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：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：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：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：US5151417A

公开(公告)日：1992-09-29

申请号：US550365

申请日：1990-07-10

申请人： Manabu Sasho ,  Hiroshi Yamauchi ,  Motosuke Yamanaka ,  Takaharu Nakamura ,  Kanemasa Katsu ,  Isao Sugiyama ,  Yuuki Komatu ,  Shigeto Negi

发明人： Manabu Sasho ,  Hiroshi Yamauchi ,  Motosuke Yamanaka ,  Takaharu Nakamura ,  Kanemasa Katsu ,  Isao Sugiyama ,  Yuuki Komatu ,  Shigeto Negi

IPC分类号： A61K31/545 ,  C07D20060101 ,  C07D501/00 ,  C07D501/22 ,  C07D501/24 ,  C07D501/34 ,  C07D501/56

CPC分类号： C07D501/00 ,  Y02P20/55

摘要： 3-Substituted vinyl cephalosporin derivatives represented by the following formula: ##STR1## wherein R.sup.1 represents a hydroxyl or lower alkoxyl group, X represents a nitrogen atom or a group represented by the formula --CH.dbd., R.sup.2 represents a carboxyl group or a carboxyl group protected with a protecting group, and R.sup.3 is as defined herein, and pharmaceutically acceptable salts thereof are potent antibacterial agents. Processes for their preparation, intermediates in such processes, and antibacterial compositions containing them as active ingredients are also described.

公开(公告)号：US5604217A

公开(公告)日：1997-02-18

申请号：US463353

申请日：1995-06-05

申请人： Shigeto Negi ,  Motosuke Yamanaka ,  Kanemasa Katsu ,  Isao Sugiyama ,  Yuuki Komatu ,  Atsushi Kamata ,  Akihiko Tsuruoka ,  Yoshimasa Machida

发明人： Shigeto Negi ,  Motosuke Yamanaka ,  Kanemasa Katsu ,  Isao Sugiyama ,  Yuuki Komatu ,  Atsushi Kamata ,  Akihiko Tsuruoka ,  Yoshimasa Machida

IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D501/00 ,  C07D501/04 ,  C07D501/06 ,  C07D501/18 ,  C07D501/26 ,  C07D501/28 ,  C07D501/34 ,  C07D501/36

CPC分类号： C07D501/00

摘要： A 7-acyl-3-substituted carbamoyloxy cephem compound represented by the following formula (1): ##STR1## wherein A means a --CH.dbd. or --N.dbd. group; R.sup.1 denotes a hydroxyl, lower alkoxyl, fluorine-substituted lower alkoxyl or protected hydroxyl group; R.sup.2 and R.sup.3 are the same or different and individually represent a lower alkyl, hydroxyl-substituted lower alkyl, a carbamoyl-substituted lower alkyl group or cyano-substituted lower alkyl group, R.sup.2 is a hydrogen atom and R.sup.3 is a lower alkoxyl or alkyl group optionally substituted by one or more halogen atoms or the group ##STR2## means a 4-6 membered heterocyclic group, which contains one nitrogen atom, or a morpholino group, said heterocyclic group or morpholino group being optionally substituted by one or more lower alkyl, hydroxyl and/or hydroxyl-substituted lower alkyl groups; and R.sup.4 denotes a carboxyl or protected carboxyl group; or a pharmaceutically acceptable salt thereof; and a process for the preparation thereof; as well as an antibacterial composition containing the above cephem compound.

摘要翻译： 由下式（1）表示的7-酰基-3-取代氨基甲酰氧基头孢烯化合物：其中A表示-CH =或-N =基团; R1表示羟基，低级烷氧基，氟取代的低级烷氧基或被保护的羟基; R2和R3相同或不同，分别表示低级烷基，羟基取代的低级烷基，氨基甲酰取代的低级烷基或氰基取代的低级烷基，R2是氢原子，R3是低级烷氧基或烷基 任选地被一个或多个卤素原子取代，或者“IMAGE”是指含有一个氮原子或吗啉基的4-6元杂环基，所述杂环基或吗啉基任选被一个或多个低级烷基取代， 羟基和/或羟基取代的低级烷基; R4表示羧基或被保护的羧基; 或其药学上可接受的盐; 及其制备方法; 以及含有上述头孢烯化合物的抗菌组合物。

