Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1997-02-12
1999-08-10
Huang, Evelyn
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
5142245, 514250, 514299, 514300, 514312, 544 32, 544101, 544250, 546123, 546156, A61K 3137, A61K 31535, C07D21556, C07D49806
Patent
active
059359528
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
This invention relates to a novel quinolone- or naphthylidone-carboxylic exhibits a strong antibacterial activity against Gram-positive bacteria and Gram-negative bacteria, particularly MRSA.
BACKGROUND ART
As a quinolone type synthetic antibacterial agent, Norfloxacin, Ciprofloxacin, Ofloxacin and the like have heretofore been widely used in clinic, but do not have a sufficient activity against Gram-positive bacteria, particularly MRSA. Therefore, it has been desired to develop synthetic antibacterial agents which are effective to these bacteria and have a broad antibacterial spectrum.
DISCLOSURE OF INVENTION
Under such circumstances, the present inventors have made extensive research to find that a quinolone- or naphthylidone-carboxylic acid excellent antibacterial activity: ##STR2## wherein R.sup.1 represents a hydrogen atom or a carboxyl-protecting group; R.sup.2 represents a substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aryl or heterocyclic group; R.sup.3 represents at least one group selected from the group consisting of a hydrogen atom, a halogen atom, a substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aryl, alkoxy or alkylthio group, a nitro group, a cyano group, an acyl group, a protected or unprotected hydroxyl group, a protected or unprotected hydroxyalkyl group, a protected or unprotected amino group, a protected or unprotected alkylamino group, a dialkylamino group, a protected or unprotected aminoalkyl group, a protected or unprotected alkylaminoalkyl group and a dialkylaminoalkyl group; R.sup.4 represents at least one group selected form the group consisting of a hydrogen atom, a halogen atom, a substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aralkyl, aryl, alkoxy or alkylthio group, a protected or unprotected hydroxyl group, a protected or unprotected hydroxyalkyl group, a protected or unprotected amino group, a protected or unprotected alkylamino group, a dialkylamino group, a protected or unprotected aminoalkyl group, a protected or unprotected alkylaminoalkyl group, a dialkylaminoalkyl group, an alkylidene group, an oxo group, an imino group and a group forming a cycloalkane ring together with the carbon atom to which R.sup.4 is bonded; R.sup.5 represents a hydrogen atom, a substituted or unsubstituted alkyl, cycloalkyl, alkylsulfonyl, arylsulfonyl, acyl or aryl group, a protected or unprotected aminoalkyl group, a protected or unprotected alkylaminoalkyl group, a dialkylaminoalkyl group or a protected or unprotected hydroxyalkyl group; R.sup.6 represents a hydrogen atom, a halogen atom, a substituted or unsubstituted alkyl, alkoxy or alkylthio group, a protected or unprotected hydroxyl group, a protected or unprotected amino group or a nitro group; ##STR3## in which Y represents a hydrogen atom, a halogen atom, a substituted or unsubstituted alkyl, alkoxy or alkylthio group or a protected or unprotected hydroxyl group or forms a group represented by the following formula together with R.sup.2 : ##STR4## in which R.sup.7 represents at least one group selected from the group consisting of a hydrogen atom, an alkyl group, a halogenoalkyl group, a protected or unprotected hydroxyalkyl group, an alkylidene group and a group forming a cycloalkane ring together with the carbon atom to which R.sup.7 is bonded and B represents an oxygen atom, a sulfur atom or an imino group which may be substituted by an alkyl group; and X represents a hydrogen atom or a halogen atom, whereby this invention has been completed.
This invention is explained in detail below.
In the present specification, unless otherwise specified, the term "halogen atom" means a fluorine atom, a chlorine atom, a bromine atom or an iodine atom; the term "alkyl group" means a straight chain or branched chain C.sub.1-10 alkyl group such as methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, pentyl, hexyl, heptyl, octyl or the like; the term "lower alkyl group" means a straight chain or branched chain C.sub.1-5 alkyl group such as methyl, ethyl, n-propyl, isop
REFERENCES:
patent: 4563459 (1986-01-01), Grohe
patent: 4945160 (1990-07-01), Kiely
patent: 5026856 (1991-06-01), Yatsunami
Hayashi Kazuya
Narita Hirokazu
Tadahata Masahiro
Todo Yozo
Watanabe Yasuo
Huang Evelyn
Toyama Chemical Co., Ltd.
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