JPH0448775B2 - - Google Patents

Description

[Detailed description of the invention]

The subject of the invention provides a method for treating a warm-blooded animal infested with parasites in order to eliminate parasites from the whole body of the animal, preferably in a part of the animal's body to be treated, preferably in a part of the back of the animal. Then, the following formula (I _A ) (wherein X represents a chlorine or bromine atom) A composition containing as active ingredient at least one compound in all possible isomeric forms corresponding to A method for the treatment of warm-blooded animals infested with parasites, characterized in that the amount of active compound used is from 0.5 to 10 mg/kg body weight. The compound of formula I _A is a known compound which can be prepared by the method described in Belgian Patents Nos. 859,894 and 873,201. The compounds of formula I _A exhibit pronounced pesticidal properties, in particular good insecticidal, acaricidal, nematocidal and fungicidal properties. So far, the methods of administration known for the use of compounds of formula I _A for the control of parasites in warm-blooded animals are gastrointestinal, parenteral or topical administration; The only known compositions were the following. It has now been discovered that excellent results are obtained in the control of parasites in animals by administering compounds of formula _IA in a manner referred to as the "pour on" method. The method involves applying a solution containing the active substance to a small surface of the animal's body, preferably the back, allowing this active substance to pass into the animal's systemic circulation and obtaining an effect on the whole body of the animal. Are known. Of course, this method is not common. This is only applicable to compounds that can pass through the skin layers and enter the systemic circulation while retaining their activity, i.e. without being degraded or broken down into active metabolites themselves. It is. None of the prior art methods use formula I _A
does not suggest the use of compounds. According to the invention, a compound of formula I _A can be used as a "pour-on"
This method therefore offers unexpected features. Furthermore, the method of the invention provides significant benefits on a commercial scale. Because, as evidenced by the test results further presented in the experimental part,
This is because excellent results can be obtained very quickly and sustainably with very small amounts of the compound of formula _IA . The method according to the invention allows a simple, clean and economical application of compounds of formula I _A. Its advantages when compared to standard methods will be clear to the expert. Administration by the gastrointestinal route, although giving good results, should be avoided if possible as gastrointestinal disturbances may occur and should be reserved especially for the extermination of parasites that have settled in the stomach. Also, administration by "bath" gives quite good results. Unfortunately, however, this requires quite large amounts of the compound. This is because pyrethrinoids generally burn and decompose easily, requiring the bath to be renewed. Parenteral administration should also be avoided if possible. This is because it is not easy to inject all animals in a herd. The method according to the invention can be applied to all warm-blooded animals, especially domestic animals such as cattle, sheep or pigs. The experimental section below specifies the results obtained on cows. The method according to the invention can eliminate parasites whether they are internal or external parasites.
In particular, they make it possible to control mites, worms, maggots and various stingers. Thus, the method of the invention can be used to control mites, especially mites, scabies, and the like. In particular, the compositions used in the methods of the invention are provided in the form of veterinary compositions. Among the compounds of formula I _A according to the invention, mention may be made of the following: (1R,cis)-2,2-dimethyl-3-(2,2
-dichloro-1,2-dibromoethyl)cyclopropane-1-carboxylic acid (S) α-cyano-3-
Phenoxybenzyl, (1R, cis)-2,2-dimethyl-3-(1,
2,2,2-tetrabromoethyl)cyclopropane-1-carboxylic acid (S)-α-cyano-3-phenoxybenzyl. The abovementioned compounds (the first of which is referred to below as compound A) can be prepared by the method described in Examples 1 and 2 of Belgian Patent No. 858,894. The amount of compound of formula _IA used will vary depending on the condition of the animal to be treated, the species, the environment and the desired result. It is generally calculated as follows:
0.5-10 mg of a compound of formula _IA . The number of treatments to be performed also depends on the same parameters discussed above as determining the dosage of the compound. However, the experiments described below show that excellent results can be obtained with a single application. As mentioned above, the composition applied in the method according to the invention contains a vehicle that is capable of passing through the skin layers. Vehicles which are capable of passing through the skin layer include dispersible compounds such as dimethylformamide, dimethyl sulfoxide or dimethylacetamide, or any vehicle that can pass through the skin layer, as long as the solubility of the compound of formula I _A is permitted. A solution, in particular an oily solution, is to be understood as a solution, especially an oily solution, containing all agents that facilitate the The oily solution used preferably contains vegetable oil, such as olive oil or peanut oil. In particular, the subject of the invention is a process characterized in that the vehicle is an oily solution of dimethylformamide. Furthermore, the composition according to the invention can also contain emulsifiers or surfactants. The following examples illustrate the invention without restricting it in any way. Example 1 Test against Boophilus microplus A young bull weighing 340 g is deliberately infested with ticks of the species Boophilus microplus. Dani are present at all stages of development. A solution containing 5 mg of compound A per kg of body weight of the treated animal in solution in a mixture of dimethylformamide and olive oil (1:1) is applied to the back of the animal on the indicated day (D). 1.7g Compound A as 80ml oily solution
Use. Count the ticks and observe their developmental stages.

