BRPI1016128B1 - METHOD FOR CONTROL OR REPELLENCE OF BED BUGS, AND USE OF ALKYL KETONES AND CYCLIC KETONES - Google Patents

Abstract

METHOD FOR CONTROL OR REPELLENCE OF BED BUGS, PESTICIDE FORMULATION, ALKYL KETONES AND CYCLIC KETONES AND USE OF SAID COMPOUNDS. The present invention relates to a formulation for the control of bed bugs containing at least one compound selected from the group consisting of alkyl ketones and cyclic ketones in which the total number of carbon atoms in the alkyl ketones and cyclic ketones is 10 to 16 carbon atoms to achieve such control or repellency.

Description

Field of Invention

[001] This patent application claims the priority of US Provisional Patent Application No. 61/214,766 filed April 28, 2009.

[002] The present invention relates to compositions and methods for controlling or repelling bed bugs.

Background of the Invention

[003] There are a series of publications regarding the various characteristics of bed bugs. Read generally "The ecology of the bedbug, Cimex lectularius L." by C. Johnson, 41 Journal of Hygiene 345461 (1942); "Assembling and alerting scents produced by the bedbug, Cimex lectularius L." from H. Levinson et al., 27 Experientia: 102-103 (1971); "Action and composition of the alarm pheromone of the bedbug Cimex lectularius L." of H. Levinson et al., 61 Naturwissenschaften 684-685 (1974); "Structure of sensilla, olfactory perception, and behavior of the bedbug, Cimex lectularius, in response to its alarm pheromone" by H. Levinson et al., 20 Journal of Insect Physiology 1231-1248 (1974); "The physiology and activity of the bedbug (Cimex lectularius) in a natural infestation" by K. Mellanby, 31 Parasitology 200-211 (1939); and "The ability of Rhodnius prolixus (Hemiptera; Reduviidae) to approach a thermal source solely by its infrared radiation" by H. Schmitz et al., 46 Journal of Insect Physiology 745-751 (2000).

[004] Bedbugs feed on human blood. So bed bugs aren't merely unpleasant, they leave unsightly litters on your skin. As much as this is problematic in homes, it is an even more serious problem for hotels and the like. In the case of such commercial rooms, there is a greater chance that outside sources will bring bed bugs into the premises, and if there is an unknown infestation which causes discomfort to customers before discovery, there is a greater risk of customer dissatisfaction and negative publicity. probably leading to a significant worsening of the establishment's reputation in the long term.

[005] Recent data suggest that bed bug (Cimex species) infestations of human homes are growing. At least 92 species of bedbug have been identified around the world, of which at least 16 are found on the continent of North America. In general, bedbugs are parasitic pests that have humans and various domestic animals among their possible hosts. It is believed that bed bug infestations are becoming more problematic now, at least in part, because long-acting residual insecticides are no longer used to keep bed bug populations under control. Furthermore, the increase in international travel and resistance to insecticides have caused bed bug infestations to spread and control with insecticides has become increasingly difficult. In terms of scale, such infestations are of particular concern to hoteliers, cruise ships, trains, day care facilities and the like because of the risk to establishment replication posed by bad advertising and reviews. Other problem areas tend to include nursing homes, military housing, dormitories, hospitals, and various other forms of high-density housing. However, isolated family homes can also be adversely impacted.

[006] There have been attempts to control bed bug infestations by applying chemical insecticides to infected areas and materials (especially mattresses). This approach has some drawbacks. For example, it may expose someone using a treated area or mattress shortly after application to odors or other unwanted characteristics of the chemical pesticide. Furthermore, unless chemicals are used regularly, regardless of whether it is known whether an infestation exists or not (a procedure which would significantly increase costs) those sleeping in an infected area may be bitten before it is known when to begin treatment.

[007] Bedbugs had almost been eradicated by the unrestricted use of potent insecticides such as DDT. However, many of these stronger insecticides have been banned in the US and replaced by weaker insecticides such as pyrethroids. Many bed bugs have become resistant to weaker insecticides. In a study from the University of Kentucky, bed bugs were randomly collected from across the United States. These "wild" bed bugs have been shown to be thousands of times more resistant to pyrethroids than laboratory bed bugs. The other problem with the present use of insecticides is that the broad-spectrum insecticides for cockroaches and ants that are no longer used had a collateral impact on bed bug infestations. Recently, there has been a switch to bait insecticides that have proven effective against cockroaches but allow bed bugs to escape indirect treatment.

