Arthropod control composition

Abstract

The present invention relates to arthropod control compositions, methods and uses for controlling arthropods, and arthropod control articles comprising the same.

Description

Technical Field

[0001] This invention relates to arthropod control compositions, methods and uses for controlling arthropods, and arthropod control articles comprising the same. Background Technology

[0002] Many mammals, including humans, are vulnerable to arthropods. Some arthropods, such as mosquitoes and ticks, are undesirable to vertebrates, such as mammals, especially humans, because they bite and can cause itching, the spread of disease and / or bacteria, or may be the cause of other diseases and / or conditions.

[0003] Arthropod control compositions contain active substances that, when applied to skin, clothing, or other surfaces, may prevent arthropods from landing on or climbing those surfaces. Arthropod control agents help prevent and control outbreaks of arthropod-borne diseases such as malaria.

[0004] However, some known arthropod control agents and compositions have certain drawbacks because they may have negative effects, namely negative olfactory properties, such as no odor or an unpleasant odor, or conversely, only weak arthropod control, especially arthropod repellency properties.

[0005] There is a need for arthropod control compositions that provide good olfactory properties, i.e., good pleasurable effects, and good arthropod control, especially arthropod repellent properties.

[0006] The arthropod control composition according to the present invention is not disclosed or implied in the prior art. Attached Figure Description

[0007] Figure 1: Number of mosquitoes landing on warm bodies treated with different concentrations of different substances within 2 minutes. Tests using only ethanol (control) showed 0 mg / m³.

[0008] Figure 2: Number of mosquitoes landing on the body within 2 minutes after the air in the cage was treated with different concentrations of different substances. Tests using only solvent (control) showed 0 μg / L air, while nd indicates no data.

[0009] Figure 3 Percentage of avoidance in cage arm test. Each bar represents the mean avoidance ± SD of 3 volunteers, while nd indicates no data. Detailed Implementation

[0010] This invention relates to a preferred arthropod insect control composition comprising one or more substances selected from the group consisting of: (E)-1-(2,6,6-trimethylcyclohexyl-2-en-1-yl)but-2-en-1-one, (3Z)-3-butanediol-2-benzofuran-1-one, 4-vinyl-2-methoxyphenol, natural Cognacoil green, Labdanum extract (Cistus spp.), 5-pentyloxolan-2-one, chromen-2-one, (2E)-3,7-dimethyloctyl-2,6-dienal, 4-hydroxy-3-methoxybenzaldehyde, (5R)-2-methyl-5-prop-1-en-2-ylcyclohexyl-2-en-1-one, spearmint. Spiciata oil, 6-hexyloxan-2-one, 5-methyl-2-propane-2-ylcyclohexyl acetate, Nigella damascena oil, 2-phenylethanol, 6-pentyloxan-2-one, methyl (4-methoxyphenyl) acetate, Syzygium aromaticum oil, 3,4,4a,5,6,7,8,8a-octahydrobenzopyran-2-one, (1S,6R)-3,7,7-trimethylbicyclo[4.1.0]hept-3-ene, 2-phenylethyl 2-methylpropionic acid, methyl 2-(3-oxo-2-pent-2-enylcyclopentyl)acetate, (4R)-4-(2-methoxypropane-2-yl)-1-methylcyclohexene, Mentha peppermint. Piperrita oil, 2-methoxy-4-[(E)-prop-1-enyl]phenol, 2-methyl-3-(4-propane-2-ylphenyl)propanal and (4-methoxyphenyl)methanol.

[0011] The substances in the compositions of this invention are known in the art and can be readily synthesized or obtained. The following list provides the CAS number for each substance: 5-pentyloxetane-2-one (CAS No. 104-61-0), benzopyran-2-one (CAS No. 91-64-5), 2-methyl-3-(4-propane-2-ylphenyl)propanal (CAS No. 103-95-7), (4-methoxyphenyl)methanol (CAS No. 105-13-5), (2E)-3,7-dimethyloctyl-2,6-dienal (CAS No. 5392-40-5), 4-hydroxy-3-methoxybenzaldehyde (CAS No. 121-33-5), (5R)-2-methyl-5-prop-1-en-2-ylcyclohex-2-en-1 ...104-61-0), benzopyran-2-one (CAS No. 104-61-0), benzopyran-2-one (CAS No. 104-61-0), benzopyran-2-one ( CAS No. 6485-40-1), 4-vinyl-2-methoxyphenol (CAS No. 7786-61-0), Rock Rose Extract (CAS No. 84775-64-4 / 8016-26-0), Natural Connect Oil (CAS No. 8016-21-5), (3Z)-3-butanediol-2-benzofuran-1-one (CAS No. 551-08-6), (E)-1-(2,6,6-trimethylcyclohexyl-2-en-1-yl)but-2-en-1-one (CAS No. 24720-09-0), 6-hexyloxetane-2-one (CAS No. 710-04-3), 5-methyl-2-propyl acetic acid [Hexyl] ester (CAS No. 2623-23-6), black cumin oil (CAS No. 73507-35-4 / 90064-31-6), 2-phenylethanol (CAS No. 60-12-8), 6-pentyloxetane-2-one (CAS No. 705-86-2), methyl (4-methoxyphenyl) acetate (CAS No. 104-21-2), 3,4,4a,5,6,7,8,8a-octahydrobenzopyran-2-one (CAS No. 4430-31-3), (1S,6R)-3,7,7-trimethylbicyclo[4.1.0]hept-3-ene (CAS No. 498-15-7), 2-phenylethyl 2-methylpropionic acid (CAS No. 103-48-0), methyl 2-(3-oxo-2-pent-2-enylcyclopentyl)acetate (CAS No. 20073-13-6), (4R)-4-(2-methoxypropane-2-yl)-1-methylcyclohexene (CAS No. 30199-25-8), 2-methoxy-4-[(E)-prop-1-enyl]phenol (CAS No. 5932-68-3), spearmint oil (CAS No. 8008-79-5 / 84696-51-5), clove oil (CAS No. 8000-34-8 / 68917-29-3) and peppermint oil (CAS No. 8006-90-4 / 84082-70-2).

