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19 条记录 (耗时 0.014 秒)

    6-Aminoalkylpenicillanic acid 1,1-dioxides and derivatives as beta-lactamase inhibitors
    4.
    发明公开
    6-Aminoalkylpenicillanic acid 1,1-dioxides and derivatives as beta-lactamase inhibitors 失效
    6-氨基烷基青霉素1,1-二氧化物和衍生物β-内酰胺酶抑制剂。

    公开(公告)号：EP0084925A1

    公开(公告)日：1983-08-03

    申请号：EP83300042.5

    申请日：1983-01-05

    申请人： PFIZER INC.

    发明人： Barth, Wayne Ernest

    IPC分类号： C07D499/00 ,  C07D499/32 ,  A61K31/43 ,  A61K31/545 ,  C07D519/00

    CPC分类号： A61K31/545 ,  A61K31/43 ,  C07D499/00

    摘要： beta-Lactamase inhibitors which are 6-alpha- and 6-beta-(aminomethyl) and (1-aminoethyl)pencillanic acid 1,1-dioxides, said aminomethyl compounds optionally substituted on amino nitrogen with benzyl, hydroxybenzyl, picolyl or phenethyl; pharmaceutically-acceptable salts thereof; conventional esters thereof hydrolyzable in vivo; bis-methanediol esters thereof; or mixed methanediol esters with said beta-lactamase inhibitors and sulbactam. Pharmaceutical compositions thereof in combination with a conventional beta-lactam antibiotic, used in the treatment of bacterial infections; compounds useful as intermediates in the synthesis of said beta-lactamase inhibitors. Antibacterial bis-methanediol esters of said beta-lactamase inhibitors and ampicillin or amoxicillin, also used in the treatment of bacterial infections; and intermediates therefor.

    摘要翻译： 所述氨基甲基化合物任选在氨基氮上被苄基，羟基苄基，吡啶甲基或苯乙基取代;所述氨基甲基化合物是6-氨基甲酰基，6-氨基乙酰基， 其药学上可接受的盐; 其在体内可水解的常规酯; 双甲烷二醇酯; 或与所述β-内酰胺酶抑制剂和舒巴坦混合的甲基二醇酯。 与其用于治疗细菌感染的常规β-内酰胺抗生素组合的药物组合物; 可用作合成所述β-内酰胺酶抑制剂的中间体的化合物。 所述β-内酰胺酶抑制剂和氨苄青霉素或阿莫西林的抗菌双甲氧基二醇酯也用于治疗细菌感染; 及其中间体。

    6-(1-Carbamoyl-1-hydroxymethyl)penicillanic-acid derivatives
    5.
    发明公开
    6-(1-Carbamoyl-1-hydroxymethyl)penicillanic-acid derivatives 失效
    6-（1-氨基甲酰基-1-羟基甲基）-penicillansäurederivate。

    公开(公告)号：EP0220939A1

    公开(公告)日：1987-05-06

    申请号：EP86308235.0

    申请日：1986-10-23

    申请人： PFIZER INC.

    发明人： Barth, Wayne Ernest

    IPC分类号： C07D499/00 ,  A61K31/43

    CPC分类号： C07D499/00

    摘要： 6-(1-Carbamoyl-1-hydroxymethyl)penicillanic acid derivatives of the formula:
    wherein

    n is 0, 1 or 2;
    R is hydrogen, a radical group forming an ester hydrolyzable under physiological conditions, or an acyloxymethyl or 1-(acyloxy)ethyl radical derived from a conventional beta-lactam antibiotic; and
    R 1 and R 2 are taken separately and are each independently for example, hydrogen, (C 1 -C 4 )alkyl, (C 5 -C 6 )cycloalkyl, phenyl benzyl or one of said groups substituted by methyl, hydroxy, (C l -C 2 )alkoxy, -COOR 3 , or -CONR 3 R 4 ; or
    R 1 and R Z are taken together with the nitrogen to which they are attached to form for example, a pyrrolidine, piperidine, perhydroazepine, morpholine 4-[formyl, (C 1 -C 4 )alkyl, phenyl benzyl, pyridyl or 2-hydroxyethyl]piperazine, indoline, isoindoline, 1,2,3,4-tetrahydroquinoline or 1,2,3,4-tetrahydroisoquinoline ring system, or one af said ring systems substituted by methyl, hydroxy, hydroxymethyl, carboxy, carbamoyl, -COOR 3 or -CONR 3 R4.

