公开(公告)号：US4489072A

公开(公告)日：1984-12-18

申请号：US304912

申请日：1981-09-23

申请人： Hiroshi Sadaki ,  Hirokazu Narita ,  Hiroyuki Imaizumi ,  Yoshinori Konishi ,  Takihiro Inaba ,  Tatsuo Hirakawa ,  Hideo Taki ,  Masaru Tai ,  Yasuo Watanabe ,  Isamu Saikawa

发明人： Hiroshi Sadaki ,  Hirokazu Narita ,  Hiroyuki Imaizumi ,  Yoshinori Konishi ,  Takihiro Inaba ,  Tatsuo Hirakawa ,  Hideo Taki ,  Masaru Tai ,  Yasuo Watanabe ,  Isamu Saikawa

IPC分类号： C07D501/24 ,  A61K31/545 ,  C07D20060101 ,  C07D501/04 ,  C07D501/18 ,  C07D501/20 ,  C07D501/38 ,  C07D501/40 ,  C07D501/46 ,  C07D501/56 ,  C07D501/57

CPC分类号： C07D501/46 ,  A61K31/545 ,  C07D501/38 ,  C07D501/56 ,  C07D501/57

摘要： Novel cephalosporins which has attached to the exomethylene group at the 3-position of the cephem ring a substituted or unsubstituted aryl, acylamino, aromatic heterocyclic, triazolyl or tetrazolyl group, said aromatic heterocyclic group being attached through a carbon-carbon bond and said triazolyl or tetrazolyl group being attached through a carbon-nitrogen bond, and has the following group attached to the amino group at the 7-position: ##STR1## wherein A represents a group of the formula, --CH.sub.2 -- or a group of the formula ##STR2## in which R.sup.5 represents a hydrogen atom or an alkyl group, and the bond represents syn or anti isomer or their mixture; R.sup.3 represents a hydrogen or halogen atom; and R.sup.4 represents a hydrogen atom or an amino group which may be protected or substituted. These cephalosporins have a broad antibacterial spectrum, are stable against .beta.-lactamase produced by bacteria, have a low toxicity, and are well absorbed when administered orally or parenterally.This invention relates to such novel cephalosporins, processes for producing said cephalosporins, intermediates for producing said cephalosporins, and a process for producing said intermediates.

摘要翻译： 在头孢烯环的3位连接到外亚甲基的新型头孢菌素是取代或未取代的芳基，酰氨基，芳族杂环，三唑基或四唑基，所述芳族杂环基通过碳 - 碳键连接，所述三唑基或 四唑基通过碳 - 氮键连接，并且具有与7-位上的氨基连接的下列基团：其中A表示下式的基团：-CH 2 - 或式 其中R 5表示氢原子或烷基，并且该键表示顺式或反式异构体或其混合物; R3表示氢或卤素原子; R4表示氢原子或可被保护或取代的氨基。 这些头孢菌素具有广泛的抗菌谱，对细菌产生的β-内酰胺酶是稳定的，具有低毒性，并且当口服或肠胃外给药时被良好吸收。 本发明涉及这种新型头孢菌素，生产所述头孢菌素的方法，用于生产所述头孢菌素的中间体，以及生产所述中间体的方法。

公开(公告)号：US4673738A

公开(公告)日：1987-06-16

申请号：US654681

申请日：1984-09-26

申请人： Hiroshi Sadaki ,  Hirokazu Narita ,  Hiroyuki Imaizumi ,  Yoshinori Konishi ,  Takihiro Inaba ,  Tatsuo Hirakawa ,  Hideo Taki ,  Masaru Tai ,  Yasuo Watanabe ,  Isamu Saikawa

发明人： Hiroshi Sadaki ,  Hirokazu Narita ,  Hiroyuki Imaizumi ,  Yoshinori Konishi ,  Takihiro Inaba ,  Tatsuo Hirakawa ,  Hideo Taki ,  Masaru Tai ,  Yasuo Watanabe ,  Isamu Saikawa

IPC分类号： C07D501/24 ,  A61K31/545 ,  C07D20060101 ,  C07D501/04 ,  C07D501/18 ,  C07D501/20 ,  C07D501/38 ,  C07D501/40 ,  C07D501/46 ,  C07D501/56 ,  C07D501/57

CPC分类号： C07D501/46 ,  A61K31/545 ,  C07D501/38 ,  C07D501/56 ,  C07D501/57

摘要： This invention relates to novel 7-(substituted or unsubstituted amino)-3-substituted methyl-.DELTA..sup.3 -cephem-4-carboxylic acids in which a substituted or unsubstituted 1,2,4-triazolyl or 2-(1,2,3,4-tetrazolyl) group attaches to the exomethylene group at the 3-position of the cephem ring through a carbon-nitrogen bond. These cephalosporins are useful intermediates for producing various novel cephalosporins. Also, this invention concerns a process for producing a compound represented by the formula: ##STR1## which comprises reacting a compound represented by the formula: ##STR2## with an optionally substituted triazole or tetrazole in the presence of an acid or a complex of the acid in an organic solvent at 0.degree. to 80.degree. C.