[0012] In one particular embodiment, the preferred mosquito repellent is selected from: rock rose extract, natural connective oil, (3Z)-3-butanediol-2-benzofuran-1-one, 2-methyl-3-(4-propane-2-ylphenyl)propanal, methyl 2-(3-oxo-2-pent-2-enylcyclopentyl)acetate, black cumin oil, (2E)-3,7-dimethyloctyl-2,6-dienal, 5-pentyloxetane-2-one, and clove oil. 4-Vinyl-2-methoxyphenol, 4-hydroxy-3-methoxybenzaldehyde, 6-pentyloxetane-2-one, (1S,6R)-3,7,7-trimethylbicyclo[4.1.0]hept-3-ene, benzopyran-2-one, 6-hexyloxetane-2-one, 2-methoxy-4-[(E)-prop-1-enyl]phenol, 5-methyl-2-propane-2-ylcyclohexyl acetate, (4-methoxyphenyl)methanol.

[0013] In one particular embodiment, the preferred mosquito repellent is selected from: (3Z)-3-butanediol-2-benzofuran-1-one, methyl 2-(3-oxo-2-pent-2-enylcyclopentyl)acetate, black cumin oil, (2E)-3,7-dimethyloctyl-2,6-dienal, eugenol, 6-pentyloxecyclohexane-2-one, benzopyran-2-one, 2-phenylethyl 2-methylpropionic acid, and 4-vinyl-2-methoxyphenol.

[0014] In one particular embodiment, the substance used for spatial repellency, more preferably mosquito spatial repellency, is selected from: natural connective oil, (E)-1-(2,6,6-trimethylcyclohexyl-2-en-1-yl)but-2-en-1-one, 2-methyl-3-(4-propane-2-ylphenyl)propanal, 4-vinyl-2-methoxyphenol, methyl 2-(3-oxo-2-pent-2-enylcyclopentyl)acetate, 6-hexyloxetane-2-one, benzopyran-2-one, 6-pentyloxetane-2-one, peppermint oil, 4-Hydroxy-3-methoxybenzaldehyde, clove oil, 5-pentyloxepane-2-one, 2-phenylethanol, black cumin oil, spearmint oil, (5R)-2-methyl-5-prop-1-en-2-ylcyclohex-2-en-1-one, 2-methoxy-4-[(E)-prop-1-enyl]phenol, (4-methoxyphenyl)methanol, (4R)-4-(2-methoxypropane-2-yl)-1-methylcyclohexene, 2-methoxy-4-[(E)-prop-1-enyl]phenol, (4-methoxyphenyl)methyl acetate.

[0015] In one particular embodiment, the substance used for space repellency, more preferably mosquito space repellency, is selected from: 4-vinyl-2-methoxyphenol, methyl 2-(3-oxo-2-pent-2-enylcyclopentyl)acetate, benzopyran-2-one, 6-pentyloxetane-2-one, peppermint oil, and 4-hydroxy-3-methoxybenzaldehyde.

[0016] In one particular embodiment, the substance used to prevent (more preferably) ticks is selected from: (E)-1-(2,6,6-trimethylcyclohex-2-en-1-yl)but-2-en-1-one, 4-vinyl-2-methoxyphenol, (3Z)-3-butyryl-2-benzofuran-1-one, 5-pentyloxetane-2-one, benzopyran-2-one, 2-methoxy-4-[(E)-prop-1-enyl]phenol, and 2-methyl-3-(4-propane-2-ylphenyl)propanal.

[0017] In one particular embodiment, the substance used to prevent ticks, more preferably, is selected from: 4-vinyl-2-methoxyphenol, (3Z)-3-butyryl-2-benzofuran-1-one, 5-pentyloxetane-2-one, and 2-methoxy-4-[(E)-prop-1-enyl]phenol.

[0018] In one particular embodiment, the arthropod control composition comprises 0.01 to 90% by weight, more preferably 0.2 to 30% by weight, of a compound or composition, based on the total weight of the composition.

[0019] In a preferred embodiment of the invention, the arthropod control composition has a good pleasurable characteristic.

[0020] The inventors readily understand that arthropod control compositions may require acceptable pleasurable characteristics. This is because the compositions are used close to consumers, and it is understood that any unpleasant pleasurable characteristics could inhibit the use of the compositions.

[0021] The term "arthropod" has its normal meaning in the hands of those skilled in the art. Arthropods include invertebrates such as insects, arachnids, and crustaceans, which have segmented bodies and articulated appendages. Arthropods typically have a chitinous exoskeleton that molts at intervals, and a dorsal forebrain that connects to the ventral chain of ganglia.

[0022] In this understanding, arthropods refer to undesirable arthropods, meaning that their presence in the air, on surfaces of objects, on plant surfaces, or on surfaces of vertebrates (e.g., human subjects or other mammals, preferably human subjects). Preferably, undesirable arthropods are harmful arthropods that affect plants and animals, such as thrips, aphids, beetles, moths, mealybugs, scale insects, etc. More preferably, harmful arthropods that affect animals, such as ants, termites, cockroaches, flies, etc. Even more preferably, blood-sucking arthropods that affect vertebrates, such as biting flies, bedbugs, assassin bugs, fleas, lice, mosquitoes, and ticks, even more preferably mosquitoes and ticks.

[0023] Reasons for not wanting the presence of arthropods may include the unpleasantness of their presence in the air for the subject, the potential for arthropods to spread diseases and / or pathogens through contact with objects, the possibility that arthropod bites may cause itching, spread of diseases and / or pathogens, or that arthropod feeding may be the cause of other diseases and / or symptoms.

[0024] In one particular implementation, the arthropod is an insect or an arachnid, preferably an insect.

[0025] The term "insect" is understood by those skilled in the art. Insects are described as having a distinct head, thorax, and abdomen, only three pairs of legs, and usually one or two pairs of wings.

[0026] In one particular implementation, the insect is a mosquito, biting fly, bed bug, assassin bug, flea, lice, ant, termite, cockroach, fly, aphid, beetle, thrips, moth, mealybug, or scale insect pest, more preferably a mosquito.

[0027] The term "arachid" has the common understanding of those skilled in the art. Arachnida are described as having a segmented body divided into two regions, with four pairs of legs in the front but no tentacles.

[0028] In one particular implementation, the arachnid is a tick, mite, chigger, or spider, preferably a tick.

[0029] The terms "prevention and control", "arthropod prevention and control", "insect prevention and control" or "arachid prevention and control" have their usual meanings for those skilled in the art.

