申请人:Ciba Geigy Corporation
公开号:US04508723A1
公开(公告)日:1985-04-02
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.
具有抗微生物作用的6-氨基青霉素化合物,化学式为##STR1## 其中R.sub.1是通过环氮原子连接的含有至少一个内部桥接原子和7到12个环原子的氮杂环烷基,可以包含双键和/或,如果需要,作为进一步的环杂原子,一个氧原子或一个氮原子,其可以连接基团X.sub.1,其中X.sub.1是氢或较低的烷基,并且/或,如果需要,与环碳原子结合的自由、酯化或醚化的羟基,R.sub.2是自由羧基或被生理可分离基团酯化的羧基,并且这些化合物的盐,它们的制备过程,包含这些化合物的制药制剂,包括这些化合物与其他抗微生物,特别是抗菌和/或抗病毒活性成分和/或减轻感染症状的其他物质或物质混合物的混合物,以及使用公式I的新化合物及其盐和新物质混合物,用于对抗微生物和通过非化学手段制备相应药物。