Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1999-05-28
2000-10-24
Seaman, D. Margaret
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
546156, C07D21516, A61K 3147
Patent
active
061368237
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP 97/04326, filed Nov. 27, 1997.
TECHNICAL FIELD
The present invention relates to novel pyridonecarboxylic acid derivatives or salts thereof which exhibit excellent antibacterial activities and peroral absorbability, and medicines comprising such a compound as an active ingredient.
BACKGROUND ART
Many compounds having a pyridonecarboxylic acid as a basic skeleton are known to be useful as synthetic antibacterial agents because they have excellent antibacterial activities and wide antibacterial spectra. Of these, norfloxacin (Japanese Patent Application Laid-Open No. 141286/1978), enoxacin (Japanese Patent Application Laid-Open No. 31042/1980), ofloxacin (Japanese Patent Application Laid-Open No. 46986/1982), ciprofloxacin (Japanese Patent Application Laid-Open No. 74667/1983), tosufloxacin (Japanese Patent Application Laid-Open No. 228479/1985) and the like are in wide clinical use as agents for treating infectious diseases.
However, these compounds have been not yet sufficient in antibacterial activity, intestinal absorbability, metabolic stability and side effects, particularly, phototoxicity, cytotoxicity, etc. Pyridone-carboxylic acid derivatives carrying cyclic amino group at the 7-position of the naphthyridine skeleton or quinoline skeleton have also been known (WO96/12704). However, It is still desired to develop compounds far excellent in absorbability and easy-to-synthesize.
It is therefore an object of the present invention to provide novel compounds satisfying all respects of antibacterial activity, oral absorbability, metabolic stability and side effects, particularly, phototoxicity, cytotoxicity, etc., and medicines containing such a compound.
DISCLOSURE OF THE INVENTION
In view of the foregoing circumstances, the present inventors have carried out intensive research, synthesized various kinds of compounds and investigated their antibacterial activities, absorbabilities, side effects and the like. As a result, it has been found that specific pyridonecarboxylic acid derivatives satisfy the above-described requirements, thus leading to completion of the present invention.
According to the present invention, there is thus provided a pyridonecarboxylic acid derivative represented by the general formula (1): ##STR2## wherein R.sub.1 is a group --OR.sup.9 (wherein R.sup.9 is a hydrogen atom or carboxy-protecting group), amino group or lower alkylamino group, R.sup.2 is a hydrogen atom, nitro group, amino or hydroxyl group which may be protected, lower alkyl group, or lower alkoxyl group, R.sup.3 is a halogen atom, hydrogen atom, nitro group, lower alkyl group, lower alkoxyl group or amino group, R.sup.4 is a nitro group, azido group, hydrazino group which may be substituted, group --NR.sup.10 R.sup.11 (wherein R.sup.10 and R.sup.11 may be the same or different from each other and are independently a hydrogen atom, lower alkyl group which may be substituted, lower alkenyl group, lower cycloalkyl group, saturated heterocyclic group or amino-protecting group), lower alkoxyl group or hydroxyl group, R.sup.5, R.sup.6 and R7 may be the same or different from one another and are independently a hydrogen atom, nitro group, halogen atom or lower alkyl group, R.sup.8 is a nitro group, amino group which may be substituted, hydroxyl group or lower alkoxyl group, A is a nitrogen atom or group C--R.sup.12 (wherein R.sup.12 is a hydrogen atom, halogen atom, lower alkyl group which may be substituted, lower alkenyl group, lower alkynyl group, lower alkoxyl group, lower alkylthio group or nitro group), and B is a nitrogen atom or group C--R.sup.13 (wherein R.sup.13 is a hydrogen atom or halogen atom), or a salt thereof.
According to the present invention, there is also provided a medicine comprising the pyridonecarboxylic acid derivative or the salt thereof as an active ingredient.
According to the present invention, there is further provided a medicinal composition comprising the pyridonecarboxylic acid derivative or the salt thereof and a pharmaceutically acceptable carri
REFERENCES:
USPatFull abstract 1999:65254, abstract of US Patent #5,910,498, 1999.
Marpat abstract #126:47239, abstract of Matsumoto, 1996.
Marpat abstract #126:47238, abstract of Matsumoto, 1996.
Marpat abstract #115:74146, abstract of Arnold, 1991.
Marpat abstract #114:247159, abstract of Bitha, 1991.
Amano Hirotaka
Hayashi Norihiro
Hirao Yuzo
Kuramoto Yasuhiro
Niino Yoshiko
Seaman D. Margaret
Wakunaga Pharmaceutical Co., Ltd.
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