[0030] In the context of this invention, "controlling" is defined as the ability of the arthropod control composition according to the invention to attract, prevent, kill or repel arthropods, preferably prevent or repel arthropods, and even more preferably repel arthropods.

[0031] According to the invention, “attracting” refers to the ability of the arthropod attractant composition according to the invention to increase or promote the contact or presence of arthropods at a source of arthropod attractant, such as in the air, on the surface of an article, or on a vertebrate such as a human subject or other mammal, preferably on the surface of an article such as a trapping device, to which the arthropod attractant compound or composition has been applied.

[0032] According to the invention, “repellency” is defined as the ability of the arthropod repellent composition according to the invention to minimize, reduce, contain or prevent arthropods from approaching or being present at a source of arthropod repellent, such as in the air, on a surface of an article or on a vertebrate, such as a human subject or other mammal, preferably a human subject, to which the arthropod repellent compound or composition has been applied.

[0033] The term "deterring" according to the invention defines the ability of the arthropod-deterring composition according to the invention to minimize, reduce, contain, or prevent the contact or presence of arthropods at the source of arthropod deterrence, such as in the air, on the surface of an article, or on the surface of a vertebrate, such as a human subject or other mammal, preferably a human subject, to which the arthropod-deterring compound or composition has been applied. Typically, a deterrent effect is observed when used as a feeding deterrent after initial tasting of the arthropod-deterring compound or composition, hindering subsequent food intake or oviposition by the pest.

[0034] The "spatial repellency" of the present invention defines the ability of the arthropod repellent composition according to the invention to minimize, reduce, contain, or prevent arthropods from approaching or being present at a source of arthropod repellency, such as in the air, on the surface of an article, or on the surface of a vertebrate, such as a human subject or other mammal, preferably a human subject, to which the arthropod repellent compound or composition has been applied. Generally, a spatial repellency effect is exhibited when a spatial repellent compound or composition is released, sprayed, dispersed, or diffused in the air or liquid, preventing pests from entering the area where the spatial repellent compound or composition is present. Therefore, the repellency effect occurs from a distance, and the pest does not necessarily come into direct contact with the treated article or organism to be protected.

[0035] The term "killing" according to the invention defines the ability of the arthropod-killing composition according to the invention to kill arthropods at an arthropod-killing source, such as in the air, on a surface of an article, or on a vertebrate, such as a human subject or other mammal, preferably a human subject, to which the arthropod-killing compound or composition has been applied. When the arthropod-killing composition is applied to a plant, animal, or human subject, it is applied in an amount that kills the arthropods but does not kill the subject.

[0036] In one particular embodiment, the arthropod control composition is an arthropod repellent composition, preferably an insect repellent composition, and more preferably a mosquito repellent composition.

[0037] In one particular implementation, the arthropod control source is a surface and / or air near the item, preferably a candle, coil, electric diffuser, wristband, patch, collar, ear patch, clothing, fabric, paper, biochar, cardboard, cellulose mat, mosquito net, screen, curtain, furniture, wall, floor or paint, or the surface of a subject, preferably a vertebrate surface, such as a human subject or other mammal, preferably a human subject, i.e. a human subject whose skin has been treated with products such as sprays, aerosols, creams, roll-ons, wristbands, lotions, soaps, shampoos, sunscreens or patches, or clothing treated with products such as laundry detergent, liquid detergent, sprays, lotions, powders, etc.

[0038] The arthropod control effect according to the present invention is achieved by using T, Kessler S, Frei J, Bourquin M, Guerin PM. An in vitro assay for testing mosquito controlling compounds employing a warm body and carbon dioxide as a behavioral activator. J Am Mosq Control Assoc. 2010; 26:381-386. The thermophysical assay (adjusted) is used to test mosquitoes.

[0039] The control efficacy, repellency, and spatial repellency of the present invention were determined by thermophysical experiments against the yellow fever mosquito (Aedes aegypti, Rockefeller strain). Aedes aegypti is a model organism used for control testing and is one of the model organisms recommended by the World Health Organization (WHO) because it is a highly aggressive, human-friendly mosquito species that typically shows low sensitivity to arthropod control compounds. Control efficacy was observed in host-seeking females of the same age (5 to 10 days old) selected as mentioned in the publications mentioned above. The tested starved females were provided with a 10% sugar solution but did not ingest blood. Further information is provided in the appended examples.

[0040] The published protocol has been modified to automatically count mosquitoes instead of manually counting them. Switching from Anopheles gambiae to Aedes aegypti resulted in a reduction in the number of mosquitoes placed in the test cages. This was due to the size difference (e.g., 30 mosquitoes instead of 50) and the increased lighting (i.e., 150 lux instead of 4 lux) because Aedes aegypti is a diurnal mosquito. Further information is provided in the accompanying examples.

[0041] The efficacy, repellency, and spatial repellency of the present invention were also determined using the cage arm method, adapted from the WHO guidelines for testing the efficacy of human skin repellents (WHO / CDS / NTD / WHOPES / 2009.4). The efficacy was evaluated by comparing untreated and treated arms inserted into a cage (40×40×40cm) three times for 30 seconds (negative control). Further information is provided in the appended examples.

[0042] use The in vitro thermometer assay protocol, as defined in T, Bourquin M, Guerin PM, 2013, "A standardized in vivo and invitro test method for evaluating tick repellents," Pestic. Biochem. Phys. 107(2):160-168, evaluates the activity of substances used to repel ticks and other arachnids. Further information is provided in the accompanying examples.

[0043] In one particular embodiment, the amount and selection of the substance are carried out in a manner that contributes to, enhances, or improves both the arthropod analgesic activity and the pleasurable properties of the composition.

[0044] In one embodiment, the arthropod control composition may further comprise an arthropod control adjuvant. "Arthropod control adjuvant" is understood to mean an ingredient that imparts additional arthropod control benefits to the arthropod control effect of the compositions described herein.

[0045] In one embodiment, the substances described herein can, for example, improve, enhance, or enhance the arthropod control efficacy of the arthropod control adjuvant by reducing the amount of the adjuvant in the composition. This may be particularly beneficial where the arthropod control adjuvant is harmful to human subjects at certain doses or where the adjuvant has negative olfactory properties at certain doses.

[0046] According to a specific implementation scheme, the combination of the substances described herein with arthropod control adjuvants produces a synergistic arthropod control effect.

