Drug – bio-affecting and body treating compositions – Fermentate of unknown chemical structure – Having a known elemental analysis
Reexamination Certificate
2000-05-12
2001-04-10
Lilling, Herbert J. (Department: 1651)
Drug, bio-affecting and body treating compositions
Fermentate of unknown chemical structure
Having a known elemental analysis
C435S252100, C514S018700, C530S321000
Reexamination Certificate
active
06214340
ABSTRACT:
The present invention relates to a novel physiologically active substance sulphostin, a process for producing the same and use thereof. The compound of this invention has a dipeptidylpeptidase IV inhibitory activity. Dipeptidylpeptidase IV which occurs on the surface of T cells is known to take part in activation of T cells (Immunol. Today, 15, 180-184 (1994)), and it plays an important role in the immune system. Dipeptidylpeptidase IV is also associated with degradation of a growth hormone-releasing hormone in serum (J. Clin. Invest., 83, 1533-1540 (1989)). The compound of the present invention, therefore, is expected to find its use as a physiologically active substance for various medicinal and pharmaceutical preparations such as immune regulators, hormone regulators, anti-HIV drugs, antiallergic drugs, antiphlogistics, antirheumatics, etc.
BACKGROUND ART
Some compounds such as Diprotin A and B (J. of Antibiotics, 37, 422-425 (1984)) have been known as physiologically active substances having the dipeptidylpeptidase IV inhibitory activity.
These compounds, however, are weak in their inhibitory activity against the above enzyme and are unsatisfactory for use as a physiologically active substance in the above medicinal and pharmaceutical preparations. Therefore, the advent of a novel compound which is suited for such uses has been waited.
DISCLOSURE OF THE INVENTION
In view of the above, the present inventors have pursued extensive research on the microbial metabolites, and as a result found that a strain belonging to the actinomycetes is capable of producing a physiologically active substance sulphostin having an excellent dipeptidylpeptidase IV inhibitory activity. The present invention has been attained on the basis of this finding.
The physiologically active substance sulphostin of the present invention can be obtained by culturing a sulphostin producing microorganism belonging to the genus Streptomyces, allowing the microorganism to produce and accumulate the physiologically active substance in the culture medium, and harvesting the substance from the culture medium.
REFERENCES:
patent: WO 94/03055 (1994-02-01), None
patent: WO 95/11689 (1995-05-01), None
patent: WO 95/29691 (1995-11-01), None
patent: WO 97/40832 (1997-11-01), None
Immunol. Today, 15, pp. 180-184 (1994) “CD26: a surface protease involved in T-cell activation”; Bernhard Fleischer.
J. Clin. Invest., 83, pp. 1533-1540 (1989); “Dipeptidylpeptidase IV and Trypsin-like Enzymatic Degradation . . . ”; Lawrence A. Frohman, et al.
J. of Antibiotics, 37, pp. 422-425 (1984); “Diprotins A and B, Inhibitors of Dipeptidyl, Aminopeptidase IV, produced by Bacteria”.
Patent Abstracts of Japan vol. 1996, No. 11, Nov. 29, 1996.
Abe Masatoshi
Akiyama Tetsuo
Hamada Masa
Muraoka Yasuhiko
Naganawa Hiroshi
Lilling Herbert J.
Nields & Lemack
Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
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