公开(公告)号：US5587473A

公开(公告)日：1996-12-24

申请号：US671342

申请日：1996-06-27

申请人： Shigeto Negi ,  Motosuke Yamanaka ,  Kanemasa Katsu ,  Isao Sugiyama ,  Yuuki Komatu ,  Atsushi Kamata ,  Akihiko Tsuruoka ,  Yoshimasa Machida

发明人： Shigeto Negi ,  Motosuke Yamanaka ,  Kanemasa Katsu ,  Isao Sugiyama ,  Yuuki Komatu ,  Atsushi Kamata ,  Akihiko Tsuruoka ,  Yoshimasa Machida

IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D501/00 ,  C07D501/04 ,  C07D501/06 ,  C07D501/18 ,  C07D501/26 ,  C07D501/28 ,  C07D501/34 ,  C07D501/36 ,  C07D501/22

CPC分类号： C07D501/00

摘要： A 7-acyl-3-substituted carbamoyloxy cephem compound represented by the following formula (1): ##STR1## wherein A means a --CH.dbd. or --N.dbd. group; R.sup.1 denotes a hydroxyl, lower alkoxyl, fluorine-substituted lower alkoxyl or protected hydroxyl group; R.sup.2 and R.sup.3 are the same or different and individually represent a lower alkyl, hydroxyl-substituted lower alkyl, a carbamoyl-substituted lower alkyl group or cyano-substituted lower alkyl group, R.sup.2 is a hydrogen atom and R.sup.3 is a lower alkoxyl or alkyl group optionally substituted by one or more halogen atoms, or the group ##STR2## means a 4-6 membered heterocyclic group, which contains one nitrogen atom, or a morpholino group, said heterocyclic group or morpholino group being optionally substituted by one or more lower alkyl, hydroxyl and/or hydroxyl-substituted lower alkyl groups; and R.sup.4 denotes a carboxyl or protected carboxyl group; or a pharmaceutically acceptable salt thereof; and a process for the preparation thereof; as well as an antibacterial composition containing the above cephem compound.

摘要翻译： 由下式（1）表示的7-酰基-3-取代氨基甲酰氧基头孢烯化合物：其中A表示-CH =或-N =基团; R1表示羟基，低级烷氧基，氟取代的低级烷氧基或被保护的羟基; R2和R3相同或不同，分别表示低级烷基，羟基取代的低级烷基，氨基甲酰取代的低级烷基或氰基取代的低级烷基，R2是氢原子，R3是低级烷氧基或烷基 任选地被一个或多个卤素原子取代，或者“IMAGE”是指含有一个氮原子或吗啉基的4-6元杂环基，所述杂环基或吗啉基任选被一个或多个低级烷基 ，羟基和/或羟基取代的低级烷基; R4表示羧基或被保护的羧基; 或其药学上可接受的盐; 及其制备方法; 以及含有上述头孢烯化合物的抗菌组合物。

公开(公告)号：US5741902A

公开(公告)日：1998-04-21

申请号：US464341

申请日：1995-06-05

申请人： Shigeto Negi ,  Motosuke Yamanaka ,  Kanemasa Katsu ,  Isao Sugiyama ,  Yuuki Komatu ,  Atsushi Kamata ,  Akihiko Tsuruoka ,  Yoshimasa Machida

发明人： Shigeto Negi ,  Motosuke Yamanaka ,  Kanemasa Katsu ,  Isao Sugiyama ,  Yuuki Komatu ,  Atsushi Kamata ,  Akihiko Tsuruoka ,  Yoshimasa Machida

IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D501/00 ,  C07D501/04 ,  C07D501/06 ,  C07D501/18 ,  C07D501/26 ,  C07D501/28 ,  C07D501/34 ,  C07D501/36 ,  C07D501/40