[0047] According to one particular embodiment, the combination of the substances described herein with arthropod prophylactic agents results in a modified, pleasant, enhanced, or improved olfactory impression of the entire composition, compared to a single component.

[0048] According to one embodiment, the arthropod control adjuvant is selected from: N,N-diethyl-3-methylbenzamide (DEET), ethyl butylacetylaminopropionate (IR3535), p-menthane-3,8-diol (PMD), 1-(1-methylpropoxycarbonyl)-2-(2-hydroxyethyl)piperidine (Icaridin), cedarwood oil (China), cedarwood oil (Texas), cedarwood oil (Virginia), cinnamon oil, citronella oil, corn peppermint oil, fractionated hydrated cyclized Cymbopogon winterianus oil, decanoic acid, Eucalyptus citriodora oil, hydrated cyclized Eucalyptus citriodora oil, eugenol, garlic oil, geraniol, geranium oil, lavender, and lavender styrax. Hybrida extract, Lavandin oil, Lemon oil, Lemongrass oil, Margosa extract, Metofluthrin, a mixture of cis- and trans-p-menthane-3,8-diol, N,N-diethyl-m-toluamide, Nonanoic acid, Rosemary oil, Thyme oil, Wintergreen oil, 2,3,4,5-bis(butyl-2-ene)tetrahydrofurfural (MGKRepellent) 11) Eucalyptol, cinnamaldehyde, citronellol, citronellol, coumarin, dibutyl phthalate, diethyl phthalate, dimethyl anthranilate, dimethyl phthalate, ethyl vanillin, eucalyptus oil, δ-octanolactone, δ-nonanolactone, δ-decanolactone, δ-undecanolactone, δ-dodecanolactone, γ-octanolactone, γ-nonanolactone, γ-decanolactone, γ-undecanolactone, γ-dodecanolactone, hydroxycitronellol, lime oil, limonene, linalool, methyl anthranilate, peppermint oil, myrcene, neem oil, juniperene, β-carnation Alkene, (1H-indol-2-yl)acetic acid, anethole, anise oil, basil oil, bay leaf oil, camphor, ethyl salicylate, evergreen oil (pine oil), (1R-trans)-2,2-dimethyl-3-(2-methylprop-1-enyl)cyclopropanecarboxylic acid (1,3,4,5,6,7-hexahydro-1,3-dioxo-2H-isoindol-2-yl)methyl ester (d-tetramethrin), (RS)-3-allyl-2-methyl-4-oxocyclopentan-2-enyl-(1R,3R;1R,3S)-2,2-dimethyl-3-(2-methylprop-1-enyl)-cyclopropanecarboxylate (a mixture of four isomers: 1R trans, 1R:1R trans, 1S:1R cis, 1R:1R cis, 1S 4:4:1:1)(d-Allethrin), (RS)-α-cyano-3-phenoxybenzyl-(1RS)-cis,trans-3-(2,2-dichlorovinyl)-2,2-dimethylcyclopropanecarboxylate (Cypermethrin), 2,2-dimethyl-3-(2-methylprop-1-enyl)cyclopropanecarboxylate 2-methyl-4-oxo-3-(prop-2-ynyl)cyclopent-2-en-1-yl ester (Prallethrin), Acetamiprid, Azadirachtin, Bendiocalb, Bifenthrin Boric acid, chlorpyrifos, deltamethrin, diazinon, dichlorvos, eugenol, fipronil, imidacloprid, linalool, malathion, maltodextrin, metofluthrin, nicotine, permethrin, pyrethroids and pyrethroids, rotenone, silica (diatomaceous earth), s-methoprene, spinosad (Spinosyn A), spinosad D, tetramethrin, transfluthrin, and mixtures thereof.

[0049] In one particular embodiment, the content of the arthropod control adjuvant ingredient is 0.02 to 80% by weight, more preferably 0.05 to 70% by weight, and even more preferably 0.1 to 60% by weight, based on the total weight of the composition. Therefore, it should be understood that the minimum amount of the arthropod control adjuvant ingredient contained in the composition is at least 0.2% by weight, at least 0.05% by weight, or at least 0.1% by weight, and the maximum amount is no more than 80% by weight, no more than 70% by weight, or no more than 60% by weight, based on the total weight of the composition.

[0050] In one particular embodiment, within the limits of the amounts of substances in the composition as described above, the substances and arthropod control adjuvants in the composition of the present invention are included in the composition in a weight range of 90:10 to 10:90, preferably 80:20 to 20:80, more preferably 65:35 to 35:65, and most preferably 60:40 to 40:60. It should also be understood herein that the substances and arthropod control adjuvants can be included in the composition in any combination of weight ranges as described above, for example, 90:10 to 20:80, preferably 35:65, and more preferably 40:60; 80:20 to 10:90, preferably 35:65, and more preferably 40:60; 65:35 to 10:90, preferably 20:80, and more preferably 40:60; or 40:60 to 10:90, preferably 20:80, and more preferably 35:65.

[0051] In one embodiment, the arthropod control composition may further comprise a fragrance component. The fragrance component is understood to contribute to, modify, enhance, or improve the olfactory characteristics of the composition, but not to contribute to, enhance, or improve the arthropod control efficacy of the composition.

[0052] Arthropod control compositions may also include a carrier. By "carrier," it should be understood as a material in which the active compound is mixed or formulated to facilitate its application at the treatment site or on other objects, or its storage, transport, and / or treatment. The carrier may be inorganic, organic, or synthetically derived from natural sources. The carrier may be liquid or solid.

[0053] As liquid carriers, emulsion systems, i.e., solvent and surfactant systems, or solvents commonly used in fragrances, can be listed as non-limiting examples. Detailed descriptions of the properties and types of solvents are generally not exhaustive. However, solvents such as butanediol or propylene glycol, glycerol, dipropylene glycol and its monoethers, 1,2,3-propanetriyltriacetate, dimethyl glutarate, dimethyl adipate, 1,3-diacetoxypropyl-2-yl acetate, diethyl phthalate, isopropyl myristate, benzyl benzoate, benzyl alcohol, 2-(2-ethoxyethoxy)-1-ethanol, triethyl citrate, 2-methylprop-1-ene and 2-(2-ethoxyethoxy)ethanol or mixtures thereof are particularly suitable, with dipropylene glycol, 2-methylprop-1-ene and 2-(2-ethoxyethoxy)ethanol and mixtures thereof being particularly suitable.

