发明名称 2-BETA-ALKENYLPENAM SULFONE AS BETA-LACTAMASE INHIBITOR
摘要 The present invention relates to penem derivatives, especially to 3 beta -alkenyl-penem derivatives of the general formula <IMAGE> wherein one of R<1> and R<2> is -COR<4>, -CN, -CH2R<5>, halogen, -CH=CHR<6> or Q and the other is hydrogen or lower alkyl or both together are a gamma -lactam ring, R<3> is hydrogen, lower alkyl, arylalkyl, allyl or a radical which can be removed in vivo, R<4> is hydrogen, lower alkyl, lower alkoxy, benzyloxy, amino, lower alkylamino or lower alkyl-lower alkoxyamino, R<5> is hydroxyl, -OCONHR<7>, -OCONH2 or a five- or six-membered heteroaromatic ring containing N, S and/or O and linked via a nitrogen atom, R<6> is -CN or -CHO, R<7> is COCH2Cl, Q is a five- or six-membered heteroaromatic ring containing N, S and/or O and n is 0, 1 or 2, and the pharmaceutically tolerable salts of these compounds. These compounds are good beta -lactamase inhibitors. They can be used, if appropriate mixed with a beta -lactam antibiotic, for the prevention or for the treatment of bacterial infections.
申请公布号 JPH0782273(A) 申请公布日期 1995.03.28
申请号 JP19940194133 申请日期 1994.08.18
申请人 F HOFFMANN LA ROCHE AG 发明人 KURISUCHIYAN YUBUSHIYUUERUREN;HANSU RIHITAA;JIYANNRIYUTSUKU SUPEKURAN
分类号 A61K31/40;A61K31/425;A61K31/43;A61K31/431;A61K31/435;A61K31/495;A61K31/545;A61P31/04;A61P43/00;C07D499/00;C07D499/86;C07D499/87;C07D499/897;(IPC1-7):C07D499/86 主分类号 A61K31/40
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