6-aminoalkylpenicillanic acid 1,1-dioxides and derivatives...

Details 6-aminoalkylpenicillanic acid 1,1-dioxides and derivatives... 6-aminoalkylpenicillanic acid 1,1-dioxides and derivatives...

C - Chemistry, Metallurgy

07

D

260/118.5, 260/1

C07D 499/00 (2006.01) A61K 31/43 (2006.01) A61K 31/545 (2006.01) C07D 519/00 (2006.01)

Patent

CA 1190921

Abstract beta-Lactamase inhibitors which are 6-alpha- and 6-beta-(aminomethyl) and (1-aminoethyl)pencillanic acid 1,1-dioxides, said aminomethyl compounds optionally substituted on amino nitrogen with benzyl, hydroxybenzyl, picolyl or phensthyl, pharmaceutically-acceptable salts thereof; conventional esters thereof hydrolyzable in vivo; bis-methanediol esters thereof; or mixed methanediol esters with said beta-lactamase inhibitors and sulbactam. Pharmaceutical compositions thereof in combination with a conventional beta-lactam antibiotic, used in the treatment of bacterial infections; compounds useful as intermediates in the synthesis of said beta- lactamase inhibitors. Antibacterial bis-methanediol esters of said beta-lactamase inhibitors and ampicillin or amoxicillin, also used in the treatment of bacterial infections; and intermediates therefor.

419181

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