, phenyl group or a phenyl group having from 1 to 3 substituents, said substituents being the same or different from one another and selected from the group consisting of a halogen atom, lower alkyl group, lower alkoxy group, hydroxyl group, carboxyl group, esterified carboxyl group, amidated carboxyl group, lower alkylthio group and phenoxy group; and (b) a phenyl group or a phenyl group having from 1 to 3 substituents.

摘要翻译： 下式的磺酰胺化合物或其药理学上可接受的盐：其中：R1是氢原子，卤素原子，低级烷基，低级烷氧基，羟基，硝基，苯氧基，氰基，乙酰基，氨基 或被保护的氨基; R2和R3可以相同或不同，各自为氢原子，卤素原子，低级烷基或低级烷氧基; R 4和R 7可以相同或不同，各自为氢原子或低级烷基; R5和R6可以相同或不同，分别为氢原子，卤素原子，低级烷氧基，氨基或被低级烷基或苯基取代的氨基; A = CH-; B为= CH-; 并且E选自其中Q是氧原子或硫原子的组; R 11为氢原子，低级烷基，可被低级烷基，低级烷氧基，2-噻吩基，2-呋喃基，苯基或苯基取代的氨基， 1至3个取代基，所述取代基彼此相同或不同，并且选自卤素原子，低级烷基，低级烷氧基，羟基，羧基，酯化羧基，酰胺化羧基，低级烷硫基 组和苯氧基; 和（b）苯基或具有1至3个取代基的苯基。

公开(公告)号：US5292758A

公开(公告)日：1994-03-08

申请号：US923345

申请日：1992-07-31

申请人： Hiroshi Yoshino ,  Norihiro Ueda ,  Hiroyuki Sugumi ,  Jun Niijima ,  Yoshihiko Kotake ,  Toshimi Okada ,  Nozomu Koyanagi ,  Tatsuo Watanabe ,  Makoto Asada ,  Kentaro Yoshimatsu ,  Atsumi Iijima ,  Takeshi Nagasu ,  Kappei Tsukahara ,  Kyosuke Kitoh

发明人： Hiroshi Yoshino ,  Norihiro Ueda ,  Hiroyuki Sugumi ,  Jun Niijima ,  Yoshihiko Kotake ,  Toshimi Okada ,  Nozomu Koyanagi ,  Tatsuo Watanabe ,  Makoto Asada ,  Kentaro Yoshimatsu ,  Atsumi Iijima ,  Takeshi Nagasu ,  Kappei Tsukahara ,  Kyosuke Kitoh

IPC分类号： C07C311/48 ,  A61K31/18 ,  A61P35/00 ,  C07C311/21 ,  C07C311/29 ,  C07C311/44 ,  C07D213/74 ,  C07D213/76 ,  C07D213/81 ,  C07D213/82 ,  C07D239/42 ,  C07D239/48 ,  C07D239/50 ,  C07D239/69 ,  C07D307/68 ,  C07D333/38 ,  C07F9/58 ,  C07H15/203 ,  C07H15/26 ,  A61K31/44

CPC分类号： C07D213/74 ,  C07C311/21 ,  C07C311/29 ,  C07C311/44 ,  C07D213/76 ,  C07D213/81 ,  C07D213/82 ,  C07D239/42 ,  C07D239/48 ,  C07D239/50 ,  C07D307/68 ,  C07D333/38 ,  C07F9/588 ,  C07H15/203 ,  C07H15/26

摘要： Sulfonamide derivatives of the general formula (I): ##STR1## wherein preferably R.sup.1 represents a lower alkoxy group, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 may be the same or different from one another and each represent a hydrogen atom, halogen atom or lower alkyl group, A and B may be the same or different from each other and each represent .dbd.N-- or .dbd.CH--, E represents an aromatic 6-membered cyclic group, which may have 1 or 2 nitrogen atoms in the ring, and be substituted with 1 to 3 substituents which may be the same or different from one another with the proviso that a combination of R.sup.1 which is a hydrogen atom, lower alkyl group, nitro group or amino group which may be protected, R.sup.2 and R.sup.3 which are each a hydrogen atom, A and B which are each .dbd.CH-- and E which is a phenyl group which may be substituted with 1 to 3 substituents G which may be the same or different from one another is excluded, or pharmacologically acceptance salts of them, have an excellent antitumor activity.

摘要翻译： 通式（I）的磺酰胺衍生物：其中优选R 1表示低级烷氧基，R 2，R 3，R 4，R 5，R 6和R 7可以彼此相同或不同，并且各自表示氢 原子，卤原子或低级烷基，A和B可以相同或不同，并且各自表示= N-或= CH-，E表示可具有1或2个氮原子的芳族6元环基 并且被1〜3个可以相同或不同的取代基取代，条件是可以被保护的是氢原子，低级烷基，硝基或氨基的R 1的组合， R 2和R 3各自为氢原子，A和B各自为CH-，E为可被1至3个彼此可相同或不同的取代基G所取代的苯基，不包括或 它们的药理学接受盐具有优异的抗肿瘤活性。