公开(公告)号：US5006649A

公开(公告)日：1991-04-09

申请号：US463519

申请日：1990-01-11

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

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

IPC分类号： C07D501/46 ,  A61K31/545 ,  A61K31/546 ,  C07D20060101 ,  C07D285/08 ,  C07D501/00 ,  C07D501/04 ,  C07D501/24 ,  C07D501/56 ,  C07D519/00

CPC分类号： C07D501/24

摘要： A 3-propenylcephem derivative of the following formula: ##STR1## wherein R.sub.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 bacteria; Process for the preparation thereof; Anti-bacterial composition; Intermediate for the 3-propenylcephem derivative; and Process for the preparation of the intermediate.

公开(公告)号：US4921850A

公开(公告)日：1990-05-01

申请号：US107631

申请日：1987-10-13

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

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

IPC分类号： C07D501/46 ,  A61K31/545 ,  A61K31/546 ,  C07D20060101 ,  C07D285/08 ,  C07D501/00 ,  C07D501/04 ,  C07D501/24 ,  C07D501/56 ,  C07D519/00

CPC分类号： C07D501/24

摘要： A 3-propenylcephem derivative of the following formula: ##STR1## wherein R.sub.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 bacteria; Process for the preparation thereof; Anti-bacterial composition; Intermediate for the 3-propenylcephem 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：其中R1表示氟取代的低级烷基或氰基取代的低级烷基，A表示环状或酰基氨基，或其药学上可接受的盐， 对革兰氏阳性菌和革兰氏阴性细菌均表现出优异的抗菌活性; 制备方法 抗菌成分; 3-丙烯基头孢烯衍生物的中间体; 和中间体的制备方法。

公开(公告)号：US5089491A

公开(公告)日：1992-02-18

申请号：US463518

申请日：1990-01-11

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

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

IPC分类号： C07D501/46 ,  A61K31/545 ,  A61K31/546 ,  C07D20060101 ,  C07D285/08 ,  C07D501/00 ,  C07D501/04 ,  C07D501/24 ,  C07D501/56 ,  C07D519/00

CPC分类号： C07D501/24

摘要： A 3-propenylcephem derivative of the following formula: ##STR1## wherein R.sub.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 bacteria; Process for the preparation thereof; Anti-bacterial composition; Intermediate for the 3-propenylcephem derivative; and Process for the preparation of the intermediate.

公开(公告)号：US4929612A

公开(公告)日：1990-05-29

申请号：US181427

申请日：1988-04-14

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

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

IPC分类号： C07D501/46 ,  C07D519/00

CPC分类号： C07D501/46 ,  C07D519/00

摘要： Novel thiadiazolylacetamide cephem derivatives of the following formula are described. ##STR1## wherein A represents a quaternary ammonio group; or a pharmaceutically acceptable salt thereof. These novel compounds are useful as antibacterial agents, because they have a broad antibacterial spectrum ranging from gram-negative bacteria to gram-positive bacteria. Processes for the preparation of these novel compounds are also described.

公开(公告)号：US5128465A

公开(公告)日：1992-07-07

申请号：US468319

申请日：1990-01-22

申请人： Takashi Kamiya ,  Toshihiko Naito ,  Yuuki Komatu ,  Yasunobu Kai ,  Takaharu Nakamura ,  Manabu Sasho ,  Shigeto Negi ,  Isao Sugiyama ,  Kanemasa Katsu ,  Hiroshi Yamauchi

发明人： Takashi Kamiya ,  Toshihiko Naito ,  Yuuki Komatu ,  Yasunobu Kai ,  Takaharu Nakamura ,  Manabu Sasho ,  Shigeto Negi ,  Isao Sugiyama ,  Kanemasa Katsu ,  Hiroshi Yamauchi

IPC分类号： C07D498/04 ,  C07C237/06 ,  C07D498/08 ,  C07D501/00 ,  C07D501/18 ,  C07D501/24 ,  C07D501/46 ,  C07D501/56 ,  C07D519/00

CPC分类号： C07D498/08 ,  C07C237/06 ,  C07D501/00 ,  Y02P20/55

摘要： A cephem derivative represented by the following formula: ##STR1## wherein R.sub.1 means a fluorine-substituted lower alkyl and A.sub.1 denotes a cyclic or acyclic ammonio group, or a non-toxic salt thereof, is prepared by reacting a compound represented by the following formula: ##STR2## wherein A.sub.1 has the same meaning as defined above, with another compound represented by the following formula: ##STR3## wherein R.sub.1 has the same meaning as defined above, and if necessary, removing the protecting groups.

