公开(公告)号：US4139701A

公开(公告)日：1979-02-13

申请号：US795585

申请日：1977-05-10

申请人： David A. Berges

发明人： David A. Berges

IPC分类号： C07D257/04 ,  C07D501/18 ,  C07D501/36

CPC分类号： C07D501/36 ,  C07D257/04 ,  C07D501/18

摘要： The compounds of this invention are cephalosporins having various acyl substituents at the 7-position and a sulfonic acid or sulfamoyl substituted tetrazolyl thiomethyl group at the 3-position of the cephem nucleus and intermediates for the preparation thereof. The 7-acylated compounds have antibacterial activity.

摘要翻译： 本发明的化合物是在7-位上具有各种酰基取代基的头孢菌素和头孢烯核的3位上的磺酸或氨磺酰取代的四唑基硫代甲基以及制备它们的中间体。 7-酰化化合物具有抗菌活性。

公开(公告)号：US4117123A

公开(公告)日：1978-09-26

申请号：US805197

申请日：1977-06-09

申请人： David Alan Berges

发明人： David Alan Berges

IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D257/04 ,  C07D501/36

CPC分类号： C07D257/04 ,  C07D501/36

摘要： Novel cephalosporins having various acyl substituents at the 7- position and a sulfamidoethyl substituted tetrazolylthiomethyl group at the 3- position of the cephem nucleus are prepared. These compounds have antibacterial activity.

摘要翻译： 7-酰基-3-头孢烯-4-羧酸，其制备方法和含有它们的组合物。 具有下式的头孢菌素：其中R表示已知可用作头孢菌素中7-氨基或青霉素6-氨基上的取代基的药学上可接受的酰基具有抗菌活性。 通过将适当取代的头孢菌素或7-氨基头孢菌素的3-乙酰氧基甲基与1-（2-氨基磺酰氨基乙基）1,4-二氢-5H-四唑-5-硫酮置换乙酰基来制备化合物，如果 需要引入所需的7-酰基。

公开(公告)号：US4113944A

公开(公告)日：1978-09-12

申请号：US588555

申请日：1975-06-19

申请人： Fumio Kai ,  Toshinori Saito ,  Shigeo Seki ,  Toyoaki Kawasaki

发明人： Fumio Kai ,  Toshinori Saito ,  Shigeo Seki ,  Toyoaki Kawasaki

IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D501/04 ,  C07D501/24 ,  C07D501/36 ,  C07D501/40 ,  C07D501/42 ,  C07D501/46 ,  C07D501/48 ,  C07D501/54 ,  C07D501/56 ,  C07D501/60

CPC分类号： C07D501/36

摘要： A cephalosporin compound represented by the formula (I) or (I') ##STR1## wherein R.sup.1 represents a phenyl group, a 2-thienyl group or a phenoxy group; R.sup.2 represents a hydrogen atom, an alkyl group having 1 to 4 carbon atoms which may be substituted with a phenyl group, an alkoxy group having 1 to 4 carbon atoms or a halogen atom, or a phenyl group which may be substituted with one or two groups selected from the group consisting of a halogen atom, a nitro group, an alkyl group having 1 to 4 carbon atoms and an alkoxy group having 1 to 4 carbon atoms; R.sup.3 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms which may be substituted with a monoalkylamino group having 1 to 4 carbon atoms in the alkyl moiety thereof, a dialkylamino group having 1 to 4 carbon atoms in each alkyl moiety thereof, a halogen atom or a phenyl group which may be substituted with one to three groups selected from the group consisting of a halogen atom, a nitro group, an alkyl group having 1 to 4 carbon atoms and an alkoxy group having 1 to 4 carbon atoms; R.sup.4 represents an alkyl group having 1 to 4 carbon atoms; A has up to 15 carbon atoms and represents a straight or branched chain alkylene group, a straight or branched chain alkenylene group, a straight or branched chain alkadienylene group or a phenylene group, and n is 0 or 1; or the salt thereof; and a process for preparing the same.

