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US 4,395,411 AGranted
Pyrimidinyl cephalosporanic acid derivatives and pharmaceutical compositions
AssigneeFujisawa Pharmaceutical Co., Ltd.
InventorsTakashi Kamiya, Tsutomu Teraji, Yoshiharu Nakai, Kazuo Sakane, Jiro Goto
Life of this patent
Estimating the term…
Abstract
This invention relates to novel 7-pyrimidinyl and pyridinyl acetamido cephem derivatives of high antibacterial activity.
Claims16
A compound of the formula:
- ##STR15## wherein R.sup.1 is a group of the formula:
- ##STR16## in which R.sub.a.sup.1 is hydrogen, amino or a protected amino group, R.sub.b.sup.1 and R.sub.c.sup.1 are each hydrogen, halogen, lower alkoxy, phenylthio, tolylthio, xylylthio, mesitylthio or naphthylthio,
- R.sup.2 is hydrogen or lower alkoxy,
- R.sup.3 is hydrogen or lower alkyl,
- R.sup.4 is hydrogen, halogen, carbamoyloxymethyl, lower alkyl, lower alkoxy, lower alkanoyloxymethyl or lower alkanoylthiomethyl,
- R.sup.5 is carboxy or a protected carboxy group, and
- X is a group of the formula:
- ##STR17## in which R.sup.6 is hydrogen, lower alkyl, mono to trihalo (lower) alkyl, lower alkenyl, lower alkynyl, phenyl, tolyl, xylyl, cumenyl, naphthyl, phenyl (lower) alkyl, mono or dihalo (lower) alkanoyl, or lower alkoxy, and non-toxic, pharmaceutically acceptable salts thereof.
5 more elements
A compound of claim 2, wherein
- R.sup.1 is a group of the formula:
- ##STR20## in which R.sub.a.sup.1 is hydrogen, amino, lower alkanoyl or trihalo(lower)alkanoyl,
- R.sub.b.sup.1 and R.sub.c.sup.1 are each hydrogen, halogen, lower alkoxy or phenylthio,
- R.sup.2 is hydrogen or lower alkoxy,
- R.sup.3 is hydrogen or lower alkyl,
- R.sup.4 is hydrogen, halogen, carbamoyloxymethyl, lower alkyl, lower alkoxy, lower alkanoyloxymethyl, or lower alkanoylthiomethyl
- R.sup.5 is carboxy, nitrophenyl(lower)alkoxycarbonyl or diphenyl(lower)alkoxycarbonyl, and
- X is a group of the formula:
- ##STR21## in which R.sup.6 is hydrogen, lower alkyl, trihalo(lower)alkyl, lower alkenyl, lower alkynyl, phenyl or phenyl(lower)alkyl, in which R.sup.6 is as defined in claim 3.
6 more elements
Dependencies are inferred from the claim text.