[008] The number of bed bug infestations has increased significantly since the beginning of the 21st century. The National Pest Management Association reported a 71% increase in calls for bed bug control from 2000 to 2005. The Steritech Group, a pest control company based in Charlotte, North Carolina, claims that 25% of the 700 hotels they inspected from 2002 to 2006 required bed bug treatment. In 2003, a couple of brothers at a Motel 6 in Chicago won $372,000 in a lawsuit after being bitten by bedbugs during their stay.

[009] With the unrestricted use of DDT in the 40s and 50s, all bed bugs practically disappeared from North America by the middle of the 20th century. Infestations continued to be common in many other parts of the world and in recent years they have reoccurred in North America. The reappearance of bed bugs has brought new challenges to controlling pests without DDT and similarly banned agents.

[010] Another reason for the increase in bed bugs is that pest control services today more often use low-toxicity gel-based pesticides to control cockroaches, the most common pest, rather than residual sprays. When residual sprays designed to kill other insects were still commonly used, their use resulted in a side insecticidal effect on possible bed bug infestations; The gel-based insecticides primarily used today have no effect on bedbugs as they are unable to feed on the baits.

[011] There is, therefore, a demand for effective and safe chemicals to control and repel bed bugs, as well as safe and effective methods of employing such chemicals to control or repel bed bugs.

Summary of the Invention

[012] Safe and effective control or repellency of bed bugs can be carried out with the use of formulations containing at least one compound selected from alkyl ketones and cyclic ketones in which the total number of carbon atoms in the alkyl ketones and cyclic ketones is 10 to 16 carbon atoms. Compounds may be present in several of their isomeric or enantiomeric forms or as mixtures of their isomers or enantiomers. Other aspects of this invention relate to the use of such formulations in various methods for controlling or repelling bed bugs. Among the various methods in which the formulations of this invention can be employed are (1) injecting the formulations into the mattress, either directly or in combination with other ingredients or solvents, (2) placing the formulations on an absorbent material and placing the material absorbent in a sachet and place the sachet containing the formulation in a location such as a mattress, basket, suitcase, linen closet or any other enclosure where bed bugs may be present, (3) prepare "drying sheets" containing the formulations to fixing in places such as mattresses, suitcases, baskets, linen closets or any other enclosure where bed bugs may be present, or in a pile of clean or dirty clothes, (4) placing the formulation in detergent or fabric softener compositions to control bed bugs during the use of these compositions in washing clothes and in sprays or in carpet or floor cleaning products such as those used to treat carpets and furniture, and (5) for topical application of the formulation intended for use on humans or animals, such such as in the form of a lotion, powder, spray, or shampoo.

Detailed Description of the Invention

[013] Safe and effective control or repellency of bed bugs can be carried out with the use of formulations containing at least one compound selected from alkyl ketones or cyclic ketones in which the total number of carbon atoms in the alkyl ketones or cyclic ketones is 10 to 16 carbon atoms. Preferred are alkyl ketones and cyclic ketones containing 12 to 16 carbon atoms, and especially preferred are alkyl ketones and cyclic ketones containing 13 to 16 carbon atoms. As examples of such active compounds for controlling or repelling bed bugs may be mentioned, for example, geranylacetone (6,10-dimethyl-5,9-undecadien-2-one), methyl undecyl ketone (2-tridecanone), geranylcyclopentanone and also known as apritone (2-(3,7-dimethylocta-2,6-dienyl)cyclopentan-1-one), methyl apritone (2-(3,7-dimethyl-2,6-nonadienyl)-cyclopentanone ), velvioneTM (5Z) cyclohexadec-5-ene-1-one, methyl dihydrojasmonate (methyl 3-oxo-2-pentylcyclopenteacetate), octenylcyclopentanone (2-(2-octen-1-yl)- cyclopentanone), methyl decyl ketone (2-dodecanone), nootcatone (4,4a-dimethyl-6-prop-1-en-2-yl-3,4,5,6,7,8-hexahydronaphthalene- 2-one), alpha-ionone (4-(2,6,6-trimethyl-2-cyclohexenyl)-3-buten-2-one), beta ionone (4-(2,6,6- trimethyl-1-cyclohexenyl)-3-buten-2-one), alpha-isomethylionone (3-methyl-4-(2,6,6-trimethyl-2-cyclohexen-1-yl)-3 -buten-2-one), nectarylTM (2-(2-(4-methyl-3-cyclohexen-1-yl) propyl) cyclopentanone), isobutylionone ((E)-5-Methyl-1-( 2,6,6-trimethyl-1-cyclohex-2-enyl) hex-1-en-3-one), isolongifolen-9-one ((1R)-2,2,7,7-tetramethyltricyclo[ 6.2.1.01.6] undec-5-en-4-one) dimethylionone ((E)-2-methyl-1-(2,2,6-trimethyl-1-cyclohex-3-enyl) pent-1 -en-3-one), isolongifolanone (2,2,7,7-tetramethyltricycle [6.2.1.01,6] undecan-5-one), pseudoionone (6,10-dimethyl-3,5,9-undecatrien -2-one), 2-cyclopentylcyclopentanone, methyl nonyl ketone, 2-decen-2-one and l-carvone. Particularly preferred are octenylcyclopentanone, geranylcyclopentanone, methyl apritone, methyl decyl ketone, velvioneTM and other C15-C16 cyclic ketones such as metal undecyl ketone and other C13-C16 metal ketones such as geranylacetone, ionone, isolongifolenone , nootcatone, and methyl dihydrojasmonate. Most preferred are apritone, methyl apritone, methyl undecyl ketone, velvioneTM and other C15-C16 cyclic ketones and methyl dihydrojasmonate.

