Method for Controlling Mosquitoes

Abstract

The present invention relates to the use of isocycloseram for controlling mosquitoes such as vector mosquitoes of pathogenic diseases and mosquitoes with developed insecticide resistance such as pyrethroid insecticide resistance.

Description

Technical Field

[0001] The present invention relates to the technical field of mosquito control using specific isoxazoline compounds. More specifically, the present invention relates to a method for controlling mosquitoes such as mosquitoes that are vectors of pathogenic diseases, and mosquitoes that have developed insecticide resistance to pyrethroid insecticides each containing a mosquito-killing effective isoxazoline compound.

Background Art

[0002] Mosquito control manages mosquito populations to reduce damage to human health, economy, and enjoyment. Since mosquitoes transmit many diseases such as malaria, mosquito control is an important public health activity worldwide, especially in tropical regions (Wikipedia contributors, “Mosquito control”, Wikipedia).

[0003] In many countries, especially in tropical countries, many infectious diseases (e.g., malaria, dengue fever and yellow fever, lymphatic filariasis, and leishmaniasis) that debilitate and even cause death in humans and animals are transmitted by vector insects. For example, the mosquito parasite, Plasmodium falciparum, is responsible for more than 25% of childhood mortality outside the neonatal period. In certain regions of Africa, malaria is ranked first by the World Bank in terms of disability-adjusted life years lost. Many drugs are available for the treatment and / or prevention of some insect-borne diseases. However, not all diseases transmitted by mosquitoes can be treated efficiently. For example, there are currently no chemotherapeutic agents or vaccines against dengue virus. Furthermore, in the case of antimalarial drugs, treatment with currently available drugs has become less effective due to increased resistance in some Plasmodium strains. Plasmodium enters the human bloodstream as a result of a mosquito bite and causes malaria. Therefore, one of the most effective ways to prevent vector-borne diseases is to reduce the mosquito population in highly pathogen-transmitting areas and / or first prevent mosquitoes from biting. More recently, efforts have been concentrated on the control of disease-transmitting mosquitoes.

[0004] Three medically important genera of insects that transmit diseases are the Anopheles, Culex, and Aedes genera. The Culex and Aedes genera belong to the Culicinae subfamily, and the Anopheles genus belongs to the Anophelinae subfamily. Examples of diseases or pathogens transmitted by important mosquitoes are: Anopheles: malaria, filariasis; Culex: Japanese encephalitis, other viral diseases, filariasis; and Aedes: yellow fever, dengue fever, chikungunya, other viral diseases (e.g., Zika virus), and filariasis.

[0005] In attempts to reduce the problems associated with disease - transmitting mosquitoes, a wide range of insecticides and insect repellents have been developed. When mosquitoes are in the larval state or have developed into adults, they can be targeted with insecticides. Thus, insecticides used to kill larvae are called larvicides, while those used to specifically target adults are called adulticides. Most of the insecticides commonly used to prevent disease transmission are targeted at adult mosquitoes, especially female adult mosquitoes.

[0006] The organochlorine DDT was the most widespread compound used as an adulticide worldwide until its use was discontinued in most regions. Subsequently, organophosphates such as malathion, carbamates, and propoxur were widely used in vector control programs in most parts of the world, and pyrethroids, which became the most used adulticides, gradually replaced them. Due to the development of pyrethroid resistance in many important vector species, organophosphates such as pirimiphos - methyl are now being used again.

[0007] As with its predecessors, one of the most important problems associated with pyrethroids is that resistance has already developed in many insect species in several regions of the world. Pyrethroid resistance, caused by either specific detoxifying enzymes or altered target - site mechanisms (kdr - type mutations in sodium channels), has been reported in most countries in most of the medically important mosquito species such as the African Anopheles gambiae and the Asian Aedes aegypti. If resistance continues to develop and spread at its current rate, in the not - too - distant future, such insecticides in their current form may become ineffective. Since there are still no clear alternatives to many of the uses of pyrethroids, such a scenario would potentially have devastating consequences from a public health perspective.

[0008] Therefore, research on insecticides against mosquitoes, especially those resistant to pyrethroids, is ongoing.

[0009] Certain isoxazoline derivatives having insecticidal properties are disclosed, for example, in International Publication No. WO 2011 / 067272. A specific isoxazoline having insecticidal properties is isocycloseram.

[0010] Isoocycloseram is an insecticidal pesticide with the following CAS number: 2061933-85-3 and has the chemical formula (I):

Chemical formula

[0011] Isocycloseram may include the isomer (5S,4R) which is 4-[(5S)-5-(3,5-dichloro-4-fluorophenyl)-5-(trifluoromethyl)-4H-isoxazol-3-yl]-N-[(4R)-2-ethyl-3-oxoisoxazolidin-4-yl]-2-methyl-benzamide (CAS No. 1309959-62-3), optionally at least one of the isomers selected from the group consisting of the isomer (5S,4S), the isomer (5R,4R), and the isomer (5R,4S), and any combination thereof. In the present invention, the isomer (5S,4S) is 4-[(5S)-5-(3,5-dichloro-4-fluorophenyl)-5-(trifluoromethyl)-4H-isoxazol-3-yl]-N-[(4S)-2-ethyl-3-oxoisoxazolidin-4-yl]-2-methyl-benzamide; the isomer (5R,4R) is 4-[(5R)-5-(3,5-dichloro-4-fluorophenyl)-5-(trifluoromethyl)-4H-isoxazol-3-yl]-N-[(4R)-2-ethyl-3-oxoisoxazolidin-4-yl]-2-methyl-benzamide; and the isomer (5R,4S) is 4-[(5R)-5-(3,5-dichloro-4-fluorophenyl)-5-(trifluoromethyl)-4H-isoxazol-3-yl]-N-[(4S)-2-ethyl-3-oxoisoxazolidin-4-yl]-2-methyl-benzamide. When isocycloseram further includes at least one of the isomers selected from the group consisting of the isomer (5S,4S), the isomer (5R,4R), and the isomer (5R,4S), and any combination thereof, isocycloseram may contain the isomer (5S,4R) in a molar ratio of more than 50%, for example, at least 55%, 60%, 65%, 70%, 75%, 80%, 85%, 90%, 95%, 96%, 97%, 98% or 99% based on the total amount of the isomers (5S,4R), (5S,4S), (5R,4R) and (5R,4S).

[0012] Isocycloseram has been found to be particularly suitable for pathogenic disease vector mosquitoes and mosquitoes resistant to insecticides such as pyrethroids. SUMMARY OF THE INVENTION

Means for Solving the Problem

[0013] Accordingly, the present invention provides a method for controlling nuisance, disease - transmitting, or pyrethroid - resistant mosquito pests, which comprises applying an insecticidally effective amount of isocycloseram to such mosquito pests or to a location where such control is desired.

[0014] In addition to the biological effectiveness of isocycloseram against mosquitoes and resistant strains of such mosquitoes, other embodiments of the present invention relate to its safety to the environment (its toxicity, persistence), such as for users of vector control solutions; its suitability for manufacturing vector control solution products (indoor residual spray formulations, mosquito nets, or other types), its suitability for adhesion to and availability on surfaces over time (when the solution is an indoor residual spray), the ease with which the compound is available for controlling mosquitoes on the surface of a net over time, and the ability of the net to withstand multiple washings, including its suitability for incorporation into polymer products (such as nets).

[0015] In one embodiment, according to the present invention, a method for controlling nuisance, disease - transmitting, or insecticide - resistant mosquito pests, particularly pyrethroid - insecticide - resistant mosquito pests, includes methods for controlling, limiting, or eradicating mosquito pests that transmit pathogens of diseases.

