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34 条记录 (耗时 0.018 秒)

    Antibacterial cephalosporin compounds
    5.
    发明授权
    Antibacterial cephalosporin compounds 失效
    抗生素CEPHOROSPORIN化合物

    公开(公告)号：US5189157A

    公开(公告)日：1993-02-23

    申请号：US189936

    申请日：1988-05-03

    申请人： Chung-Chen Wei ,  Kevin F. West

    发明人： Chung-Chen Wei ,  Kevin F. West

    IPC分类号： C07D501/22 ,  A61K31/545 ,  C07D501/18 ,  C07D501/26 ,  C07D501/34 ,  C07D501/36 ,  C07D501/38 ,  C07D501/46 ,  C07D501/57

    CPC分类号： C07D501/36 ,  C07D501/26 ,  C07D501/34 ,  C07D501/38 ,  C07D501/46 ,  Y02P20/55

    摘要： There are presented antibacterial cephalosporins having broad antimicrobial activity as well as intermediates for their formation, such compounds having the formula ##STR1## wherein X is ##STR2## R is hydrogen or a carboxylic acid protecting group; R.sub.1 is hydrogen or an acyl group;R.sub.2 is hydrogen or lower alkoxy; andR.sub.3 is carbocyclic aryl or alkyl carbocyclic aryl substituted on the ring with two or more of hydroxy and/or lower alkanoyl ester groups, with halogen being an optional additional ring substituent;as well as the corresponding readily hydrolyzable esters, pharmaceutically acceptable salts and hydrates of these compounds where R is hydrogen.

    摘要翻译： 呈现具有广谱抗微生物活性的抗菌头孢菌素及其形成中间体，具有下式的化合物，其中X为氢或羧酸保护基; R1是氢或酰基; R2是氢或低级烷氧基; 并且R 3是在具有两个或多个羟基和/或低级烷酰基酯基团的环上被取代的碳环芳基或烷基碳环基，其中卤素是任选的另外的环取代基; 以及其中R是氢的这些化合物的相应的易水解的酯，药学上可接受的盐和水合物。

    Cephem-3-imidates and 3-amidines
    8.
    发明授权
    Cephem-3-imidates and 3-amidines 失效
    Cephem-3-imidates和3-脒基

    公开(公告)号：US4560749A

    公开(公告)日：1985-12-24

    申请号：US552960

    申请日：1983-11-18

    申请人： Douglas O. Spry

    发明人： Douglas O. Spry

    IPC分类号： C07D501/18 ,  C07D501/38

    CPC分类号： C07D501/18 ,  C07D501/38

    摘要： 3-Azido-3-cephem esters are reacted with electron rich olefins, e.g., enamines and cyclic enol ethers, to provide C.sub.3 amidines and imidates having antibacterial activity in the free acid form. For example, 3-azido-3-cephem esters react with ethyl vinyl ether to provide 3-[1-(ethoxyethylidene)amino]-3-cephem esters. The latter are deesterified to provide the free acid antibacterials.

    摘要翻译： 3-亚氨基-3-头孢烯酯与富含烯烃的烯烃（例如烯胺和环烯醇醚）反应，以提供具有游离酸形式的抗菌活性的C 3脒和亚胺化物。 例如，3-叠氮基-3-头孢烯酯与乙基乙烯基醚反应，得到3- [1-（乙氧基亚乙基）氨基] -3-头孢烯酯。 后者被酯化以提供游离酸抗菌剂。

    Cephalosporins having a 7-(carboxy substituted .alpha.-etherified oximinoarylacetamido) group
    9.
    发明授权
    Cephalosporins having a 7-(carboxy substituted .alpha.-etherified oximinoarylacetamido) group 失效
    头孢菌素具有7-（羧基取代的{60-乙酰肟基芳基乙酰胺基）基团

    公开(公告)号：US4168309A

    公开(公告)日：1979-09-18

    申请号：US838366

    申请日：1977-09-30

    申请人： Barry E. Ayres

    发明人： Barry E. Ayres

    IPC分类号： C07D501/44 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D501/38 ,  C07D501/40 ,  C07D501/46 ,  C07D501/60

    CPC分类号： C07D501/38

    摘要： Antibiotic compounds of the general formula ##STR1## [wherein R is a phenyl, thienyl or furyl group; R.sup.a and R.sup.b which may be the same or different, are each selected from hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl, phenyl, naphthyl, thienyl, furyl, carboxy, C.sub.2-5 alkoxycarbonyl and cyano, or R.sup.a and R.sup.b together with the carbon atom to which they are attached form a C.sub.3-7 cycloalkylidene or cycloalkenylidene group; m or n are each 0 or 1 such that the sum of m and n is 0 or 1; and R.sup.1 together with the nitrogen atom to which it is attached form a saturated or partially saturated 4-10 membered heterocyclic ring which may contain one or more further heteroatoms selected from 0,N and S and which may be substituted by a lower alkyl, lower alkoxy, lower acyloxy, lower alkoxycarbonyl, hydroxy, carboxy, amino, acylamino, substituted or unsubstituted carbamoyl or aryl group, or such a heterocyclic ring fused with a benzene ring] and non-toxic derivatives thereof, the compounds being syn isomers or existing as mixtures of syn and anti isomers.

    摘要翻译： 通式（I）的抗生素化合物[其中R是苯基，噻吩基或呋喃基; R a和R b可以相同或不同，各自选自氢，C 1-4烷基，C 2-4烯基，C 3-7环烷基，苯基，萘基，噻吩基，呋喃基，羧基，C 2-5烷氧基羰基和氰基，或 R a和R b与它们所连接的碳原子一起形成C 3-7亚环烷基或亚环烯基; m或n各自为0或1，使得m和n的和为0或1; 并且R 1与其连接的氮原子一起形成饱和或部分饱和的4-10元杂环，其可以含有一个或多个另外的选自O，N和S的杂原子，并且其可以被低级烷基取代，低级烷基 烷氧基，低级酰氧基，低级烷氧基羰基，羟基，羧基，氨基，酰氨基，取代或未取代的氨基甲酰基或芳基，或与苯环稠合的杂环]及其无毒衍生物，所述化合物为顺式异构体或存在 顺式和反式异构体的混合物。

    7-(.alpha.-Sulfoacylamido)cephalosporins
    10.
    发明授权
    7-(.alpha.-Sulfoacylamido)cephalosporins 失效
    7 - （{60-磺酰基氨基）头孢菌素

    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。