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    Antibacterial 6'-(2-amino-2-[4-acyloxyphenyl]acetamido)penicillanoyloxymethyl penicillanate 1,1-dioxide compounds
    3.
    发明授权
    Antibacterial 6'-(2-amino-2-[4-acyloxyphenyl]acetamido)penicillanoyloxymethyl penicillanate 1,1-dioxide compounds 失效
    抗菌6' - （2-氨基-2- [4-酰氧基苯基]乙酰氨基）青霉烷酰氧基甲基青霉素1,1-二氧化物化合物

    公开(公告)号：US4582829A

    公开(公告)日：1986-04-15

    申请号：US734504

    申请日：1985-05-15

    Applicant: Michael S. Kellogg

    Inventor： Michael S. Kellogg

    IPC: C07D499/00 ,  C07D499/32 ,  C07D519/00 ,  A61K31/43

    CPC classification number: C07D499/00 ,  Y02P20/55

    Abstract: 6-(2-Amino-2-[4-acyloxyphenyl]acetamido)penicillanoyloxymethyl esters of penicillanic acid 1,1-dioxide are useful as antibacterial agents. Derivatives of the aforesaid antibacterial agents which have an amino protecting group on the amino function in the 2-amino-2-(4-acyloxyphenyl)acetamido side chain are useful intermediates to the antibacterial agents themselves.

    Abstract translation: 青霉烷酸1,1-二氧化物的6-（2-氨基-2- [4-酰氧基苯基]乙酰氨基）青霉烷酰氧基甲基酯可用作抗菌剂。 在2-氨基-2-（4-酰氧基苯基）乙酰氨基侧链中具有氨基功能的氨基保护基的上述抗菌剂的衍生物是抗菌剂本身的有用的中间体。

    Bis-esters of methanediol with penicillins and penicillanic acid 1,1-dioxide
    4.
    发明授权
    Bis-esters of methanediol with penicillins and penicillanic acid 1,1-dioxide 失效
    甲基二醇与青霉素和青霉烷酸1,1-二氧化物的双酯

    公开(公告)号：US4432903A

    公开(公告)日：1984-02-21

    申请号：US446612

    申请日：1982-12-03

    Applicant: Eric C. Bigham

    Inventor： Eric C. Bigham

    IPC: C07D499/32

    CPC classification number: C07D499/32

    Abstract: 6'-Acylaminopenicillanoyloxymethyl esters of penicillanic acid 1,1-dioxide and useful as antibacterial agents. The 6'-aminopenicillanoyloxymethyl ester, halomethyl esters, alkylsulfonyloxymethyl esters and arylsulfonyloxymethyl esters of penicillanic acid 1,1-dioxide are all useful intermediates for the aforesaid antibacterial agents.

    Abstract translation: 青霉烷酸1,1-二氧化物的6'-酰基氨基青霉酰氨基甲基酯，可用作抗菌剂。 青霉烷酸1,1-二氧化物的6'-氨基青霉酰氨基甲基酯，卤甲基酯，烷基磺酰氧基甲基酯和芳基磺酰氧基甲酯都是上述抗菌剂的有用的中间体。

    Processes for preparing .beta.-lactams
    5.
    发明授权
    Processes for preparing .beta.-lactams 失效
    制备β-内酰胺的方法

    公开(公告)号：US4407751A

    公开(公告)日：1983-10-04

    申请号：US291081

    申请日：1981-08-07

    Applicant: Wagn O. Godtfredsen ,  Welf von Daehne

    Inventor： Wagn O. Godtfredsen ,  Welf von Daehne

    IPC: C07D499/00 ,  C07D499/32 ,  C07D503/00 ,  C07D519/00 ,  C07D499/04

    CPC classification number: C07D503/00 ,  C07D499/00

    Abstract: The present invention relates to hitherto unknown compounds of the general formula I: ##STR1## in which R.sub.1 stands for a phenyl, 4-hydroxyphenyl, 1,4-cyclohexadienyl or a 3-thienyl group; R.sub.2 represents a primary amino or a carboxy group; R.sub.3 is a hydrogen atom, or a lower alkyl, aryl or aralkyl radical, and A stands for a radical of a .beta.-lactamase inhibitor containing a .beta.-lactam ring as well as a carboxy group, A being connected via the carboxy group.The present invention provides new compounds useful in the treatment of bacterial infections. The new compounds are in particular strongly active against .beta.-lactamase producing bacteria.