[014] One of the embodiments of the invention comprises a method for controlling or repelling bed bugs by placing the bed bugs with at least one repellent compound selected from the group consisting of alkyl ketones and cyclic ketones in which the total number of carbon atoms in alkyl ketones and cyclic ketones it is 10 to 16 carbon atoms so that bed bugs come into contact with the vapors of the compound(s). Compounds may be present in any of their isomeric or enantiomeric forms or as a mixture of their isomers or enantiomers. Another embodiment of this invention comprises a method for controlling or repelling bed bugs by allocating to an area suspected of containing bed bugs a formulation containing at least one compound selected from the group containing alkyl ketones and cyclic ketones in which the total number of atoms of carbon in alkyl ketones and cyclic ketones is 10 to 16 carbon atoms so that bed bugs come into contact with the compound(s) or the vapors of the compound(s). Other embodiments of the invention consist of the aforementioned methods in which the formulation is sprayed onto or injected into the mattress. Yet another embodiment of the invention consists of the aforementioned methods in which the formulation is on an absorbent material located in a sachet placed in a suspicious area such as a mattress, basket, suitcase, linen closet or other enclosure where bedbugs may be present. Yet another embodiment of the invention consists of the aforementioned methods such that the formulation is included in a detergent or fabric softener composition. Yet another embodiment of the invention consists of the aforementioned methods such that the formulation is included in a form similar to drying sheets which can be placed on a mattress, basket, suitcase, linen closet or in piles of laundry, including dirty or dirty clothes. clean. Another embodiment of the invention in which the formulation is preferably in the form of a spray or aerosol is for application to or on furniture, fabrics, clothing, footwear, carpets or suitcases (including in public or common areas such as hotels, airport baggage compartments). or other storage facilities to prevent cross-contamination. The formulation can be incorporated into a treatment for protecting luggage, furniture or goods for storage or transportation. square area and are placed in clothes dryers to eliminate static, soften fabrics and impart fragrance. A product similar to such drying sheets can be made using the compounds presented in this invention in place of or in addition to the fragrance. surface area of drying sheets is ideal for promoting rapid volatilization of active ingredients in areas where bed bugs may be present. Yet another embodiment of this invention consists of the use of such formulations in the aforementioned methods such that the formulation is in the form of a powder or as a spray or aerosol, suitable for application to furniture or carpets. Additionally, the aforementioned compound(s) can be incorporated into various household cleaning products for use on carpets, floors, walls, cabinets, furniture and the like, or in products intended for application to humans and animals such as lotions, powders, sprays or shampoos.

[015] The active compound(s) of this invention, the alkyl ketones and cyclic ketones in which the total number of carbon atoms in the alkyl ketones and cyclic ketones is 10 to 18 carbon atoms, can be employed with any suitable carrier material. The compounds in the formulations of this invention can also be used in conjunction with fragrances, detergents, fabric softeners, as well as other pesticides with which they may exhibit other beneficial or synergistic effects.

[016] As used herein, the term "vehicle" refers to a material which may be inorganic or organic and of synthetic or natural origin with which the active compound is mixed or formulated to facilitate its application to the site or to any object to be treated, or the way in which it is stored, transported and/or handled. In general, all materials that can be customarily employed as carriers in pesticide formulations are suitable for use in the present invention. The pesticidal compositions herein can be integrated alone or in the form of mixtures with such solid and/or liquid dispersible carriers. As used herein, the term "vehicles" includes conventional inert pesticide extenders or diluents of the type that may be used in conventional pesticide compositions or formulations, e.g., conventional dispersible pesticide vehicle carriers such as solutions, emulsions, suspensions, emulsifiable concentrates. , sprayable powders, pastes, soluble powders, granules, foams, pastes, tablets, aerosols, natural and synthetic materials impregnated with active compounds, microcapsules, fumigation cartridges, fumigation cans and fumigation coils as well as cold or air nebulization formulations warm.