[0016] In one embodiment, the method and the isocycloseram according to other aspects of the present invention are particularly useful for controlling mosquitoes that are vectors of disease pathogens or that transmit disease pathogens, and more particularly mosquitoes that are insecticide resistant, such as pyrethroid insecticide resistant, selected from the genera Anopheles, Culex, and Aedes. Examples include Aedes aegypti, Aedes albopictus, Aedes japonicas, Aedes vexans, Coquillettidia perturbans, Culex molestus, Culex pallens, Culex pipiens, Culex quinquefasciatus, Culex restuans, Culex tarsalis, Anopheles albimanus, Anopheles albitarsis, Anopheles annularis, Anopheles aquasalis, Anopheles arabiensis, Anopheles aconitus, Anopheles atroparvus, Anopheles balabacensis, Anopheles coluzzii, Anopheles culicifacies, Anopheles darlingi, Anopheles dirus, Anopheles farauti, Anopheles flavirostris, Anopheles flaviatilis (Anophelesfluviatilis), Anopheles freeborni, Anopheles funestus, Anopheles gambiae s.l., Anopheles koliensis, Anopheles labranchiae, Anopheles lesteri, Anopheles leucosphyrus, Anopheles maculatus, Anopheles marajoara, Anopheles melas, Anopheles merus, Anopheles messeae, Anopheles minimus, Anopheles moucheti, Anopheles nili, Anopheles nuneztovari, Anopheles plumbeus, Anopheles pseudopunctipennis, Anopheles punctipennis, Anopheles punctulatus, Anopheles quadrimaculatus, Anopheles sacharovi, Anopheles sergentii, Anopheles sinensis, Anopheles stephensi, Anopheles subpictus, Anopheles sundaicus, Anophelessuperpictus), and Mansonia titillans, Ochlerotatus stimulans, Ochlerotatus japonicas (each an example of a mosquito capable of carrying or transmitting a pathogenic disease) are mentioned.

[0017] Control means being used in a way to kill or repel mosquitoes so that bites do not occur, or to reduce the mosquito population so that bites do not occur frequently, or to inhibit the target mosquitoes from sucking blood.

[0018] In another embodiment, isocycloseram is useful for controlling one or more species of mosquitoes selected from the genus Anopheles, Culex, and Aedes, particularly Aedes aegypti, Aedes albopictus, Aedes japonicas, Aedes vexans, Culex molestus, Culex pallens, Culex pipiens, Culex quinquefasciatus, Culex restuans, Culex tarsalis, Anopheles albimanus, Anopheles arabiensis, Anopheles coluzzii, Anopheles darlingi, Anopheles dirus, Anopheles funestus, Anopheles gambiae s.l., Anopheles gambiae s.s. (Ifakara strain), Anopheles gambiae Tiassale, Anopheles gambiae Kisumu, Anopheles gambiae KisKDR, Anopheles gambiae M’Be, Anopheles melas, Anopheles minimus, Anopheles sinensis, Anopheles stephensi, Mansonia titillans, and is useful for controlling one or more of them.

[0019] In another embodiment, isocycloseram is useful in the methods and other aspects of the invention for controlling adult mosquitoes.

[0020] Insecticide-resistant mosquito species have also been discovered, and thus in another embodiment, isocycloseram is suitable for controlling insecticide-resistant mosquitoes such as pyrethroids and / or carbamates.

[0021] Pyrethroids are the only insecticides recommended by the WHO for malaria vectors in both indoor residual spraying (IRS) and long-lasting insecticidal nets (LLINs) in the form of alpha-cypermethrin, bifenthrin, permethrin, deltamethrin, lambda-cyhalothrin, and etofenprox. Pyrethroids have been the chemical class of choice for agricultural and public health applications over the past few decades due to their relatively low toxicity to humans, rapid knockdown action, relatively long lifespan (3 - 6 months when used as IRS), and low cost. However, the extensive use of pyrethroids in agricultural applications and for vector control has led to the emergence of resistance in major malaria and dengue vectors. Strong resistance has been reported for pyrethroid deltamethrin (and permethrin) against the Anopheles gambiae Tiassale strain (from southern Cote d’Ivoire) (Constant V.A. Edi et al., Emerging Infectious Diseases; Vol.18, No.9, September 2012). Pyrethroid resistance has also been reported for permethrin, deltamethrin, and lambda-cyhalothrin against the Aedes aegypti Cayman Island strain (Angela F.Harris et al., Am.J.Trop.Med.Hyg., 83(2), 2010), and for alpha-cypermethrin, permethrin, and lambda-cyhalothrin against certain Anopheles (Win Van Bortel, Malaria Journal, 2008, 7:102).

[0022] In another embodiment of the invention, isocycloseram is suitable for use against insecticide-resistant mosquitoes selected from Anopheles gambiae RSPH, Anopheles gambiae Tiassale, Anopheles gambiae Akron, Anopheles gambiae Kisumi Rdl, Anopheles arabiensis NDjamina, Anopheles coluzzii VK7, Anopheles funestus FUMOZ, Aedes aegypti Grand Cayman, Culex quinquefasciatus strain POO, and highly pyrethroid-resistant Anopheles arabiensis (Kingani strain).

[0023] In another embodiment, the method of the invention is useful against resistant mosquitoes such as the mosquitoes shown below.

[0024] The Anopheles gambiae RSPH strain is a multi-resistant mosquito (target-site and metabolic resistance) described in the reagent catalog of the Malaria Research and Reference Reagent Resource Center (www.MR4.org; MR4-number: MRA-334).

[0025] The Anopheles gambiae Tiassale strain is a multi-resistant mosquito (target and metabolic resistance strains) that shows cross-resistance among carbamates, organophosphates, and pyrethroids, as described in Constant V.A. Edi et al., Emerging Infectious Diseases; Vol. 18, No. 9, September 2012, and Ludovic P.A. Ahoua Alou et al., Malaria Journal 9:167, 2010).

[0026] The Anopheles gambiae Akron strain is a multi-resistant mosquito (target and metabolic resistance strains), as described in Djouaka F. Rousseau et al., BMC Genomics, 9:538; 2008.

[0027] The Anopheles coluzzii VK7 strain is a target-resistant mosquito, as described in Dabire Roch Kounbobr et al., Malaria Journal, 7:188, 2008.

[0028] The Anopheles funestus FUMOZ strain is a metabolic resistance strain, as described in Hunt et al., Med Vet Entomol. 2005 Sep;19(3):271-5). In this paper, Anopheles funestus, one of the major malaria vector mosquitoes in Africa, was reported to show resistance to pyrethroid and carbamate insecticides in South Africa.

[0029] Anopheles arabiensis (Kingani strain) (high pyrethroid-resistant strain) originating from Ifakara and in the colony in Bagamoyo.

[0030] Anopheles gambiae Kisumi Rdl strain, a dieldrin-resistant strain from Kenya.

[0031] Anopheles arabiensis NDjamina strain, a pyrethroid-resistant strain from Chad.

[0032] Aedes aegypti Grand Cayman strain is a target-resistant mosquito and is described in Angela F. Harris, Am. J. Trop. Med. Hyg. 83(2), 2010.

[0033] Culex quinquefasciatus (metabolic resistance to DDT strain P00); obtained from Texchem, Penang, Malaysia.

