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filingDate 1982-08-24-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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publicationDate 1983-03-09-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber EP-0073454-A2
titleOfInvention 6-Alpha-methoxy-penicillins, their salts, process for their preparation and therapeutic agents containing these compounds
abstract in der A die Phenyl-, p-Hydroxyphenyl-, 2- oder 3-Thienylgruppe, R die Cyclopropylgruppe, eine Gruppe der allgemeinen Formel -NHR 1 , wobei R 1 einen gegebenenfalls ab Kohlenstoffatom 2 durch eine Hydroxygruppe substituierten aliphatischen, verzweigten oder unverzweigten Kohlenwasserstoffrest mit 1 bis 4 Kohlenstoffatomen, einen gegebenenfalls durch eine Hydroxygruppe substituierten Cycloalkylrest mit 3 bis 6 Kohlenstoffatomen oder eine gegebenenfalls durch eine Hydroxy-, Methylsulfinyl-, Methylsulfonyl- oder Aminosulfonylgruppe substituierte 3-Pyridyl-, 2-Furylmethyl-, 2-Thienylmethyl-, 3-lmidazolylmethyl-, 2-Thiazolylmethyl- oder 3-Pyridylmethylgruppe darstellt, eine Gruppe der allgemeinen Formeln , wobei n die Zahl 0 oder 1, R 2 und R 3 , die gleich oder verschieden sein können Wasserstoffatome, Hydroxy-, Acetylamino-, Aminocarbonylamino-, Nitro-, Aminocarbonyl-, Cyan-, Methylsulfinyl-, Methylsulfonyl-, Aminosulfonyl-, Methylaminosulfonyl-, Aminocarbonylmethylaminosulfonyl-, 2'-Hydroxyäthylaminosulfonyl-, Cyanaminosulfonyl-, Aminocarbonylaminosulfonyl-, Acetylaminosulfonyl-, Methylsulfonylaminosulfonyl- oder Acetylhydrazinosulfonylgruppen darstellen,n wobei m die Zahl 2,3 oder4 darstellt, oder eine Gruppe der Formeln bedeuten und deren Salze mit anorganischen oder organischen Basen, welche eine Wirkung gegen grampositive und gramnegative Bakterien, beispielsweise gegen β-Lactamasetragende Escherichia coli- und Klebsiella pneumoniae-Bakterien, aufweisen. New 6 a-methoxy-penicillins of the general formula in the A is the phenyl, p-hydroxyphenyl, 2- or 3-thienyl group, R is the cyclopropyl group, a group of the general formula -NHR 1 , where R 1 is an aliphatic, branched or unbranched hydrocarbon radical with 1 to 4 carbon atoms which is optionally substituted from carbon atom 2 by a hydroxyl group, an optionally substituted by a hydroxyl group cycloalkyl radical with 3 to 6 carbon atoms or an optionally by a hydroxy, methylsulfinyl, methylsulfonyl or aminosulfonyl group substituted 3-pyridyl, 2-furylmethyl, 2-thienylmethyl, 3-imidazolylmethyl, 2-thiazolylmethyl or 3-pyridylmethyl group, a group of the general formula , where n is the number 0 or 1, R 2 and R 3 , which may be the same or different, are hydrogen atoms, hydroxyl, acetylamino, aminocarbonylamino, nitro, aminocarbonyl, cyan, methylsulfinyl, methylsulfonyl, aminosulfonyl, methylaminosulfonyl, aminocarbonylmethylaminosulfonyl, 2'- Represent hydroxyethylaminosulfonyl, cyanaminosulfonyl, aminocarbonylaminosulfonyl, acetylaminosulfonyl, methylsulfonylaminosulfonyl or acetylhydrazinosulfonyl groups, where m represents the number 2, 3 or 4, or a group of the formula mean and their salts with inorganic or organic bases which have an action against gram-positive and gram-negative bacteria, for example against Escherichia coli and Klebsiella pneumoniae bacteria carrying β-lactamase. n n n The new compounds can be prepared by methods customary for analog compounds.
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