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1. 发明公开

EP0295603A1 Benzimidazol derivatives and therapeutic agent for ulcer comprising the same 失效
标题翻译：吡啶衍生物和治疗剂，死亡物质Mittel gegen溃疡。
公开(公告)号：EP0295603A1
公开(公告)日：1988-12-21
申请号：EP88109374.4
申请日：1988-06-13
申请人： Eisai Co., Ltd.
发明人： Souda, Shigeru , Ueda, Norihiro , Miyazawa, Shuhei , Tagami, Katsuya , Nomoto, Seiichiro , Okita, Makoto , Shimomura, Naoyuki , Kaneko, Toshihiko , Fujimoto, Masatoshi , Murakami, Manabu , Oketani, Kiyoshi , Fujisaki, Hideaki , Shibata, Hisashi , Wakabayashi, Tsuneo
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.
wherein R¹ and R² 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, R³ and R⁴ 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

- -, or a group represented by the formula
and n is an integer of 1 to 6, provided that R³ and R⁴ 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R 1和R 2可以相同或不同，分别为氢原子，低级烷基，低级烷氧基，卤代低级烷基或卤素原子，R 3为和R 4可以相同或不同，分别为氢原子或低级烷基，X为由式-S-表示的基团，由式 - 表示的基团，或由式通式，n为1〜6的整数，条件是当n为1时R 3和R 4不同时为氢原子。

2. 发明授权

EP0654471B1 Pyridine derivatives, pharmaceutical compositions comprising the same, the use of the same for the manufacture of medicaments having therapeutic or preventative value, and process for preparing the same 失效
标题翻译：吡啶衍生物，它们的药物组合物，它们对于具有治疗或预防价值制备药物的用途，以及它们的制备方法
公开(公告)号：EP0654471B1
公开(公告)日：1998-07-08
申请号：EP95102165.8
申请日：1987-11-13
申请人： Eisai Co., Ltd.
发明人： Souda, Shigeru , Ueda, Norihiro , Miyazawa, Shuhei , Tagami, Katsuya , Nomoto, Seiichiro , Okita, Makoto , Shimomura, Naoyuki , Kaneko, Toshihiko , Fujimoto, Masatoshi , Murakami, Manabu , Oketani, Kiyoshi , Fujisaki, Hideaki , Shibata, Hisashi , Wakabayashi, Tsuneo
IPC分类号： C07D401/12 , A61K31/44 , C07D401/14 , C07D405/14 , C07D413/12 , C07D417/12
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D413/12 , C07D417/12 , C07D417/14

3. 发明授权

EP0229370B1 Guanidinobenzoic ester derivative, a process for preparing same and pharmaceutical compositions containing same 失效
标题翻译：胍基苯甲酸衍生物，其制备方法和含有其的药物组合物
公开(公告)号：EP0229370B1
公开(公告)日：1989-04-19
申请号：EP86117885.3
申请日：1986-12-22
申请人： Eisai Co., Ltd.
发明人： Souda, Shigeru , Shimomura, Naoyuki , Ueda, Norihiro , Miyazawa, Shuhei , Yamanaka, Takashi , Miyamoto, Kaname , Hishinuma, Ieharu , Nagakawa, Junichi , Nagaoka, Naoko , Kawashima, Hidetoshi , Kawata, Tsutomu , Nagaoka, Junsaku , Wakabayashi, Tsuneo
IPC分类号： C07C149/437 , C07D207/404 , C07D209/48 , C07D263/44 , A61K31/245 , A61K31/40 , A61K31/42
CPC分类号： C07D207/404 , C07C323/20 , C07D209/48 , C07D263/44