[0034] Anopheles gambiae s.s. population from M’Be: Koffi, A.A., Ahoua Alou, L.P., Adja, M.A. et al. Insecticide resistance status of Anopheles gambiae s.s population from M’Be: a WHOPES-labelled experimental hut station, 10 years after the political crisis in Cote d’Ivoire. Malar J12, 151(2013).

[0035] Vector control solutions are means for controlling vectors such as mosquitoes. Examples of such means are compositions, products and treated articles, a substrate or non-biological material incorporated with (e.g., coated or impregnated with) isocycloseram, a spray product containing isocycloseram (e.g., indoor residual spray and aerosol products), a paint composition containing isocycloseram, and a product or treated article containing isocycloseram.

[0036] Examples of the integrated management or control solutions for vector mosquitoes of the present invention include, for example, solutions for preventing mosquito bites, blood sucking, or reducing related mosquito populations. Examples of the use of such compositions, products, treated articles, and substrates of the present invention are at potential or known interaction sites between vector mosquitoes and animals such as humans who are susceptible to pathogenic disease infections transmitted by such vectors. Appropriate integrated solutions within the scope of the present invention also include identifying mosquito breeding sites and placing the compositions, products, treated articles, and substrates of the present invention at such sites.

[0037] Examples of the substrates or abiotic materials of the present invention are self - standing films / sheets (e.g., screens) incorporated (e.g., coated or impregnated) with isocycloseram, threads, fibers, yarns, pellets, fabrics (or cloth (e.g., for clothing)), nets, tents, and curtains, which can be used to protect from mosquito bites and reduce blood sucking. Specifically, it is well known that a mosquito net coated with an insecticide can protect a sleeping human from mosquito bites. To prevent mosquitoes from entering a dwelling, the coated or impregnated fabrics of the present invention can also be used as curtains in front of windows, eaves of door openings, or openings of ventilation devices.

[0038] The use of the compound in the substrates of the invention (e.g., nets and fabrics) serves the following purposes: · Good insecticidal action · Immediate insecticidal effectiveness · Persistent insecticidal effectiveness · Uniform release of the active ingredient · Long - term durability (e.g., withstand multiple washings over a long period) · Simple manufacture · At least one of the safety for users is achieved.

[0039] The nets and fabrics (or cloths) of the present invention incorporating isocycloseram (e.g., coated or impregnated) are made of various natural and synthetic fibers, as knitted products or knitted fibers, and also as blends in the form of woven or non-woven fabrics. Natural fibers are, for example, cotton, raffia, jute, linen, sisal, hessian, wool, silk or hemp. Synthetic fibers can be made of polyamide, polyester, polyacrylonitrile, polyolefin, such as polypropylene or polyethylene, Teflon, and also mixtures of fibers, such as mixtures of synthetic fibers and natural fibers. Polyamide, polyolefin and polyester are preferred as fiber materials. Polyester such as polyethylene terephthalate is particularly preferred. Most preferred are the nets made of polyethylene and / or polypropylene.

[0040] In the art, methods suitable for incorporating (by coating) a compound into nets and fabrics by dipping or immersing them in a pesticide formulation, or alternatively by spraying this formulation onto their surface, have been disclosed (see WO 2003 / 034823, WO 2008 / 122287, WO 01 / 37662, US 2009036547, WO 2007 / 036710). After treating the nets and fabrics of the present invention, they can be easily dried at ambient temperature (see also below for further background). Such methods are also suitable for incorporating isocycloseram (by coating).

[0041] In the art, methods suitable for incorporating a polymer material, which is made into fibers, then into yarns or threads and then extruded, into a net or fabric by impregnating the net or fabric with a compound in the presence of isocycloseram are also disclosed (see, for example, WO 08 / 004711, WO 2009 / 121580, WO 2011 / 128380, WO 2011 / 141260, WO 2010 / 118743). Such nets and fabrics have an effective amount of the compound available at the surface of the net and fabric for controlling mosquito bites. Generally, the compound is mixed with the molten polymer. Such methods are also suitable for incorporating isocycloseram (by impregnation).

DETAILED DESCRIPTION OF THE INVENTION

[0042] In the context of the compounds, additives, and other insecticides of the present invention, the terms "incorporated" or "incorporating" mean that a substrate or non-living material contains or comprises the defined compounds, additives, and / or insecticides, respectively, by means such as coating or impregnation.

[0043] Preferably, the substrate of the present invention is a net, and preferably, by coating the net with a composition containing isocycloseram, or by manufacturing a polymer material in the presence of such isocycloseram and then processing the obtained polymer material into the net of the present invention, a long-lasting net incorporating isocycloseram is obtained.

[0044] According to the present invention, when isocycloseram is used in a polymer, the isocycloseram is released to the surface of the net during the use of the net or fabric made from the polymer, and mosquito bites are controlled, and such control persists at an appropriate level and for an appropriate period.

[0045] Examples of suitable polymers are polyamides, polyesters, polyacrylonitrile, polyolefins, such as polyethylene compositions that can be made from various polyethylene polymers; these can be LDPE, LLDPE, MDPE, and HDPE. LLDPE (linear low density polyethylene) is a substantially linear polymer of polyethylene having a significant number of short branches, which is typically produced by copolymerization of ethylene and long chain olefins. MDPE is medium density polyethylene, a substantially linear polymer of polyethylene having a shorter chain length compared to HDPE. HDPE (high density polyethylene) or polyethylene high density (PEHD) is a polyethylene thermoplastic resin. HDPE has few branches and thus imparts stronger intermolecular forces and tensile strength compared to low density polyethylene. HDPE is also harder, more opaque, and can withstand somewhat higher temperatures (120 °C / 248 °F for short periods, 110 °C / 230 °F continuously). HDPE yarn is stronger than LDPE blended polyethylene yarn. LLDPE is structurally different from conventional low density polyethylene (LDPE) in that it has no long chain branches. These polyethylene compositions (HDPE, LDPE, LLDPE, and mixtures thereof) are generally used to manufacture yarns and polyethylene-based fabric products. Methods for incorporating pesticidal compounds into polymers without weakening the resulting properties are known in the art, for example, mixtures of HDPE and LDPE are used. Using such methods, isocycloseram can also be incorporated into the polymer.

[0046] Examples of the spray products of the present invention are indoor residual sprays or space sprays containing isocycloseram. Indoor residual spraying (IRS) is a technique for applying a residual deposit of insecticide on indoor surfaces where disease vectors rest, such as walls and ceilings. The main purpose of indoor residual spraying is to shorten the lifespan of vector mosquitoes, thereby reducing or blocking disease transmission. A secondary effect is a reduction in the density of mosquitoes within the treated area. IRS is an approved, proven, and cost-effective intervention method for malaria control and is also used in the management of leishmaniasis and Chagas disease. Many malaria vector mosquitoes are associated with the human environment and rest indoors after blood-feeding. These mosquitoes are particularly susceptible to control by indoor residual spraying (IRS) containing isocycloseram. As the name implies, IRS involves coating the walls and other surfaces of the house with a residual insecticide. Mosquitoes that come into contact with these surfaces are killed by isocycloseram for several months. IRS does not directly prevent people from being bitten by mosquitoes. Rather, IRS usually kills mosquitoes after blood-feeding when they come to rest on the sprayed surfaces. Thus, IRS prevents the transmission of infectious diseases to others. To be effective, IRS must be applied to a very high proportion (usually over 70%) of the households in an area. Communities play a passive role in IRS programs, but collaboration with IRS efforts is important for their success. Community participation in IRS often consists of removing food and covering surfaces before spraying, collaborating with the spraying team, and refraining from covering treated surfaces with new paint or plaster. However, opposition to IRS by communities or individual households due to odors, disruption, potential chemical exposure, or sheer inconvenience has been a serious problem in some areas. Therefore, the spray according to the present invention having good residual efficacy and an acceptable odor is particularly suitable as a component of an integrated management or control solution for vector mosquitoes.