[0054] For compositions that also contain a carrier, in addition to the carriers described in detail above, other suitable carriers may be ethanol, water / ethanol mixtures, limonene or other terpenes, isoparaffins, such as those marketed under trademarks. Those known to the public (source: Exxon Chemical), or glycol ethers and glycol ether esters, such as those marketed under trademarks Those commonly known (source: Dow Chemical Company), or hydrogenated castor oil, such as those marketed as trademarks... Those well-known figures in RH 40 (Source: BASF).

[0055] A solid carrier is a material to which arthropod control compositions or certain elements thereof can be chemically or physically bonded. Typically, such solid carriers are used to stabilize compositions or control the evaporation rate of compositions or certain components. Solid carriers are currently used in the art, and those skilled in the art know how to achieve the desired effects. However, as non-limiting examples of solid carriers, absorbent adhesives or polymers or inorganic materials, such as porous polymers, cyclodextrins, wood-based materials, organic or inorganic gels, clay, gypsum, talc, or zeolite, can be listed.

[0056] Other non-limiting examples of solid carriers include encapsulating materials. Examples of such materials may include wall-forming and plasticizing materials, such as monosaccharides, disaccharides, or trisaccharides, natural or modified starches, hydrocolloids, cellulose derivatives, polyvinyl acetate, polyvinyl alcohol, proteins, or pectins, or as described in references such as H. Scherz, Hydrokolloide: Stabilisatoren, Dickungs- und Geliermittel in Lebensmitteln, Band 2der Schriftenreihe Lebensmittelchemie, The materials listed in Behr's Verlag GmbH & Co., Hamburg, 1996. Encapsulation is a method well known to those skilled in the art and can be carried out, for example, by using techniques such as spray drying, agglomeration, or extrusion; or by encapsulation of coatings including agglomeration and composite agglomeration techniques.

[0057] As a non-limiting example of a solid carrier, a core-shell capsule may be specifically cited, which uses resins of the type of amino plastics, polyamides, polyesters, polyureas, or polyurethanes, or mixtures thereof (all of which are well known to those skilled in the art), and is carried out by a phase separation method initiated by using techniques such as polymerization, interfacial polymerization, coagulation, or these techniques together (all of which have been described in the prior art), and optionally in the presence of a polymer stabilizer or a cationic copolymer.

[0058] Resins can be produced by polycondensation of aldehydes (e.g., formaldehyde, 2,2-dimethoxyacetaldehyde, glyoxal, glyoxylic acid, or hydroxyacetaldehyde and mixtures thereof) with amines such as urea, benzoguanamine, glycyrrhizin, melamine, hydroxymethyl melamine, methylated hydroxymethyl melamine, guanidine, etc., and mixtures thereof. Alternatively, pre-formed resins can be used to alkylate polyamines, for example, under trademarks... (Source: Cytec Technology Corp.) (Source: Cytec Technology Corp.) or (Source: BASF) Those that are commercially available.

[0059] Other resins are produced by the formation of trimers from polyols such as glycerol and polyisocyanates such as hexamethylene diisocyanate, isophorone diisocyanate, or phenyl diisocyanate, or biuret of hexamethylene diisocyanate, or trimers of phenyl diisocyanate and trimethylolpropane (as trade name). Those produced by the condensation polymerization of known sources (Mitsui Chemicals), wherein preferably, the trimer of phenyl diisocyanate with trimethylolpropane and the biuret of hexamethylene diisocyanate.

[0060] Some research literature relating to the encapsulation of fragrances via the condensation of melamine resins with aldehydes includes articles such as those by K. Dietrich et al., Acta Polymerica, 1989, vol. 40, pages 243, 325, and 683, and 1990, vol. 41, page 91. These articles have described various parameters affecting the preparation of such core-shell microcapsules according to prior art methods, which are further detailed and exemplified in patent literature. Wiggins Teape Group Limited's US 4'396'670 is a relevant early example of the latter. Since then, many other authors have enriched the literature in this field, and it is impossible to cover all published advances here, but general knowledge of encapsulation techniques is essential. More recent targeted publications also address suitable uses of such microcapsules, such as the article by HY Lee et al., Journal of Microencapsulation, 2002, vol. 19, pages 559-569, and International Patent Publication WO01 / 41915 or S. The article by Chimia et al., 2011, vol. 65, pages 177-181, is representative.

[0061] The present invention also relates to a method for the control of preferred arthropod insects, the method comprising bringing the preferred arthropod insects into direct contact with the above composition or into contact with the vapor of the above composition.

[0062] For clarity, the arthropod control composition of the present invention can be applied to the air, the surface of an article, the air near the surface of an article, or the surface of a subject by conventional methods known in the art, such as spraying, smearing, wearing, or spreading.

[0063] In one particular embodiment, the arthropod control composition according to the invention is applied to the surface of an article, to the air near the surface of the article, or to the surface of an animal or subject.

[0064] In one particular implementation, the article may be an arthropod control article as described below, and specifically may be a candle, coil, electric diffuser, wristband, patch, collar, ear patch, clothing, fabric, paper, biochar, cardboard, cellulose mat, mosquito net, screen, curtain, furniture, paint, wall, floor, spray, aerosol, cream, roll-on, wristband, lotion, soap, shampoo, sunscreen, laundry detergent, liquid detergent, spray, lotion, powder.

[0065] In one particular implementation, the subject's surface is the surface of a human or animal subject, preferably the human subject's skin.

[0066] The present invention also relates to the use of compositions as defined above for the control of arthropods, preferably insects.

[0067] The present invention also relates to arthropod control articles comprising the arthropod control composition as described above.

[0068] The term "arthropod control article" should be understood to refer to a consumer product that provides arthropod control effects to at least the surface or space to which it is applied (e.g., skin, hair, textiles, or household surfaces). In other words, the arthropod control article according to the invention is a consumer product comprising a functional formulation corresponding to the desired consumer product, optional additional beneficial agents, and at least one substance in an arthropod control amount. For clarity, the consumer product is a non-edible product.

[0069] The nature and type of the ingredients of consumer products are not guaranteed to be described in greater detail here, and are in no way exhaustive. Skilled workers can select them based on their common sense and the characteristics of the product and the desired effect.

