Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1998-05-06
1999-07-13
Krass, Frederick
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514242, 514245, 514252, 514396, 514399, 514451, 514454, 514455, A61K 3171, A61K 3135, C07D47318
Patent
active
059227095
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to an antifungal composition which is useful in the pharmaceutical field and which is more specifically novel.
BACKGROUND ART
In the field of antifungal agents, many compounds have already been practically used as pharmaceutical products. However, their effects are not necessarily adequate against various types of harmful fungi. Further, emergence of resistant strains against these pharmaceutical agents, particularly resistant strains against azole type antifungal agents which are frequently used, has become a clinically serious problem. Accordingly, it has been desired to develop a pharmaceutical agent effective against such harmful fungi and resistant strains.
DISCLOSURE OF THE INVENTION
It is an object of the present invention to provide a novel antifungal agent which is capable of satisfying the above demand. Namely, it is a problem to be solved by the present invention to present a pharmaceutical agent which provides antifungal effects also against various harmful fungi and resistant strains against which conventional antifungal agents can not provide adequate effects.
The present inventors have conducted extensive studies to solve the above problem and as a result, have found that by combining a compound represented by the general formula (I) or its pharmaceutically acceptable salt, and an azole type antifungal agent, such a composition has excellent antifungal activities, and the present invention has been accomplished.
Namely, the present invention relates to an antifungal composition comprising a compound represented by the general formula (I): ##STR2## wherein R is an acetyl group or a lower alkyl group, or its pharmaceutically acceptable salt, and an azole type antifungal agent, as active ingredients.
The symbols and terms used in this specification will be described.
The lower alkyl group means a C.sub.1-6 linear or branched alkyl group, and, for example, a methyl group, an ethyl group, a propyl group, an isopropyl group, a butyl group, a sec-butyl group, a tert-butyl group, a pentyl group or a hexyl group may be mentioned. Particularly preferred is a methyl group.
The pharmaceutically acceptable salt of the compound represented by the general formula (I) may, for example, be a salt such as a base-addition salt at the carboxyl group.
Such a base-addition salt may, for example, be an alkali metal salt such as a sodium salt or a potassium salt; an alkaline earth metal salt such as a calcium salt or a magnesium salt; an ammonium salt; or an organic amine salt such as a trimethylamine salt, a triethylamine salt, a dicyclohexylamine salt, an ethanolamine salt, a diethanolamine salt, a triethanolamine salt, a procaine salt or an N,N'-dibenzylethylenediamine salt.
Among the compounds represented by the general formula (I), a compound wherein R is an acetyl group, will be hereinafter referred to as BE-31405.
BE-31405 is a compound found by the present inventors, and its physicochemical properties, production process and pharmacological activities are disclosed in detail in a Japanese Laid Open Patent Publication (JP-A-6-157582).
The production of said compound can be carried out, for example, by means of Penicillium sp. F-31405, as disclosed in JP-A-6-157582, or by means of a microorganism such as Penicillium sp. F31405-17M which is a mutant of said strain and which is excellent in the production of said compound.
Penicillium sp. F31405-17M has the following mycological characteristics.
(1) Morphology
The configuration of F31405-17M strain is the same as the original strain Penicillium sp. F-31405. Namely, conidiophores are 110 to 210.times.1.8 to 3.6 .mu.m and have a smooth surface or fine projections. Further, they form symmetrical double verticillate penicilli. Metulae are 10.0 to 13.1.times.2.3 to 3.1 .mu.m, and from 4 to 8 metulae fasciculate. Phialides are (9.7 to) 11.4 to 15.0.times.1.8 to 2.6 .mu.m and verticillate. Conidia have a smooth surface and are subspherical to oval or egg shaped, and their sizes are 3.5 to 4.4.times.2.6 to 3.5 .mu.m.
REFERENCES:
Natural Product Letters,1995, vol. 7, "Xylarin, an Antifungal Xylaria Metabolite with an Unusual Tricyclic Uronic Acid Moiety", G. Schneider, et al. p. 309-316.
The Journal of Antibiotics, 1995, vol. 48, No. 10, "SCH57404, an Antifungal Agent Possessing the Rare Sodaricin Skeleton and a Tricyclic Sugar Moiety", Stephen J. Coval, et al.p. 1171-1172.
Kamiya Seigou
Kojiri Katsuhisa
Nagashima Masao
Okada Hiromasa
Suda Hiroyuki
Banyu Pharmaceutical Co. Ltd.
Krass Frederick
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