1-, AND 1,1- DISUBSTITUTED -6- SUBSTITUTED -2- CARBAMIMIDOYL -1- CARBADETHIAPEN-2-EM -3- CARBOXYLIC ACIDS

摘要

TITLE OF THE INVENTION1-, AND 1,1-DISUBSTITUTED-6-SUBSTITUTED-2-CARBAM-IMIDOYL-1-CARBADETHIAPEN-2-EM-3-CARBOXYLIC ACIDSABSTRACT OF THE DISCLOSUREDisclosed are 1-, and 1,1-disubstituted-6-substituted-2-carbamimidoyl-1-carbadethiapen-2-em--3-carboxylic acids having the structure:- 2 -wherein R9 and R10 are, inter alia, hydrogen(R9 and R10 are not both hydrogen) alkyl,cycloalkyl, aryl, and aralkyl; R9 and R10 may bejoined; R6 and R7 are, inter alia, independentlyselected from the group consisting of hydrogen,alkyl, alkenyl, aryl, aralkyl; A is a direct, singlebond connecting the indicated S and C atoms, or A isa cyclic or acylic connecting group selected, interalia, from alkyl, cycloalkyl, aryl, heteroaryl,heteroalkyl; R1 and R2, which define thecarbamimidoyl function, are, inter alia,independently selected from hydrogen, alkyl, aryl;additionally, said carbamimidoyl is characterized bycyclic structures achieved by the joinder of the twonitrogen atoms via their substituents and by theirjoinder to connecting group A; additionally,"carbamimidiums" are disclosed by quarternization ofone of the nitrogen atoms of said carbamimidoyl.Such compounds as well as their pharmaceuticallyacceptable salt, ester and amide derivatives areuseful as antibiotics. Also disclosed are processesfor the preparation of such compounds; pharmaceuticalcompositions comprising such compounds; and methodsof treatment comprising administering such compoundsand compositions when an antibiotic effect isindicated.