[0047] Unlike the IRS where effective isocycloseram needs to bind to the surfaces of a house such as walls and ceilings, the space spray products of the present invention rely on the production of a large number of small pesticide droplets that are intended to be distributed throughout a large volume of air over a given period. When these droplets affect the target mosquitoes, a lethal dose of isocycloseram is delivered. Conventional methods of manufacturing space sprays include thermal spraying (by which a thick cloud of pesticide droplets showing the appearance of a dense fog is formed) and ultra-low volume (ULV) spraying, by which droplets are produced by a low-temperature mechanical aerosol generator.

[0048] Since a large area can be treated at one time, this method is a very effective way to rapidly reduce the population of mosquitoes flying in a particular area. Since the residual effect from this application is very limited, the application must be repeated at intervals of 5 to 7 days in order to be fully effective. This method can be particularly effective in epidemic situations where a rapid reduction in the number of mosquitoes is required. Therefore, it can be used in urban dengue control campaigns.

[0049] Effective space spraying generally depends on the following specific principles: · Target insects usually fly through the spray cloud (or are sometimes affected while resting on the exposed surface). Therefore, the efficiency of contact between the spray droplets and the target insects is important. This is achieved by ensuring that the spray droplets remain airborne for an optimal period and contain an appropriate dose of pesticide. These two problems are mainly addressed by optimizing the droplet size. · If the droplets are too large, the droplets will fall to the ground too rapidly and will not penetrate the plants or other obstacles encountered during application (the effective area of application is limited). If one of these large droplets affects an individual insect, this effect is also an "overkill" since a high dose is delivered per individual insect. · If the droplets are too small, they will not attach to the target insects due to aerodynamics (no effect) or can be carried upward in the atmosphere by convection. · The optimal size of the droplets for space spray applications is droplets having a volume median diameter (VMD) of 10 to 25 microns.

[0050] The compositions of the present invention can be utilized in spray products as aerosol-based applications such as aerosolized foaming applications. A pressurized can is a common means of transportation for aerosol formation. An aerosol propellant compatible with the pesticidal compound is used. Preferably, a liquefied gas type propellant is used. Suitable propellants include compressed air, carbon dioxide, butane, and nitrogen. The concentration of the propellant in the isocycloseram composition is about 5 to about 40% by weight, preferably about 15 to about 30% by weight, based on the isocycloseram composition.

[0051] In one embodiment, the isocycloseram formulation of the present invention may also include one or more foaming agents. Foaming agents that can be used include sodium lauryl sulfate, cocamide DEA, and cocamidopropyl betaine. Preferably, sodium lauryl sulfate, cocamide DEA, and cocamidopropyl are used in combination. The concentration of the foaming agent(s) in the isocycloseram composition is about 10 to about 25% by weight, more preferably 15 to 20% by weight, based on the composition.

[0052] When the isocycloseram formulation is used in aerosol applications that do not contain a foaming agent, the compositions of the present invention can be used without the need to mix immediately before use. However, aerosol formulations containing a foaming agent need to be mixed (i.e., shaken) immediately before use. Further, when using a formulation containing a foaming agent for an extended period of time, it may be necessary to mix further at regular intervals during use.

[0053] The living area can also be treated with the isocycloseram composition of the present invention by using a combustible formulation such as a candle, mosquito coil, or a stick of incense containing the composition. For example, the composition can be included in household articles such as "heated type" air fresheners that release the pesticidal composition when heated, for example, electrically or by combustion.

[0054] The composition used in the present invention containing isocycloseram can be utilized as an aerosol, mosquito-repellent incense, and / or a spray product as a vaporizer or atomizer.

[0055] The concentration of isocycloseram in each of the polymer materials, fibers, yarns, fabrics, nets or substrates of the present invention can vary within a relatively wide concentration range, for example, from 0.05 to 15% by weight, preferably from 0.2 to 10% by weight, more preferably from 0.4 to 8% by weight, particularly from 0.5 to 5% by weight, for example, from 1 to 3% by weight.

[0056] The above percentages are percentages based on the dry weight of the net or substrate or non-biological material.

[0057] Similarly, the concentration of the compound of the present invention in the composition (regardless of whether it is for treating the surface or coating fibers, yarns, nets, fabrics) can vary within a relatively wide concentration range, for example, from 0.1 to 70% by weight, for example, from 0.5 to 50% by weight, preferably from 1 to 40% by weight, more preferably from 5 to 30% by weight, particularly from 10 to 20% by weight.

[0058] The concentration should be selected according to the application field so that the requirements regarding insecticidal efficacy, durability and toxicity are met. It is also possible to achieve adaptation of the material properties, and thus obtain custom-made fabrics.

[0059] When used in the IRS method of the present invention, isocycloseram (AI) is present on the surface of the house at a coating rate of AI 0.01 to 2 g / m 2 , suitably AI 0.05 to 1 g / m 2 , preferably AI 0.1 to 0.7 g / m 2 , particularly AI 100 to 200 mg / m 2 .

[0060] Therefore, the effective amount of isocycloseram can vary depending on how it is used, which mosquitoes control is most desired against, and the environment in which it is used. Thus, the effective amount of isocycloseram is an amount sufficient to achieve mosquito control: · When used as an IRS formulation, the effective amount is such that the coverage rate of AI on the surface is 0.01 - 2 g / m 2 , preferably 0.05 - 1 g / m 2 , particularly 0.1 - 0.7 g / m of AI 2 , particularly 100 - 200 mg / m of AI 2 ; · When used incorporated into a net or substrate, the effective amount is 0.05 - 15% by weight, preferably 0.2 - 10% by weight, more preferably 0.4 - 8% by weight, particularly 0.5 - 5% by weight, for example 1 - 3% by weight.

[0061] Generally, when used in a particular product of the present invention, the pyridine compound is continuously distributed in the yarn, thread, net or fabric, but may also be distributed partially or discontinuously in the yarn, thread, net or fabric. For example, the net may contain certain parts composed of coated or impregnated fibers and certain other parts that are not, and instead, a part of the fibers constituting the net may be impregnated with the compound of the present invention, or this part may be coated with the compound of the present invention, while a part of the other fibers is not impregnated or coated, or these other fibers are impregnated or coated with another insecticide compound (see below).

[0062] The net of the present invention impregnated or coated with isocycloseram can meet the criteria of the WHOPES instructions for insecticide-containing long-lasting mosquito nets with only up to 20 washes (“Guidelines for laboratory and field testing of long-lasting mosquito nets”, 2005, http: / / www.who.int / whopes / guidelines / en / ), which means that such a net should not lose its biological activity after only about 20 wash cycles.

[0063] In one embodiment, the net of the present invention impregnated or coated with isocycloseram can have a biological activity according to the WHOPES guidelines of 95 - 100% knockdown after 60 minutes, or 80 - 100% mortality after 24 hours, after being washed at least 20 times, for example 25 times, preferably at least 30 times, and even more preferably at least 35 times.

[0064] It should be understood that the "WHOPES Directive" means the "Guidelines for laboratory and field testing of long - lasting mosquito nets" Directive, 2005). This directive is searchable at the following mutual address: http: / / www.who.int / whopes / guidelines / en / .

