BETA-LACTAM COMPOUND

摘要

beta -lactams are described, to be precise those of the general formula in which R denotes lower alkoxycarbonyl, lower alkoxycarbonylamino, the acyl radical of an alpha - or beta -amino acid or a radical of the general formula Q-X-Y- (a> in which Q denotes a 3,6-membered ring optionally containing nitrogen, sulphur and/or oxygen and optionally bonded to a fused ring, X denotes a direct bond or a linear spacer consisting of carbon, nitrogen, oxygen and/or sulphur and having up to 6 atoms, of which up to 2 atoms can be nitrogen atoms and 1 atom can be oxygen or sulphur, and Y represents one of the groups -CO-, -CS-, -CONH- and (if X contains neither sulphur nor carbonyl as an end member) represents -SO2-; and in which additionally R<1> represents hydrogen, halogen, carbamoyloxy, lower alkanoyloxy or a group of the formula -S-Het, Het represents a 5-6-membered heteroaromatic group containing nitrogen, sulphur and/or oxygen and R<2> represents the sulphur group -SO3H or R<1> and R<2> together denote a group of the formula in which A represents hydrogen or a radical which can be used in the 3-position of cephalosporin antibiotics, and in which additionally R<3> represents hydrogen or R<1> and R<3> together represent a group of the general formula =CH-R (c> in which R denotes one of the groups -COR (c<1>) -CH2-OCOR (c<2>) -CH2-NRR (c<3>) -CH2-S-Het (c<4>) in which R represents lower alkoxy or amino, R represents lower alkyl, phenyl or amino, R and R each represents hydrogen or lower alkyl or together with the N atom represent a 5- or 6-membered N-heterocycle optionally containing a further nitrogen, oxygen or sulphur atom and Het represents a 5-6-membered heteroaromatic group containing nitrogen, sulphur and/or oxygen, and pharmaceutically tolerable salts of these compounds. Furthermore also a process for the preparation of these beta -lactams and intermediates obtained in this process. In addition also corresponding medicaments. The products have beta -lactamase-inhibiting properties. They are useful in the control of beta -lactamase-forming disease pathogens in combination with beta -lactam antibiotics.