Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Reexamination Certificate
1997-09-24
2001-04-10
Wessendorf, T. D. (Department: 1627)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
C514S009100, C514S002600, C530S323000, C530S322000, C530S320000, C530S319000, C530S317000, C435S071300, C435S071200, C435S071100
Reexamination Certificate
active
06214793
ABSTRACT:
FIELD OF THE INVENTION
A novel depsipeptide has been isolated from a new marine strain L-13-ACM2-092 belonging to the family Micromonosporaceae. Its production by aerobic fermentation under controlled conditions of the strain, and the isolation and purification of PM-93135 are described herein. The compound shows good activity against Gram positive bacteria. The compound and the fermentation broth also demonstrate significant activity against several cancer cell lines.
BACKGROUND OF THE INVENTION
Many common bacteria are evolving resistance to more and more antibiotics. According to published reports, resistant bacterial infections killed 19,000 U.S. hospital patients (and contributed to the deaths of 58,000 more) in 1992. For instance, strains of Pneumococcus, which can cause ear infections, meningitis, pneumonia and blood infections, became resistant to penicillin and to four other antibiotics in just the last six years. Some 20 percent of TB microbes resistisoniazid, the treatment of choice, and gonorrhea microbes resist penicillin. More than half the known strains of
Staphylococcus aureus,
which causes blood poisoning, resist everything but vancomycin. Clearly, the need for a constant supply of new antibiotic materials is never ending. Accordingly, one object of the present invention is to provide a new antibiotic agent arbitrarily designated herein as PM-93135.
New antineoplastic compounds are also needed for treatment against several human carcinomas. Accordingly, another object of the present invention is to provide a new antitumor agent, namely the compound PM-93135. This compound is a thiodepsipeptide with significant inhibitory activity of RNA synthesis.
Yet another object of this invention is to provide pharmaceutical compositions for administering to a patient in need of treatment using the active compound described herein. Still another object is directed to the production of the active compound by controlled aerobic fermentation using a biologically pure culture of an organism capable of producing the active compound in appropriate nutrient media, and to methods for the recovery and concentration from the fermentation broth, and to the final purification of the active compound.
SUMMARY OF THE INVENTION
This invention provides a compound with the proposed formula I:
In this invention the process of obtaining PM-93135 is also described, and the preferred process comprises cultivating a strain of a microorganism capable of producing PM-93135 in an aqueous nutrient medium with assimilable carbon and nitrogen sources and salts, under controlled submerged aerobic conditions. The compound PM-93135 is recovered and purified from the cultured broth.
The preferred culture is strain L-13-ACM2-092, and belongs to the family Micromonosporaceae, being taxonomically classified as Micromonospora sp.
As described above, the compound PM-93135 has been found to be effective against several strains of Gram positive and Gram negative bacteria, and it has also been found to have good activity against murine and human tumor cell lines, including P-388, HT-29, A-549 and MEL-28. This compound shows selective activity against RNA synthesis.
REFERENCES:
patent: 4366309 (1982-12-01), Ganguly et al.
Otsuka et al, The Journal of Antibiotics, Sec. A, pp. 128-131, (May, 1966).*
Williamson et al, The Journal of Antibiotics, vol. XXXV(I), pp. 62-66 (Jan. 1982).*
Yoshida et al, Journal of Bacteriology, vol. 93(4), pp. 1327-31, (1967).*
Bergeron et al, Biochemical & Biophysical Res. Comm., vol. 12(3), pp. 848-854, (Jun. 29, 1984).*
Okada et al, The Journal of Antibiotics, vol. 47(2), pp. 129-135 (1994).
Baz Julia Perez
De Quesada Teresa Garcia
Garcia Gravalos Dolores
Millan Francisco Romero
Banner & Witcoff , Ltd.
Linek Ernest V.
Pharma Mar S.A.
Wessendorf T. D.
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