    Abstract translation: 本发明涉及迄今未知的通式Ⅰ化合物：其中R1代表苯基，4-羟基苯基，1,4-环己二烯基或3-噻吩基; R2表示伯氨基或羧基; R3是氢原子或低级烷基，芳基或芳烷基，A代表含有β-内酰胺基的羧基的羧基，A通过羧基连接。 本发明提供了可用于治疗细菌感染的新化合物。 新化合物特别对β-内酰胺酶生产细菌具有强烈的活性。

    Pyridylmethyl esters of selected bio-affecting carboxylic acids
    6.
    发明授权
    Pyridylmethyl esters of selected bio-affecting carboxylic acids 失效
    所选生物影响羧酸的吡啶甲基酯

    公开(公告)号：US4376767A

    公开(公告)日：1983-03-15

    申请号：US222030

    申请日：1981-01-02

    Applicant: Kenneth B. Sloan

    Inventor： Kenneth B. Sloan

    IPC: A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4425 ,  A61K31/4427 ,  A61P9/12 ,  A61P25/04 ,  A61P29/00 ,  A61P31/04 ,  C07D213/30 ,  C07D213/89 ,  C07D401/12 ,  C07D499/00 ,  C07D499/32 ,  C07D501/20 ,  C07J43/00 ,  C07J71/00 ,  A61K31/625 ,  C07D213/55 ,  C07D501/38

    CPC classification number: C07D213/30 ,  C07D213/89 ,  C07D499/00 ,  C07J43/003 ,  C07J71/0031

    Abstract: Novel pharmaceutically useful derivatives of selected known bio-affecting carboxylic acids are disclosed, said derivatives having the structural formula ##STR1## wherein R.sub.1 and R.sub.2, which can be the same or different, are each hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, C.sub.1 -C.sub.5 alkylthio, phenyl, or substituted phenyl having one or more substituents each of which is selected from the group consisting of C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, chloro and dialkylamino wherein the alkyl portions, which can be the same or different, each have 1 to 5 carbon atoms, with the proviso that when R.sub.1 is alkoxy or alkylthio, then R.sub.2 cannot be alkoxy or alkylthio; X and X', which can be the same or different, are each hydrogen, C.sub.1 -C.sub.5 alkyl, carboxy, C.sub.2 -C.sub.6 alkoxycarbonyl, halo, C.sub.1 -C.sub.5 alkoxy, dialkylcarbamyl wherein the alkyl portions, which can be the same or different, each have 1 to 5 carbon atoms, phenyl, or substituted phenyl the pyridyl ring is oriented such that it is attached to the ##STR2## portion of the molecule via a carbon-carbon bond; and R-COO- is the acyloxy residue of a monocarboxylic acid; a steroidal monocarboxylic acid; or a cephalosporin or penicillin antibiotic.

    Abstract translation: 所公开的具有结构式（I）的衍生物，其中可以相同或不同的R 1和R 2各自为氢，C 1 -C 5烷基，C 1 -C 5烷氧基，C 1 -C 5烷硫基，苯基或具有一个或多个取代基的取代苯基，其各自选自C 1 -C 5烷基，C 1 -C 5烷氧基，氯和二烷基氨基，其中烷基部分可以是 相同或不同，各自具有1至5个碳原子，条件是当R 1为烷氧基或烷硫基时，则R 2不能为烷氧基或烷硫基; X和X'可以相同或不同，各自为氢，C 1 -C 5烷基，羧基，C 2 -C 6烷氧基羰基，卤素，C 1 -C 5烷氧基，二烷基氨基甲酰基，其中烷基部分可以相同或不同， 各自具有1至5个碳原子，苯基或取代的苯基，吡啶环被取向使得其通过碳 - 碳键连接到分子的部分; 和R-COO-是一元羧酸的酰氧基残基; 甾体单羧酸; 或头孢菌素或青霉素抗生素。

    Bis-esters of 1,1-alkanediols with 6-beta-hydroxymethylpenicillanic acid 1,1-dioxide
    7.
    发明授权
    Bis-esters of 1,1-alkanediols with 6-beta-hydroxymethylpenicillanic acid 1,1-dioxide 失效
    1,1-链烷二醇与6-β-羟甲基青霉烷酸1,1-二氧化物的双酯

    公开(公告)号：US4376076A

    公开(公告)日：1983-03-08

    申请号：US380174

    申请日：1982-05-20

    Applicant: Michael S. Kellogg

    Inventor： Michael S. Kellogg

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

    CPC classification number: C07D499/00 ,  Y10S514/962

    Abstract: Bis-Esters of 1,1-alkanediols with 6-beta(hydroxymethyl)penicillanic acid 1,1-dioxide and 6-betaacylaminopenicillanic acids are useful as antibacterial agents. Intermediates useful for the preparation of these compounds include halomethyl, alkylsulfonyloxymethyl and arylsulfonyloxymethylesters of 6-beta(hydroxymethyl)penicillanic acid 1,1-dioxide and 6-beta-aminopenicillanoyloxymethyl-6'-beta-(hydroxymethyl)penicillanate 1,1-dioxide.

    Abstract translation: 具有6-β（羟甲基）青霉烷酸1,1-二氧化物和6-β-酰基氨基青霉烷酸的1,1-链烷二醇的双酯可用作抗菌剂。 可用于制备这些化合物的中间体包括6-β（羟甲基）青霉烷酸1,1-二氧化物和6-β-氨基青霉烷酰氧基甲基-6'-β-（羟甲基）青霉素1,1-二氧化物的卤代甲基，烷基磺酰氧基甲基和芳基磺酰氧基甲基酯。

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