[0070] Non-restricted examples of suitable consumer products include perfumes, such as perfumes, sprays, or eau de perfumes, colognes, or shaving lotions or aftershaves; fabric care products, such as liquid or solid detergents, laundry powders, fabric softeners, liquid or solid fragrance enhancers, fabric fresheners, ironing solutions, paper products, bleach, carpet cleaners, and curtain care products; body care products, such as hair care products (e.g., shampoos, colorants, or hair sprays, color-correcting products, hair styling products), dental care products, disinfectants, and feminine hygiene products; cosmetic preparations (e.g., skin creams or lotions, cold creams, deodorants, or antiperspirants, such as sprays or roll-ons), depilatories, tanning agents, sunscreens or after-sun products, nail products, skin cleansing products, and cosmetics); or skin care products (e.g., soaps, bath or tub mousse, bath oils or shower gels, or hygiene products or foot / hand care products); and air fresheners. Products, such as air fresheners or "ready-to-use" powder air fresheners, which can be used in home spaces (rooms, refrigerators, cabinets, shoes, or cars) and / or public spaces (lobby, hotels, shopping malls, etc.); or home care products, such as mold removers, furniture care products, wipes, dishwashing liquids, or hard surface cleaners (e.g., floor, bathroom, sanitary ware, or window cleaners); leather care products; car care products, such as polishes, waxes, or plastic cleaners; candles; sprayers, coils, electric diffusers, diffusers, rubber diaphragms, wristbands, patches, collars, earplugs, clothing, fabrics, paper, biochar, cardboard, cellulose mats, mosquito nets, screens, curtains, varnishes, or coatings, more preferably candles, sprayers, coils, electric diffusers, diffusers, rubber diaphragms, wristbands, patches, collars, earplugs, clothing, fabrics, paper, biochar, cardboard, cellulose mats, mosquito nets, screens, curtains, varnishes, or coatings.

[0071] In a preferred embodiment of the invention, the consumer product is an electro-diffuser. In this embodiment of the invention, the substance in the arthropod-preferably insect control composition is present in a certain amount.

[0072] Therefore, if the consumer product is an electro-diffuser, the substance is selected from: (2E)-3,7-dimethyloctyl-2,6-dienal; benzopyran-2-one; 2-methoxy-4-[(E)-prop-1-enyl]phenol; (5R)-2-methyl-5-prop-1-en-2-ylcyclohex-2-en-1-one; (4-methoxyphenyl)methyl acetate; 2-methyl-3-(4-propane-2-ylphenyl)propanal; (4-methoxyphenyl)methanol; 2-phenylethanol; 4-hydroxy-3-methoxybenzaldehyde; spearmint oil; clove oil; 5-pentyloxacyclopentan-2-one; (1S,6R)-3,7,7-trimethylbicyclo[4.1.0]hept-3-ene; (4-methoxyphenyl)methyl acetate; 2-phenylethyl 2-methylpropionic acid.

[0073] Furthermore, if the consumer product is an electro-diffuser, the following amounts are preferred, expressed as a percentage of the total diffuser liquid: (2E)-3,7-dimethyloct-2,6-dienal, 100% or less; benzopyran-2-one, 33% or less; 2-methoxy-4-[(E)-prop-1-enyl]phenol, 100% or less; (5R)-2-methyl-5-prop-1-en-2-ylcyclohex-2-en-1-one, 16.9% or less; (4-methoxyphenyl)methyl acetate, 20% or less; 2-methyl-3-(4-propane-2-yl) (Phenyl)propionaldehyde, 15.6% or less; (4-methoxyphenyl)methanol, 13.8% or less; 2-phenylethanol, 20% or less; 4-hydroxy-3-methoxybenzaldehyde, 20% or less; spearmint oil, 9% or less; clove oil, 9% or less; 5-pentyloxetane-2-one, 20% or less; (1S,6R)-3,7,7-trimethylbicyclo[4.1.0]hept-3-ene, 20% or less; (4-methoxyphenyl)methyl acetate, 20% or less; 2-phenylethyl 2-methylpropionate, 20% or less.

[0074] Some of the aforementioned consumer products may represent corrosive media of members of the flavoring ingredient family, and therefore may need to be protected from premature degradation, for example by encapsulation or by chemically binding them to another chemical substance that is suitable for releasing the ingredients of the present invention when subjected to suitable external stimuli, such as enzymes, light, heat or pH changes.

[0075] Example

[0076] The invention will be described in more detail through the following embodiments.

[0077] 1. Description of arthropod control experiments

[0078] Arthropod rejection was tested using the in vitro and in vivo testing methods described herein.

[0079] 1.1. External thermobody test of insects such as mosquitoes

[0080] Aedes aegypti is a model organism used for control testing and is one of the model organisms recommended by the World Health Organization (WHO) because it is a highly aggressive, blood-feeding mosquito species that is generally less sensitive to arthropod control compounds.

[0081] use T, Bourquin M, Guerin PM, 2010. An in vitro assay for testing mosquito controlling compounds employing a warm body and carbon dioxide as a behavioral activator. J Am Mosq Control Assoc. 26:381-386. The thermophysical test (adapted) as defined in the J Am Mosq Control Assoc. 26:381-386 evaluates the repellency effect of the compositions according to the invention. In this in vitro test, the number of mosquitoes landing on the test thermophysical body (warm body) is measured, simulating an attractive host treated with the test stimulus, to evaluate the repellency effect.

[0082] The published protocol has been adjusted to automatically count mosquitoes instead of manually counting them. Switching from Anopheles gambiae to Aedes aegypti resulted in a reduction in the number of mosquitoes placed in the test cages due to the size difference (i.e., 30 mosquitoes instead of 50) and the increased lighting (i.e., 150 lux instead of 4 lux) because Aedes aegypti is a diurnal mosquito.

[0083] Furthermore, because the inventors were interested in evaluating the spatial repellency with or without increased deterrent effect, two different techniques were used to apply the substance. Whether as... As described by et al. (2010), the blocking and repelling effects (i.e., effects similar to most body care applications such as lotions) were studied by applying these substances to sandblasted glass petri dishes placed on warm bodies. Alternatively, spatial repellency (i.e., effects similar to most home care applications such as electric liquid dispensers) was investigated, and these substances were introduced into the cage space using the forced evaporation system described in Chappuis C JF, Niclass Y, Vuilleumier C, Starkenmann C. 2015. Quantitative Headspace Analysis of Selected Odorants from Latrines in Africa and India. Environ. Sci. Technol. 49:6134-6140.

