.beta.-lactams

C - Chemistry – Metallurgy – 07 – D

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260/118.5

C07D 499/00 (2006.01) C07F 9/6561 (2006.01)

Patent

CA 1180005

RAN 4410/149 Abstract The .beta.-lactams of the general formula Image I wherein R1 signifies cyano or a group of the formula R4-CO- or R5-A-CO- R2 signifies hydrogen, lower alkyl or halogen, R3 signifies hydrogen or a group readily cleavable by hydrolysis, n signifies the number 0, 1 or 2, R4 signifies hydrogen, hydroxy, lower alkoxy, lower alkyl, aryl or a group of the formula R6ON=C-COOR7, R5 signifies halogen, lower alkoxy, lower alkylthio, lower alkylsulphinyl, lower alkyl- sulphonyl, aryl, aryloxy, arylthio, arylsulphinyl, arylsulphonyl or di -(lower alkoxy)-phosphinyl, R6 and R7 each signify lower alkyl and A signi- fies lower alkylene, and pharmaceutically acceptable salts of carboxylic acids of formula I with bases are novel and have pronounced .beta.-lactamase-inhibiting properties. They can accordingly be used in the control of .beta.-lactamase-forming pathogens with .beta.-lactam antibiotics such as the penicillins and cephalosporins. These novel active substances can be manufactured from starting materials some of which are also novel and can be brought into galenical administration forms.

386073

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