4. 发明公开

EP0654471A1 Pyridine derivatives, pharmaceutical compositions comprising the same, the use of the same for the manufacture of medicaments having therapeutic or preventative value, and process for preparing the same 失效
标题翻译：吡啶衍生物，它们的药物组合物，它们对于具有治疗或预防价值制备药物的用途，以及它们的制备方法。
公开(公告)号：EP0654471A1
公开(公告)日：1995-05-24
申请号：EP95102165.8
申请日：1987-11-13
申请人： Eisai Co., Ltd.
发明人： Souda, Shigeru , Ueda, Norihiro , Miyazawa, Shuhei , Tagami, Katsuya , Nomoto, Seiichiro , Okita, Makoto , Shimomura, Naoyuki , Kaneko, Toshihiko , Fujimoto, Masatoshi , Murakami, Manabu , Oketani, Kiyoshi , Fujisaki, Hideaki , Shibata, Hisashi , Wakabayashi, Tsuneo
IPC分类号： C07D401/12 , A61K31/44 , C07D401/14 , C07D405/14 , C07D413/12 , C07D417/12
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要： The invention provides pyridine derivatives represented by general formula:

wherein R¹ and R² may be the same or different from each other and each stand for a hydrogen atom, a C₁₋₆ alkyl, C₁₋₆ alkoxy, halogenated C₁₋₆ alkyl, (C₁₋₆ alkoxy)carbonyl or carboxyl group or a halogen atom;
X stands for a group represented by the formula:
-O-, -S- or

(wherein R³ stands for a hydrogen atom or a C₁₋₆ alkyl, phenyl, benzyl or (C₁₋₆ alkoxy)carbonyl group);
Z stands for

① a group represented by the general formula:

-O-(CH₂) q -R⁵

wherein q stands for an integer of 1 to 3 and R⁵ stands for a naphthyl group, which may be substituted with a C₁₋₆ alkoxy group, a hydroxyl group or a halogen atom; a pyridyl group or a furyl group,
② a group represented by the general formula:

―OR⁹

wherein OR⁹ stands for a phenyl, tolyl, xylyl or naphthyl group,
n stands for an integer of 0 to 2; m stands for an integer of 2 to 10; and
J and K may be the same or different from each other and each stand for a hydrogen atom or a C₁₋₆ alkyl group,
and a pharmaceutically acceptable salt thereof.
Pharmaceutical compositions comprising these derivatives are also provided, together with the use of the derivatives for the manufacture of medicaments having therapeutic or preventative value in the treatment of peptic ulcers. Processes for preparing such pyridine derivatives are also provided.
摘要翻译：本发明提供了由通式的吡啶衍生物： worin - [R <1>和R <2>可以相同或彼此不同，各代表氢原子，C 1-6烷基，C 1-6烷氧基，卤代C 1-6烷基，（C 1-6烷氧基）羰基或羧基基团或卤原子; X代表由下式表示的基团：-O - ， - S-或（worin - [R <3>代表氢原子或C 1-6烷基，苯基，苄基或（C 1-6烷氧基）羰基）; Z代表1 /＆CIR＆由通式表示的基团：-O（CH 2）●<5> worin q以1整数表示到3和R <5>表示的萘基，其可以是substituiertem与 C 1-6烷氧基，羟基或卤原子; 吡啶基或呋喃基，2 /＆CIR＆由通式表示的基团：-OR <9> worin OR <9>表示苯基，甲苯基，二甲苯基或萘基，n代表在0整数2 ; m表示在2〜10的整数; 和J和K可以相同或彼此不同，各代表氢原子或C 1-6烷基，和其药学上可接受的盐。被设置成药物组合物，其包括本文的衍生物，通过使用衍生物用于具有消化性溃疡的治疗中的治疗或预防价值的药物的制备一起。因此，提供用于制备寻求吡啶衍生物的方法。

