Acaricidal compositions

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

Reexamination Certificate

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C514S535000, C514S537000

Reexamination Certificate

active

06221890

ABSTRACT:

BACKGROUND OF THE INVENTION
1. Field of the Invention
The instant invention relates to acaricidal compositions and methods of controlling acarina.
2. Description of Related Art
Japanese laid open patent Hei 8-319202 describes trifluoromethanesulfonanilide compounds as possessing an acaricidal activity.
WO 93/22297 describes oxazoline compounds as possessing an acaricidal activity.
In cases of using the trifluoromethanesulfonanilide compounds or the oxazoline compounds as a singular active ingredient in a composition for controlling acarina, a large amount of the active ingredient is needed to effectively control acarina.
SUMMARY OF THE INVENTION
The instant invention provides superior acaricidal compositions which can be utilized to effectively control acarina. As such, the acaricidal compositions of the instant invention possess a synergistic acaricidal activity which is unexpectedly superior to that provided from individually utilizing a trifluoromethanesulfonanilide compound or an oxazoline compound as a sole active ingredient in a composition.
The instant invention fulfills such acaricidal properties by providing acaricidal compositions which comprise 2-methylcarbonyl-4-chlorotrifluoromethanesulfonanilide and 2-(2,6-difluorophenyl)-4-(2-ethoxy-4-tert-butylphenyl)-2-oxazoline together as active ingredients therein. Additionally, the instant invention provides methods of controlling acarina which comprise applying 2-methoxycarbonyl-4-chlorotrifluoromethanesulfonanilide and 2-(2,6-difluorophenyl)-4-(2-ethoxy-4-tert-butylphenyl)-2-oxazoline to acarina or a locus of where the acarina inhabits.
DETAILED DESCRIPTION OF THE INVENTION
An acaricidal composition of the instant invention comprises 2-methoxycarbonyl-4-chlorotrifluoromethanesulfonanilide and 2-(2,6-difluorophenyl)-4-(2-ethoxy-4-tert-butylphenyl)-2-oxazoline together as active ingredients. Preferably the weight to weight ratio of 2-methoxycarbonyl-4-chlorotrifluoromethanesulfonanilide to 2-(2,6-difluorophenyl)-4-(2-ethoxy-4-tert-butylphenyl)-2-oxazoline in the acaricidal composition is from about 1:0.1 to 1:10. In addition, the total amount of the active ingredients in said acaricidal composition is generally from about 0.02 to 99% by weight, wherein said percentage by weight is based on the total weight of the provided acaricidal composition. For example, the acaricidal compositions can comprise 2-methoxycarbonyl-4-chlorotrifluoromethanesulfonanilide in an amount of from about 0.01 to 90% by weight and 2-(2,6-difluorophenyl)-4-(2-ethoxy-4-tert-butylphenyl)-2-oxazoline in an amount of from about 0.01 to 90% by weight, wherein said percentages by weight are based on the total weight of the provided acaricidal composition.
The acaricidal compositions of the instant invention are usually formulated into sheets, tablets, fumigants, granules, oily solutions, emulsifiable concentrates, dusts, aerosols, and the like. Such formulations are preferably applied to the acarina or are utilized in locations in which a control of acarina is desired, in order to control acarina. Illustrative and non-limiting examples of locations of where said formulations may be utilized to control acarina include indoor floors, a habitat of an acarina, carpets, sofas, and the like.
The formulations of the inventive acaricidal compositions can treat such locations so that an acaricidally effective amount of the active ingredients is utilized to treat such locations. Such an acaricidally effective amount of the active ingredients may vary, but the formulations preferably utilize from about 0.01 to 2 g of the active ingredients per 1 m
2
of a locus or from about 0.001 to 2 g of the active ingredients per 1 m
3
of space to effectively control acarina.
It is preferable for the sheet formulations of the acaricidal compositions to have 2-methoxycarbonyl-4-chlorotrifluoromethanesulfonanilide and 2-(2,6-difluorophenyl)-4-(2-ethoxy-4-tert-butylphenyl)-2-oxazoline supported on a sheet. In order to produce the sheet formulations of the inventive acaricidal compositions, the active ingredients can be spread on a sheet or a sheet can be soaked in a solution or suspension containing the active ingredients to produce the sheet formulation. Further, the acaricidal compositions can also be formed to a sheet formulation by forming sheet material which already contain the active ingredients into said sheet formulations. Furthermore, a solvent which comprises the active ingredients may also be utilized to support said active ingredients on a sheet. When adding the active ingredients to the sheet material, the active ingredients may be kneaded into said sheet material. In addition, the active ingredients in the sheet formulations can be distributed therein so that the concentration of said active ingredients is from about 0.01 to 2 g per 1 m
2
of the sheet formulation.
Such solvents which are utilized to contain the active ingredients and produce the sheet formulations are preferably organic solvents, with examples of the organic solvents including ketone solvents such as acetone, alcohol solvents such as methanol, ester solvents such as ethyl acetate, halogenated aliphatic hydrocarbon solvents such as dichloromethane, aromatic hydrocarbons such as benzene and toluene, aliphatic hydrocarbons such as hexane and kerosene, and the like, but are not limited thereto.
The sheets which are utilized to formulate the sheet formulations of the inventive acaricidal compositions may have the dimensions of a generally flat shape, in which the thickness thereof may be from about 0.01 to 10 mm. In such cases, a sheet material which is utilized to produce the sheet formulations can comprise a synthetic resin film such as paper, polyolefin, polyester or polyvinylchloride, a woven textile of natural-occurring fibers such as jute, silk, wool or cotton, or the like.
The tablet formulations of the acaricidal compositions additionally comprise a porous carrier. Porous carriers which can be in the tablet formulations should preferably be able to preserve the active ingredients therein and also allow the active ingredients to release therefrom at an appropriate temperature. Illustrative and non-limiting examples of the porous carriers include cotton linters, ceramic boards, non-woven fabric, thick paper, and the like.
When utilizing the tablet formulations to control acarina, it is preferable to heat the tablet formulations to a temperature which allow the active ingredients therein to vaporize and disperse the active ingredients into the surrounding spaces thereof. Such temperatures may vary, but a temperature of from about 100 to 300° C. is preferable to vaporize the active ingredients in the tablet formulations. A commercially available mosquito mat heater may be utilized to heat the tablet formulation, if so desired. The size of the tablet formulations is typically from about 10 mm×20 mm×1 mm to 35 mm×50 mm×4 mm, preferably about 22 mm×35 mm×2.8 mm, and that may be utilized in commercial heater for controlling mosquitoes.
The fumigant formulations of the acaricidal compositions can additionally comprise a foaming agent therein. The foaming agents in the fumigant formulations are preferably organic and can provide a gas such as nitrogen when activated or heat decomposed. Illustrative and non-limiting examples of organic foaming agents which can be utilized in a combustion or non-combustion type fumigant formulation include azodicarbonamide, azobisisobutyronitrile, 2-(carbamoylazo)isobutyronitrile, dinitroisopentamethylenetetramine, p,p′-oxybis(benzenesulfonylhydrazide and the like.
Said combustion type fumigant formulations of the acaricidal compositions are generally produced by mixing 2-methoxycarbonyl-4-trifluoromethanesulfonanilide, 2-(2,6-difluorophenyl)-4-(2-ethoxy-4-tert-butylphenyl)-2-oxazoline, the foaming agent and a combusting agent. Preferably, in order to produce the combustion type fumigant formulations, water is additionally mixed into the mixture, the achieved mixture is kneaded into an useful form such as a granule, and the mixture

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