    The compounds are useful as antibacterial agents and/or betalactamase inhibitors.

    摘要翻译： 6-（1-氨基甲酰基-1-羟甲基）青霉烷酸衍生物，其结构如下：... 其中... n为0,1或2; R为氢，在生理条件下形成酯可水解的自由基，或 衍生自常规β-内酰胺抗生素的酰氧基甲基或1-（酰氧基）乙基; R 1和R 2分别独立地为氢，（C 1 -C 4）烷基，（C 5 -C 6）环烷基，苯基苄基或被甲基，羟基， （C 1 -C 2）烷氧基，-COOR 3或-CONR 3 R 4; 或R 1和R 2与它们所连接的氮一起形成例如吡咯烷，哌啶，全氢氮杂吗啉，吗啉4- [甲酰基，（C 1 -C 4）烷基，苯基苄基， 吡啶基或2-羟乙基]哌嗪，二氢吲哚，异二氢吲哚，1,2,3,4-四氢喹啉或1,2,3,4-四氢异喹啉环系，或被甲基，羟基，羟甲基，羧基， 氨基甲酰基，-COOR 3或-CONR 3 R 4。 该化合物可用作抗菌剂和/或β-内酰胺酶抑制剂。

    6-(Aminoacyloxymethyl) penicillanic acid 1, 1-dioxides as beta-lactamase inhibitors
    6.
    发明公开
    6-(Aminoacyloxymethyl) penicillanic acid 1, 1-dioxides as beta-lactamase inhibitors 失效
    6-（氨基酰氧基甲基）青霉烷-1,1-二氧化物酶β-内酰胺酶抑制剂。

    公开(公告)号：EP0154444A1

    公开(公告)日：1985-09-11

    申请号：EP85301115.3

    申请日：1985-02-20

    申请人： PFIZER INC.

    发明人： Barth, Wayne Ernest

    IPC分类号： C07D499/00 ,  C07D519/00 ,  A61K31/43

    CPC分类号： C07D499/861

    摘要： beta-Lactamase inhibitors which are aminoacid esters of 6-alpha- and 6-beta-(hydroxymethyl)pencillanic acid 1,1-dioxides; pharmaceutically-acceptable salts thereof; conventional esters thereof which are hydrolyzable in vivo; bis-methanediol esters thereof; or mixed methanediol esters with said beta-lactamase inhibitors and sulbactam. Pharmaceutical compositions comprising said beta-lactamase inhibitors and a conventional beta-lactam antibiotic, said compositions useful in the treatment of bacterial infections. Compounds useful as intermediates in the synthesis of said beta-lactamase inhibitors. Antibacterial mixed bis-methanediol esters of said aminoacyloxymethyl penicillanic acid 1.1-dioxides and ampicillin or amoxicillin, also useful in the treatment of bacterial infections; and intermediates therefor.

