derivatives of acid ammidinopeni cillanico process for their preparation and pharmaceutical compositions containing these derivatives

摘要

The present invention relates to new 6 beta -amidino-penicillanic acids of the formula: IMAGE I in which X is oxygen or sulphur, -A- is aliphatic hydrocarbon, or a single bond, -B- is aliphatic hydrocarbon, or a single bond; R1 and R2 stand for hydrogen, lower alkyl, phenyl or phenyl-lower alkyl; or R2 is acyl or guanyl; or R1 and R2 together with the nitrogen atom can form a monocyclic, saturated ring or represent IMAGE in which R3 and R4 each stands for hydrogen, lower alkyl, phenyl, or phenyl-lower alkyl, or R3 and R4 together with nitrogen form a monocyclic, saturated ring; -W- stands for IMAGE which represent saturated, monocyclic, bicyclic or spirocyclic ring systems, respectively; salts of the compounds of formula I, and easily hydrolyzable, esters thereof, and salts of such esters; the invention further relating to methods of producing the compounds; to intermediates in their preparation; to pharmaceutical compositions containing the compounds; and to dosage units thereof, and to their use. The compounds of the present invention are active against a variety of pathogenic microorganisms, including gram-positive and gram-negative bacteria.