摘要翻译： 由下式表示的头孢烯衍生物：其中R1表示氟取代的低级烷基，A1表示环状或无环氨基，或其无毒盐，通过使下式表示的化合物 其中A 1具有与上述定义相同的含义，另外由下式表示的化合物：其中R 1具有与上述相同的含义，如有必要，除去保护基。

公开(公告)号：US5373000A

公开(公告)日：1994-12-13

申请号：US861717

申请日：1992-04-01

申请人： Yoshimasa Machida ,  Takashi Kamiya ,  Shigeto Negi ,  Toshihiko Naito ,  Yuuki Komatu ,  Seiichiro Nomoto ,  Isao Sugiyama ,  Hiroshi Yamauchi

发明人： Yoshimasa Machida ,  Takashi Kamiya ,  Shigeto Negi ,  Toshihiko Naito ,  Yuuki Komatu ,  Seiichiro Nomoto ,  Isao Sugiyama ,  Hiroshi Yamauchi

IPC分类号： A61K31/545 ,  C07D501/24 ,  C07D501/34

CPC分类号： C07D501/24

摘要： A cephalosporin derivative represented by the formula: ##STR1## wherein R.sub.1 represents a lower alkyl group, and A is selected from: a group of the following formula: ##STR2## where R.sub.2 and R.sub.3 are the same or different lower alkyl group, R.sub.4 represents a substituted lower alkyl or amino group;a group which may be substituted and which is represented by the following formula: ##STR3## where R.sub.5 represents a lower alkyl group; or a group of the following formula: ##STR4## where R.sub.5 is as defined above, R.sub.6 represents a hydroxyl lower alkyl or carboxyl group, or its pharmacologically acceptable salt, and a process for preparing the same, as well as an antibacterial agent containing the same.

摘要翻译： 由下式表示的头孢菌素衍生物：其中R 1表示低级烷基，A选自：下式的基团：其中R 2和R 3是相同或不同的低级烷基，R 4表示 取代的低级烷基或氨基; 可以被取代并由下式表示的基团：其中R 5表示低级烷基; 或下式的基团：其中R 5如上定义，R 6表示羟基低级烷基或羧基或其药理学上可接受的盐，以及其制备方法，以及含有 相同。

公开(公告)号：US4698336A

公开(公告)日：1987-10-06

申请号：US821914

申请日：1986-01-23

申请人： Isao Saito ,  Seiichiro Nomoto ,  Takashi Kamiya ,  Hiroshi Yamauchi ,  Isao Sugiyama ,  Yoshimasa Machida ,  Shigeto Negi

发明人： Isao Saito ,  Seiichiro Nomoto ,  Takashi Kamiya ,  Hiroshi Yamauchi ,  Isao Sugiyama ,  Yoshimasa Machida ,  Shigeto Negi

IPC分类号： A61K31/545 ,  C07D20060101 ,  C07D501/04 ,  C07D501/46

CPC分类号： C07D501/46

摘要： Described herein is 3-(pyrrolidinio)methyl-3-cephem derivative represented by the general formula: ##STR1## wherein Y stands for CH or nitrogen atom, R.sub.1 and R.sub.2 are the same or different, and represent a lower alkyl group, R.sub.3 denotes a hydroxy-substituted lower alkyl group, a lower alkyl group, or a carbamoyl group, and when Y stands for CH, R.sub.3 denotes a hydroxy-substituted lower alkyl group. The derivative is useful as antibacterial composition. Also described herein are process for the production of the derivative and antibacterial composition.

