Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1998-10-30
2000-11-14
Pak, John
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514546, 514547, 514549, 514552, 514557, 514558, 514560, 514786, 514919, 4241951, 424DIG10, A01N 4340, A01N 3702, A01N 3706, A01N 3700
Patent
active
061470910
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to compositions for repelling arthropods, these compositions being based on piperidine derivatives and fatty acids and fatty acid derivatives as synergists.
It has been disclosed that certain piperidine derivatives can be employed as agents for repelling insects and mites (cf. EP-A 0 281 908 and EP-A 0 289 842). However, a considerable disadvantage of the known repellents is their long-term action, which is relatively short in some cases.
A considerable disadvantage of the known repellents is their long-term action, which is relatively short in some cases.
The prolonged activity of certain repellents, for example Deet.RTM., due to a combination with vegetable oils and/or fatty acids and/or their esters has also been disclosed (cf., for example, DE-A 38 42 232 and JP 042 44 001). Again, the long-term action of these mixtures is not always satisfactory.
It has been found that mixtures of piperidine derivatives of the formula (I) ##STR2## in which R represents alkyl or alkoxy arthropod-repellent properties.
The repellent action of the mixtures according to the invention is considerably more potent than that of the pure piperidine derivatives, the fatty acids causing not only an additive, but a synergistic, increase in activity.
The compositions according to the invention are therefore a valuable enrichment of the art.
Formula (I) provides a general definition of the piperidine derivatives. Preferred compounds are those in which R represents C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy. Especially preferred compounds are those in which R represents C.sub.3 -C.sub.4 -alkyl or C.sub.3 -C.sub.4 -alkoxy.
Very especially preferred compounds of the formula (I) which can be used according to the invention are the following: ##STR3##
The piperidine derivatives which can be used according to the invention have been disclosed (cf. EP-A 0 281 908 and EP-A 0 289 842).
Synergists which are suitable for the mixtures according to the invention are preferably even-numbered, straight-chain higher fatty acids, in particular C.sub.6 -C.sub.18 -fatty acids, or their derivatives such as, in particular, fatty acid esters.
Synergists which may especially preferably be mentioned are caprylic acid (C.sub.8) and capric acid (C.sub.10) and their alkyl esters such as, in particular, the methyl esters.
The fatty acids or their derivatives can be employed singly or in the form of variously composed mixtures of a variety of fatty acids/fatty acid derivatives.
It is also possible to employ substances which contain a mixture of various fatty acids in the first place, such as, preferably, vegetable oils.
Examples which may be mentioned are: citronella oil, clove oil, patchouli oil, rapeseed oil, juniper oil or coconut oil.
The compositions of the inventive mixtures of compounds of formula (I) and fatty acids and/or fatty acid derivatives can vary within a substantial range. Preferably the mixtures contain 1 to 90 percent per weight, more preferred 1 to 50 percent per weight and especially preferred 1 to 20 percent per weight of components of formula (I).
In a special embodiment, the mixtures according to the invention of piperidine derivatives of the formula (I) with fatty acids or fatty acid derivatives as synergists may also comprise other arthropod repellents. All repellents which can conventionally be used may be employed (cf., for example, K. H. Buchel, Chemie der Pflanzenschutz-und Schadlingsbekampfungsmittel [Chemistry of Crop Protection Products and Pesticides]; Editor: R. Wegler, Vol. 1, Springer Verlag Berlin Heidelberg New York, 1970, p. 487 et seq.).
Substances which are preferably used are repellent carboxamides, 1,3-alkanediols, carboxylates, lactone derivatives and also .beta.-alanine derivatives which are disubstituted on the nitrogen. Individual examples which may be mentioned are: N,N-diethyl-3-methylbenzamide (Deet), N,N-diethylphenylacetamide (DEPA), 2-ethyl-hexane-1,3-diol (Rutgers 612), dimethyl phthalate, 1,1,4,5,6,7,8,8a-octahydro-3H-2-benzopyran-3-one and ethyl 3-(N-n-butyl-N-acetyl
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K.H. Buchel, Chemie der Pflanzenschutz-und Schadlingsbekampfungsmittel (Chemistry of Crop Protection Products and Pesticides); Edition: R. Wegler, vol. 1, Springer Verlag Berlin Heidelberg, New York, 1970, p. 487 et seq.)
Kruger Bernd-Wieland
Nentwig Gunther
Roder Klaus
Bayer Aktiengesellschaft
Pak John
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