5. 发明公开

EP0472053A2 Sulfonamide derivatives 失效
标题翻译：磺酰胺衍。
公开(公告)号：EP0472053A2
公开(公告)日：1992-02-26
申请号：EP91113256.1
申请日：1991-08-07
申请人： Eisai Co., Ltd.
发明人： Yoshino, Hiroshi , Ueda, Norihiro , Sgumi, Hiroyuki , Niijima, Jun , Kotake, Yoshihiko , Okada, Toshimi , Koyanagi, Nozomu , Watanabe, Tatsuo , Asada, Makoto , Yoshimatsu, Kentaro , Iijima, Atsumi , Nagasu, Takeshi , Tsukahara, Kappei , Kitoh, Kyosuke
IPC分类号： C07D213/76 , C07D213/81 , C07D213/82 , C07D213/74 , C07D239/48 , C07D239/50 , C07D239/42 , C07D333/38 , C07D307/68 , C07F9/58 , C07H15/203
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： To provide new sulfonamide derivatives having an excellent antitumor activity and only a low toxicity and a process for producing them.
Sulfonamide derivatives of the general formula (I):
wherein preferably R 1 represents a lower alkoxy group, R 2 , R 3 , R 4 , R 5 , R 6 and R 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 = N- or = CH-, E represents an aromatic 6- membered cyclic group (which may have 1 or 2 nitrogen atoms in the ring) which may 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 1 which is a hydrogen atom, lower alkyl group, nitro group or amino group which may be protected, R 2 and R 3 which are each a hydrogen atom, A and B which are each = 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.
摘要翻译：提供具有优异的抗肿瘤活性和低毒性的新型磺酰胺衍生物及其生产方法。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可以相同或不同，各自表示氢原子，卤素原子或低级烷基，A和B可以相同或不同，各自表示= N-或= CH-， E表示芳族6元环基（其可以在环中具有1或2个氮原子），其可被1至3个可以彼此相同或不同的取代基取代，条件是R“ 1，其可以被保护的氢原子，低级烷基，硝基或氨基，R 2和R 3各自为氢原子，A和B各自为CH-和E，是可以被1〜3个可以相同或不同的取代基G所取代的苯基，或它们的药理学接受盐。

6. 发明公开

EP1074542A1 SULFONAMIDE-CONTAINING INDOLE COMPOUNDS 有权
标题翻译：磺酰胺类化合物
公开(公告)号：EP1074542A1
公开(公告)日：2001-02-07
申请号：EP00905321.6
申请日：2000-02-24
申请人： Eisai Co., Ltd.
发明人： Haneda, Toru , Tsuruoka, Akihiko , Kamata, Junichi , Okabe, Tadashi , Takahashi, Keiko , Nara, Kazumasa , Hamaoka, Shinichi , Ueda, Norihiro , Ohwa, Takashi , Wakabayashi, Toshiaki , Funahashi, Yasuhiro , Semba, Taro , Hata, Naoko , Yamamoto, Yuji , Ozawa, Yoichi , Tsukahara, Naoko
IPC分类号： C07D209/08 , C07D209/30 , C07D209/42 , C07D401/12 , C07D403/12 , C07D409/12 , A61K31/404 , A61K31/4439 , A61K31/506 , A61P43/00 , A61P35/00 , A61P19/02 , A61P27/02
CPC分类号： C07D401/12 , C07D209/04 , C07D209/30 , C07D209/42 , C07D403/12 , C07D409/12
摘要： Novel neovascularization inhibitors are constructed to provide antitumor agents which are superior in safety to conventional antitumor agents, are surely efficacious and can be administered over a prolonged period of time. Namely, indole compounds represented by general formula (I) or pharmacologically acceptable salts thereof or hydrates of the same wherein R 1 represents hydrogen, etc.; R 2 and R 3 are the same or different and each represents hydrogen, etc.; R 4 represents hydrogen or lower (C 1-4 ) alkyl; and the ring A represents cyanophenyl, etc., provided that the following cases are excluded; the one where R 1 , R 2 and R 3 are all hydrogen atoms; the one where R 2 and R 3 are both hydrogen atoms; and the one where the ring A is an aminosulfonylphenyl group and R 1 and R 2 are both halogen atoms; and provided that when the ring A is a cyanophenyl, 2-amino-5-pyridyl or 2-halogeno-5-pyridyl group and R 1 is a cyano group or a halogen atom, then at least one of R 2 and R 3 is not hydrogen.
摘要翻译：构建新型新血管形成抑制剂以提供对常规抗肿瘤剂的安全性优异的抗肿瘤剂，确实有效并且可以在较长时间内施用。即，由通式（I）表示的吲哚化合物或其药学上可接受的盐或其中R 1表示氢等的其水合物; R 2和R 3相同或不同，各自表示氢等。 R 4表示氢或低级（C 1-4）烷基; 并且环A表示氰基苯基等，条件是排除以下情况; 其中R 1，R 2和R 3均为氢原子; 其中R 2和R 3都是氢原子; 环A是氨基磺酰基苯基，R 1和R 2都是卤素原子; 并且条件是当环A是氰基苯基，2-氨基-5-吡啶基或2-卤代-5-吡啶基并且R 1是氰基或卤素原子时，则R 2， R 3不是氢。