摘要翻译： 本文描述的是由以下通式表示的3-（吡咯烷基）甲基-3-头孢烯衍生物：其中Y代表CH或氮原子，R1和R2相同或不同，代表低级烷基，R3表示 羟基取代的低级烷基，低级烷基或氨基甲酰基，当Y代表CH时，R3表示羟基取代的低级烷基。 该衍生物可用作抗菌组合物。 本文还描述了制备衍生物和抗菌组合物的方法。

公开(公告)号：US4748171A

公开(公告)日：1988-05-31

申请号：US818824

申请日：1986-01-14

申请人： Hiroshi Yamauchi ,  Isao Sugiyama ,  Isao Saito ,  Seiichiro Nomoto ,  Takashi Kamiya ,  Yoshimasa Machida ,  Shigeto Negi

发明人： Hiroshi Yamauchi ,  Isao Sugiyama ,  Isao Saito ,  Seiichiro Nomoto ,  Takashi Kamiya ,  Yoshimasa Machida ,  Shigeto Negi

IPC分类号： C07D471/08 ,  C07D501/46 ,  A61K31/54

CPC分类号： C07D471/08

摘要： Described herein is a cephem derivative represented by the general formula: ##STR1## wherein n stands for 1 or 2, Y stands for CH or nitrogen atoms, R.sub.1 represents a lower hydrocarbon group or a carboxyl-substituted, a carbamoyl-substituted, or a cyclopropyl-substituted lower alkyl group, and R.sub.2 denotes hydroxyl group, a lower alkyl group, a hydroxy-substituted lower alkyl group, or carbamoyl group. The derivative is useful as an antibacterial agent. Also described herein are processes for the production of the derivative, antibacterial composition, intermediate of the derivative and process for the production thereof.

摘要翻译： 本文描述的是由以下通式表示的头孢烯衍生物：其中n代表1或2，Y代表CH或氮原子，R 1代表低级烃基或羧基取代的氨基甲酰基 取代或环丙基取代的低级烷基，R 2表示羟基，低级烷基，羟基取代的低级烷基或氨基甲酰基。 该衍生物可用作抗菌剂。 本文还描述了制备衍生物，抗菌组合物，衍生物的中间体及其制备方法的方法。

公开(公告)号：US5010188A

公开(公告)日：1991-04-23

申请号：US167152

申请日：1988-03-16

申请人： Hiroshi Yamauchi ,  Isao Sugiyama ,  Isao Saito ,  Seiichiro Nomoto ,  Takashi Kamiya ,  Yoshimasa Machida ,  Shigeto Negi

发明人： Hiroshi Yamauchi ,  Isao Sugiyama ,  Isao Saito ,  Seiichiro Nomoto ,  Takashi Kamiya ,  Yoshimasa Machida ,  Shigeto Negi

IPC分类号： C07D471/08 ,  C07D501/46

CPC分类号： C07D471/08

摘要： Described herein is a cephem derivative represented by the general formula: ##STR1## wherein n stands for 1 or 2, Y stands for CH or nitrogen atom, R.sub.1 represents a lower hydrocarbon group or a carboxyl-substituted, a carbamoyl-substituted, or a cyclopropyl-substituted lower alkyl group, and R.sub.2 denotes hydroxyl group, a lower alkyl group, a hydroxy-substituted lower alkyl group, or carbamoyl group. The derivative is useful as an antibacterial composition. Also described herein are processes for the production of the derivative, antibacterial composition, intermediate of the derivative and process for the production thereof.

公开(公告)号：US5008260A

公开(公告)日：1991-04-16

申请号：US167153

申请日：1988-03-16

申请人： Hiroshi Yamauchi ,  Isao Sugiyama ,  Isao Saito ,  Seiichiro Nomoto ,  Takashi Kamiya ,  Yoshimasa Machida ,  Shigeto Negi

发明人： Hiroshi Yamauchi ,  Isao Sugiyama ,  Isao Saito ,  Seiichiro Nomoto ,  Takashi Kamiya ,  Yoshimasa Machida ,  Shigeto Negi

IPC分类号： C07D471/08 ,  C07D501/46

CPC分类号： C07D471/08

摘要： Described herein is a cephem derivative represented by the general formula: ##STR1## wherein n stands for 1 or 2, Y stands for CH or nitrogen atom, R.sub.1 represents a lower hydrocarbon group or a carboxyl-substituted, a carbamoyl-substituted, or a cyclopropyl-substituted lower alkyl group, and R.sub.2 denotes hydroxyl group, a lower alkyl group, a hydroxy-substituted lower alkyl group, or carbamoyl group. The derivative is useful as an antibacterial agent. Also described herein are processes for the production of the derivative, antibacterial composition, intermediate of the derivative and process for the production thereof.