公开(公告)号：US4079060A

公开(公告)日：1978-03-14

申请号：US727382

申请日：1976-09-27

申请人： Yutaka Kuwada ,  Kanji Meguro ,  Yoshiaki Sato ,  Takeshi Fugono

发明人： Yutaka Kuwada ,  Kanji Meguro ,  Yoshiaki Sato ,  Takeshi Fugono

IPC分类号： C07D495/04 ,  C07D495/14

CPC分类号： C07D495/04

摘要： Novel thienopyridine-carboxylic acid derivatives, which are shown by the general formula ##STR1## wherein R.sup.1 represents hydrogen or a lower alkyl; R.sup.2 represents hydrogen, a lower alkyl or a halogen, or R.sup.1 and R.sup.2, taken together, may represent an alkylene to form a 5- or 6-membered ring with or without alkyl substituents; each of R.sup.4 and R.sup.5 represents hydrogen or a lower alkyl; and their pharmaceutically acceptable salts obtainable when R.sup.4 is hydrogen, which are useful medicines such as chemotherapeutic agents of bacterial infections.

摘要翻译： 新的噻吩并吡啶 - 羧酸衍生物，其通式为：其中R 1表示氢或低级烷基; R 2表示氢，低级烷基或卤素，或者R 1和R 2一起可以表示亚烷基以形成具有或不具有烷基取代基的5-或6-元环; R 4和R 5各自表示氢或低级烷基; 以及当R4为氢时可获得的药学上可接受的盐，其为有用的药物，例如细菌感染的化学治疗剂。

公开(公告)号：US3997545A

公开(公告)日：1976-12-14

申请号：US612743

申请日：1975-09-12

申请人： Yutaka Kuwada ,  Kanji Meguro ,  Yoshiaki Sato ,  Takeshi Fugono

发明人： Yutaka Kuwada ,  Kanji Meguro ,  Yoshiaki Sato ,  Takeshi Fugono

IPC分类号： C07D495/04 ,  C07D513/00

CPC分类号： C07D495/04

摘要： Novel thienopyridine-carboxylic acid derivatives, which are shown by the general formula ##STR1## wherein R.sup.1 represents hydrogen or a lower alkyl; R.sup.2 represents hydrogen, a lower alkyl or a halogen; or R.sup.1 and R.sup.2, taken together, may represent an alkylene to form a 5- or 6-membered ring with or without alkyl substituents; each of R.sup.4 and R.sup.5 represents hydrogen or a lower alkyl; and their pharmaceutically acceptable salts obtainable when R.sup.4 is hydrogen, which are useful medicines such as chemotherapeutic agents of bacterial infections.

摘要翻译： 新的噻吩并吡啶 - 羧酸衍生物，其通式为：其中R 1表示氢或低级烷基; R2代表氢，低级烷基或卤素; 或者R 1和R 2一起可以表示亚烷基以形成具有或不具有烷基取代基的5-或6-元环; R 4和R 5各自表示氢或低级烷基; 以及当R4为氢时可获得的药学上可接受的盐，其为有用的药物，例如细菌感染的化学治疗剂。

公开(公告)号：US3951989A

公开(公告)日：1976-04-20

申请号：US490704

申请日：1974-07-22

申请人： Yutaka Kuwada ,  Kanji Meguro ,  Yoshiaki Sato ,  Takeshi Fugono

发明人： Yutaka Kuwada ,  Kanji Meguro ,  Yoshiaki Sato ,  Takeshi Fugono

IPC分类号： C07D333/36 ,  C07D333/38 ,  C07D333/66 ,  C07D333/68 ,  C07D495/04 ,  C07D213/28

CPC分类号： C07D495/04 ,  C07D333/36 ,  C07D333/38 ,  C07D333/66 ,  C07D333/68

摘要： Novel thienopyridine-carboxylic acid derivatives, which are shown by the general formula ##SPC1##Wherein R.sup.1 represents hydrogen or a lower alkyl; R.sup.2 represents hydrogen, a lower alkyl or a halogen; or R.sup.1 and R.sup.2, taken together, may represent an alkylene to form a 5- or 6-membered ring with or without alkyl substituents; each of R.sup.4 and R.sup.5 represents hydrogen or a lower alkyl; and their pharmaceutically acceptable salts obtainable when R.sup.4 is hydrogen, which are useful medicines such as chemotherapeutic agents of bacterial infections.