[0084] As As described by [Authors' Name] (2010), starved females aged 10 to 12 days, who could freely consume a 10% sugar solution but did not ingest blood, were selected for the experiment. For each test substance, at least three different concentrations were evaluated, ranging from 0.0016% to 1% in ethanol for deterrence and repellency assessment, and from 0.001 mg / mL to 100 mg / mL in propylene glycol for space repellency.

[0085] 1.2. Insect, such as mosquito, internal cage arm test

[0086] The cage-in-arm method was adapted from the WHO guidelines for testing the efficacy of mosquito repellents on human skin (WHO / CDS / NTD / WHOPES / 2009.4). The detection activity was determined by inserting an untreated arm into a cage (40×40×40cm) for 30 seconds three times (once at the start, once at the fourth hour, and once at the eighth hour) to assess the readiness of detection in 100 starved female Aedes aegypti mosquitoes. The product was then applied to the forearm skin of human volunteers (1 ml / 600cm). 2 After 5 minutes, the arm was inserted into the cage and exposed for 3 minutes. The determination was performed on three different volunteers in a temperature (27±2℃) and humidity (80±10%RH) regulated chamber.

[0087] 1.3. External thermoplate test of arachnids such as ticks

[0088] To evaluate the repellency efficacy of different substances against sheep tick, *Ixodes ricinus* L., one of the recommended model organisms mentioned in the Guidance on the European Biological Products Regulation [Vol II, Efficacy-Assessment & Evaluation (Parts B+C), v.3.0, April 2018]. The repellency efficacy was observed in the final stages of nymphal repellency.

[0089] use T, Bourquin M, Guerin PM. 2013. A standardized in vivo and invitro test method for evaluating tick repellents. Pestic. Biochem. Phys. 107(2):160–168. The in vitro thermometer test protocol is used to evaluate repellent efficacy.

[0090] 2. Evaluation of the arthropod control efficacy of the present invention

[0091] 2.1. Results of ectothermometry tests on insects such as mosquitoes

[0092] 2.1.1. In vitro test results of blocking and spatial avoidance

[0093] Covering the warm body (28.3cm) 2 100 μL of the substance diluted in ethanol at different concentrations was added to a sandblasted glass culture dish. The number of mosquitoes landing on the body was counted for each stimulus, with N,N-diethyl-3-methylbenzamide (DEET) and ethyl 3-[acetyl(butyl)amino]propionate (IR3535) used as baselines, and pure ethanol used as a control.

[0094] All tested substances caused a significant reduction in mosquito falls associated with increasing dosage. At a concentration of 0.04%, two substances (benzopyran-2-one and 4-hydroxy-3-methoxybenzaldehyde) achieved similar numbers of falls to DEET, totaling less than 10 falls. At this 0.04% concentration, all other tested substances were as effective as the second benchmark IR3535, with approximately 10 falls per minute (Table 1). At higher concentrations of 1%, all seven tested substances showed similar but lower mosquito falls to DEET than IR3535, with fewer than 2 mosquitoes falling per minute (Table 1).

[0095]

[0096] Table 1: Number of mosquitoes landing on bodies treated with different concentrations of different substances within 2 minutes. The test using only ethanol (control) resulted in 59.3 ± 6.9 mosquito landings.

[0097] All tested substances caused a significant reduction in mosquito falls associated with increasing dosage. At a concentration of 0.04%, two substances (4-vinyl-2-methoxyphenol and (3Z)-3-butylidene-2-benzofuran-1-one) achieved similar numbers of falls to DEET, totaling less than 10 falls. At this 0.04% concentration, most other tested substances were as effective as the second benchmark IR3535, with approximately 10 falls per minute (Table 2). At higher concentrations of 1%, six of the eight substances tested showed similar but lower mosquito falls to DEET than IR3535, with fewer than 3 mosquitoes falling per minute (Table 2).

[0098]

[0099] Table 2: Number of mosquitoes landing on bodies treated with different concentrations of different substances within 2 minutes. The test using only ethanol (control) resulted in 67.1 ± 9.1 mosquito landings.

[0100] All tested substances caused a significant reduction in fall rates associated with increasing dosage. At a concentration of 0.04%, three substances (methyl 2-(3-oxo-2-pent-2-enylcyclopentyl)acetate, 6-pentyloxetane-2-one, and 3,4,4a,5,6,7,8,8a-octahydrobenzopyran-2-one) achieved similar fall rates to DEET, totaling less than 10 fall rates. At the same 0.04% concentration, three other stimulants (2-methoxy-4-[(E)-prop-1-enyl]phenol, (4R)-4-(2-methoxypropane-2-yl)-1-methylcyclohexene) and clove oil achieved similar fall rates to IR3535, approximately 10 fall rates per minute (Table 3). At higher concentrations of 1%, nine of the 12 substances tested showed similar but lower mosquito landing rates to DEET, less than three mosquitoes per minute. 3,7,7-trimethylbicyclo[4.1.0]hept-3-ene and methyl acetate (4-methoxyphenyl) ester achieved similar repellency results to IR3535 at this 1% concentration, while 1% peppermint oil achieved an 80% reduction in mosquito landings (Table 3).

[0101]

[0102] Table 3: Number of mosquitoes landing on bodies treated with different concentrations of different substances within 2 minutes. The test using only ethanol (control) resulted in 67.0 ± 8.8 mosquito landings.

[0103] As can be seen from the data in Figure 1, similar results were found when the above-mentioned stimulants were tested at additional concentrations.

[0104] 2.1.2. In vitro test results of space avoidance

[0105] The forced evaporation system allowed the cage volume to be filled with the irritant being tested, with 2,2-dimethyl-3-(2-methylprop-1-enyl)cyclopropanecarboxylic acid 2-methyl-4-oxo-3-(prop-2-ynyl)cyclopent-2-en-1-yl ester (pyrethroid) and N,N-diethyl-3-methylbenzamide (DEET) used as baselines. To limit the potential dead volume in the cage, the cage was rinsed five times, followed by a 2-minute test during which the number of mosquito landings was counted.