公开(公告)号：US4107433A

公开(公告)日：1978-08-15

申请号：US755159

申请日：1976-12-29

申请人： Peter Hubert Bentley ,  John Peter Clayton

发明人： Peter Hubert Bentley ,  John Peter Clayton

IPC分类号： C07D501/26 ,  C07D501/30 ,  C07D501/34 ,  C07D501/36

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

摘要： Phthalidyl and substituted phthalidyl esters of certain cephalosporins are absorbed by the oral route into the serum, where they are hydrolyzed to the parent antibacterially active cephalosporin.

摘要翻译： 某些头孢菌素的邻苯二甲酰基和取代的酞基酯被口服途径吸收到血清中，在那里将其水解成亲本的抗菌活性头孢菌素。

公开(公告)号：US4092476A

公开(公告)日：1978-05-30

申请号：US755240

申请日：1976-12-29

申请人： Peter Hubert Bentley ,  John Peter Clayton

发明人： Peter Hubert Bentley ,  John Peter Clayton

IPC分类号： C07D501/26 ,  C07D501/30 ,  C07D501/34 ,  C07D501/36

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

摘要： Phthalidyl and substituted phthalidyl esters of certain cephalosporins are absorbed by the oral route into the serum, where they are hydrolyzed to the parent antibacterially active cephalosporin.

摘要翻译： 某些头孢菌素的邻苯二甲酰基和取代的酞基酯被口服途径吸收到血清中，在那里将其水解成亲本的抗菌活性头孢菌素。

公开(公告)号：US4086422A

公开(公告)日：1978-04-25

申请号：US714420

申请日：1976-08-16

申请人： Hermann Breuer ,  Uwe Treuner

发明人： Hermann Breuer ,  Uwe Treuner

IPC分类号： C07D501/20 ,  C07D501/34 ,  C07D501/36 ,  C07D501/38 ,  C07D501/44

CPC分类号： C07D501/36 ,  C07D501/20

摘要： Carbamoyalkylureido cephalosporins of the formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, diphenyl-lower alkyl, tri(lower alkyl)silyl, trihaloethyl, a salt forming ion, or the group ##STR2## R.sub.1 is hydrogen or methoxy; A is straight or branched chain alkylene of 1 to 6 carbons; R.sub.2 and R.sub.3 are independently selected from hydrogen and straight chain alkyl of 1 to 4 carbons, or R.sub.2 is hydrogen and R.sub.3 is branched chain alkyl of 3 or 4 carbons, phenyl, benzyl or phenethyl, or R.sub.2 and R.sub.3 taken together with N atom to which they are attached form ##STR3## R.sub.4 is hydrogen or lower alkyl; R.sub.5 is hydrogen, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, phenyl, phenyl-lower alkyl, substituted phenyl, substituted phenyl-lower alkyl, or certain heterocyclic groups; R.sub.6 is hydrogen or lower alkyl; R.sub.7 is lower alkyl; and X is hydrogen, lower alkanoyloxy, ##STR4## or certain heterothio groups; are disclosed. These compounds are useful as antibacterial agents.

摘要翻译： 其中R为氢，低级烷基，苯基 - 低级烷基，二苯基 - 低级烷基，三（低级烷基）甲硅烷基，三卤代乙基，成盐离子或基团R1为氢或碳原子数为1的碳原子数1〜8的烷硫基烷基脲基头孢菌素 甲氧基 A是1至6个碳的直链或支链亚烷基; R2和R3独立地选自氢和1至4个碳的直链烷基，或者R2是氢，R3是3或4个碳的支链烷基，苯基，苄基或苯乙基，或R2和R3与N原子一起 它们是连接的，其中R 4是氢或低级烷基; R5是氢，低级烷基，环烷基，环烯基，环链二烯基，苯基，苯基 - 低级烷基，取代的苯基，取代的苯基 - 低级烷基或某些杂环基; R6是氢或低级烷基; R7是低级烷基; X是氢，低级烷酰氧基，或者某些杂硫基; 被披露。 这些化合物可用作抗菌剂。

公开(公告)号：US4039535A

公开(公告)日：1977-08-02

申请号：US663885

申请日：1976-03-04

申请人： Robin D. G. Cooper

发明人： Robin D. G. Cooper

IPC分类号： C07D501/36

CPC分类号： C07D501/36

摘要： 7-[.alpha.-(guanyl-1-ureido)phenylacetamido]-3-(1-methyl-1H-tetrazol-5-ylthiomethyl)-3-cephem-4-carboxylic acid, 7-[.alpha.-(3-guanyl-1-ureido)phenylacetamido]-3-(5-methyl-1,3,4-thiadiazol-2-ylthiomethyl)-3-cephem-4-carboxylic acid and related compounds, the pharmaceutically acceptable non-toxic salts and certain esters thereof are valuable broad spectrum antibiotics demonstrating high levels of activity against Pseudomonas species.

