Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai
Patent
1999-07-02
2000-10-10
Geist, Gary
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ester doai
A61K 3122
Patent
active
061302503
DESCRIPTION:
BRIEF SUMMARY
The invention relates to pleuromutilin derivatives. It concerns the veterinary use of the compound of formula I ##STR1## i.e. 14-O-[1-[(R)-2-amino-3-methylbutyrylamino]-2-methylpropan-2-ylthioacetyl]m utilin in free base or in veterinarily acceptable salt form, in the therapy of veterinary diseases the expression of which is enhanced by increasing stocking density, hereinafter briefly named "the use of the invention."
The compound of formula I in free base or in veterinarily acceptable salt form (Econor.RTM.) is hereinafter briefly named "the agent of the invention". It preferably is in salt, especially in hydrochloride salt form. In that form it is known under the generic name valnemulin hydrochloride.
The term "therapy" is to be understood as applying for prophylactic as well as curative treatment.
The compound of formula I in free base form or in chemotherapeutically or veterinarily acceptable salt form is known from e.g. EP 153 277 and its equivalents, e.g. U.S. Pat. No. 4,675,330, specifically as Example 12 therein.
Known therefrom is, further, of ca. 0.008 to 25 .mu.g/ml; at concentrations of ca. 0.008 to 0.5 .mu.g/ml; and on hens, using mycoplasm strains, at a dosage of ca. 12 to 50 mg/kg body weight; at dosages of 20-150 mg/kg of feed; and mg/kg of feed, thus making the compound useful as an antibacterially active antibiotic generally and, as a veterinary agent, in particular for the chemotherapeutic treatment of coccidioses in fowl as well as a growth promoter in hen and pig.
It has now been found that, surprisingly, the agent of the invention is particularly effective in the therapy of veterinary diseases the expression of which is enhanced by increased stocking density, such as enzootic pneumonia in swine caused by Mycoplasma hyopneumoniae infection, swine dysentery caused by Serpulina (formerly Treponema) hyodysenteriae infection, swine colitis (inflammation of the colon) associated with Serpulina pilosicoli infection, ileitis in swine (porcine proliferative enteropathy; porcine intestinal adenomatosis) associated with Lawsonia intracellularis infection, chronic respiratory disease and arthritis in poultry associated with Mycoplasma gallisepticum infection, secondary pneumonia in swine associated with Pasteurella multocida, Actinobacillus (Haemophilus) pleuropneumoniae and/or Haemophilus parasuis infection, pneumonia in lambs, sheep and cattle (Shipping Fever, Transit Fever, Calf Respiratory Complex, Bovine Pneumonic Pasteurellosis) associated with Pasteurella haemolytica infection and polyarthritis in swine associated with Mycoplasma hyosynoviae infection.
Further, even more surprisingly, it has been found that induction of resistance to the drug is extremely low.
The invention thus concerns the veterinary use as defined above.
It also concerns the use of the agent of the invention for the manufacture of a medicament for use in the therapy of veterinary diseases the expression of which is enhanced by increasing stocking density.
It further concerns a method of treatment of veterinary diseases the expression of which is enhanced by increasing stocking density, comprising administration of a therapeutically effective amount of the agent of the invention to an animal in need of such treatment.
It further concerns a veterinary agent for use in the therapy of veterinary diseases the expression of which is enhanced by increasing stocking density, comprising the compound of formula I in free base or in veterinarily acceptable salt form, together with at least one veterinarily acceptable carrier or diluent.
If further concerns a process for the preparation of a medicament for use as defined above, which comprises mixing the agent of the invention together with at least one veterinarily acceptable carrier or diluent.
The animal suffering from veterinary diseases the expression of which is enhanced by increasing stocking density may e.g. not already be treated antibacterially with the agent of the invention, or not already be receiving the agent of the invention for growth promotion.
Mycoplasma hyopneum
REFERENCES:
patent: 4675330 (1987-06-01), Berner
patent: 5164526 (1992-11-01), Macher
Horkovics-Kovats et al., "Physiologically based pharmacokinetic modelling with valnemulin and its metabolites after multiple oral administration in pigs", J. Pharm. Med., vol. 6, No. 3-4, 1996, pp. 149-167.
Burch David George Sidney
Ripley Paul Howard
Zeisl Erich
Biochemie Gesellschaft m.b.H.
Geist Gary
Kalinchak Stephen G.
Maier Leigh C.
McNally Lydia T.
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