Chemistry: molecular biology and microbiology – Micro-organism – tissue cell culture or enzyme using process... – Preparing nitrogen-containing organic compound
Reexamination Certificate
2000-03-07
2001-10-16
Lilling, Herbert J. (Department: 1651)
Chemistry: molecular biology and microbiology
Micro-organism, tissue cell culture or enzyme using process...
Preparing nitrogen-containing organic compound
C564S161000, C564S167000, C564S169000, C435S911000
Reexamination Certificate
active
06303350
ABSTRACT:
This application is a 371 of PCT/JP98/02530, Jun. 9, 1998.
TECHNICAL FIELD
The present invention relates to biologically active substances TKR2449 analog(s), which are useful for a therapeutic agent for fungal infection diseases and immune disorders, a method for their production, and microorganisms being capable of producing the biologically active substances TKR2449.
BACKGROUND ART
Fungi are known to cause a variety of infectious diseases in man, animals, and plants. In man, for instance, they cause superficial mycosis affecting the skin, oral cavity, etc. and systemic mycosis affecting the viscera, brain, etc. They cause similar infections in pet and domestic animals as well. Furthermore, fungi inflict various hazardous effects on plants such as orchard trees and vegetables.
As the principal pathogenic fungi causing systemic mycosis in man, those of the genera Candida, Cryptococcus, and Aspergillus, among others, are known. As to superficial mycosis, genus Candida affecting the skin, oral cavity, and vagina and trichophytons infecting the skin of the extremities are regarded as the major pathogenic fungi. Besides those fungi, many other fungi exist in the environment and are suspected to contaminate the animals and plants.
Recently allergic disorders including asthma, atopic dermatitis, and allergic rhinitis are rapidly increasing. There are lots of allergic disorders in which various substances in the environment such as mites and all kinds of pollen, or antigens contained in foods actas allergens. Also there are many allergic disorders caused by fungi, and allergens derived from Candida, Aspergillus, Alternaria, Cladosporium, Malassezia, Penicillium, etc. act as their causes. Further, lots of immune disorders other than allergic disorders, in which immune responses are exacerbated are known.
As antimycotics of use for the prevention and treatment of such fungal infections and contaminations, only a very few are known nowadays. Among them, as therapeutic drugs for systemic mycosis in animals especially including men, for instance, amphotericin B, flucytosine, miconazole, and fluconazole can be mentioned. However, those compounds are not fully satisfactory in potency, toxic potential, or antifungal spectrum, thus being not impeccable as therapeutic drugs.
Although there are lots of therapeutics for immune disorders including allergic diseases, they cannot treat a variety of immune disorders sufficiently. In particular, there is only a few drugs that have plural good functions like activity to control immune disorders and antifungal activity.
SUMMARY OF THE INVENTION
In view of the above-mentioned prior art, the present invention has for its object to provide novel biologically active substances which are of value as a therapeutic agent for fungal infections and immune disorders.
In the search for a novel biologically active substance, the inventors isolated a large number of microorganisms from the natural kingdom, isolated the biologically active substances they produced, and scrutinized their biological properties. As a result, they discovered that the culture broth of a strain of microorganism belonging to the genus Aureobasidium contains a biologically active substance having antifungal activity against pathogenic fungi inclusive of
Candida albicans
and
Cryptococcus neoformans
. Accordingly, the inventors isolated this biologically active substance and studied its physicochemical properties. As a result, they discovered that the above substance is a novel substance having distinct physicochemical characteristics and not having mentioned in the literatures, and they named it TKR2449. Furthermore, they discovered that TKR2449 shows a biologically active effect on an immune system and completed the present invention.
The present invention, therefore, is directed to a biologically active substance TKR2449 analog(s) which is represented by the following general formula (A);
(In the formula, R
1
, R
2
and R
3
are the same or differ each other, and each represents hydrogen or an alkyl group of carbon number of 1 to 4. R
4
is a linear or branched alkyl or alkenyl group of carbon number of 1 to 8.)
The present invention is further directed to a method of preparing the biologically active substance TKR2449 which comprises culturing a strain of microorganism belonging to the genus Aureobasidium and being capable of producing the biologically active substance TKR2449, and isolating the objective substance from the resulting culture broth.
In addition, the present invention is directed to a microorganism belonging to the genus Aureobasidium and being capable of producing the biologically active substance TKR2449.
REFERENCES:
patent: 0 526 936 A2 (1993-02-01), None
patent: WO 94/18157 (1994-08-01), None
patent: WO 97/01275 (1997-01-01), None
Aureobasidium sp. SN-115, Journal of Fermentation Technology, Japanese Ed., vol. 66, No. 4, pp. 217-223.
Zajic et al, Flocculant and Chemical Properties of a Polysaccharide fromPullularia pullulans, Applied Microbiology,Apr. 1973, pp. 628-635.
Schmidtchen et al, Utility of the Cleavage of Nitrosamides for the Preparation of Chiral Acids after Chromatographic Separation of their Diastereomeric Amides, Zeitschrift fuer Naturforschung Section B, vol. 32, No. 1, 1977, pp. 98-104.
Awazu Naoyuki
Kato Ikunoshin
Takesako Kazutoh
Ueno Mitsuhiro
Uno Yoko
Connolly Bove Lodge & Hutz
Lilling Herbert J.
Takara Shuzo Co. Ltd.
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