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US 4,540,580 AGranted
2-[(1'R)-1'-Aminoalkyl]penems
AssigneeSchering Corporation
InventorsAdriano Afonso, Jay Weinstein
Life of this patent
Estimating the term…
Abstract
Disclosed are 6-(1'-hydroxyethyl)-2-[(1'R)-1'-aminoalkyl]penem-3-carboxylic acids and salts and esters thereof. The compounds are useful and potent antibacterial agents and can be formulated into a variety of forms suitable for oral, parenteral or topical use.
Claims29
A compound of the formula ##STR14## wherein n is 0-4;
- R' and R" are indpendently hydrogen, lower alkyl, lower alkenyl, phenyl, substituted phenyl, wherein the substituents are one or more groups selected from chloro, bromo, fluoro, lower alkyl, hydroxy, nitro, amino, aminomethyl, lower monoalkylamino, lower dialkylamino, lower alkoxy and carboxy, or heteroaryl of 5 to 7 ring atoms of which 3 to 6 are carbon atoms and the remaining ring atoms are nitrogen, sulfur or oxygen, or R' is hydrogen and R" is CH.sub.3 (CH.sub.2).sub.p CO-- or CH.sub.3 (CH.sub.2).sub.q SO.sub.2 --, wherein p is 0-16 and q is 1-17, or R', R" and the N to which they are attached form a group of the formula ##STR15## wherein X is hydrogen, lower alkyl or amino;
- Z is hydrogen, COOR', OR', NR'R", SR', 4-imidazolyl, 3-indolyl, phenyl, p-hydroxyphenyl or branched lower alkyl, and the pharmaceutically acceptable salts and metabolizable esters thereof, in racemic or optically active form.
Dependencies are inferred from the claim text.