Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1999-07-30
2000-10-24
Cook, Rebecca
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514 86, 514 89, 514 99, 514122, 514131, 514136, 514147, 514343, 514345, 514357, 514404, 514453, 514464, 514467, 514721, 514758, A61K 31415
Patent
active
061368369
DESCRIPTION:
BRIEF SUMMARY
This is a 371 of PCT/EP97/06965 filed Dec. 9, 1997.
The present invention relates to compositions for the systematic control of warm-blooded animal parasites comprising an effective quantity of a particular arylbenzoylurea.
More specifically, the present invention relates to compositions comprising an effective quantity of 1-[3-chloro-4-(1,1,2-trifluoro-2-trifluoromethoxyethoxy)phenyl]-3-(2,6-dif luorobenzoyl)urea and a pharmaceutically acceptable carrier and their use for the systematic control of warm-blooded animal parasites.
The present invention also relates to the use of 1-[3-chloro-4-(1,1,2-trifluoro-2-trifluoromethoxyethoxy)phenyl]-3-(2,6-dif luorobenzoyl)urea as such for the systemic control of warm-blooded animal parasites.
European patent EP 271.923 describes the compound corresponding to 1-[3-chloro-4-(1,1,2-trifluoro-2-trifluoromethoxyethoxy)phenyl]-3-(2,6-dif luorobenzoyl)urea having formula (I): ##STR1## as having a high insecticidal activity.
The above patent also discloses a method for fighting infestations caused by harmful insects which consists in distributing the compound having formula (I), as such or in the form of a suitable composition, onto the surface of the infested area. This method of application is effective for the treatment of agricultural cultivations, basins and waterways, industrial and civil sites, but its utility is limited if the compound having formula (I) is to be adopted in the veterinary and zootechnical field, for example., for protecting domestic animals from these parasites which feed by sucking their host's blood, such as flees, ticks, louse, etc.
The Applicant has now found that the compound having formula (I) is surprisingly effective in protecting warm-blooded animals from ectoparasites and endoparasites, if it is systemically carried into the blood of the animal host as such or, preferably, by means of a suitable pharmaceutically acceptable composition.
In addition, as it has been observed that the compound having formula (I) has a very low oral toxicity, both acute and chronic, on mammals and birds, it does not have mutagen and tetragen effects and does not have the tendency to accumulate in adipose tissues, the use of this compound having formula (I), as well as being particularly effective, is also safe and harmless for the animals treated.
The present invention therefore relates to compositions comprising an effective quantity of 1-[3-chloro-4-(1,1,2-trifluoro-2-trifluoromethoxyethoxy)phenyl] 3-(2,6-difluorobenzoyl)urea having formula (I): ##STR2## and a pharmaceutically acceptable carrier.
The above compositions can be used for the systemic control of warm-blooded animal parasites.
The compound having formula (I) can be prepared by means of a process which comprises the reaction of 3-chloro-4-(1,1,2-trifluoro-2-trifluoromethoxyethoxy)-aniline having formula (II): ##STR3## with 2,6-difluorobenzoylisocyanate having formula (III): ##STR4##
Alternatively, the compound having formula (I) can be prepared by a process which comprises the reaction of 3-chloro-4-(1,1,2-trifluoro-2-trifluoromethoxyethoxy)phenylisocyanate having formula (IV): ##STR5## with 2,6-difluorobenzamide having formula (V): ##STR6##
The above processes are carried out in an anhydrous environment and in the presence of an inert solvent, at a temperature ranging from 0.degree. C. and the boiling point of the reaction mixture.
Examples of inert solvents suitable for the purpose are aromatic hydrocarbons such as, for example, benzene, toluene, xylene, chlorobenzene; chlorinated hydrocarbons such as, for example, methylene chloride, chloroform, carbon tetrachloride, dichloroethane; ethers such as, for example, diisopropylether, tetrahydrofuran, dioxane.
The compounds having formula (III) and (V) can be prepared according to methods which are well known in literature. The compound having formula (V) is also commercially available.
The compound having formula (II) can be prepared as described, for example, in European patent EP 271.923.
The compound having formula (IV) can be prepared starting f
REFERENCES:
patent: 5135953 (1992-08-01), Potter et al.
Bettarini Franco
Piccardi Paolo
Cook Rebecca
Isagro S.p.A.
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