摘要翻译： 新的噻吩并吡啶 - 羧酸衍生物，其通式如下：其中R1表示氢或低级烷基; R2代表氢，低级烷基或卤素; 或者R 1和R 2一起可以表示亚烷基以形成具有或不具有烷基取代基的5-或6-元环; R 4和R 5各自表示氢或低级烷基; 以及当R4为氢时可获得的药学上可接受的盐，其为有用的药物，例如细菌感染的化学治疗剂。

公开(公告)号：US4160830A

公开(公告)日：1979-07-10

申请号：US842153

申请日：1977-10-14

申请人： Shiro Morimoto ,  Hiroaki Nomura ,  Takeshi Fugono ,  Isao Minami

发明人： Shiro Morimoto ,  Hiroaki Nomura ,  Takeshi Fugono ,  Isao Minami

IPC分类号： A61K31/54

CPC分类号： C07D501/38

摘要： A method of combating bacterial infections in humans involves the administration of an antibacterially effective amount of a compound of the formula: ##STR1## wherein R is phenyl or thienyl group, and R' is a group which constitutes together with the adjacent nitrogen atom a pyridinium group that is unsubstituted or substituted by carbamoyl, or a 4'-methyl-5'-(.beta.-hydroxyethyl)-thiazolium or a pharmaceutically acceptable salt thereof, to a patient. This method is effective particularly against Pseudomonas aeruginosa as well as against other Gram negative and positive microorganisms.

摘要翻译： 一种抗人类细菌感染的方法包括施用抗菌有效量的下式化合物：其中R是苯基或噻吩基，R'是与相邻氮原子一起构成的一个吡啶鎓 未取代或被氨基甲酰基取代的基团，或4'-甲基-5' - （β-羟乙基） - 噻唑鎓或其药学上可接受的盐。 该方法特别针对铜绿假单胞菌以及其他革兰氏阴性和阳性微生物有效。

公开(公告)号：US4132789A

公开(公告)日：1979-01-02

申请号：US715495

申请日：1976-08-18

申请人： Hiroaki Nomura ,  Takenori Hitaka ,  Hiroshi Akimoto ,  Isao Minami ,  Fumio Kiriki ,  Tatsuichi Matsuda ,  Takeshi Fugono

发明人： Hiroaki Nomura ,  Takenori Hitaka ,  Hiroshi Akimoto ,  Isao Minami ,  Fumio Kiriki ,  Tatsuichi Matsuda ,  Takeshi Fugono

IPC分类号： C07D501/20 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D277/20 ,  C07D501/24 ,  C07D501/34 ,  C07D501/36 ,  C07D501/46

CPC分类号： C07D277/20 ,  C07D501/24

摘要： Novel cephalosporins shown by the general formula: ##STR1## wherein Y is an acyloxy group, a quaternary ammonium group or a group of the formula: --S--R in which R is a nitrogen-containing heterocyclic group, and pharmaceutically acceptable salts thereof have high antibacterial properties against Gram-positive and Gram-negative bacteria including Pseudomonas aeruginosa and Serratia marcescens.

摘要翻译： 新型头孢菌素，其通式如下：其中Y为酰氧基，季铵基团或其中R为含氮杂环基的-SR基团及其药学上可接受的盐具有高抗菌性 对革兰氏阳性和革兰氏阴性菌（包括铜绿假单胞菌和粘质沙雷氏菌）的特性。

公开(公告)号：US4029656A

公开(公告)日：1977-06-14

申请号：US711565

申请日：1976-08-04

申请人： Toshihiro Ishiguro ,  Takeshi Fugono ,  Hiroaki Nomura

发明人： Toshihiro Ishiguro ,  Takeshi Fugono ,  Hiroaki Nomura

IPC分类号： C07D501/36 ,  C07D501/50 ,  C07D501/54

CPC分类号： C07D501/36 ,  C07D501/24 ,  C07D501/26

摘要： Novel cephalosporanic acid derivatives which are active against both Gram positive and Gram negative pathogenic bacteria, particularly Pseudomonas, and which have .alpha.-sulfoacylamino group at 7-position. A few examples of the compounds are 7-(.alpha.-sulfophenylacetamido)-cephalosporanic acid, 7-(.alpha.-sulfopropionamido)-cephalosporanic acid, 7-(.alpha.-sulfocapronamido)-cephalosporanic acid. They are prepared by condensing 7-aminocephalosporanic acid or salts thereof with .alpha.-sulfocarboxylic acid or functional derivatives thereof in the presence of a solvent at -2.degree. - 10.degree. C.

