Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Reexamination Certificate
1998-11-17
2001-12-25
Jones, Dwayne C. (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
Reexamination Certificate
active
06333355
ABSTRACT:
BACKGROUND OF THE INVENTION
The present invention relates to a method for controlling ecto-parasites of animals. In detail, the present invention relates to a method for controlling ecto parasites of animals wherein 1-(2,6-difluorobenzoyl)-3 -[2-fluoro-4-(1,1,2,3,3,3-hexafluoropropoxy)phenyl]urea (hereinafter, recited as Compound #1) is applied to the said animals.
Ecto-parasites have-been responsible for the transmission of disease. Fleas have been a particular problem because of their ability to completely infest an environment. The female flea lays her eggs on the host animal after mating. The eggs are able to fall off the host and be distributed to the host's environment. By this mechanism, the eggs are able to cover a larger area.
It is disclosed in Japanese patent publication (laid-open) No. 2-138247 that Compound #1 has an insecticidal activity. The publication discloses that benzoylurea compounds including Compound #1 in the publication are excreted as they are and therefore, can control the larvae and eggs of such insects like houseflies that breed in the excretion of domestic animals when they are applied to the domestic animals orally.
It is disclosed in U.S. Pat. No. 4,089,975 that benzoylurea compounds such as 1-(2,6-difluorobenzoyl)-3 (4-trifluoromethoxyphenyl)urea (hereinafter, recited as Compound A) and 1-(2,6-difluorobenzoyl)-3-[4-(1,1,2,2-tetrafluoroethoxy)phenyl]urea (hereinafter, recited as Compound B) can also be used for controlling insects which inhabit in excretion of domestic animals.
On the other hand, Japanese patent publication (laid-open) No. 63-72631 discloses a method for defending dogs or cats from re-infection of fleas by applying juvenile hormone like chemical compounds, triazine derivatives that regulate the growth of fleas and benzoylurea derivatives (specifically, N-3-(5-trifluoromethylpyridin-2-yl)phenyl-N′-benzoylurea derivatives) that regulate the growth of fleas to dogs or cats. However, the effectiveness of the method generally do not last a sufficient amount of time.
SUMMARY OF THE INVENTION
The present invention relates to a method for systemic control of ecto-parasites of animals.
More specifically, the present invention relates to a method that effectively controls ecto-parasites for a comparably long period of time by applying Compound #1 to the host animal. The propagation of ecto-parasites is prevented by applying an effective amount of Compound #1 to the host animal and letting the ecto-parasites feed thereon.
DETAILED DESCRIPTION OF THE INVENTION
Compound #1, employed in the present invention, may be produced by employing Japanese patent publication (laid-open) No. 2-138247 (recited above).
The objective ecto-parasites of the present invention are pests that live externally to the host animal but necessitate blood from the host animal to achieve normal reproductive abilities. More specifically, the objective ecto-parasites of the present invention are not only limited to the kinds of mites and/or ticks (Acarina) such as
Boophilus microplus
and
Haemaphxalis longicornis
; Pulicidae (fleas) such as
Ctenocephalides felis
(cat fleas),
Ctenocephalides canis
(dog fleas), and
Xenopsylla cheopis
; and Anoplura (lice) such as
Haematopinus eurysternus
and
Damalinia ovis
that live external to the host organism but, may include blood sucking Dipthera insects such as
Tabanus chrysurus, Culicoides oxystoma
, and
Simulium iwatens.
The objective host animals for the present invention are warm-blooded animals whose blood will permit an ecto-parasite to achieve normal reproductive capabilities. More specifically, the objective host animals include pet animals such as dogs, cats, mice, rats, hamsters, squirrels, rabbits, ferrets, and birds (for example, pigeons, parrots, minas, java sparrows, love birds, and canaries) but, are not limited to the kinds of domestic animals such as cattle, horses, swine, sheep, ducks, drakes, and poultry.
The manner which Compound #1 is administered as an efficacious dosage may vary. Compound #1 may be administered to the host animals at a rate from about 0.01 mg to about 1000 mg per each kilogram of the host animal (i.e. 0.01-1000 mg of Composition #1/kg of the host animal), and preferably at the rate from about 0.1 mg to about 500 mg per each kilogram of the host animal (i.e., 0.1-500 mg Composition #1/kg of the host animal). The preferred dosage for controlling a given ecto-parasite is determined individually, but it is generally necessary to have an efficacious amount of Compound #1 present in the bloodstream of the treated host animal to control the given ecto-parasite. The systemic control of ecto-parasites is achieved by having the ecto-parasites ingest blood from the treated host animal so that the said ecto-parasite is exposed to an efficacious amount of Compound #1. As used herein, “efficacious amount” means an amount that leads to a reduced rate of the hatching of eggs and/or to the inability to fertilize.
Compound #1 is may be applied in pure form, but preferably in the form of a composition which comprises Compound #1 in an amount of 0.1% to 99% by weight in the composition.
Compound #1 may be applied to host animals by oral or non-oral application.
In oral application, examples of the form of the composition includes tablets, liquids, capsules, wafers, biscuits, emulsifiable concentrates, and/or so on. The oral application includes a method to apply the composition and a method to apply the mixture of Compound #1 or the composition with feed for the host animals. To prevent hydrolysis or degradation by constituents of animal feed, Compound #1 may previously be formulated in a protective matrix such as gelatin, and be further protected by formulation with preservatives and anti-oxidents such as sodium benzoate, parabens, BHT (butylated hydroxytoluene), and BHA (butylated hydroxyanisole).
In non-oral application, examples of the form of the composition includes a water soluble suspension, oily suspension, implants comprising of resins and soluble/erodible materials and/or so on. The non-oral application includes parenteral applications such as subcutaneous, intravenous, and intramuscular injection; percutaneous applications such as spot-on and pour-on application; implants application.
The tablet formulation for oral application generally employs sugars such as lactoses, sucroses, mannitols, and sorbitols; excipien agents such as celluloses and calcium phosphates; binders such as powdered starches, gelatins, gum arabic, tragacanth, methylcelluloses, agars, alginic acids, and alginic acid salts; lubricants such as silicas, talcs, stearic acids, and stearic acid salts; Dragee cores such as polyvinyl pyrrolidones, polyethylene glycols, and titanium dioxides; and/or so on in addition to Compound #1. Coloring agents and food additives may also be employed when necessary.
The capsule formulation for oral application may be a dry-filled capsule comprising of gelatins, a soft capsule comprising of gelatins and plasticisers such as glycerins, sorbitols, and so on. The said dry-filled capsule, may include excipien agents such as lactoses, binders such as powdered starches, lubricants such as talc and stearic acid salts, stabilizers, and so on. The soft capsule formulation generally comprises. Compound #1 dissolved or suspended in a suitable solvent such as fatty oils, parraffin oils, liquid polyethylene glycols, and so on. In addition, the soft capsule formulation may also comprise of a stabilizer when necessary.
The composition for a non-orally applied injection may be water-soluble suspensions or oily suspensions which comprise animal/plant oils such as sesame oils; esters of fatty acids such as ethyl oleates; triglycerides; thicking agent such as sodium carboxymethylcellulose, sorbitol, and dextran; and so on in addition to Compound #1.
The composition for percutaneous application may be a spot-on formulation or a pour-on formulation which comprises Compound #1 dissolved or suspende
Mori Tatsuya
Sakamoto Noriyasu
Sembo Satoshi
Birch & Stewart Kolasch & Birch, LLP
Jones Dwayne C.
Sumitomo Chemical Company Limited
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