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    6-Azaoligocycloalkylmethyleneaminopenam compounds
    4.
    发明授权
    6-Azaoligocycloalkylmethyleneaminopenam compounds 失效
    6-氮杂环烷基亚甲基氨基戊酸化合物

    公开(公告)号：US4508723A

    公开(公告)日：1985-04-02

    申请号：US385139

    申请日：1982-06-04

    申请人： Karl Schaffner ,  Riccardo Scartazzini

    发明人： Karl Schaffner ,  Riccardo Scartazzini

    IPC分类号： A61K31/43 ,  A61P31/04 ,  C07D499/00 ,  C07D499/10 ,  C07D499/21 ,  A61K31/38 ,  C07D499/32

    CPC分类号： C07D499/00

    摘要： 6-Amino-penam compounds, having an antimicrobial action, of the formula ##STR1## in which R.sub.1 is an azaoligocycloalkyl radical which is bonded via the ring nitrogen atom and contains at least one endo-bridge atom and a total of 7 to 12 ring atoms and can contain a double bond and/or, if desired, as a further ring hetero-atom, an oxygen atom, or a nitrogen atom which can link the radical X.sub.1, where X.sub.1 is hydrogen or lower alkyl, and/or, if desired, free, esterified or etherified hydroxyl which is bonded to a ring carbon atom, and in which R.sub.2 is free carboxyl or carboxyl esterified by a physiologically detachable group, and salts of such compounds, processes for their preparation, pharmaceutical preparations which contain these compounds, including mixtures of these compounds with other antimicrobial, especially antibacterial and/or antiviral, active ingredients and/or additional substances or substance mixtures which alleviate the symptoms in the case of infections, the use of the novel compounds of the formula I and their salts, and of the novel substance mixtures, for combating micro-organisms and the preparation of corresponding medicaments by non-chemical means.

    摘要翻译： 具有抗微生物作用的6-氨基 - penam化合物，其具有式（I），其中R1是通过环氮原子键合并且含有至少一个内桥原子并且总共7个的氮杂稠环烷基 至12个环原子，并且可以含有双键和/或如果需要，作为另外的环杂原子，氧原子或可连接基团X 1的氮原子，其中X 1是氢或低级烷基，和/ 或者如果需要，与环碳原子键合的游离的，酯化的或醚化的羟基，其中R2是通过生理上可分离的基团游离羧基或羧基酯化的化合物，以及这些化合物的盐，其制备方法，药物制剂 包含这些化合物，包括这些化合物与其他抗微生物剂，特别是抗细菌和/或抗病毒活性成分和/或其他物质或物质混合物的混合物，其在感染的情况下减轻症状，使用nove 1种式I化合物及其盐，以及新型物质混合物，用于防治微生物和通过非化学方法制备相应的药物。

    Ester of 6-[(hexahydro-1H-azepin-1-yl)methyleneamino]penicillanic acid, and its use as antibacterial agent
    6.
    发明授权
    Ester of 6-[(hexahydro-1H-azepin-1-yl)methyleneamino]penicillanic acid, and its use as antibacterial agent 失效
    6 - [（六氢-1H-吖庚因-1-基）亚甲基氨基]青霉烷酸酯，其用作抗菌剂

    公开(公告)号：US4416891A

    公开(公告)日：1983-11-22

    申请号：US399132

    申请日：1982-07-16

    申请人： Fumio Sakamoto ,  Shoji Ikeda ,  Goro Tsukamoto

    发明人： Fumio Sakamoto ,  Shoji Ikeda ,  Goro Tsukamoto

    IPC分类号： A61K31/43 ,  A61P31/04 ,  C07D317/40 ,  C07D499/00 ,  C07D499/08 ,  C07D499/10 ,  C07D499/21 ,  C07D499/32 ,  A61K31/425

    CPC分类号： C07D499/00 ,  C07D317/40

    摘要： (5-Methyl-2-oxo-1,3-dioxolen-4-yl)methyl 6-[(hexahydro-1H-azepin-1-yl)methyleneamino]penicillanate of the following formula (I) ##STR1## or its pharmaceutically acceptable acid addition salt. The compound is useful as an antibacterial agent and may be prepared by reacting (5-methyl-2-oxo-1,3-dioxolen-4-yl)-methyl 6-aminopenicillanate of the following formula (II) ##STR2## or its acid addition salt with chloro-N,N-hexamethyleneformiminium chloride, and as required, converting the resulting compound to its pharmaceutically acceptable acid addition salt.

