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US 4,198,503 AGranted
3-Carbamoyl substituted-7-ureido substituted cephalosporins
AssigneeBeecham Group Limited
InventorsNorman H. Rogers, Robert Stevenson
Life of this patent
Estimating the term…
Abstract
A class of 3-carbamoyloxymethyl-7-.alpha.-acylureido cephalosporins have a broad spectrum of antibacterial activity.
Claims13
A 3-carbamoyloxymethyl-7-.alpha.-acylureido cephalosporin of formula (II) or a pharmaceutically acceptable salt or acid addition salt or in vivo hydrolyzable ester thereof:
- ##STR15## wherein Y is oxygen or sulphur, R.sup.1 is methyl, ethyl, n- or isopropyl, n-, sec, or tert-butyl, n-pentyl, n-hexyl, n-heptyl, .omega.-methylheptyl, n-octyl, .omega.,.omega.-dimethyloctyl, prop-2-enyl, 3-methylprop-2-enyl, 1-methylprop-2-enyl, but-2-enyl-, oct-2-enyl, 2-phenylethyl, 2-phenylethenyl, 2-(2.sup.1 -methoxyphenyl)ethenyl, 2-(4.sup.1 -nitrophenyl)ethenyl, 2-(3.sup.1, 4.sup.1, 5.sup.1 -trimethoxyphenyl)ethenyl, 2-(fur-2.sup.1 -yl)enyl, 3-phenylpropyl, 1-methyl-2-phenylethenyl, 4-phenylbut-2-enyl, 5-phenyl-pent-2-enyl, methoxy, ethoxy, n- or sec-propoxy, n-, sec or tert-butoxy, n-pentoxy, n-hexyloxy, cyclohexyloxy, methylamino, dimethylamino, phenyl, 2-methoxyphenyl, 2-chlorophenyl, 2-methoxyphenyl, 3,4,5-trimethoxyphenyl, 4-nitrophenyl, 2-methoxyphenyl, 4-methylphenyl, methoxymethyl, ethoxymethyl, methylthiomethyl, phenoxymethyl;
- R.sup.2 is alkyl having from 1 to 3 carbon atoms, or benzyl;
- or R.sup.1 and R.sup.2 together with the carbon and nitrogen atoms to which they are attached form one of the following ring systems:
- ##STR16## in which n is an integer from 3 to 5 and m is an integer from 2 to 4 and R.sub.a is hydrogen, C.sub.1-3 alkyl, C.sub.1-3 acyl or C.sub.1-3 alkylsulphonyl;
- R.sup.3 is phenyl, 4-hydroxyphenyl, 3-chloro-4-hydroxyphenyl, 4-nitrophenyl, 4-aminophenyl, 2-thienyl, 3-thienyl, cyclopropyl, cyclohexyl, cyclohexa-1,4-dienyl, iso-propyl or methyl.
2 more elements
Dependencies are inferred from the claim text.