Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1999-11-18
2000-07-11
Owens, Amelia
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514454, 549283, A61K 3135, C07D31102
Patent
active
060873906
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention is useful in the pharmaceutical field. More specifically, the present invention relates to a novel antifungal agent.
BACKGROUND ART
In the field of antifungal agents, a number of compounds have already come into practical use as pharmaceuticals. However, their effects on various harmful strains are not always satisfactory, and emergence of strains resistant to these pharmaceuticals, especially to azole type antifungal agents in wide use, has become a serious clinical problem. Therefore, development of pharmaceuticals effective against these harmful strains and resistant strains is demanded.
JP-A-6-157582, J. Antibiotics, vol. 48, pp.1171-1172 (1995) and Nat. Prod. Lett., vol. 7, pp.309-316 (1995) disclose structural analogues of the compounds of the present invention which show excellent antifungal action, but neither disclose nor suggest anything specific about the compounds of the present invention.
Further, the present inventors have recently found that compounds containing the compounds disclosed by the above-mentioned references and azole type antifungal agents have excellent antifungal action (PCT/JP96/00353).
However, development of even more excellent antifungal agents is still demanded.
DISCLOSURE OF THE INVENTION
The object of the present invention is to provide novel antifungal agents which meet the above-mentioned demand. Namely, the problem that the present invention is to solve is to provide agents which show antifungal action against various harmful strains and resistant strains against which conventional antifungal agents are not satisfactorily effective.
The present inventors have conducted extensive research to solve the above-mentioned problem, and as a result, have found that the compounds represented by general formula (I) and pharmaceutically acceptable salts or esters thereof have excellent antifungal activities, and the present invention has been accomplished.
Namely, the present invention provides a compound represented by general formula (I) or a pharmaceutically acceptable salt or ester thereof: ##STR2## wherein each of R.sup.1 and R.sup.2 is independently a hydrogen atom, a C.sub.1 -C.sub.16 alkyl group, a C.sub.2 -C.sub.10 alkenyl group, a C.sub.3 -C.sub.6 alkynyl group, a C.sub.6 -C.sub.12 aryl group, a C.sub.7 -C.sub.15 aralkyl group or a heterocyclic group which is not substituted, a C.sub.1 -C.sub.16 alkyl group, a C.sub.2 -C.sub.10 alkenyl group, a C.sub.3 -C.sub.6 alkynyl group, a C.sub.6 -C.sub.12 aryl group, a C.sub.7 -C.sub.15 aralkyl group or a heterocyclic group which has one to five substituents selected from the group consisting of halogen atoms, cyano groups, hydroxyl groups, C.sub.1 -C.sub.16 alkyloxy groups, C.sub.1 -C.sub.16 alkylcarbonyloxy groups, amino groups, mono-C.sub.1 -C.sub.16 alkylamino groups, di-C.sub.1 -C.sub.16 alkylamino groups, carboxyl groups, C.sub.1 -C.sub.16 alkyloxycarbonyl groups, aminocarbonyl groups, sulfo groups, C.sub.6 -C.sub.12 aryl groups, C.sub.6 -C.sub.12 aryloxy groups, C.sub.7 -C.sub.15 aralkyloxy groups and heterocyclic groups, or a group represented by --Y--R.sup.3 ; Y is a carbonyl group, a thiocarbonyl group or a sulfonyl group; and R.sup.3 is a C.sub.1 -C.sub.16 alkyl group, a C.sub.2 -C.sub.10 alkenyl group, a C.sub.3 -C.sub.6 cycloalkyl group, a C.sub.3 -C.sub.6 cycloalkyl-C.sub.1 -C.sub.16 alkyl group, a C.sub.6 -C.sub.12 aryl group, a C.sub.7 -C.sub.15 aralkyl group, a C.sub.7 -C.sub.15 aralkylamino group or a heterocyclic group which is not substituted, or a C.sub.1 -C.sub.16 alkyl group, a C.sub.2 -C.sub.10 alkenyl group, a C.sub.3 -C.sub.6 cycloalkyl group, a C.sub.3 -C.sub.6 cycloalkyl-C.sub.1 -C.sub.16 alkyl group, a C.sub.6 -C.sub.12 aryl group, a C.sub.7 -C.sub.15 aralkyl group, a C.sub.7 -C.sub.15 aralkylamino group or a heterocyclic group which has one to four substituents selected from the group consisting of halogen atoms, cyano groups, hydroxyl groups, amino groups and carboxyl groups, and hydroxyl groups, amino groups and carboxyl groups having a C.sub.1 -C.sub.1
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patent: 5922709 (1999-07-01), Okada et al.
Stephen J. Coval, et al., The Journal of Antibiotics, vol. 48, pp. 1171-1172, "SCH57404, an Antifungal Agent Possessing the Rare Sodaricin Skeleton and a Tricyclic Sugar Moiety", 1995.
G. Schneider, et al., National Product Letters, vol. 7, pp. 309-316, "Xylarin, an Antifungal Xylaria Metabolite with an Unusual Tricyclicuronic Acid Moiety", 1995.
Hirano Atsushi
Kamiya Seigo
Kojiri Katsuhisa
Nagashima Masao
Ogawa Hidenori
Banyu Pharmaceutical Co. Ltd.
Owens Amelia
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