2.beta.-Chloromethyl-2.alpha.-methylpenam-3.alpha.-carboxylic acid sulfone and salts and esters thereof
AssigneeBristol-Myers Company
InventorWilliam J. Gottstein
Life of this patent
Estimating the term…
Abstract
2.beta.-Chloromethyl-2.alpha.-methylpenam-3.alpha.-carboxylic acid sulfone and salts and esters thereof were synthesized and found to be potent inhibitors of .beta.-lactamases.
Claims17
The acid having the formula ##STR68## or a pharmaceutically acceptable salt of said acid or an ester of said acid having the formula ##STR69## wherein R is phenacyl, acetoxymethyl, pivaloyloxymethyl, .alpha.-acetoxyethyl, .alpha.-acetoxybenzyl, .alpha.-pivaloyloxyethyl, 3-phthalidyl, 5-indanyl, methoxymethyl, benzoyloxymethyl, .alpha.-ethylbutyryloxymethyl, propionyloxymethyl, valeryloxymethyl, isobutyryloxymethyl, 6-[(R)-2-amino-2-phenylacetamido]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3 .2.0]heptane-2-carbonyloxymethyl or 6-[(R)-2-amino-2-p-hydroxyphenylacetamido]-3,3-dimethyl-7-oxo-4-thia-1-aza bicyclo[3.2.0]heptane-2-carbonyloxymethyl.
The acid having the formula ##STR70##
An ester having the formula ##STR71## wherein R is phenacyl, acetoxymethyl, pivaloyloxymethyl, .alpha.-acetoxyethyl, .alpha.-acetoxybenzyl, .alpha.-pivaloyloxyethyl, 3-phthalidyl, 5-indanyl, methoxymethyl, benzoyloxymethyl, .alpha.-ethylbutyryloxymethyl, propionyloxymethyl, valeryloxymethyl, isobutyryloxymethyl, 6-[(R)-2-amino-2-phenylacetamido]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3 .2.0]heptane-2-carbonyloxymethyl or 6-[(R)-2-amino-2-p-hydroxyphenylacetamido]-3,3-dimethyl-7-oxo-4-thia-1-aza bicyclo[3.2.0]heptane-2-carbonyloxymethyl.
The ester having the formula ##STR72##
The ester having the formula ##STR73##
Dependencies are inferred from the claim text.