[017] Examples of conventional vehicle vehicles for use of this invention include, but are not limited to, aerosol propellants which are gaseous at normal temperatures and pressures, such as propane, butane, isobutane and carbon dioxide; inert dispersible liquid diluent vehicles, including inert organic solvents such as aromatic hydrocarbons such as, for example, benzene, toluene, xylene, alkyl naphthalenes, halogenated aromatic hydrocarbons, cycloalkanes, for example, cyclohexane, paraffins, for example, petroleum or fractions of mineral oil, chlorinated aliphatic hydrocarbons such as, for example, methylene chloride, chloroethylenes, alcohols, such as, for example, methanol, ethanol, propanol, butanol, ethylene or propylene glycol, as well as ethers and esters thereof, such as, for example, glycol monomethyl ether, amines such as ethanolamine, amides such as dimethyl formamide, sulfoxides such as dimethyl sulfoxide, acetonitrile, ketones such as acetone, methyl ethyl ketones, methyl isobutyl ketone , cyclohexanone and/or water, as well as inert dispersible finely divided solid carriers such as ground natural minerals such as, for example, kaolins, clays, vermiculite, alumina, silica, chalk, i.e. calcium carbonate, talc, attapulgite, montmorillonite, kieselguhr, and ground synthetic minerals such as highly dispersed silicic acid and silicates such as alkaline silicates.

[018] The formulations of this invention are formulated to provide surface concentrations at the site being treated of 1 mcg (microgram) to 5 mg (milligram) per square inch, or liquid solutions of 0.01% to 10%, or applied directly with force maximum. Topical application can vary from around 0.1% to 100%, preferably in a concentration of 1% to 15%.

[019] The usefulness and effectiveness of the invention is illustrated by, but not limited to, the following examples.

[020] This test was carried out using free insects. Two semicircular filter paper discs with a radius of 9 cm treated with 1 ml of solution to moisten the entire surface (one treated with an acetone solution of the test compound and the other treated only with acetone) were placed on the lid of a Petri dish. Five replicates of ten (10) bedbugs were released in the center of the lids of the Petri dishes with the choice of the one treated with the test compound or the one treated only with acetone. The distribution of bed bugs was recorded at 1, 1, 6 and 24 hours after treatment. Paired t-tests were conducted for each treatment. Whether or not there were statistically significant differences in the number of bed bugs on the treated disks versus the untreated disks. The results for the compounds tested were as presented in the following Table in which the values represent a proportion of the bedbugs in the treated portion of the disc to the total number of bedbugs in both the treated and untreated discs at each indicated second of time. Table

[021] While the exact mechanism that guarantees the superiority of compounds of the invention containing 12 to 16 carbon atoms in relation to compounds of this invention with less than 12 carbon atoms or more than 16 carbon atoms is unknown, it is believed It is believed that the number of carbon atoms is related to the better adaptation of the compounds with the bedbug receptors or binding proteins.

[022] Although the invention has been described here with reference to specific presentations thereof, changes, modifications and variations can be appreciated without departing from the spirit and scope of the inventive concept disclosed herein. In this way, it is intended to cover all these changes, modifications and variations that fall within the spirit and scope of the attached claims.

Claims (9)