7. 发明公开

EP0786461A1 Pyridine derivatives, pharmaceutical compositions comprising the same, the use of the same for the manufacture of medicaments having therapeutic or preventative value, and a process for preparing the same 失效
标题翻译：吡啶衍生物，它们的药物组合物，它们对于具有治疗或预防价值制备药物的用途，以及它们的制备方法
公开(公告)号：EP0786461A1
公开(公告)日：1997-07-30
申请号：EP97105924.1
申请日：1987-11-13
申请人： Eisai Co., Ltd.
发明人： Souda, Shigeru , Ueda, Norihiro , Miyazawa, Shuhei , Tagami, Katsuya , Nomoto, Seiichiro , Okita, Makoto , Shimomura, Naoyuki , Kaneko, Toshihiko , Fujimoto, Masatoshi , Murakami, Manabu , Oketani, Kiyoshi , Fujisaki, Hideaki , Shibata, Hisashi , Wakabayashi, Tsuneo
IPC分类号： C07D401/12 , A61K31/44 , C07D413/12 , C07D417/12 , C07D401/14
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要： The invention provides pyridine derivatives represented by the general formula:

wherein R 1 and R 2 may be the same or different from each other and each stand for a hydrogen atom, a C 1-6 alkyl, C 1-6 alkoxy, halogenated C 1-6 alkyl, (C 1-6 alkoxy) carbonyl or carboxyl group or a halogen atom;
X stands for a group represented by the formula: -O-, -S-or
(wherein R 3 stands for a hydrogen atom or a C 1-6 alkyl, phenyl, benzyl or (C 1-6 alkoxy)carbonyl group);
Z stands for

① a group represented by the general formula:

-0-(CH 2 ) q -R 5

wherein q stands for an integer of 1 to 3 and R 5 stands for a halogen atom or an (C 1-6 alkoxy) carbonyl, aryl or heteroaryl group,
② a group represented by the general formula:

-0-(CH 2 ) r -0-(CH 2 ) s -0-R 6

wherein r and s each stand for an integer of 1 to 5 and R 6 stands for a hydrogen atom or a C 1-6 alkyl group,
③ a group represented by the formula:

④ a group represented by the general formula:
wherein t stands for an integer of 0 to 2 and A stands for a group represented by the general formula:
(wherein B stands for a group represented by the formula: -NH-, -0- or -S-), a C 1-6 aklyl, (C 1-6 alkoxy)carbonylmethyl, pyridyl or furyl group or a group represented by the general formula:
(wherein R 7 stands for a hydrogen atom, a C 1-6 alkyl or C 1-6 alkoxy group or a halogen atom and w stands for an integer of 0 or 1),
⑤ a group represented by the general formula:
wherein R 8 stands for an acetoxy or C1-6 alkyl group,

n stands for an integer of 0 to 2, m stands for an integer of 2 to 10, and
J and K may be the same or different from each other and each stand for a hydrogen atom or a C 1-6 alkyl group,
and a pharmaceutically acceptable salt thereof.

Pharmaceutical compositions comprising these derivatives are also provided, together with the use of the derivatives for the manufacture of medicaments having therapeutic or preventative value in the treatment of peptic ulcers. Processes for preparing such pyridine derivatives are also provided.
摘要翻译：本发明提供由以下通式表示的吡啶衍生物： worin - [R <1>和R <2>可以相同或彼此不同，各代表氢原子，C1-6烷基，C1-6 烷氧基，卤代C 1-6烷基，（C 1-6烷氧基）羰基或羧基基团或卤原子; X代表由下式表示的基团：-O - ， - S-或（worin - [R <3>代表氢原子或C 1-6烷基，苯基，苄基或（C 1-6烷氧基）羰基）; Z代表1个CIR＆由通式表示的基团：-O-（CH 2）●<5> worin q为烷氧基的1整数的至3和R <5>代表卤素原子或（C 1-6 ）羰基，芳基或杂芳基，②=由通式表示的基团：-O-（CH 2）R-O-（CH 2）S-0-R <6> worin r和s各自代表以1整数到5和R <6>代表氢原子或C 1-6烷基，3 CIR＆由下式表示的基团： 4＆CIR＆由通式表示的基团： worin t代表在为2和A 0的整数代表由下述通式表示的基团：（worin B代表由下式表示的基团：-NH - ， - O-或-S-），一个C 1-6 aklyl ，（C 1-6烷氧基） - 羰基，吡啶基或呋喃基或由以下通式表示的基团：（worin - [R <7>代表氢原子，C 1-6烷基或C 1-6烷氧基或卤原子和w为在0或整数1），5 CIR＆由一般的形式表示的基团乌拉： worinř<8>表示在乙酰氧基或C 1-6烷基，n代表在0至2的整数，m，在2的整数表示〜10，J和K可以相同或从海誓山盟不同，并且各自代表氢原子或C 1-6烷基，和其药学上可接受的盐。被设置成药物组合物，其包括本文的衍生物，通过使用衍生物用于具有消化性溃疡的治疗中的治疗或预防价值的药物的制备一起。因此，提供用于制备寻求吡啶衍生物的方法。

