| 摘要 |
.beta.-Lactams are described, namely of the general formula <IMG> I in which Z signifies methylene, oxygen or sulphur and R signifies hydrogen, lower (cyclo)alkyl optionally substituted by carboxy, lower alkoxycarbonyl, carbamoyl, lower alkylcarbamoyl, phenylcarbamoyl or hydroxyphenylcarbamoyl, lower alkenylmethyl, lower alkenylmethoxycarbonyl, formyl, lower (cyclo)alkanoyl or (cyclo)alkylsulphonyl optionally substituted by halogen, cyano, carbamoyl-lower-alkoxy, carbamoyl-lower alkylthio or carbamoyl-lower alkylamino, carbamoyl optionally substituted by lower (cyclo)alkyl, lower alkoxycarbonyllower alkyl, benzyloxycarbonyl-lower alkyl or carboxylower alkyl or a ring structure of the general formulae Q-X-CO- (a1) Q-X-SO2- (a2) wherein Q represents a 5- or 6-membered ring optionally containing nitrogen, sulphur and/or oxygen and X represents a direct bond or one of the groups -CH2-, -CH2CH2-, -CH=CH-, -NH-, -NHCH2-, -CH2NH-, -CH(NH2)-, -CH2CH2NH-, -C(=NOCH3)-, -OCH2- and -SCH2-; and wherein further A signifies lower alkyl, hydroxy-lower alkyl, vinyl, cyanovinyl, lower alkoxy, optionally phenyl-substituted lower (cyclo)alkanoyloxy or (cyclo)alkylsulphonyloxy, optionally lower-(cyclo)alkyl-substituted benzoyloxy or phenylsulphonyloxy, a residue -S-Het or -S-CH2-Het, wherein Het represents a 5- or 6-membered heterocycle containing nitrogen, sulphur and/or oxygen, or a residue -CH2-L, wherein L represents optionally phenyl-substituted lower (cyclo)alkanoyloxy or (cyclo)alkylsulphonyloxy, optionally lower (cyclo)alkyl-substituted benzoyloxy or phenylsulphonyloxy, carbamoyloxy, lower (cyclo)alkoxycarbonyl, carboxy, azido, amino, lower (cyclo)alkanoylamino, lower (cyclo)alkylsulphonylamino, lower (cyclo)alkylamino, dilower (cyclo)alkylamino, a 5- or 6-membered ring bonded to a nitrogen atom or a residue -S-Het or -S-CH2-Het, wherein Het has the above significance, and pharmaceutically compatible, readily hydrolyzable esters and salts of these compounds. A process for the manufacture of the .beta.-lactams described above as well as intermediates occurring therein are also described, as are corresponding medicaments. The products have .beta.-lactamase inhibiting properties and are useful in the control of .beta.-lactamase-forming pathogens in combination with .beta.-lactam antibiotics. They also exhibit antibacterial activity of their own and can accordingly be used themselves in the control of infectious diseases.
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