1. Method for controlling or repelling bed bugs, characterized by the fact that it comprises placing bed bugs in direct contact or with the vapors of a formulation for controlling bed bugs containing a compound selected from the group consisting of geranylacetone (6,10 -dimethyl-5,9-undecadien-2-one), methyl undecyl ketone (2-tridecanone), geranylcyclopentanone and also known as apritone (2-(3,7-dimethylocta-2,6-dienyl)cyclopentan-1-one ), methyl apritone (2-(3,7-dimethyl-2,6-nonadienyl)-cyclopentanone), (5Z) cyclohexadec-5-ene-1-one, methyl dihydrojasmonate (methyl 3-oxo-2 - pentylcyclopenteacetate), octenylcyclopentanone (2-(2-octen-1-yl)- cyclopentanone), methyl decyl ketone (2-dodecanone), nootcatone (4,4a-dimethyl-6-prop-1-en-2-yl- 3,4,5,6,7,8-hexahydronaphthalen-2-one), alphaionone (4-(2,6,6-trimethyl-2-cyclohexenyl)-3-buten-2-one), alpha-isomethylionone (3-methyl-4-(2,6,6-trimethyl-2-cyclohexen-1-yl)-3-buten-2-one), isobutylionone ((E)-5-methyl-1 -(2,6,6-trimethyl-1-cyclohex-2-enyl)hex- 1-en-3-one), dimethylionone ((E)-2-methyl-1-(2,2,6- trimethyl-1-cyclohex-3-enyl)pent-1-en-3-one), 2-cyclopentylcyclopentanone, and methyl nonyl ketone, excluding methods of treatment or application to the human or animal body. 2. Method according to claim 1, characterized by the fact that the formulation contains methyl undecyl ketone. 3. Method according to claim 1, characterized by the fact that the formulation contains octenylcycloptanone. 4. Method according to claim 1, characterized by the fact that the formulation is sprayed onto or injected into a mattress. 5. Method according to claim 1, characterized in that the formulation is sprayed on or placed on a fabric, furniture, clothing, footwear, carpet or luggage. 6. Method according to claim 1, characterized in that the formulation is incorporated into a detergent, fabric softener, carpet or floor cleaning product. 7. Method according to claim 1, characterized by the fact that the formulation is incorporated into a treatment for protecting luggage, furniture or goods for storage or transport. 8. Method for controlling or repelling bed bugs according to claim 1, characterized by the fact that it comprises placing in an area suspected of containing bed bugs a formulation containing a compound selected from the group consisting of geranylacetone (6,10-dimethyl -5,9-undecadien-2-one), methyl undecyl ketone (2-tridecanone), geranylcyclopentanone and also known as apritone (2-(3,7-dimethylocta-2,6-dienyl)cyclopentan-1-one), methyl apritone (2-(3,7-dimethyl-2,6-nonadienyl)-cyclopentanone), (5Z) cyclohexadec-5-ene-1-one, methyl dihydrojasmonate (methyl 3-oxo-2-pentylcyclopenteacetate ), octenylcyclopentanone (2-(2-octen-1-yl)-cyclopentanone), methyl decyl ketone (2-dodecanone), nootcatone (4,4a-dimethyl-6-prop-1-en-2-yl-3, 4,5,6,7,8-hexahydronaphthalen-2-one), alpha-ionone (4-(2,6,6-trimethyl-2-cyclohexenyl)-3-buten-2-one), alpha-isomethylionone (3-methyl-4-(2,6,6-trimethyl-2-cyclohexen-1-yl)-3-buten-2-one), isobutylionone ((E)-5-methyl-1 -(2,6,6-trimethyl-1-cyclohex-2-enyl)hex- 1-en-3-one), dimethylionone ((E)-2-methyl-1-(2,2,6- trimethyl-1-cyclohex-3-enyl)pent-1-en-3-one), 2-cyclopentylcyclopentanone, and methyl nonyl ketone, so that bedbugs can come into contact with the vapors of the formulation so that they cannot direct contact with the formulated or liquid application method is necessary, excluding methods of treatment or application to the human or animal body. 9. Use of a compound selected from the group consisting of geranylacetone (6,10-dimethyl-5,9-undecadien-2-one), methyl undecyl ketone (2-tridecanone), geranylcyclopentanone and also known as apritone (2- (3,7-dimethylocta-2,6-dienyl)cyclopentan-1-one), methyl apritone (2-(3,7-dimethyl-2,6-nonadienyl)-cyclopentanone), (5Z) cyclohexadec-5 -ene-1-one, methyl dihydrojasmonate (methyl 3-oxo-2-pentylcyclopenteacetate), octenylcyclopentanone (2-(2-octen-1-yl)-cyclopentanone), methyl decyl ketone (2-dodecanone), nootcatone ( 4,4a-dimethyl-6-prop-1-en-2-yl-3,4,5,6,7,8-hexahydronaphthalen-2-one), alphaionone (4-(2,6,6- trimethyl-2-cyclohexenyl)-3-buten-2-one), alpha-isomethylionone (3-methyl-4-(2,6,6-trimethyl-2-cyclohexen-1-yl)-3- buten-2-one), isobutylionone ((E)-5-methyl-1-(2,6,6-trimethyl-1-cyclohex-2-enyl)hex- 1-en-3-one), dimethylionone ((E)-2-methyl-1-(2,2,6-trimethyl-1-cyclohex-3-enyl)pent-1-en-3-one), 2-cyclopentylcyclopentanone, and methyl nonyl ketone, characterized by the fact that it is in the preparation of a pesticide formulation for the control or repellence of bedbugs.