8. 发明授权

EP0295603B1 Benzimidazol derivatives and therapeutic agent for ulcer comprising the same 失效
标题翻译：苯并咪唑衍生物和含有它们的对溃疡的治疗组合物
公开(公告)号：EP0295603B1
公开(公告)日：1996-09-18
申请号：EP88109374.4
申请日：1988-06-13
申请人： Eisai Co., Ltd.
发明人： Souda, Shigeru , Ueda, Norihiro , Miyazawa, Shuhei , Tagami, Katsuya , Nomoto, Seiichiro , Okita, Makoto , Shimomura, Naoyuki , Kaneko, Toshihiko , Fujimoto, Masatoshi , Murakami, Manabu , Oketani, Kiyoshi , Fujisaki, Hideaki , Shibata, Hisashi , Wakabayashi, Tsuneo
IPC分类号： C07D401/12 , A61K31/44
CPC分类号： C07D401/12

9. 发明授权

EP1074542B1 SULFONAMIDE-CONTAINING INDOLE COMPOUNDS 有权
标题翻译：含磺酰胺的吲哚衍生物
公开(公告)号：EP1074542B1
公开(公告)日：2006-05-03
申请号：EP00905321.6
申请日：2000-02-24
申请人： Eisai Co., Ltd.
发明人： Haneda, Toru , Tsuruoka, Akihiko , Kamata, Junichi , Okabe, Tadashi , Takahashi, Keiko , Nara, Kazumasa , Hamaoka, Shinichi , Ueda, Norihiro , Owa, Takashi , Wakabayashi, Toshiaki , Funahashi, Yasuhiro , Semba, Taro , Hata, Naoko , Yamamoto, Yuji , Ozawa, Yoichi , Tsukahara, Naoko
IPC分类号： C07D209/08 , C07D209/30 , C07D209/42 , C07D401/12 , C07D403/12 , C07D409/12 , A61K31/404 , A61K31/4439 , A61K31/506 , A61P43/00 , A61P35/00 , A61P19/02 , A61P27/02
CPC分类号： C07D401/12 , C07D209/04 , C07D209/30 , C07D209/42 , C07D403/12 , C07D409/12
摘要： Novel neovascularization inhibitors are constructed to provide antitumor agents which are superior in safety to conventional antitumor agents, are surely efficacious and can be administered over a prolonged period of time. Namely, indole compounds represented by general formula (I) or pharmacologically acceptable salts thereof or hydrates of the same wherein R1 represents hydrogen, etc.; R?2 and R3¿ are the same or different and each represents hydrogen, etc.; R4 represents hydrogen or lower (C¿1-4?) alkyl; and the ring A represents cyanophenyl, etc., provided that the following cases are excluded: the one where R?1, R2 and R3¿ are all hydrogen atoms; the one where R?2 and R3¿ are both hydrogen atoms; and the one where the ring A is an aminosulfonylphenyl group and R?1 and R2¿ are both halogen atoms; and provided that when the ring A is a cyanophenyl, 2-amino-5-pyridyl or 2-halogeno-5-pyridyl group and R1 is a cyano group or a halogen atom, then at least one of R?2 and R3¿ is not hydrogen.

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