Acidic polycyclic ether useful as an anticoccidial agent and as

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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Details

514 25, 549343, 435119, 435118, 435 74, 435898, 435886, 536126, C07D31196, C12P 1718, A61K 3135

Patent

active

052062635

DESCRIPTION:

BRIEF SUMMARY
BACKGROUND OF THE INVENTION

The present invention concerns a new acidic polycyclic ether antibiotic having the absolute stereochemical formula ##STR1## wherein Me=CH.sub.3 ; pharmaceutically acceptable cationic salts thereof; nutrient feed compositions comprising said antibiotic for poultry, cattle or swine; it use as an anticoccidial agent in poultry, or as a growth promotant in cattle or swine; a fermentation method for its preparation; and the Streptomyces hygroscopicus microorganism which produces said antibiotic in said fermentation method.
The compound (I) is a new member of the acidic polycyclic ether group of antibiotics. This family includes such well known agents as monensin (The Merck Index, 10th Ed., Merck and Co., Inc., Rahway, N.J., 1983, monograph no. 6100), nigericin (loc. cit., monograph no. 6390), narasin (loc. cit., monograph no. 6271), lasalocid (loc. cit., monograph no. 5204), and salinomycin (loc. cit., monograph no. 8193). The subject has been reviewed by Westley, "Polyether Antibiotics", Adv. Appl. Microbiol., vol. 22, pp. 177-223 (1977). These compounds are generally known as coccidiostats and/or as feed additive-growth promotants.


SUMMARY OF THE INVENTION

A culture of Streptomyces hygroscopicus, ATCC 53626, when fermented under aerobic conditions in aqueous media, produces a new acidic polycyclic ether antibiotic, a compound having the formula (I), as specified above.
The present invention is directed to said compound of the formula (I), including the pharmaceutically-acceptable cationic salts thereof, and to a process for its preparation which comprises fermentation of said S. hygroscopicus ATCC 53626 in an aqueous nutrient medium comprising an assimilable source of carbon and nitrogen until a recoverable amount of said compound of the formula (I) is formed, preferably under submerged aerobic conditions. For use as an anticoccidial agent and/or a growth promotant, the compound (I) is not necessarily separated from the fermentation and isolated in substantially pure form, but is alternatively used in crude form, either in precipitated form admixed with mycelium (recovered by filtration of the fermentation medium), or in solids obtained by spray- or freeze-drying the entire fermentation medium.
Said pharmaceutically-acceptable cationic salts include, but are not limited to, those of sodium, potassium, calcium, ammonia, N,N'-dibenzylethylene-diamine, N-methylglucamine (meglumine) and diethanolamine. The preferred cationic salts are those of potassium and sodium.
The present invention is also directed to nutrient feed compositions, one for cattle or swine which comprises the compound of the formula (I) in an amount effective to promote growth and/or improve the feed utilization of said cattle or swine, and the other for poultry which comprises the compound of the formula (I) in an amount effective to control coccidial infection in said poultry.
The present invention is further directed to a method for promoting growth and/or increasing the efficiency of feed utilization in swine or cattle which comprises administering to said swine or cattle a growth promoting or feed-utilization efficiency promoting amount of the compound of the formula (I), particularly in the form of a nutrient feed composition; and to a method for controlling coccidial infections in poultry which comprises administering to said poultry an anticoccidially effective amount of the compound of the formula (I), particularly in the form of a nutrient feed composition.
Finally, the present invention is directed to a biologically pure culture of Streptomyces hygroscopicus ATCC 53626, said culture being capable of producing the compound of the formula (I) in a recoverable quantity upon fermentation in an aqueous nutrient medium comprising assimilable sources of carbon and nitrogen; including said culture in freeze-dried form.


DETAILED DESCRIPTION OF THE INVENTION

The culture capable of producing the present polycyclic ether antibiotic of the formula (I) is designated Streptomyces hygroscopicus, and has been deposit

REFERENCES:
patent: 3577531 (1981-10-01), Gorman et al.
patent: 4150152 (1979-04-01), Celmer et al.
patent: 4293650 (1981-10-01), Florent et al.
patent: 4366311 (1982-12-01), Mizutani et al.
patent: 4427655 (1984-01-01), Stapley
patent: 4504584 (1985-03-01), Kitaura et al.
patent: 4591559 (1986-05-01), Liu et al.
Hamill et al., J. Antibiotics (Japan), vol. 22, pp. 161-164 (1969).
Liu et al., J. Antibiotics (Japan), vol. 29, 21-28 (1976).
Perry, Chemical Engineers' Handbook, Fifth Edition, pp. 20-58 to 20-63, (1973).

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