摘要翻译： 新型头孢菌素酸衍生物，其对革兰氏阳性和革兰氏阴性致病菌特别是假单胞菌具有活性，并且在7-位具有α-磺酰氨基。 化合物的一些实例是7-（α-磺基苯基乙酰胺基） - 头孢烷酸，7-（α-亚磺基丙酰氨基） - 头孢烷酸，7-（α-磺基己内酰胺基） - 头孢烷酸。 它们通过将7-氨基头孢烷酸或其盐与α-磺基羧酸或其官能衍生物在溶剂存在下在-2°-10℃下进行缩合来制备。

公开(公告)号：US3988327A

公开(公告)日：1976-10-26

申请号：US547169

申请日：1975-02-05

申请人： Toshihiro Ishiguro ,  Takeshi Fugono ,  Hiroaki Nomura

发明人： Toshihiro Ishiguro ,  Takeshi Fugono ,  Hiroaki Nomura

IPC分类号： C07D501/26 ,  C07D501/28 ,  C07D501/32

CPC分类号： C07D501/36 ,  C07D501/24 ,  C07D501/26

摘要： Novel cephalosporanic acid derivatives which are active against both Gram positive and Gram negative pathogenic bacteria, particularly Pseudomonas, and which have an .alpha.-sulfoacylamino group at 7-position. A few examples of the compounds are 7-(.alpha.-sulfophenylacetamido)-cephalosporanic acid, 7-(.alpha.-sulfopropionamido)-cephalosporanic acid, 7-(.alpha.-sulfocapronamido)-cephalosporanic acid. They are prepared by condensing 7-aminocephalosporanic acid or salts thereof with .alpha.-sulfocarboxylic acid or functional derivatives thereof in the presence of a solvent at -2.degree. - 10.degree. C.

摘要翻译： 新型的头孢菌素酸衍生物，其对革兰氏阳性和革兰氏阴性致病菌，特别是假单胞菌属均具有活性，在7-位具有α-磺酰氨基。 化合物的一些实例是7-（α-磺基苯基乙酰胺基） - 头孢烷酸，7-（α-亚磺基丙酰氨基） - 头孢烷酸，7-（α-磺基己内酰胺基） - 头孢烷酸。 它们通过将7-氨基头孢烷酸或其盐与α-磺基羧酸或其官能衍生物在溶剂存在下在-2°-10℃下进行缩合来制备。

公开(公告)号：US4065619A

公开(公告)日：1977-12-27

申请号：US719704

申请日：1976-09-02

申请人： Shiro Morimoto ,  Hiroaki Nomura ,  Takeshi Fugono ,  Isao Minami

发明人： Shiro Morimoto ,  Hiroaki Nomura ,  Takeshi Fugono ,  Isao Minami

IPC分类号： A61K31/545 ,  C07D501/38 ,  C07D501/44 ,  C07D501/46

CPC分类号： C07D501/38

摘要： Novel cephalosporins of the formula, ##STR1## wherein R is a hydrogen atom or an alkyl, aryl or thienyl group, and R' is a group which constitutes together with the adjacent nitrogen atom a 5- or 6-membered ring containing 1 or 2 nitrogen atoms, which are effective particularly against Pseudomonas aeruginosa as well as against other Gram negative and positive microorganisms, for example, N-[7-(.alpha.-sulfophenylacetamido)ceph-3-em-3-ylmethyl] pyridinium 4-carboxylate, N-[7-(.alpha.-sulfo-3'-thienylacetamido)ceph-3-em-3-ylmethyl] pyridinium-4-carboxylate, and their pharmaceutically acceptable salts thereof. Sodium salt of the former is prepared by, e.g. reacting sodium 7-(.alpha.-sulfophenylacetamido) cephalosporanate with pyridine in water.

摘要翻译： 新颖的下式头孢菌素其中R是氢原子或烷基，芳基或噻吩基，R'是与相邻氮原子一起构成含有1或2的5-或6-元环的基团 氮原子，其特别对绿脓假单胞菌以及其他革兰氏阴性和阳性微生物有效，例如N- [7-（α-磺基苯基乙酰氨基）头孢-3-烯-3-基甲基]吡啶鎓4-羧酸盐，N - [7-（α-磺基-3'-噻吩基乙酰胺基）头孢-3-烯-3-基甲基]吡啶鎓-4-羧酸盐及其药学上可接受的盐。 前者的钠盐通过例如 使7-（α-磺基苯基乙酰氨基）头孢菌素钠与吡啶在水中反应。