    摘要翻译： β-内酰胺酶抑制剂，其为6-α和6-β-（羟甲基）青霉酸1,1-二氧化物的氨基酸酯; 其药学上可接受的盐; 其在体内可水解的其常规酯; 双甲烷二醇酯; 或与所述β-内酰胺酶抑制剂和舒巴坦混合的甲基二醇酯。 包含所述β-内酰胺酶抑制剂和常规β-内酰胺抗生素的药物组合物，所述组合物可用于治疗细菌感染。 用作合成所述β-内酰胺酶抑制剂的中间体的化合物。 所述氨基酰氧基甲基青霉素酸1,1-二氧化物和氨苄青霉素或阿莫西林的抗菌混合双甲磺酸酯也可用于治疗细菌感染; 及其中间体。

    Bis-esters of alkanediols, pharmaceutical compositions thereof and intermediates therefor
    7.
    发明公开
    Bis-esters of alkanediols, pharmaceutical compositions thereof and intermediates therefor 失效
    烷二醇，药物组合物和中间体的双酯。

    公开(公告)号：EP0059046A1

    公开(公告)日：1982-09-01

    申请号：EP82300704.2

    申请日：1982-02-12

    申请人： PFIZER INC.

    发明人： Barth, Wayne Ernest

    IPC分类号： C07D499/00 ,  C07D499/32 ,  A61K31/43

    CPC分类号： C07D499/00

    摘要： 6-Acylaminopenicillancyloxymethyl esters and 1-(6-acyl- aminopenicillanoyloxy)ethyl esters of 2-beta-acetoxymethyl-2- alpha-methyl-(5R)penam-3-alpha-carboxylic acid 1,1-dioxide are useful as antibacterial agents. The 6-aminopenicillanoyloxymethyl ester, the 1-(6-aminopenicillanoyloxy)ethyl ester and certain other mono-substituted methyl and ethyl esters of 2-beta-acetoxymethyl-2-alpha-methyl-(5R)penam-3-alpha- carboxylic acid 1,1-dioxide are useful intermediates to the aforesaid antibacterial agents.

    摘要翻译： 6- Acylaminopenicillancyloxymethyl酯和2-β-乙酰氧基甲基-2-α-甲基 - （5R）青霉烷-3--α-羧酸-1,1-二氧化物的1-（6- acylaminopenicillanoyloxy）乙基酯是作为抗菌剂是有用的。 6 aminopenicillanoyloxymethyl酯，1-（6- aminopenicillanoyloxy）乙酯和2-β-乙酰氧基甲基-2-α-甲基的某些其它单甲基和乙基酯substituiertem（5R）青霉烷-3--α-羧酸 1,1-二氧化物是有用的中间体，以上述的抗菌剂。

    Penicillanic acid derivatives, processes for their preparation and pharmaceutical compositions containing them
    8.
    发明公开
    Penicillanic acid derivatives, processes for their preparation and pharmaceutical compositions containing them 失效
    Penicillansäurederivate，涉及它们的制备方法和含有它们的药物组合物。

    公开(公告)号：EP0002927A1

    公开(公告)日：1979-07-11

    申请号：EP78300860.0

    申请日：1978-12-19

    申请人： PFIZER INC.

    发明人： Barth, Wayne Ernest

    IPC分类号： C07D499/42 ,  A61K31/43

    CPC分类号： C07D499/00 ,  Y02P20/55

    摘要： 6-Aminopenicillanic acid 1,1-dioxide, esters thereof readily hydrolyzable in vivo, and the pharmaceutically-acceptable salts of these compounds, are useful for enhancing the effectiveness of certain β-lactam antibiotics against certain β-lactamase producing bacteria. Derivatives of 6-ammopenicillanic acid 1,1-dioxide protected by a conventional carboxy protecting group are useful intermediates to 6-aminopenicillanic acid 1,1-dioxide and esters thereof readily hydrolyzable in vivo. Processes for their preparation and pharmaceutical compositions are described.

    摘要翻译： 6-氨基青霉烷酸-1,1-二氧化物或其酯在体内易于水解的，和合成的化合物的药学上可接受的盐，用于增强的β-内酰胺抗生素对某些β-内酰胺酶产生菌的某些效力是有用的。 6-氨基青霉烷酸-1,1-二氧化物用常规羧基保护基团保护的衍生物是有用的中间体，以6-氨基青霉烷酸-1,1-二氧化物及其酯在体内易于水解。 其制备方法和药物组合物的过程进行说明。