[0065] When "impregnating" the net with isocycloseram to produce the net of the present invention, the fibers constituting the net are produced by melting a polymer, isocycloseram, and optionally other compounds, such as other insecticides, additives, stabilizers. When such isocycloseram is impregnated into the net, the net of the present invention contains synthetic fibers; on the other hand, the net of the present invention coated with such isocycloseram contains synthetic fibers and / or natural fibers.

[0066] Polymer materials useful in the composition of the present invention incorporated with isocycloseram can be produced by mixing such isocycloseram with a polymer in a liquid phase, optionally other additives (such as binders and / or synergists), and other insecticidal compounds.

[0067] Methods for producing and then processing suitable polymer materials are described in the art, see for example WO 09121580, WO 2011 / 141260.

[0068] For example, a net based on a polymer material containing the isocycloseram insecticide has the following steps: a) A step of melting the polymer used and one or more insecticidally active ingredients together or separately at a temperature of 120 to 250 °C. b) A step of forming the melt from step a) into spun yarns and cooling them. c) Optionally, a step of passing the spun yarns formed in step b) through a stretching system, stretching them, and then optionally curing the yarns. d) A step of knitting the spun yarns to form a net. e) A step of subjecting the net to a heat curing operation, wherein the temperature of the heat curing operation is selected to be 20 °C lower than the melting temperature of the polymer used. It is produced by.

[0069] A washing step is carried out prior to the heat curing in step e) of the production of this net. Water and a detergent are preferably used for this. The heat curing is preferably carried out in a dry atmosphere.

[0070] The production of the net incorporated with the insecticide compound can be carried out at a single location, but it is also envisaged that different steps can be carried out at different locations. Therefore, the present invention provides that a composition containing isocycloseram can be produced in a concentrated state and then processed into a polymer. Accordingly, the present invention also provides a composition containing isocycloseram in a concentrated state, which composition may also contain additives (binders and / or synergists), and other insecticidal compounds (the composition is expressly prepared to produce a polymer material impregnated with isocycloseram (such a composition is often referred to as a'masterbatch')). The amount of isocycloseram in this masterbatch can vary depending on the situation, but generally can be 10 to 95% by weight, for example 20 to 90% by weight, preferably 30 to 85% by weight, more preferably 35 to 80% by weight, particularly 40 to 75% by weight.

[0071] In addition, in the present invention, a composition or formulation containing isocycloseram is also used for coating walls, floors and ceilings in a building, and for coating a substrate or a non-biological material. Considering the purpose, the composition of the present invention can be prepared using known techniques, and this composition may contain a binder to promote the binding of the compound to the surface or other substrates. Agents useful for binding are known in the art and tend to take the form of polymers. The type of binder suitable for a composition applied to a wall surface having specific porosity and binding properties will be different from fibers, yarns, fabrics or meshes, and an appropriate binder will be selected based on the teachings known to those skilled in the art.

[0072] Common binders are polyvinyl alcohol, modified starch, polyvinyl acrylate, polyacrylic acid, polyvinyl acetate copolymer, polyurethane and modified vegetable oil. Suitable binders can include latex dispersions derived from a wide variety of polymers and copolymers, and combinations thereof. Latices suitable for use as binders in the compositions of the present invention include polymers and copolymers of styrene, alkylstyrene, isoprene, butadiene, acrylonitrile lower alkyl acrylate, vinyl chloride, vinylidene chloride, lower carboxylic acids and vinyl esters of α,β-ethylenically unsaturated carboxylic acids, for example polymers containing three or more different monomer species copolymerized, and post-dispersion suspensions of silicone or polyurethane. Also, polytetrafluoroethylene (PTFE) polymers for binding active ingredients to other surfaces may also be suitable.

[0073] The formulation according to the present invention contains at least one compound (or pesticide (A)) shown in Table 1, a carrier such as water (C), optionally a polymer binder or carrier (B), and a further component (D).

[0074] The polymer binder binds isocycloseram to the surface of the non-biological material and ensures long-term action. By using the binder, the elimination of isocycloseram pesticide from the non-biological material due to environmental influences such as rain or due to human influences on the non-biological material such as washing and / or cleaning is reduced. Further components can be additional pesticide compounds, synergists, UV stabilizers.

[0075] The composition of the present invention can be in many different forms or formulation types such as suspensions, capsule suspensions, etc., and those skilled in the art can prepare the relevant composition based on the properties of the specific isocycloseram, its use and application type.

[0076] For example, the isocycloseram used in other aspects of the method of the present invention can be encapsulated in the formulation. The encapsulated compound can improve the wash fastness and also impart longer-term effectiveness. The formulation can be organic-based or water-based, and preferably can be water-based.

[0077] Microencapsulated isocycloseram suitable for use in the compositions and methods according to the present invention is produced using any suitable technique known in the art. For example, various processes for microencapsulating materials have already been developed. These processes can be classified into three categories: physical methods, phase separation, and interfacial reactions. In the category of physical methods, the microcapsule wall material and the core particles are physically combined into one, and the wall material flows around the core particles to form microcapsules. In the category of phase separation, microcapsules are formed by emulsifying or dispersing the core material in an immiscible continuous phase, in which the wall material is dissolved and physically separated from the continuous phase, for example, by coacervation, and deposited around the core particles. In the category of interfacial reactions, microcapsules are formed by emulsifying or dispersing the core material in an immiscible continuous phase, and then an interfacial polymerization reaction is caused on the surface of the core particles. The concentration of the pyridine compound present in the microcapsules can vary from 0.1 to 60% by weight of the microcapsules.

[0078] The formulation according to the present invention can optionally be formed by mixing all the components with water, using appropriate mixing and / or dispersion of the aggregates. Generally, the formulation is formed at a temperature of 10 to 70 °C, preferably 15 to 50 °C, more preferably 20 to 40 °C.

[0079] It is possible to use a pesticide (A) (i.e., isocycloseram alone or in combination with other suitable insecticides), a solid polymer (B), and optionally additional additives (D), and to disperse them in an aqueous component (C).

[0080] When a binder is present in the composition of the present invention, it is preferred to use an aqueous dispersion of the polymeric binder (B) and an aqueous formulation of the pesticide (A) in water previously prepared separately. Such separate formulations may each contain additional additives for stabilizing (A) and / or (B) in the respective formulations and are commercially available. In a second treatment step, such raw formulations and optionally additional water (component (C)) are added.

[0081] Combinations are also possible, i.e., it is also possible to use a pre-formed dispersion of (A) and / or (B) and mix it with solid (A) and / or (B).

[0082] The dispersion of the polymer binder (B) may be a dispersion pre-manufactured by the manufacturer of the chemical product.

[0083] However, it is also within the scope of the present invention to use a "homemade" dispersion, i.e., a dispersion manufactured on a small scale by the end user. Such a dispersion can be produced by providing a mixture of about 20% of the binder (B) in water, heating this mixture to a temperature of 90 - 100 °C, and vigorously stirring the mixture for several hours.

[0084] For the process according to the present invention, it is also possible to manufacture the formulation as a final product so that it can be easily used by the end user. However, of course, it is also possible to manufacture a concentrate, which can be diluted with additional water (C) to the desired concentration for use by the end user.

[0085] In one embodiment, a coating formulation containing a composition suitable for IRS use or isocycloseram contains an active ingredient and a carrier such as water, and may also contain one or more co-formulants selected from a dispersant, a wetting agent, an antifreeze, a thickener, a preservative, an emulsifier, and a binder or spreading agent.