[0106] Similar to both benchmarks, the efficacy of all substances in preventing landing on the body increased with dose, except for 3,7-dimethyloctyl-2,6-dienal, which reduced landing by approximately 67% at all tested concentrations. A two-thirds reduction in landing was observed in most substances tested at a dose of 0.0017 μg / μL air. For all tested substances, the number of landings decreased to less than five per minute at doses of 1.7 and / or 17 μg / L air (Table 4).

[0107]

[0108] Table 4: Number of mosquitoes landing on the body within 2 minutes when the air in the cage is saturated with irritants. The average number of landings when there are no substances in the cage is 54.7 ± 3.2. Each concentration was repeated n = 1 to 4 times.

[0109] For all substances, the reduction in the number of falls was associated with an increase in the amount of the substance present in the cage air. Four substances (natural connective oil, 4-vinyl-2-methoxyphenol, (E)-1-(2,6,6-trimethylcyclohexyl-2-en-1-yl)but-2-en-1-one, and 6-hexyloxecyclohexane-2-one) successfully fell less than 5 times within 2 minutes at a low dose of 0.17 μg / L in air. Except for 3-butyryl-2-benzofuran-1-one, all other substances achieved a 90% repulsion level at doses of 1.7 and / or 17 μg / L in air. (E)-1-(2,6,6-trimethylcyclohexyl-2-en-1-yl)but-2-en-1-one was particularly effective, exhibiting over 80% repulsion at all five tested concentrations (Table 5).

[0110]

[0111] Table 5: Number of mosquitoes landing on the body within 2 minutes when the air in the cage is saturated with irritants. The average number of landings when there are no substances in the cage is 56.0 ± 3.6. Each concentration was repeated n = 1 to 4 times. nd indicates no measures were taken.

[0112] For all substances, we observed a reduction in fall rates associated with an increase in the amount of the substance present in the cage air. However, for some substances, such as 2-phenylethanol, this reduction was very small, with a 41% reduction in falls at the highest dose tested. In contrast, some substances were very effective, reducing falls by more than 90% at a dose of 0.017 μg / μL. (Table 6)

[0113]

[0114] Table 6: Number of mosquitoes landing on the body within 2 minutes when the air in the cage is saturated with irritants. The average number of landings when there are no substances in the cage is 54.1 ± 4.9. Each concentration was repeated n = 1 to 4 times. nd indicates no action was taken.

[0115] These dose-response interactions can be clearly seen from the data presented in Figure 2.

[0116] 2.2. Results of an experiment on an arm inside a cage containing insects such as mosquitoes

[0117] The cage arm test is a mandatory testing method for most fungicide registrations, used to assess the efficacy of the substance. This is a very challenging test because the treated arm of a volunteer is placed in a cage with a density of 3125 blood-sucking mosquitoes / m². 3 In the air. 20% 4-hydroxy-3-methoxybenzaldehyde was applied to the skin of the arm (600cm) of three different volunteers. 2 At different test times after application (5 minutes, 1 hour, 2 hours, 3 hours and 4 hours, respectively), the percentage of mosquitoes landing on the arm was reduced by 82±5.2%, 78±2.6%, 66±8.0%, 61±6% and 63±2%, respectively.

[0118] Similarly, other compounds also exhibited related repellency effects, particularly 6-pentyloxetane-2-one, which achieved a repellency rate of over 75% for more than 4 hours. Figure 3 (Data provided in China).

[0119] 2.3. Results of external thermoplate tests on arachnids such as ticks

[0120] If ticks exhibit a pre-specified negative geotaxis response in in vitro tests, it indicates that the test substance does not prevent ticks from climbing up to find suitable blood-feeding attachment sites in nature. Therefore, using ethyl 3-[acetyl(butyl)amino]propionate (IR3535) as a baseline and pure ethanol as a control, the average percentage of ticks affected by the three concentrations of the substance diluted in ethanol was measured on 12–24 ticks.

[0121] A clear biodosage response was measured, meaning the number of ticks affected by all substances increased with increasing amounts of the applied substance. The most effective test substances were benzopyran-2-one and 5-pentyloxacyclopentan-2-one, both of which provided responses similar to the baseline IR3535 at all three test concentrations. Even the least effective substance, at the highest tested concentration of 1% (25 μg / cm³), showed a response similar to the baseline IR3535. 2 Under these conditions, the number of ticks climbing up to find foraging sites can be reduced by more than 50% (Table 7).

[0122]

[0123] Table 7: Average percentage of ticks affected by ethanol dilution. In tests using ethanol (control), only 1.0 ± 1.2% of ticks were affected.

[0124] 3-Butylidene-2-benzofuran-1-one exhibited stronger tick repellency than the benchmark compound IR3535; at the lowest tested dose (0.04%), over three-quarters of the ticks were affected, while at the intermediate tested dose (0.2%), all tested ticks were affected and did not seek out feeding sites. All other substances showed dose-responsive efficacy in repelling ticks, achieving a minimum repellency of 50% at a concentration of 1%. 4-Vinyl-2-methoxyphenol at 1% (25 μg / cm³) showed similar repellency. 2 Even at the highest concentration, all tested ticks were successfully prevented from climbing up to find foraging sites (Table 8).

[0125]

[0126] Table 8: Average percentage of ticks affected by ethanol diluent. In tests conducted with ethanol (control), only 4.3 ± 2.1% of ticks were affected.

[0127] Both tested substances reduced the percentage of ticks climbing onto foraging sites. At 0.2% and 1% (5 and 25 μg / cm³, respectively)... 2 At the highest test dose (Table 9), the rejection percentage was similar to that of the baseline IR3535.

[0128]

[0129] Table 9: Average percentage of ticks affected by ethanol dilution. In tests using ethanol (control), only 0.6 ± 0.5% of ticks were affected.

Claims

1. A method for arthropod control, comprising bringing the arthropod into direct contact with an arthropod control composition or into vapor contact with the arthropod control composition, wherein the arthropod control composition comprises 0.04 to 0.2% by weight of (3Z)-3-butanediol-2-benzofuran-1-one, wherein the arthropod is a tick.

2. The use of an arthropod control composition for the control of arthropods, wherein, based on the total weight of the composition, the arthropod control composition comprises 0.04 to 0.2% by weight of (3Z)-3-butanediol-2-benzofuran-1-one, wherein the arthropod is a tick.

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