摘要翻译： 7- [α-（脒基-1-脲基）苯基乙酰氨基] -3-（1-甲基-1H-四唑-5-基噻吩基）-3-头孢烯-4-羧酸，7- [3- -1-脲基）苯基乙酰氨基] -3-（5-甲基-1,3,4-噻二唑-2-基硫代甲基）-3-头孢烯-4-羧酸及其相关化合物，药学上可接受的无毒盐和某些 其酯是有价值的广谱抗生素，表现出对假单胞菌属物种的高水平活性。

公开(公告)号：US4036834A

公开(公告)日：1977-07-19

申请号：US620552

申请日：1975-10-08

申请人： Masuo Murakami ,  Masaru Iwanami ,  Ichiro Isaka ,  Yoshinobu Nagano ,  Masaharu Fujimoto ,  Tetsuya Maeda

发明人： Masuo Murakami ,  Masaru Iwanami ,  Ichiro Isaka ,  Yoshinobu Nagano ,  Masaharu Fujimoto ,  Tetsuya Maeda

IPC分类号： A61K20060101 ,  A61K31/545 ,  C07D20060101 ,  C07D501/04 ,  C07D501/36

CPC分类号： C07D501/36

摘要： Novel 7-(.alpha.-hydroxy-substituted pyridylcarboxamido-.alpha.-phenylacetamido)-3-substituted thiomethyl-.DELTA..sup.3 -cephem-4-carboxylic acid derivatives are disclosed. The compounds of this invention have high water solubility and show excellent antibacterial activities against various strains of Pseudomonas and Proteus.

摘要翻译： 公开了新的7-（α-羟基取代的吡啶基甲酰氨基-α-苯基乙酰胺基）-3-取代的硫代甲基-D-TA-头孢烯-4-羧酸衍生物。 本发明化合物具有高水溶性，对各种假单胞菌和变形菌菌株均具有优异的抗菌活性。

公开(公告)号：US4034089A

公开(公告)日：1977-07-05

申请号：US664218

申请日：1976-03-05

申请人： Murray Arthur Kaplan ,  Alphonse Peter Granatek

发明人： Murray Arthur Kaplan ,  Alphonse Peter Granatek

IPC分类号： A61K31/545

CPC分类号： C07D501/36 ,  A61K31/545

摘要： The antibacterial agent 7-[D-.alpha.-amino-.alpha.-(p-hydroxyphenyl)acetamido]-3-(1,2,3-triazol-5-ylthiomethyl)-3-cephem-4-carboxylic acid, which is a zwitterion, is both purified and converted to a form highly suitable for use in aqueous suspensions by converting it to the crystalline 7-[D-.alpha.-amino-.alpha.-(p-hydroxyphenyl)acetamido]-3-(1,2,3-triazol-5-ylthiomethyl)-3-cephem-4-carboxylic acid 1,2-propylene glycolate, said propylene glycolate containing 1.0 - 1.6 moles of 1,2-propylene glycol per mole of cephalosporin zwitterion.

摘要翻译： 抗菌剂7- [D-α-氨基-α-（对羟基苯基）乙酰氨基] -3-（1,2,3-三唑-5-基硫甲基）-3-头孢烯-4-羧酸，其为 将两性离子两者纯化并转化成高度适用于水性悬浮液的形式，将其转变为结晶7- [D-α-氨基-α-（对羟基苯基）乙酰氨基] -3-（1,2,3 - 三唑-5-基硫甲基）-3-头孢烯-4-羧酸1,2-丙二醇乙酸酯，所述丙二醇酸酯每摩尔头孢菌素两性离子含有1.0-1.6摩尔1,2-丙二醇。

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。