[Table] Conclusion Compound A shows remarkable activity. Example 2 Test against Boufilus microplus (Mexico variety) Young bulls intentionally infected with Boufilus microplus are used. Control batches receive no treatment. A batch is coated with 100 c.c. of the same solution as used in Example 1 containing 5 mg of Compound A per kg of body weight of treated animals on the indicated day (D). Count the ticks before and after the treatment date. Count the number of ticks on treated and control animals. The results obtained are as follows.

【table】

[Table] Conclusion Compound A shows remarkable activity. Example 3 Test against Boufuilus microplus (Mexico breed) Eight young bulls were infested with the larvae of this mite so that all developmental stages of Boufillus microplus (susceptible Mexico breed) were represented. Compound A was administered at a dose of 5 mg/kg of body weight of treated animals;
Administered as a solution of a mixture consisting of 85 g dimethylformamide, 7 g Emulsogen and 3 g Arcopal in doses of 2.5 mg and 1 mg, with an application volume of 40 or 30 c.c. did. Arcopal is a surfactant consisting of nonionic alkyl phenol polyglycol ethers. Emulsogen is an emulsifier for oils, paraffins or organic solvents. The ticks are counted before and after the treatment day and the number of ticks on treated animals is compared to the number on control animals. Determine the activity (%) of the compound. The results obtained are as follows.

[Table] At doses of 5mg/Kg, 2.5mg/Kg and 1mg/Kg,
The efficacy of compound A was 99.4%, 97.6% and
It was determined to be 94.3%. Conclusion: Compound A shows significant activity. Example 4 Lipicephalus appendeiquilatus,
(Rhipicephalus appendiculatus), Rhipicephalus evertsi (Rhipicephalus evertsi),
Rhipicephalus
simus), Amblyomma habraeum and Hyalomma species Compound A was administered at 5 mg per kg of body weight of treated animals;
It was administered in doses of 2.5 mg and 1 mg/Kg. The animals naturally had large numbers of several species of mites. The results obtained after 1, 2 and 3 days of treatment are summarized in the table below.

[Table] Conclusion: Compound A exhibits remarkable activity in the natural state of several different mites. Example 5 Test on tick-infested livestock from Africa Adult female cows and calves approximately 8 months old are used. These animals have ticks. These animals should be treated with 4 to 5 mg per kg of body weight.
Treat with a solution containing 10 mg or 10 mg of compound A. Count the mites on the day of treatment and thereafter. The results are as follows.

【table】 Conclusion Compound A shows significant activity. Example 6 Examples of compositions A composition corresponding to the following formulation was prepared. Compound A...1.7g Dimethylformamide …40c.c. Olive oil…40c.c. Example 7 Examples of compositions A composition corresponding to the following formulation was prepared. Compound A...1.6g Dimethylformamide …85c.c. Emulzogen…7g Alcopal…3g

Claims (1)

[Claims] 1. When exterminating parasites from the whole body of a warm-blooded animal (excluding humans) infected with parasites, the following formula (I _A ) is applied to a part of the animal's body. (wherein X represents a chlorine or bromine atom) a composition containing as active ingredient at least one compound in all possible isomeric forms corresponding to and the amount of active compound used ranges from 0.5 to 10 mg/kg body weight.
A method for exterminating parasites from a warm-blooded animal (excluding humans) infested with parasites. 2. The method according to claim 1, wherein the composition is administered to a part of the back of the animal. 3 The active compound is (1R, cis)-2,2-dimethyl-3-(2,2-dichloro-1,2-dibromoethyl)cyclopropane-1-carboxylic acid (S)
The method according to claim 1, characterized in that it is α-cyano-3-phenoxybenzyl. 4 The active compound is (1R, cis)-2,2-dimethyl-3-(1,2,2,2-tetrabromoethyl)
The method according to claim 1, characterized in that cyclopropane-1-carboxylic acid (S) α-cyano-3-phenoxybenzyl. 5. A method according to any one of claims 1 to 3, characterized in that the vehicle capable of passing through the skin layers is an oily solution of the dispersible compound. 6. The method according to claim 4, wherein the dispersing compound is a substance selected from the group consisting of dimethylformamide, dimethylsulfoxide and dimethylacetamide. 7. Claims 1 to 7, characterized in that the vehicle is a solution of dimethylformamide in vegetable oil.
The method described in any of Section 5.