摘要翻译： 本发明涉及新的7-（取代或未取代的氨基）-3-取代的甲基-D-三头孢烯-4-羧酸，其中取代或未取代的1,2,4-三唑基或2-（1,2,3 ，4-四唑基）基团通过碳 - 氮键连接在头孢烯环的3-位上的外亚甲基基团。 这些头孢菌素是生产各种新型头孢菌素的有用中间体。 此外，本发明涉及一种制备由下式表示的化合物的方法：该方法包括使下式表示的化合物与任选取代的三唑或四唑在酸或其复合物的存在下反应： 酸在有机溶剂中于0〜80℃

公开(公告)号：US5144027A

公开(公告)日：1992-09-01

申请号：US707221

申请日：1991-05-24

申请人： Hiroshi Sadaki ,  Hirokazu Narita ,  Hiroyuki Imaizumi ,  Yoshinori Konishi ,  Takihiro Inaba ,  Tatsuo Hirakawa ,  Hideo Taki ,  Masaru Tai ,  Yasuo Watanabe ,  Isamu Saikawa

发明人： Hiroshi Sadaki ,  Hirokazu Narita ,  Hiroyuki Imaizumi ,  Yoshinori Konishi ,  Takihiro Inaba ,  Tatsuo Hirakawa ,  Hideo Taki ,  Masaru Tai ,  Yasuo Watanabe ,  Isamu Saikawa

IPC分类号： C07D501/24 ,  A61K31/545 ,  C07D20060101 ,  C07D501/04 ,  C07D501/18 ,  C07D501/20 ,  C07D501/38 ,  C07D501/40 ,  C07D501/46 ,  C07D501/56 ,  C07D501/57

CPC分类号： C07D501/46 ,  A61K31/545 ,  C07D501/38 ,  C07D501/56 ,  C07D501/57

摘要： Novel cephalosporins which has attached to the exomethylene group at the 3-position of the cephem ring a substituted or unsubstituted aryl, acylamino, aromatic heterocyclic, triazolyl or tetrazolyl group, said aromatic heterocyclic group being attached through a carbon-carbon bond and said triazolyl or tetrazolyl group being attached through a carbon-nitrogen bond, and has the following group attached to the amino group at the 7-position: ##STR1## wherein A represents a group of the formula, --CH.sub.2 -- or a group of the formula ##STR2## in which R.sup.5 represents a hydrogen atom or an alkyl group, and the bond.about.represents syn or anti isomer or their mixture; R.sup.3 represents a hydrogen or halogen atom; and R.sup.4 represents a hydrogen atom or an amino group which may be protected or substituted. These cephalosporins have a broad antibacterial spectrum, are stable against .beta.-lactamase produced by bacteria, have a low toxicity, and are well absorbed when administered orally or parenterally.

摘要翻译： 在头孢烯环的3位连接到外亚甲基的新型头孢菌素是取代或未取代的芳基，酰氨基，芳族杂环，三唑基或四唑基，所述芳族杂环基通过碳 - 碳键连接，所述三唑基或 四唑基通过碳 - 氮键连接，并且具有与7-位上的氨基连接的下列基团：其中A表示下式的基团：-CH 2 - 或式 其中R 5表示氢原子或烷基，并且键差D代表顺式或反式异构体或其混合物; R3表示氢或卤素原子; R4表示氢原子或可被保护或取代的氨基。 这些头孢菌素具有广泛的抗菌谱，对细菌产生的β-内酰胺酶是稳定的，具有低毒性，并且当口服或肠胃外给药时被良好吸收。

公开(公告)号：US4879381A

公开(公告)日：1989-11-07

申请号：US22433

申请日：1987-03-06

申请人： Hiroshi Sadaki ,  Narita Hirokazu ,  Hiroyuki Imaizumi ,  Yoshinori Konishi ,  Takihiro Inaba ,  Tatsuo Hirakawa ,  Hideo Taki ,  Masaru Tai ,  Yasuo Watanabe ,  Isamu Saikawa

发明人： Hiroshi Sadaki ,  Narita Hirokazu ,  Hiroyuki Imaizumi ,  Yoshinori Konishi ,  Takihiro Inaba ,  Tatsuo Hirakawa ,  Hideo Taki ,  Masaru Tai ,  Yasuo Watanabe ,  Isamu Saikawa

IPC分类号： C07D501/24 ,  A61K31/545 ,  C07D20060101 ,  C07D501/04 ,  C07D501/18 ,  C07D501/20 ,  C07D501/38 ,  C07D501/40 ,  C07D501/46 ,  C07D501/56 ,  C07D501/57

CPC分类号： C07D501/46 ,  A61K31/545 ,  C07D501/38 ,  C07D501/56 ,  C07D501/57

摘要： Novel cephalosporins which has attached to the exomethylene group at the 3-position of the cephem ring a substituted or unsubstituted aryl, acylamino, aromatic heterocyclic, triazolyl or tetrazolyl group, said aromatic heterocyclic group being attached through a carbon-carbon bond and said triazolyl or tetrazolyl group being attached through a carbon-nitrogen bond, and has the following group attached to the amino group at the 7-position: ##STR1## wherein A represents a group of the formula, --CH.sub.2 -- or a group of the formula ##STR2## in which R.sup.5 represents a hydrogen atom or an alkyl group, and the bond represents syn or anti isomer or their mixture; R.sup.3 represents a hydrogen or halogen atom; and R.sup.4 represents a hydrogen atom or an amino group which may be protected or substituted. These cephalosporins have a broad antibacterial spectrum, are stable against .beta.-lactamase produced by bacteria, have a low toxicity, and are well absorbed when administered orally or parenterally.

摘要翻译： 在头孢烯环的3位连接到外亚甲基上的新型头孢菌素取代或未取代的芳基，酰氨基，芳族杂环，三唑基或四唑基，所述芳族杂环基通过碳 - 碳键连接，所述三唑基或 四唑基通过碳 - 氮键连接，并且具有与7-位上的氨基连接的下列基团：其中A表示下式的基团：-CH 2 - 或式 其中R 5表示氢原子或烷基，并且该键表示顺式或反式异构体或其混合物; R3表示氢或卤素原子; R4表示氢原子或可被保护或取代的氨基。 这些头孢菌素具有广泛的抗菌谱，对细菌产生的β-内酰胺酶是稳定的，具有低毒性，并且当口服或肠胃外给药时被良好吸收。