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    1,1-Alkanediol dicarboxylate linked antibacterial agents
    1.
    发明授权
    1,1-Alkanediol dicarboxylate linked antibacterial agents 失效
    1,1-二醇二羧酸酯连接抗菌剂

    公开(公告)号：US4457924A

    公开(公告)日：1984-07-03

    申请号：US429915

    申请日：1982-09-30

    Applicant: Vytautas J. Jasys ,  Michael S. Kellogg

    Inventor： Vytautas J. Jasys ,  Michael S. Kellogg

    IPC: C07D499/87 ,  A61K31/43 ,  A61P31/04 ,  C07D499/00 ,  C07D499/08 ,  C07D499/32 ,  C07D499/60 ,  C07D499/74 ,  C07D499/86 ,  C07D499/861 ,  C07D499/897 ,  C07D519/00 ,  A61K31/655 ,  C07D263/00

    CPC classification number: C07D499/00

    Abstract: Useful antibacterial agents in which a penicillin and/or a beta-lactamase inhibitor are linked via 1,1-alkanediol dicarboxylates are of the formula ##STR1## where A is the residue of certain dicarboxyic acids, R.sup.3 is H or (C.sub.1 -C.sub.3), n is zero or 1 such that when n is zero R is P or B and R.sup.1 is the residue of certain esters, H or a salt thereof; and when n is 1, one of R and R.sup.1 is P and the other is B, and P is ##STR2## where R.sup.2 is H or certain acyl groups, and B is the residue of a beta-lactamase inhibiting carboxylic acid; a method for their use, pharmaceutical compositions thereof and intermediates useful in their production.

    Abstract translation: 其中青霉素和/或β-内酰胺酶抑制剂通过1,1-链烷二醇二羧酸酯连接的有用的抗菌剂具有下式：其中A是某些二羧酸的残基，R3是H或（C1 -C 3），n为0或1，使得当n为零时，R为P或B，R 1为某些酯，H或其盐的残基; 当n为1时，R和R 1中的一个为P，另一个为B，P为，其中R 2为H或某些酰基，B为β-内酰胺酶抑制羧酸的残基; 其使用方法，其药物组合物和可用于其生产的中间体。

    Derivatives of penam-3-carboxylic acid and a pharmaceutical composition containing the same
    3.
    发明授权
    Derivatives of penam-3-carboxylic acid and a pharmaceutical composition containing the same 失效
    吡啶-3-羧酸的衍生物和含有它们的药物组合物

    公开(公告)号：US4202900A

    公开(公告)日：1980-05-13

    申请号：US900696

    申请日：1978-04-28

    Applicant: Karoly Kocsis ,  Bruno Fechtig ,  Hans Bickel

    Inventor： Karoly Kocsis ,  Bruno Fechtig ,  Hans Bickel

    IPC: C07D499/00 ,  C07D499/64 ,  C07D499/74 ,  A61K31/43 ,  C07D499/68

    CPC classification number: C07D499/00

    Abstract: 6-Acylamino-penam-3-carboxylic acids and 7-acylamino-3-cephem-4-carboxylic acids in which the acyl group has the formula ##STR1## in which R.sub.1 is hydrogen, R.sub.2 is optionally substituted phenyl, thienyl or furyl or R.sub.1 and R.sub.2 together are optionally substituted cycloalkyl, n and m independently of one another represent 0 or 1 and B represents an optionally substituted 2,6-dioxo- or 2,6-dithioxo-1,2,3,6-tetrahydro-pyrimidyl, 2-thioxo-6-oxo-1,2,3,6-tetrahydropyrimidyl, 2,6-dihydroxy- or 2,6-dimercapto-pyrimidyl, 2-mercapto-6-hydroxy-pyrimidyl, 2,6-diaminopyrimidyl, 2-amino-6-hydroxy-pyrimidyl or 2,6-dihalogenopyrimidyl radical, these radicals being bonded in the 4- or 5-position.

    Abstract translation: 6-酰基氨基 - penam-3-羧酸和其中酰基具有式“IMAGE”的7-酰基氨基-3-头孢烯-4-羧酸，其中R 1是氢，R 2是任选取代的苯基，噻吩基或呋喃基，或 R 1和R 2一起为任选取代的环烷基，n和m彼此独立地表示0或1，B表示任选取代的2,6-二氧代 - 或2,6-二硫代-1,2,3,6-四氢 - 嘧啶基 2-硫代-6-氧代-1,2,3,6-四氢嘧啶基，2,6-二羟基 - 或2,6-二巯基嘧啶基，2-巯基-6-羟基 - 嘧啶基，2,6-二氨基嘧啶基， 2-氨基-6-羟基 - 嘧啶基或2,6-二卤代嘧啶基，这些基团键合在4-或5-位上。

    Process for etherifying .beta.-lactam antibiotics
    4.
    发明授权
    Process for etherifying .beta.-lactam antibiotics 失效
    醚化的方法{62-内酰胺抗生素

    公开(公告)号：US3994885A

    公开(公告)日：1976-11-30

    申请号：US545451

    申请日：1975-01-30

    Applicant: Gary A. Koppel

    Inventor： Gary A. Koppel

    IPC: C07D499/04 ,  A61K31/43 ,  A61P31/04 ,  C07D20060101 ,  C07D499/00 ,  C07D499/21 ,  C07D499/32 ,  C07D499/44 ,  C07D499/46 ,  C07D499/60 ,  C07D499/62 ,  C07D499/64 ,  C07D499/68 ,  C07D499/70 ,  C07D499/74 ,  C07D499/80 ,  C07D501/20 ,  C07D501/57 ,  C07D501/60 ,  C07D513/20

    CPC classification number: C07D501/57 ,  C07D499/00 ,  C07D499/44

    Abstract: 6-Alkoxylated-6-acylamidopenicillanic acids and 7-alkoxylated-7-acylamidocephalosporin acids and esters thereof, are provided by reacting a 6-acylamidopenicillanic acid ester or a 7-acylamidocephalosporin ester under anhydrous conditions at -90.degree. C. to -15.degree. C. with an alkali metal salt of a lower alkyl alcohol in the presence of an excess of the corresponding alcohol to produce, in situ, the anionic form of the antibiotic which on halogenation with a positive halogen compound, e.g. t-butyl hypochlorite, yields the compound of the invention. Compounds of the invention, e.g. 6-methoxy-6-phenoxyacetamidopenicillanic acid and 7-methoxy-7-[2-(2-thienyl)acetamido]cephalosporanic acid are useful antibiotics.

    Abstract translation: 6-烷氧基化-6-酰氨基青霉烷酸和7-烷氧基化-7-酰基酰氨基头孢菌素酸及其酯通过6-酰基氨基青霉烷酸酯或7-酰基酰氨基头孢菌素酯在-90℃至-15℃的无水条件下反应来提供 用低级烷基醇的碱金属盐在过量相应的醇的存在下，原位生成阴离子形式的抗生素，其用正卤素化合物卤化，例如 叔丁基次氯酸盐，得到本发明的化合物。 本发明的化合物，例如 6-甲氧基-6-苯氧基乙酰氨基青霉烷酸和7-甲氧基-7- [2-（2-噻吩基）乙酰氨基]头孢烷酸是有用的抗生素。

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