    摘要翻译： （I）的（5-甲基-2-氧代-1,3-二氧杂环戊烯-4-基）甲基6 - [（六氢-1H-吖庚因-1-基）亚甲基氨基]青霉烷酸 或其药学上可接受的酸加成盐。 该化合物可用作抗菌剂，并且可以通过使下式（II）的（5-甲基-2-氧代-1,3-二氧杂环戊烯-4-基） - 6-氨基青霉烷酸甲酯（II） ）或其与氯-N，N-六亚甲基酰亚胺氯化物的酸加成盐，并根据需要将所得化合物转化为其药学上可接受的酸加成盐。

    6-Perhaloalkylsulfonyloxy-penicillanic acids and derivatives thereof
    7.
    发明授权
    6-Perhaloalkylsulfonyloxy-penicillanic acids and derivatives thereof 失效
    6-全卤烷基磺酰氧基 - 青霉烷酸及其衍生物

    公开(公告)号：US4356122A

    公开(公告)日：1982-10-26

    申请号：US214846

    申请日：1980-12-10

    申请人： John E. G. Kemp

    发明人： John E. G. Kemp

    IPC分类号： C07F7/08 ,  C07D499/00 ,  C07D499/10 ,  C07D499/32 ,  C07D499/86 ,  C07D499/87 ,  C07D499/897

    CPC分类号： C07D499/00 ,  Y02P20/55

    摘要： 6-Alpha and 6-beta-substituted penicillanic acid derivatives of the formula: ##STR1## wherein R is H or a conventional penicillin carboxy protecting group or an ester forming residue readily hydrolyzable in vivo and R.sup.1 is a perhaloalkyl group of from 1 to 4 carbon atoms wherein the halogen atoms are fluoro or chloro, undergo SN.sub.2 nucleophilic displacement with halide or azide ions with inversion of configuration at C-6 to yield the corresponding 6-beta or 6-alpha-halo- or azido-substituted product.

    摘要翻译： 6-α和6-β取代的青霉烷酸衍生物，其分子式如下：其中R为H或常规青霉素羧基保护基或酯形成残基在体内容易水解，R 1为全卤代烷基 1至4个碳原子，其中卤素原子是氟或氯，通过在C-6处具有反型构型的卤化物或叠氮化物离子进行SN2亲核置换，得到相应的6-β或6-α-卤代或叠氮取代的产物 。

    Penicillins and processes for their preparation and use
    10.
    发明授权
    Penicillins and processes for their preparation and use 失效
    青霉素及其制备和使用的过程

    公开(公告)号：US4031229A

    公开(公告)日：1977-06-21

    申请号：US692930

    申请日：1976-06-04

    申请人： Hans-Bodo Konig ,  Karl Georg Metzger ,  Wilfried Schrock

    发明人： Hans-Bodo Konig ,  Karl Georg Metzger ,  Wilfried Schrock

    IPC分类号： C07D499/10 ,  C07D233/32 ,  C07D233/38 ,  C07D499/00 ,  C07D499/04 ,  C07D499/64 ,  C07D499/66 ,  C07D499/68 ,  C07D499/70 ,  A61K31/43

    CPC分类号： C07D233/32 ,  C07D233/38 ,  C07D499/00

    摘要： 6-[.alpha.-(Imidazolidin-2-on-1-carbonylamido)acetamido]-penicillanic acids substituted in the 3-position of the imidazolidinone ring with phenyl or a substituted phenyl group and on the .alpha.-carbon atom of the acetamido bridge with a phenyl, thienyl, cyclohexenyl or cyclohexadienyl group, and their salts, are antibacterial agents. The compounds, of which .alpha.-(3-phenylimidazolidin-2-on-1-ylcarbonylamino)benzylpenicillin is a representative example, are prepared by acylation of the corresponding 6-(.alpha.-aminoacetamido)penicillanic acid or a derivative thereof.

    摘要翻译： 在咪唑啉酮环的3位被苯基或取代的苯基取代的6- [α-（咪唑烷-2-酮-1-羰基酰氨基）乙酰氨基] - 青霉烷酸和乙酰氨基桥的α-碳原子上， 苯基，噻吩基，环己烯基或环己二烯基及其盐是抗菌剂。 通过酰化相应的6-（α-氨基乙酰氨基）青霉烷酸或其衍生物，制备其中α-（3-苯基咪唑烷-2-酮-1-基羰基氨基）苄青霉素的代表性实例的化合物。