Antibacterial preparation or bactericide comprising 2-aminothiaz

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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A61K 31425

Patent

active

058563474

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD

This invention relates to an antibacterial preparation or a bactericide, comprising a 2-aminothiazole derivative and/or a salt thereof. The term "bactericide" used herein connotes disinfectants.


BACKGROUND ART

Prior art will be described. At the outset, thiazoles having a trifluoromethanesulfonylamino group at the 2-position are described in U.S. Pat. Nos. 3,923,810 and 3,923,811. Japanese Pat. Appln. Laid-Open Gazettes Nos. Sho 64-40474 (40474/89) and Sho 64-75475 (75475/89) describe thiazole derivatives having anti-inflammatory action and analgesic action. Phenyl pivalate derivatives are described as an elastase inhibitor in U.S. Pat. No. 4,801,610 and Japanese Pat. Appln. Laid-Open Gazette No. Hei 3-20253 (20253/91). Further, the compounds or part of the compounds of this invention are described also in Japanese Pat. Appln. Laid-Open Gazettes Nos. Hei 3-173876 (173876/91) and Hei 5-70446 (70446/93). However, the antibacterial action or bactericidal action of the compounds of this invention is not disclosed at all, nor is it suggested.


DISCLOSURE OF THE INVENTION

An object of this invention is to provide an antibacterial preparation or a bactericide each of which comprises a comprising a 2-aminothiazole derivative and/or a salt thereof, exhibits a tendency of low bacterial tolerance thereto and low toxicity and has antibacterial activity or bactericidal activity, and the object is also to provide a pharmaceutical comprising the antibacterial preparation or the bactericide.
This invention relates to a novel antibacterial agent or bactericide comprising 2-aminothiazole derivatives and/or salts thereof as effective ingredients.
More specifically, this invention relates to 2-aminothiazole derivatives represented by the following general formula (1) and their salts useful as pharmaceutical preparations: ##STR2## wherein R.sup.1 represents a lower alkyl group except when R.sup.2 is a hydrogen atom; a substituted or unsubstituted phenyl group except 2,6-disubstituted phenyl group; a thiophene, benzoyl, benzoylmethyl or p-pivaloyloxyphenyl group; or --CH.sub.2 COOR.sub.4 wherein R.sub.4 is a hydrogen atom, or a lower alkyl or substituted or unsubstituted benzyl group; cycloalkyl, substituted or unsubstituted phenyl, benzoyl, substituted or unsubstituted benzyl or p-pivaloyloxyphenyl group; --COOR.sub.3 wherein R.sub.3 is a hydrogen atom or a lower alkyl group; or --CH.sub.2 COOR.sub.4 unsubstituted benzyl group; and each represent a hydrogen atom; a lower alkanesulfonyl, halo lower alkanesulfonyl, or substituted or unsubstituted phenyl group except p-chlorophenyl group; a substituted benzyl, substituted or unsubstituted benzenesulfonyl, substituted or unsubstituted lower alkanoyl or amidino group; --CO--R.sub.5 wherein R.sub.5 is a lower alkyl, substituted or unsubstituted phenyl group, --(CH.sub.2).sub.m --COOH wherein m is an integer of 1 to 5, or --(CH.sub.2).sub.n --NH--R.sub.6 wherein n is an integer of 1 to 5 and R.sub.6 is a hydrogen atom or a tert-butoxycarbonyl or benzyloxycarbonyl group; or --(CH.sub.2).sub.Q --R.sub.7 wherein Q is an integer of 0 to 5 and R.sub.7 is a lower alkoxy, substituted or unsubstituted phenyl, substituted or unsubstituted pyridyl or cyclic amino group; or A.sup.1 and A.sup.2 may combine with each other and the nitrogen atom to form a cyclic amino group.
The general formula (I) will be described in detail. The halogen atoms for R.sup.2 include Fluorine, chlorine, bromine and iodine. The lower alkyl groups for R.sup.1, R.sub.4, R.sup.2, R.sub.3 and R.sub.5 include C.sub.1 -C.sub.8 alkyl groups such as methyl, ethyl, n-propyl, iso-propyl, n-butyl, iso-butyl and tert-butyl groups. When R.sup.2 is a hydrogen atom, however, R.sup.1 will not be a lower alkyl group. The lower cycloalkyl groups for R.sup.2 include C.sub.3 -C.sub.6 cycloalkyl groups such as cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl groups. The lower alkoxy groups for R.sub.7 include C.sub.1 -C.sub.6 alkoxy groups such as methoxy, ethoxy, n-propoxy, iso-propoxy, n-butoxy, iso-butoxy and t

REFERENCES:
patent: 5449783 (1995-09-01), Saita et al.

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