[0086] Furthermore, at least: · a first component containing at least one compound shown in Table 1(A); and · a second component containing at least one polymer binder (B); · a further component (D), which can be a third separate component of the kit or can already be mixed with components (A) and / or (B); It may also be possible to ship the formulation to the end user as a kit comprising:

[0087] The end user can prepare the formulation for use by simply adding water (C) to the components of the kit and mixing them.

[0088] The components of the kit can also be formulations in water. Of course, it is also possible to combine one aqueous formulation of the components with the dry formulations of the other component(s).

[0089] As an example, this kit is: · One formulation of the compound (A) shown in Table 1 and optionally water (C); and · A second separate formulation of at least one polymer binder (B), water as component (C), and optionally component (D); may comprise.

[0090] Thus, in a further aspect, the present invention provides a kit for treating fibers, yarns, nets and fabrics by coating them with insecticidal properties that are wash-resistant, the kit comprising a first sachet containing a pre-measured amount of at least one compound shown in Table 1, and a second sachet containing a pre-measured amount of at least one polymer binder. The resulting treated fibers, yarns, nets and fabrics are imparted with the insecticidal properties necessary for controlling vector organisms, such as for controlling mosquitoes carrying vector organisms.

[0091] The concentrations of components (A), (B), (C) and optionally (D) are selected by those skilled in the art according to the techniques used for coating / treating.

[0092] Generally, the amount of the pesticide (A) can be up to 50% by weight, preferably 5 - 50% by weight, for example 10 - 40% by weight, particularly 15 - 30% by weight, based on the weight of the composition.

[0093] The amount of the polymer binder (B) can range from 0.01 - 30% by weight, preferably 0.5 - 15% by weight, more preferably 1 - 10% by weight, particularly 1 - 5% by weight, based on the weight of the composition.

[0094] When present, generally the amount of the additional component (D) is 0.1 to 20% by weight, preferably 0.5 to 15% by weight, based on the weight of the composition. When present, the appropriate amount of the pigment and / or dye is generally 0.01 to 5% by weight, preferably 0.1 to 3% by weight, more preferably 0.2 to 2% by weight, based on the weight of the composition.

[0095] Ready-to-use normal formulations contain 0.1 to 40%, preferably 1 to 30% of components (A), (B) and optionally (D), and the remaining amount is water (C).

[0096] The general concentration of the concentrate to be diluted by the end user can contain 5 to 70%, preferably 10 to 60% of components (A), (B) and optionally (D), and the remaining amount is water (C).

[0097] The formulations of the present invention can be applied to polymer materials, for example, still in the form of yarns or sheets, before being formed into the required products or after the formation of related products.

[0098] In the case of a net and / or a fabric, a process of coating the net and / or the fabric, comprising the following steps: a) (a1) A step of passing the material through the formulation; or (a2) A step of bringing the material into contact with a roller partially or completely immersed in the formulation and picking up the formulation on the surface of the material in contact with the roller; or (a3) A step of immersing the material in the formulation; or (a4) A step of spraying the formulation onto the material; or (a5) A step of applying the formulation onto or into the material with a brush; or (a6) A step of applying the formulation as a foam, or (a7) A step of coating the formulation onto the material; A step of treating the net and / or the fabric with the aqueous formulation according to the present invention by any of the procedural steps selected from the group of: b) Optionally, removing excess formulation by squeezing the material between rollers or by means of a doctor blade; and c) Drying the material; A process for coating a net and / or fabric, comprising at least:

[0099] If the raw material contains residues from a previous manufacturing process, such as sizing agents, spinning finishes, other auxiliaries and / or impurities, it may be beneficial to perform a washing step prior to coating.

[0100] Specifically, the following details are important for steps a), b) and c). Step a1) The formulation is applied by passing the material through an aqueous formulation. This step is known to those skilled in the art as padding. In a preferred embodiment, the material is completely immersed in the aqueous formulation in a bath containing the liquor or passed through the formulation held between two horizontally oriented rollers. According to the present invention, the material may be passed through the formulation or the formulation may be passed through the material. The uptake of the formulation will be affected by the stability of the concentrated bath, the need for level distribution, the density of the material, and the desire to reduce the energy costs of the drying and curing steps. Normal liquor uptake can be between 40% and 150% of the weight of the material. Those skilled in the art are proficient in determining the optimum value. Step a1) is preferred for coating open-width material that will later be made into a net.

[0101] For small-scale production or recoating of untreated nets, a simple hand-held roller may be sufficient.

[0102] Step a2) It is further possible to apply the aqueous formulation to the material by means of a roller that is partially immersed in the dispersion, thereby applying the dispersion to the surface of the material that contacts the roller (kiss rolling). By this method, it is possible to coat only one side of the material, which is advantageous, for example, when direct contact between human skin and the insecticide-treated material should be avoided.

[0103] The coating of the material in step a1), a2) or a3) is usually carried out at a temperature of 10 to 70 °C, preferably 15 to 50 °C, more preferably 20 to 40 °C.

[0104] Step a4) In a suitable fiber machine equipped with a spraying device, for example, in an open pocket clothes washer / dehydrator, spraying can be applied in a continuous process or a batch process. Such a device is particularly suitable for impregnating a ready-made net.

[0105] Step a6) The foam contains less water than the above-mentioned dispersion. Therefore, the drying process can be very short. This treatment can be carried out by injecting a gas or a blend of gases (e.g., air) into it. Preferably, the addition of a surfactant having film-forming properties may be required. Suitable surfactants and the necessary technical devices are known to those skilled in the art.

[0106] Step a7) The coating process can preferably be carried out by a doctor blade process. The conditions of this process are known to those skilled in the art.

[0107] Step b) Generally, by squeezing the material, preferably passing the material between rollers as known in the art, the excess emulsion is removed, thereby achieving a defined liquid uptake. The squeezed-out liquid can be reused. As an alternative method, the excess aqueous emulsion or aqueous dispersion can be removed by centrifugation or vacuum suction.

[0108] Step c) Drying can be carried out at ambient temperature. In particular, such passive drying can be carried out in a hot and dry climate. Of course, by applying a high temperature, the drying process can be accelerated. The active drying process is usually carried out during large-scale processing. The drying is generally carried out at a temperature below 200 °C. A preferred temperature is 30 to 170 °C, more preferably room temperature. The choice of temperature is determined by the thermal stability of the pesticide in the formulation and the thermal stability of the non-biological material to be impregnated.

[0109] Regarding the method according to the present invention, an aqueous formulation containing at least one pigment and / or at least one dye can be used such that the material is not only coated with the isocycloseram pesticide but is also colored simultaneously.

[0110] In a further aspect, the present invention provides a method for treating fibers, yarns, nets and fabrics by coating them with a wash-resistant pesticide, comprising: (i) preparing a treatment composition containing at least one compound shown in Table 1; (ii) treating the fibers, yarns, nets and fabrics; and (iii) drying the obtained treated fibers, yarns, nets and fabrics.

[0111] The polymer binder (B) can be dispersed in an aqueous formulation and contains one or more fluorinated acrylic polymers useful in water-resistant and oil-resistant formulations, and examples include copolymers prepared by polymerization of perfluoroalkyl acrylate monomers and comonomers, particularly acrylate monomers. The binder may be a fluorocarbon resin (described in WO 2006 / 128870).

[0112] Only water is used as the solvent in the formulation. However, a trace amount of an organic solvent miscible with water may be present. Examples of the solvent include water-miscible alcohols such as monoalcohols like methanol, ethanol or propanol, higher alcohols such as ethylene glycol or polyether polyol, and ether alcohols such as butyl glycol or methoxypropanol. Preferably, the content of the organic solvent is 5% by weight or less (based on component (C)), more preferably 1% by weight or less (based on component (C)), particularly 0.1% by weight or less based on component (C).

