Cephalosporin analogs for oral use
AssigneeShionogi & Co., Ltd.
InventorsMasayuki Narisada, Tetso Okada, Tadashi Yoshida, Shinzo Matsuura
Life of this patent
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Abstract
7.beta.-(2-Cyano-aliphatic acylamino)-7.alpha.-methoxy-3-heterocyclic thiomethyl-1-dethia-1-oxa-3-cephem-4-carboxylic acids and salts or pharmacologically acceptable esters generically represented by the following formula are potent antibacterials and esters are prospective oral drugs: ##STR1## (wherein A is a lower alkyl, lower alkenyl or lower alkynyl group; B is a hydrogen atom, salt forming atom, salt forming group or physiologically hydrolyzable ester group; and Het is a heterocyclic group).
Claims20
A 7.beta.-(2-cyanoaliphatic acyl)amino-7.alpha.-methoxy-3-heterocyclic thiomethyl-1-dethia-1-oxa-3-cephem-4-carboxylic acid compound represented by the following formula:
- ##STR24## wherein A is C.sub.1 to C.sub.8 alkyl, C.sub.2 to C.sub.8 alkenyl or C.sub.2 to C.sub.8 alkynyl;
- B is (1) a hydrogen atom, (2) a salt forming light metal atom selected from the group of lithium, sodium, potassium, magnesium, calcium and aluminum, (3) C.sub.1 to C.sub.8 -alkanoyloxy- C.sub.1 to C.sub.5 -alkyl, (4) C.sub.1 to C.sub.5 -alkoxycarbonyloxy-C.sub.1 to C.sub.4 -alkyl or (5) phthalidyl;
- and
- Het is a heterocyclic radical selected from the group of triazolyl, tetrazolyl, thiadiazolyl, oxadiazolyl, thiazolyl, oxazolyl, isoxazolyl, triazinyl, pyridyl and pyrimidyl, said heterocyclic radicals being unsubstituted or substituted by (a) alkyl, (b) haloalkyl, (c) hydroxyalkyl, (d) alkoxyalkyl, (e) carboxylalkyl, (f) BOOC-alkyl wherein B is as defined above, (g) carbamoylalkyl, (h) N-alkylcarbamoylalkyl, (i) dialkylaminoalkyl, (j) sulfamoylalkyl, (k) alkylthioalkyl, all of the above said groups (a) to (k) containing 1 to 6 carbon atoms, (l) hydroxy, (m) oxo or (n) halogen.
Dependencies are inferred from the claim text.