公开(公告)号：US4352801A

公开(公告)日：1982-10-05

申请号：US218402

申请日：1980-12-19

申请人： Seiichiro Nomoto ,  Hironori Ikuta ,  Yoshimasa Machida ,  Shigeto Negi ,  Isao Sugiyama ,  Hiroshi Yamauchi ,  Kenro Nakatsuka ,  Isao Saito

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

IPC分类号： C07D501/34 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D311/22 ,  C07D501/24 ,  C07D501/36

CPC分类号： C07D311/22

摘要： Cephem derivatives represented by the formula: ##STR1## wherein R.sub.1 represents a hydrogen atom or a hydroxyl group, R.sub.2 represents a lower alkyl group or a chloro-substituted lower alkyl group, and R.sub.3 represents a lower alkanoyloxy group or a nitrogen-containing heterocyclic thio group,and the pharmaceutically acceptable salts thereof. The cephem derivatives exhibit excellent antibacterial activity and are effective against Gram-positive and Gram-negative bacteria.

公开(公告)号：US4331606A

公开(公告)日：1982-05-25

申请号：US218404

申请日：1980-12-19

申请人： Seiichiro Nomoto ,  Hironori Ikuta ,  Yoshimasa Machida ,  Shigeto Negi ,  Isao Sugiyama ,  Hiroshi Yamauchi ,  Takeo Kanai ,  Isao Saito

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

IPC分类号： C07D311/22 ,  C07D501/36 ,  C07D311/24

CPC分类号： C07D311/22

摘要： N-(Substituted chromone-3-carbonyl)phenylglycine derivatives. These derivatives are useful intermediates for cephem compounds which are excellent as antibacterial agents.

摘要翻译： N-（取代的色酮-3-羰基）苯基甘氨酸衍生物。 这些衍生物是作为抗菌剂优异的头孢烯化合物的有用的中间体。

公开(公告)号：US4309354A

公开(公告)日：1982-01-05

申请号：US218403

申请日：1980-12-19

申请人： Seiichiro Nomoto ,  Hironori Ikuta ,  Yoshimasa Machida ,  Shigeto Negi ,  Isao Sugiyama ,  Hiroshi Yamauchi ,  Kenro Nakatsuka ,  Isao Saito

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

IPC分类号： C07D501/34 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D311/22 ,  C07D501/24 ,  C07D501/36

CPC分类号： C07D311/22

摘要： New chromone derivatives having the formula: ##STR1## wherein A represents a hydrogen atom, a halogen atom or a hydroxyl group, and R.sub.1 represents a lower alkyl or a chloro-substituted lower alkyl group. The derivatives are useful intermediates for synthesis of cephem derivatives as antibacterial drugs.

摘要翻译： 具有下式的新色酮衍生物：其中A表示氢原子，卤素原子或羟基，R 1表示低级烷基或氯取代的低级烷基。 该衍生物是合成头孢烯衍生物作为抗菌药物的有用中间体。

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。

公开(公告)号：US5559225A

公开(公告)日：1996-09-24

申请号：US209484

申请日：1994-03-14

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 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：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。