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US 5,348,961 AGranted
4-oxoquinoline-3-carboxylic acid derivatives and their use
AssigneeSankyo Company, Limited
InventorsMasayuki Iwata, Tomio Kimura, Teruhiko Inoue, Yoshimi Fujihara, Tetsushi Katsube
Life of this patent
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Abstract
Compounds of formula (I): ##STR1## (in which: R.sup.1 represents fluorinated methoxy; R.sup.2 represents a nitrogen-containing heterocyclic group and R.sup.3 represents hydrogen or amino) and pharmaceutically acceptable salts, esters and amides thereof are valuable antibacterial agents, which may be prepared by reacting a compound similar to that of formula (I) but in which R.sup.2 is replaced by a halogen atom with a compound providing the required group R.sup.2.
Claims14
A compound of formula (I):
- ##STR20## in which R.sup.1 represents a methoxy group having at least one fluorine substituent;
- R.sup.2 represents groups of formula (III):
- ##STR21## in which:
- R.sup.6 represents a hydrogen atom;
- a C.sub.1 -C.sub.6 alkyl group;
- a substituted C.sub.1 -C.sub.6 alkyl group having at least one substituent selected from the group consisting of substituents (b), defined below;
- a hydroxy group;
- a C.sub.1 -C.sub.6 alkoxy group;
- or a C.sub.1 -C.sub.6 alkoxy group having at least one fluorine substituent;
- R.sup.7 represents a group of formula R.sup.8 R.sup.9 N-(CH.sub.2).sub.q -. in which R.sup.8 and R.sup.9 are independently selected from the group consisting of hydrogen atoms, C.sub.1 -C.sub.6 alkyl groups and aralkyl groups, and q represents 0 or 1;
- a hydroxy group;
- or a C.sub.1 -C.sub.6 alkoxy group;
- B represents a methylene group, an ethylene group, a trimethylene group, or a tetramethylene group;
- and
- n represents 1 or 2;
- substituents (b) are selected from the group consisting of:
- hydroxy groups, C.sub.1 -C.sub.6 alkoxy groups, and halogen atoms;
- and
- said aralkyl groups have from 1 to 4 carbon atoms in the alkyl part and have an aryl part which has from 6 to 10 carbon atoms and which is unsubstituted or has at least one substituent selected from the group consisting of substituents (c), defined below;
- substituents (c) are selected from the group consisting of:
- hydroxy groups, C.sub.1 -C.sub.6 alkyl groups, C.sub.1 -C.sub.6 alkoxy groups, C.sub.2 -C.sub.6 aliphatic acyloxy groups, C.sub.2 -C.sub.6 aliphatic acyl groups, carboxy groups, C.sub.2 -C.sub.6 alkoxycarbonyl groups, sulfo groups, nitor groups, cyano groups, amino groups, C.sub.2 -C.sub.6 aliphatic acylamino groups, and mono- and di-(C.sub.1 -C.sub.6 alkyl) substituted amino groups;
- or a pharmaceutically acceptable salt, ester or amide thereof.
19 more elements
Dependencies are inferred from the claim text.