Penem-3-carboxylic acid derivatives
AssigneeSankyo Company, Limited
InventorsEiji Ohki, Sadao Oida, Akira Yoshida, Teruo Hayashi, Shinichi Sugawara
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AssigneeSankyo Company, Limited
InventorsEiji Ohki, Sadao Oida, Akira Yoshida, Teruo Hayashi, Shinichi Sugawara
Estimating the term…
Penem-3-carboxylic acid derivatives of formula (I): ##STR1## (wherein: R.sup.1 represents a hydrogen atom, an alkyl group, an alkoxy group, a hydroxyalkyl group, an acyloxyalkyl group, an alkylsulphonyloxyalkyl group, an arylsulphonyloxyalkyl group or a trialkylsilyloxyalkyl group; R.sup.2 represents a hydrogen atom or an alkyl group; R.sup.3 represents a hydrogen atom, an amino-protecting group or a group of formula ##STR2## in which R.sup.5 and R.sup.6 are the same or different and each represents a hydrogen atom or an alkyl group; A represents a branched-chain alkylene group; and R.sup.4 represents a carboxy group or a protected carboxy group) and pharmaceutically acceptable salts thereof, may be prepared by heating a corresponding phosphorus-ylide compound or by reacting a corresponding azetidin-2-one with a suitable phosphorous acid triester or triamide, and have been found to have excellent antibacterial activity accompanied by a very low acute toxicity.
Compounds of formula (I):
In a pharmaceutical composition comprising an antibiotic and a pharmaceutically acceptable carrier or diluent, the improvement which comprises employing as antibiotic a compound of formula:
2-(2-Amino-1-methylethylthio)-6-(1-hydroxyethyl)penem-3-carboxylic acid and pharmaceutically acceptable salts thereof.
(5R,6S)-(2-Amino-1-methylethylthio)-6-[(R)-1 -hydroxyethyl]penem-3-carboxylic acid and pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.