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。

公开(公告)号：EP0239729B1

公开(公告)日：1991-04-17

申请号：EP87100824.9

申请日：1987-01-22

申请人： Eisai Co., Ltd.

发明人： Koyama, Noritoshi ,  Ikeuchi, Takayuki ,  Araki, Seiichi ,  Kitoh, Kyosuke ,  Ida, Katsumi

IPC分类号： A61K31/045 ,  A61K9/10 ,  A61K47/00

CPC分类号： A61K31/685 ,  A61K31/045 ,  Y10S514/946 ,  A61K2300/00

公开(公告)号：EP0264091B1

公开(公告)日：1992-02-05

申请号：EP87114843.3

申请日：1987-10-12

申请人： Eisai Co., Ltd.

发明人： Kamiya, Takashi ,  Naito, Toshihiko ,  Negi, Shigeto ,  Komatu, Yuuki ,  Kai, Yasunobu ,  Nakamura, Takaharu ,  Sugiyama, Isao ,  Machida, Yoshimasa ,  Nomoto, Seiichiro ,  Kitoh, Kyosuke ,  Katsu, Kanemasa ,  Yamauchi, Hiroshi

IPC分类号： C07D501/24 ,  A61K31/545 ,  C07D285/08

CPC分类号： C07D501/24

公开(公告)号：EP0114899A1

公开(公告)日：1984-08-08

申请号：EP83100239.9

申请日：1983-01-13

申请人： Eisai Co., Ltd.

发明人： Negi, Shigeto ,  Machida, Yoshimasa ,  Nomoto, Seiichiro ,  Saito, Isao ,  Kamiya, Takashi ,  Kitoh, Kyosuke

IPC分类号： C07D311/22

CPC分类号： C07D311/22

摘要： A novel 2-methylchromone derivative represented by the general formula:
wherein R, means a hydrogen atom or a lower alkanoyl group. The above derivative is a useful intermediate for the synthesis of cephem activities, which are also effective against infections of the urinary tract. etc. A preparation process of the above chromone derivative is also disclosed.

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

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。

公开(公告)号：EP0062328A2

公开(公告)日：1982-10-13

申请号：EP82102830.5

申请日：1982-04-02

申请人： Eisai Co., Ltd.

发明人： Machida, Yoshimasa ,  Saito, Isao ,  Sugiyama, Isao ,  Negi, Shigeto ,  Nomoto, Seiichiro ,  Ikuta, Hironori ,  Yamauchi, Hiroshi ,  Kitoh, Kyosuke

IPC分类号： C07D501/24 ,  C07D499/68 ,  A61K31/545 ,  A61K31/43

CPC分类号： C07D335/06 ,  C07D215/54 ,  C07D215/56 ,  C07D311/16 ,  C07D499/00

摘要： A compound represented by the formula:
wherein R, is hydrogen or methoxy; R 2 is hydrogen or hydroxy; R is
wherein R 3 and R 4 are hydroxy or acyloxy, Y is oxygen, sulfur or N-R 5 wherein R 5 is hydrogen or lower alkyl, and Z is sulfur or N-R 5 wherein R 5 has the same meanings as defined above; and X is
wherein R 6 is acyloxy or nitrogen-containing hetero- cyclicthio which may have substituent(s), a pharmaceutically acceptable salt thereof, and a carboxylic ester thereof, a process for preparing the same and antibacterial composition containing the novel compounds.
This compound has improved antibacterial activity against Kleb. pneumoniae and Pseid. aeruginosa.

公开(公告)号：EP0472053B1

公开(公告)日：1998-06-17

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

公开(公告)号：EP0472053A3

公开(公告)日：1994-08-10

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.

公开(公告)号：EP0264091A2

公开(公告)日：1988-04-20

申请号：EP87114843.3

申请日：1987-10-12

申请人： Eisai Co., Ltd.

发明人： Kamiya, Takashi ,  Naito, Toshihiko ,  Negi, Shigeto ,  Komatu, Yuuki ,  Kai, Yasunobu ,  Nakamura, Takaharu ,  Sugiyama, Isao ,  Machida, Yoshimasa ,  Nomoto, Seiichiro ,  Kitoh, Kyosuke ,  Katsu, Kanemasa ,  Yamauchi, Hiroshi

IPC分类号： C07D501/24 ,  A61K31/545 ,  C07D285/08

CPC分类号： C07D501/24

摘要： A 3-propenylcephem derivative of the following formula:
wherein R 1 represents a fluoro-substituted lower alkyl group or a cyano-substituted lower alkyl group, and A represents a cyclic or an acylic ammonio group, or a pharmaceutically acceptable salt thereof. exhibiting excellent anti-bacterial activities against both Gram-positive bacteria and Gram-negative bactena; Process for the preparation thereof; Anti-bacterial composition; Intermediate for the 3-propenylcehem derivative; and Process for the preparation of the intermediate.

摘要翻译： 下式的3-丙烯基头孢烯衍生物： worin R1 darstellt一个氟substituiertem低级烷基或氰基substituiertem低级烷基，和A darstellt环状或无环的铵基团，或者其药学上可接受的盐， 显示出对革兰氏阳性菌和革兰氏阴性菌优异的抗菌活性; 过程用于其制备; 抗细菌组合物; 中间体3- propenylcehem衍生物; 和处理用于在中间体的制备。