[0113] Depending on the purpose of use of the non-biological material to be treated, the formulation according to the present invention may further contain one or more components or additives (D) selected from preservatives, surfactants, fillers, impact resistance improvers, anti-fogging agents, foaming agents, clarifying agents, nucleating agents, coupling agents, fixing agents, cross-linking agents, conductivity improvers (antistatic agents), stabilizers such as antioxidants, radical scavengers for carbon and oxygen, and peroxide decomposers, flame retardants, mold release agents, agents having UV protection properties, spreading agents, anti-blocking agents, migration inhibitors, foam forming agents, antifouling agents, thickeners, further biocides, wetting agents, plasticizers and film forming agents, adhesives or anti-adhesives, fluorescent whitening agents, pigments and dyes.

[0114] The general amount of the polymer binder (B) is 0.01 to 10% by weight (dry weight) based on the weight (dry) of the material. As a general guideline, the weight ratio of the insecticide to the binder (B) should be approximately constant depending on the insecticidal and migratory ability of the insecticide, that is, the greater the amount of the insecticide, the greater the amount of the binder (B). The preferred amount of the binder (B) is 0.1 to 5% by weight, more preferably 0.2 to 3% by weight based on the (dry) weight of the material.

[0115] The coated material can contain at least one type of pigment and / or at least one type of dye. The amount of the at least one type of pigment and / or dye is generally 0.05 to 10% by weight, preferably 0.1 to 5% by weight, more preferably 0.2 to 3.5% by weight, based on the (dry) weight of the material.

[0116] The method of coating or treating the non-biological material is not limited to a specific technique. The coating can be carried out by dipping or immersing the non-biological substrate in the formulation, or by spraying the formulation onto the surface of the non-biological material. After treatment, the treated non-biological substrate can be easily dried at ambient temperature.

[0117] Therefore, sophisticated techniques are not required for the coating, and thus this coating process can be carried out by the end user himself on a small scale.

[0118] For example, an ordinary end user can use the formulation according to the present invention to coat / treat the net itself, for example, within his home. For this purpose, it is particularly advantageous to use the kit defined herein.

[0119] In one embodiment, the present invention provides a polymer, fiber, thread, yarn, net or fabric containing one or more compounds (shown in Table 1), which, when incorporated, can be one or more other conventional materials used in the production of such polymers, and the polymer, fiber, thread, yarn, net or fabric can optionally further incorporate one or more other insecticides and / or synergists.

[0120] In one embodiment, the present invention provides a net or fabric incorporated with one or more isocycloserams (shown in Table 1), and optionally further incorporates one or more other insecticides and / or synergists.

[0121] As described in the background art, the isocycloseram useful in the method and other aspects of the present invention can be used alone or in combination with other insecticides, synergists, insect repellents, sterilants, flame retardants, UV protectants / absorbers, and / or additives for controlling release properties.

[0122] When used in accordance with the present invention, isocycloseram may be used alone to control mosquitoes in IRS products and space spray products, or in formulations for treating non-biological substrate materials such as nets and fabrics, or in polymers for manufacturing non-biological substrates such as nets and fabrics, in combination with one or other known insecticides and / or one or more additives (such as synergists).

[0123] In one embodiment, the present invention provides a composition comprising one or more compounds of the present invention (useful for coating polymer materials or products made therefrom, or useful as a spray product), which composition optionally further comprises one or more other insecticides and / or synergists, and one or more other additives.

[0124] Examples of synergists are piperonyl butoxide (PBO), sebacic acid esters, fatty acids, fatty acid esters, vegetable oils, esters of vegetable oils, alcohol alkoxylates, and antioxidants.

[0125] Suitable sebacic acid esters are, for example, dimethyl sebacate, diethyl sebacate, dibutyl sebacate, dibenzyl sebacate, bis(N-succinimidyl) sebacate, bis(2-ethylhexyl) sebacate, bis(1-octyloxy-2,2,6,6-tetramethyl-4-piperidyl) sebacate, bis(2,2,6,6-tetramethyl-4-piperidyl) sebacate, and bis(1,2,2,6,6-pentamethyl-4-piperidinyl) sebacate (BLS292).

[0126] Suitable fatty acids are fatty acids having a chain length of 12 to 24 carbon atoms (preferably monovalent or polyvalent unsaturated fatty acids), such as palmitoleic acid, oleic acid, elaidic acid, vaccenic acid, eicosenoic acid, cetoleic acid, erucic acid, nervonic acid, linoleic acid, α-linolenic acid, γ-linolenic acid, arachidonic acid, timnodonic acid, clupanodonic acid, and selacholeic acid. Oleic acid, linoleic acid, α-linolenic acid, and γ-linolenic acid are particularly preferred.

[0127] Suitable fatty acid esters are preferably methyl or ethyl esters of the above fatty acids. Methyl esters are particularly preferred. The fatty acids and their esters may each be present even in a mixture.

[0128] Useful vegetable oils include all plant-derived oils that can usually be used in pesticide compositions. Examples include sunflower oil, rapeseed oil, olive oil, castor oil, rapeseed oil, corn kernel oil, cottonseed oil, and soybean oil. Rapeseed oil is preferred.

[0129] Suitable esters of vegetable oils are methyl or ethyl esters of the above oils. Methyl esters are particularly preferred.

[0130] Antioxidants useful as additives include, for example, butylhydroxytoluene, butylhydroxyanisole, and L-ascorbic acid.

[0131] Essential oils can also be used in indoor residual spray compositions; examples thereof are essential oils selected from citronella, peppermint oil, d-limonene, and abyssinian. This essential oil material is known, used for other purposes, can be prepared by those skilled in the art using known methods, and is also commercially available.

[0132] In addition to isocycloseram, the methods, compositions, polymers, products, substrates and / or integrated mosquito management solutions according to the present invention may contain one or more additional insecticidally active ingredients. Specific examples are organophosphates, pyrethroids, carbamates, methoxyacrylates or neonicotinoids, and further DDT, indoxacarb, nicotine, bensultap, cartap, spinosad, camphechlor, chlordane, endosulfan, γ-HCH, HCH, heptachlor, lindane, methoxychlor, acetoprole, ethiprole, fipronil, pyrafluprole, pyriprole, vaniliprole, abamectin, emamectin, emamectin benzoate, ivermectin, milbemycin, diofenolan, epofenonan, phenoxycarb, hydroprene, kinoprene, methoprene, pyriproxyfen, triprene, chromafenozide, halofenozide, methoxyfenozide, tebufenozide, bistrifluron, chlorfluazuron, diflubenzuron, flucycloxuron, flufenoxuron, hexaflumuron, lufenuron, novaluron, noviflumuron, penfluron, teflubenzuron, triflumuron, buprofezin, cyromazine, diafenthiuron, azocyclotin, cyhexatin, fenbutatin oxide, chlorfenapyr, binapacryl, dinobuton, dinocap, DNOC, phenazakine, fenpyroximate, pyrimidifen, pyridaben, tebufenpyrad, tolfenpyrad, hydramethylnon, dicofol, rotenone, acequinocyl, flubendiamide, Bacillus thuringiensis strains, spirodiclofen, spirotetramat, 3-(2,5-dimethylphenyl)-8-methoxy-2-oxo-1-azaspiro[4.5]deca-3-en-4-yl ethyl carbonate (alias: carbonic acid, 3-(2,5-dimethylphenyl)-8-methoxy-2-oxo-1-azaspiro[4.5] Deca-3-en-4-yl ethyl ester, CAS registration number: 382608-10-8), flonicamid, amitraz, propargite, flubendiamide, chlorantraniliprole, thicyclam hydrogen oxalate, thiosultap sodium, azadirachtin, Bacillus species, Beauveria species, Metarrhizium species, Paecilomyces species, tsingyensin, Verticillium species, aluminium phosphid, methyl bromide, sulfuryl fluoride, cryolite, flonicamid, pymetrozine, clothianidin, etoxazole, hexythiazox, amidoflumet, benclothiaz, benzoximate, biphenazate, bromopropylate, buprofezin, chinomethionate, chlordimeform, chlorobenzilate, chloropicrin, chlorthiazoben, cycloprothrin, siflumetofen, diclalanil, phenoxazrim, fentrifanil, flubenimine, flufenoxur, flutenzin, gossyplure, hydramethylnon, japonilure, methoxadiazone, petroleum, piperonyl butoxide, kaliumoleat, pyridalyl, sulfotep, tetradifon, tetrasul, triarathene and verbascine; is one or more active ingredients from the class of.

