C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 487/04 (2006.01) A61K 31/395 (2006.01) A61K 31/43 (2006.01) C07D 471/16 (2006.01) C07F 7/10 (2006.01)
Patent
CA 2064945
RAN 44 10/229 Abstract There are described .beta.-lactams, namely of the general formula Image I in which R signifies lower alkoxycarbonyl, lower alkoxy- carbonylamino, the acyl residue of an .alpha.- or .beta.-amino acid or a residue of the general formula Q-X-Y- (a) wherein Q signifies a 3-6-membered ring which optionally contains nitrogen, sulphur and/or oxygen and which is optionally bonded with a fused ring, X signifies a direct bond or a linear "spacer" with up to 6 atoms consisting of carbon, nitrogen, oxygen and/or sulphur, 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 (where X contains neither sulphur nor carbonyl as a terminal component) -SO2-; and in which R1 signifies hydrogen, halogen, carbamoyloxy, lower alkanoyloxy or a group of the formula -S-Het, wherein Het represents a 5-6-membered heteroaromatic group containing nitrogen, sulphur and/or oxygen, and R2 represents the sulpho group -SO3H or R1 and R2 together signify a group of the formula Image (b) wherein A represents hydrogen or a residue which is usable in the 3-position of cephalosporin antibiotics, and in which R 3 represents hydrogen or R1 and R3 together represent a group of the general formula =CH-Ra (c) wherein Ra signifies one of the groups -CORb (c1) -H2-OCORc (c2) -CH2-NRdRe (c3) -CH2-S-Het (c4) in which Rb represents lower alkoxy or amino, Rc represents lower alkyl, phenyl or amino, Rd and Re each represent hydrogen or lower alkyl or together with the N atom represent a 5- or 6-membered N-heterocycle which optionally contains a further nitrogen, oxygen or sulphur atom and Het represents a 5-6-membered heteroaromatic group containing nitrogen, sulphur and/or oxygen, and pharmaceutically compatible salts of these compounds. Further, also a process for the manufacture of these .beta.- lactams as well as intermediates thereby obtained. Further- more, also corresponding medicaments. The products have .beta.-lactamase inhibiting properties. They are useful in combination with .beta.-lactam antibiotics in the control of .beta.-lactamase forming pathogens.
Charnas Robert
Gubernator Klaus
Heinze Ingrid
Hubschwerlen Christian
F. Hoffmann-La Roche Ag
Gowling Lafleur Henderson Llp
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