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1. 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。

2. 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.

3. 发明公开

EP1506962A3 Nitrogen-containing aromatic heterocycles 有权
标题翻译：含氮芳香杂环
公开(公告)号：EP1506962A3
公开(公告)日：2005-03-02
申请号：EP04025700.8
申请日：2001-10-19
申请人： Eisai Co. Ltd.
发明人： Funahashi, Yasuhiro , Tsuruoka, Akihiko , Matsukura, Masayuki , Haneda, Toru , Fukuda, Yoshio , Kamata, Junichi , Takahashi, Keiko , Matsushima, Tomohiro , Miyazaki, Kazuki , Nomoto, Ken-ichi , Watanabe, Tatsuo , Obaishi, Hiroshi , Yamaguchi, Atsumi , Suzuki, Sachi , Nakamura, Katsuji , Mimura, Fusalo , Yamamoto, Yuji , Matsui, Junji , Matsui, Kenji , Yoshiba, Takako , Suzuki, Yasuyuki , Arimoto, Itaru
IPC分类号： C07D213/74 , C07D213/75 , C07D215/48 , C07D239/47 , C07D401/12 , C07D401/14 , C07D413/12 , C07D405/12 , C07D409/12 , A61K31/47 , A61P35/00
CPC分类号： C07D213/73 , A61K31/4706 , A61K31/4745 , A61K31/517 , A61K31/519 , C07D207/34 , C07D213/26 , C07D213/68 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/82 , C07D215/18 , C07D215/233 , C07D215/36 , C07D215/38 , C07D215/48 , C07D239/34 , C07D239/42 , C07D239/47 , C07D239/88 , C07D249/04 , C07D261/14 , C07D277/48 , C07D307/68 , C07D319/06 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04
摘要： A compound represented by the following general formula: wherein A is a further optionally substituted group represented by the formula: X is an oxygen atom, a sulfur atom, -SO- or -SO 2 ; Y is an optionally substituted C 6-14 aryl group, an optionally substituted 5- to 14-membered aromatic heterocyclic group or an optionally substituted C 1-6 alkylene group; E is a single bond or -NR 2 -.
摘要翻译：由下列通式表示的化合物：其中A为由下式表示的另外任选取代的基团：X为氧原子，硫原子，-SO-或-SO 2; Y是任选取代的C 6-14芳基，任选取代的5至14元芳族杂环基或任选取代的C 1-6亚烷基; E是单键或-NR 2 - 。

4. 发明公开

EP1506962A2 Nitrogen-containing aromatic heterocycles 有权
标题翻译： Stickstoff enthaltende aromatische Heterozyklen
公开(公告)号：EP1506962A2
公开(公告)日：2005-02-16
申请号：EP04025700.8
申请日：2001-10-19
申请人： Eisai Co. Ltd.
发明人： Funahashi, Yasuhiro , Tsuruoka, Akihiko , Matsukura, Masayuki , Haneda, Toru , Fukuda, Yoshio , Kamata, Junichi , Takahashi, Keiko , Matsushima, Tomohiro , Miyazaki, Kazuki , Nomoto, Ken-ichi , Watanabe, Tatsuo , Obaishi, Hiroshi , Yamaguchi, Atsumi , Suzuki, Sachi , Nakamura, Katsuji , Mimura, Fusalo , Yamamoto, Yuji , Matsui, Junji , Matsui, Kenji , Yoshiba, Takako , Suzuki, Yasuyuki , Arimoto, Itaru
IPC分类号： C07D213/74 , C07D213/75 , C07D215/48 , C07D239/47 , C07D401/12 , C07D401/14 , C07D413/12 , C07D405/12 , C07D409/12 , A61K31/47 , A61P35/00
CPC分类号： C07D213/73 , A61K31/4706 , A61K31/4745 , A61K31/517 , A61K31/519 , C07D207/34 , C07D213/26 , C07D213/68 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/82 , C07D215/18 , C07D215/233 , C07D215/36 , C07D215/38 , C07D215/48 , C07D239/34 , C07D239/42 , C07D239/47 , C07D239/88 , C07D249/04 , C07D261/14 , C07D277/48 , C07D307/68 , C07D319/06 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04
摘要： Compounds represented by the following general formula:
[wherein A g is an optionally substituted 5- to 14-membered heterocyclic group, etc.; X g is -O-, -S-, etc.; Y g is an optionally substituted C 6-14 aryl group, an optionally substituted 5- to 14-membered heterocyclic group, etc.; and T g1 is a group represented by the following general formula:
(wherein E g is a single bond or -N(R g2 )-, R g1 and R g2 each independently represent a hydrogen atom, an optionally substituted C 1-6 alkyl group, etc. and Z g represents a C 1-8 alkyl group, a C 3-8 alicyclic hydrocarbon group, a C 6-14 aryl group, etc.)], salts thereof or hydrates of the foregoing.
摘要翻译：由以下通式表示的化合物：其中A是下式表示的另外任意取代的基团：其中X是氧原子，硫原子，-SO-或-SO 2; Y是任选取代的C 6-14芳基，任选取代的5至14元芳族杂环基或任选取代的C 1-6亚烷基; E是单键或-NR 2 - 。