CPC分类号： C07D501/00

摘要： A 7-acyl-3-substituted carbamoyloxy cephem compound represented by the following formula (1): ##STR1## wherein A means a --CH.dbd. or --N.dbd. group; R.sup.1 denotes a hydroxyl, lower alkoxyl, fluorine-substituted lower alkoxyl or protected hydroxyl group; R.sup.2 and R.sup.3 are the same or different and individually represent a lower alkyl, hydroxyl-substituted lower alkyl, a carbamoyl-substituted lower alkyl group or cyano-substituted lower alkyl group, R.sup.2 is a hydrogen atom and R.sup.3 is a lower alkoxyl or alkyl group optionally substituted by one or more halogen atoms, or the group ##STR2## means a 4-6 membered heterocyclic group, which contains one nitrogen atom, or a morpholino group, said heterocyclic group or morpholino group being optionally substituted by one or more lower alkyl, hydroxyl and/or hydroxyl-substituted lower alkyl groups; and R.sup.4 denotes a carboxyl or protected carboxyl group; or a pharmaceutically acceptable salt thereof; and a process for the preparation thereof; as well as an antibacterial composition containing the above cephem compound.

公开(公告)号：US5563265A

公开(公告)日：1996-10-08

申请号：US393074

申请日：1995-02-23

申请人： Shigeto Negi ,  Motosuke Yamanaka ,  Kanemasa Katsu ,  Isao Sugiyama ,  Yuuki Komatu ,  Atsushi Kamata ,  Akihiko Tsuruoka ,  Yoshimasa Machida

发明人： Shigeto Negi ,  Motosuke Yamanaka ,  Kanemasa Katsu ,  Isao Sugiyama ,  Yuuki Komatu ,  Atsushi Kamata ,  Akihiko Tsuruoka ,  Yoshimasa Machida

IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D501/00 ,  C07D501/04 ,  C07D501/06 ,  C07D501/18 ,  C07D501/26 ,  C07D501/28 ,  C07D501/34 ,  C07D501/36 ,  C07D501/60

CPC分类号： C07D501/00

摘要： A 7-acyl-3-substituted carbamoyloxy cephem compound represented by the following formula (1): ##STR1## wherein A means a --CH.dbd. or --N.dbd. group; R.sup.1 denotes a hydroxyl, lower alkoxyl, fluorine-substituted lower alkoxyl or protected hydroxyl group; R.sup.2 and R.sup.3 are the same or different and individually represent a lower alkyl, hydroxyl-substituted lower alkyl, a carbamoyl-substituted lower alkyl group or cyano-substituted lower alkyl group, R.sup.2 is a hydrogen atom and R.sup.3 is a lower alkoxyl or alkyl group optionally substituted by one or more halogen atoms, or the group ##STR2## means a 4-6 membered heterocyclic group, which contains one nitrogen atom, or a morpholino group, said heterocyclic group or morpholino group being optionally substituted by one or more lower alkyl, hydroxyl and/or hydroxyl-substituted lower alkyl groups; and R.sup.4 denotes a carboxyl or protected carboxyl group; or a pharmaceutically acceptable salt thereof; and a process for the preparation thereof; as well as an antibacterial composition containing the above cephem compound.

摘要翻译： 由下式（1）表示的7-酰基-3-取代氨基甲酰氧基头孢烯化合物：其中A表示-CH =或-N =基团; R1表示羟基，低级烷氧基，氟取代的低级烷氧基或被保护的羟基; R2和R3相同或不同，分别表示低级烷基，羟基取代的低级烷基，氨基甲酰取代的低级烷基或氰基取代的低级烷基，R2是氢原子，R3是低级烷氧基或烷基 任选地被一个或多个卤素原子取代，或者“IMAGE”是指含有一个氮原子或吗啉基的4-6元杂环基，所述杂环基或吗啉基任选被一个或多个低级烷基 ，羟基和/或羟基取代的低级烷基; R4表示羧基或被保护的羧基; 或其药学上可接受的盐; 及其制备方法; 以及含有上述头孢烯化合物的抗菌组合物。