公开(公告)号：US4513145A

公开(公告)日：1985-04-23

申请号：US457394

申请日：1983-01-12

申请人： Shigeto Negi ,  Seiichiro Nomoto ,  Takashi Kamiya ,  Yoshimasa Machida ,  Isao Saito ,  Kyosuke Kitoh

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

IPC分类号： C07D311/22 ,  C07D501/36

CPC分类号： C07D311/22

摘要： A novel 2-methylchromone derivative represented by the general formula: ##STR1## wherein R.sub.1 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.

摘要翻译： 由通式（I）表示的新型2-甲基色酮衍生物，其中R 1表示氢原子或低级烷酰基。 上述衍生物是合成头孢烯活性的有用中间体，其也有效地抵抗尿道感染等。上述色酮衍生物的制备方法也被公开。

公开(公告)号：US4546176A

公开(公告)日：1985-10-08

申请号：US544406

申请日：1983-10-20

申请人： Yoshimasa Machida ,  Shigeto Negi ,  Seiichiro Nomoto ,  Takashi Kamiya ,  Kyosuke Kitoh ,  Isao Saito

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

IPC分类号： C07D311/22 ,  C07D405/12 ,  C07D501/04 ,  C07D501/24 ,  C07D501/34 ,  C07D501/36 ,  C07D501/46 ,  C07D501/57 ,  C07D501/00 ,  A61K31/54 ,  C07D501/14

CPC分类号： C07D405/12 ,  C07D311/22

摘要： 7-Carboxymethoxyphenylacetamido-3-cephem derivatives represented by the formula ##STR1## wherein R.sub.1 means hydroxy, C.sub.1 -C.sub.4 alkanoyloxy or C.sub.1 -C.sub.4 alkoxycarbonyloxy, R.sub.2 is hydrogen or methoxy, R.sub.3 denotes C.sub.1 -C.sub.4 alkanoyloxy, substituted or unsubstituted nitrogen-containing heterocyclic-thio or substituted or unsubstituted pyridinium with a proviso that, when R.sub.3 denotes the substituted or unsubstituted pyridinium, R.sub.3 forms an intramolecular salt with the carboxy at the 4-position of the cephem nucleus, and A is a group of the following formula: ##STR2## in which R.sub.4 and R.sub.5 are individually hydrogen or C.sub.1 -C.sub.4 alkyl, and their pharmaceutically acceptable salts, exhibit excellent anti-bacterial activities against Gram-negative bacteria, particularly, Pseud. aeruginosa, Kleb. pneumoniae, Ser. marcescens and the like.

摘要翻译： 其中R 1表示羟基，C 1 -C 4烷酰氧基或C 1 -C 4烷氧羰基氧基，R 2为氢或甲氧基，R 3表示C 1 -C 4烷酰氧基，取代或未取代的含氮杂环基 硫代或取代或未取代的吡啶鎓，条件是当R3表示取代或未取代的吡啶鎓时，R3与头孢烯核的4位上的羧基形成分子内的盐，A是下式的基团： 其中R 4和R 5独立地为氢或C 1 -C 4烷基及其药学上可接受的盐，对抗革兰氏阴性细菌，特别是Pseude显示出优异的抗细菌活性。 铜绿假单胞菌 肺炎支原体 粘液囊等。

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：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：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：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：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.

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.