5. 发明公开

EP0530579A1 Condensed pyrimidine derivatives antitumor agents 失效
标题翻译： Kondensierte Pyrimidinderivate als Antitumorverbindungen。
公开(公告)号：EP0530579A1
公开(公告)日：1993-03-10
申请号：EP92114005.9
申请日：1992-08-17
申请人： Eisai Co., Ltd.
发明人： Nomura, Hiroaki , Haneda, Toru , Kotake, Yoshihiko , Ueda, Norohiro , Kitoh, Kyosuke
IPC分类号： C07D239/70 , C07D487/04 , A61K31/505
CPC分类号： C07D487/04 , C07D239/70
摘要： A novel pyrimidine derivative having an excellent antitumor activity, which is represented by the following general formula (I) or a pharmacologically acceptable salt thereof:

wherein R¹ represents a hydroxyl or amino group; R² represents a phenylene, pyridinediyl, thiendiyl, furandiyl or thiazoldiyl group, -CO₂R⁵ and -CO₂R⁶ may be the same or different from each other and each represents a carboxyl group or a carboxylic acid ester, the part 〉X-Y-Z- represents 〉N-CH₂-CH₂-, 〉N-CH=CH- or 〉CH-CH₂-CH₂-, A represents an oxygen atom, a group represented by the formula:

(wherein R³ and R⁴ may be the same or different from each other and each represents a hydrogen or halogen atom or a hydrocarbon group which may be substituted, or alternatively R³ and R⁴ may be united to form an alkylidene group which may be substituted) or a group represented by the formula:

(wherein R⁷⁰ represents a hydrogen atom or a hydrocarbon group), and n is an integer of 1 to 3, provided that the compound in which R¹ represents oxygen, and hydrogen is attached to nitrogen at 3-position is included in the above shown definition, a process for preparation the same, and an antitumor drug containing the same.
摘要翻译：一种具有优异抗肿瘤活性的新型嘧啶衍生物，其由下列通式（I）表示或其药理学上可接受的盐：其中R 1表示羟基或氨基; R 2表示亚苯基，吡啶二基，噻二烷基，呋喃基或噻二唑基，-CO 2 R 5和-CO 2 R 6可以相同或不同，各自表示羧基或羧酸酯，部分＆rdurule＆XYZ-表示＆rdurule＆N-CH2-CH2-，＆rdurule＆N-CH = CH-或＆rdurule＆CH-CH2-CH2-，A表示氧原子，由下式表示的基团：其中R 3 >和R 4可以相同或不同，并且各自表示氢或卤素原子或可被取代的烃基，或者R 3和R 4可以一起形成亚烷基可以被取代的基团）或由下式表示的基团：其中R 7表示氢原子或烃基，n表示1〜3的整数，条件是化合物其中R 1表示氧，并且氢在3-位上与氮连接，包括在上述定义中，其制备方法和抗肿瘤药含有相同的药物。

6. 发明授权

EP0530579B1 Condensed pyrimidine derivatives antitumor agents 失效
标题翻译：稠合的嘧啶衍生物作为抗肿瘤化合物
公开(公告)号：EP0530579B1
公开(公告)日：1998-11-11
申请号：EP92114005.9
申请日：1992-08-17
申请人： Eisai Co., Ltd.
发明人： Nomura, Hiroaki , Haneda, Toru , Kotake, Yoshihiko , Ueda, Norohiro , Kitoh, Kyosuke
IPC分类号： C07D239/70 , C07D487/04 , A61K31/505
CPC分类号： C07D487/04 , C07D239/70

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