[0133] In a further aspect, the present invention provides a method of protecting mammals such as humans against mosquitoes, the method comprising applying to the mosquitoes, or to a potential or known site of interaction between the mammal and the mosquito, a vector control solution comprising a compound selected from the group consisting of isocycloseram in a mosquito-killing effective amount.

[0134] Another aspect of the present invention is a method of controlling the spread of vector-borne diseases, the method comprising: identifying vector mosquitoes; and contacting the vector mosquitoes or their environment with a vector control solution comprising a compound selected from the group consisting of isocycloseram in a mosquito-killing effective amount.

[0135] One aspect of the present invention also includes a method for killing mosquitoes, which comprises contacting a vector control solution containing a compound selected from the group consisting of isocycloseram in a mosquito-killing effective amount with mosquitoes or their environment.

[0136] The present invention also provides a method comprising: (i) identifying a potential or known interaction site between vector mosquitoes and mammals such as humans who are susceptible to pathogenic disease infection when contacted by such vectors; and (ii) placing at that site a vector control solution containing a compound selected from the group consisting of isocycloseram in a mosquito-killing effective amount.

[0137] It is also expected that the present invention through mosquito control will control many viruses carried by such vectors. As an example, Zika infection can be controlled by controlling mosquitoes of the genus Aedes, such as by using one or more of the compounds defined in Table 1 as part of the vector control solution. Examples of mosquitoes reported to spread Zika virus are mosquitoes of the genus Aedes, such as Aedes aegypti and Aedes albopictus. Thus, in one aspect, the present invention provides a method for controlling Zika virus infection, wherein one or more of the compounds defined in Table 1 are present in a mosquito-killing effective amount in the vicinity of mosquitoes of the genus Aedes, such as Aedes aegypti and Aedes albopictus. The vicinity of a mosquito means an area where mosquitoes are likely to be present, for example, generally the environment, specifically indoors, or an area such as the site on the skin surface where a mosquito bites an individual or a mammal.

[0138] In each of the methods according to the present invention, the vector control solution is preferably one or more of a composition, a product, and a treated article, each containing a compound selected from the group consisting of isocycloseram.

[0139] As used herein, "fiber" simply means a thin, thread-like portion typically made of natural materials such as cotton or jute.

[0140] In each aspect and embodiment of the present invention, "consisting essentially of" and its variations are preferred embodiments of "comprising" and its variations, and "consisting of" and its variations are preferred embodiments of "consisting essentially of" and its variations.

[0141] The disclosure in this application enables the use of each and all combinations of the embodiments disclosed herein.

[0142] The following examples serve to illustrate the present invention. They do not limit the present invention.

Example

[0143] Biological Example: Examples B1 - B3: Guideline-based bottle assay for evaluating insecticide resistance in arthropods using the CDC bottle assay 1 ml of acetone containing the test compound at a specified concentration and 1500 ppm of Mero (Bayer Crop Science) were added to a 250 ml glass bottle. The bottle was placed on a rotating table and the inner surface was coated as the solvent evaporated. Once dry, approximately 25 non-bloodfed female adult mosquitoes of the appropriate species and strain (2 or 3 days old each) were aspirated from the stock culture and gently blown into the exposure bottle. The bottle cap was replaced and the bottle was stood upright, avoiding direct sunlight, under standard culture conditions (nominally 28°C and 60 - 80% relative humidity).

[0144] A stopwatch was started and knockdown was evaluated after 60 minutes. According to the CDC definition, a mosquito was shown to be knocked down if it could not stand.

[0145] After 1 hour, the mosquitoes were carefully removed from the vials using a suction device and placed into collection cups. The mosquitoes were provided with 10% sucrose solution contained in plugs of absorbent cotton and stored under culture conditions. Mortality was evaluated after 24 hours and 48 hours.

[0146] Each treatment was repeated at least three times, and the mean knockdown or mortality was recorded. In each study, a known insecticide-susceptible strain of mosquitoes from the same genus as the resistant strain was established in one set of vials. The results are shown in Tables B1 - B3.

[0147]

Table 1

[0148]

Table 2

[0149]

Table 3

Claims

1. The use of isocycloceram in mosquito pest control.

2. The use of isocycloceram in the control of mosquito pests, which are disease vectors.

3. The use of isocycloceram in the control of mosquito pests, which are malaria vectors.

4. The use of isocycloceram according to any one of claims 1 to 3, wherein the mosquito is an insecticide-resistant mosquito.

5. The use of isocycloceram according to any one of claims 1 to 3, wherein the mosquito is a pyrethroid insecticide-resistant mosquito.

6. The use of isocycloceram according to any one of claims 1 to 3, wherein the mosquito is selected from the genera Anopheles, Culex, and Aedes.

7. The aforementioned mosquitoes include Aedes aegypti, Aedes albopictus, Aedes japonicas, Aedes vexans, Culex molestus, Culex pallens, Culex pipiens, Culex quinquefasciatus, Culex restuans, Culex tarsalis, and Anopheles albimanas. Anopheles alabiensis, Anopheles coluzzii, Anopheles darlingi, Anopheles dirus, Anopheles funestus, Anopheles gambiae s. l., Anopheles gambiae s. s. (Ifakara strain), Anofeles gambiae Tiassale; Anofeles gambiae Kisumu, Anofeles gambiae KisKDR, Anofeles gambiae M'Be, Anofeles melas, Anofeles minimus, Anofeles sinensis, Anofeles stephensi, and Mansonia tichirans Use of isocycloceramium according to any one of claims 1 to 3, selected from (titillans).

8. A method for producing a polymer material impregnated with isocycloceram, wherein the material is useful for producing base materials or non-biological materials such as threads, fibers, yarns, pellets, nets and fabrics, and the method comprises mixing a polymer with isocycloceram at a temperature of 120 to 250°C.

9. A method for controlling a nuisance, disease-transmitting, or pyrethroid-resistant mosquito pest, comprising applying an effective mosquito-killing dose of isocycloceram to such mosquito pest or to a location where such control is desired.

10. The method according to claim 9 for controlling mosquito pests, comprising: (a) applying an effective amount of a liquid composition comprising isocycloceram, optionally a polymer binder or carrier, one or more other insecticides and / or a synergistic agent to the surface of a dwelling; and / or (b) placing a substrate or non-biological material incorporating isocycloceram, optionally an additive, one or more other insecticides and / or a synergistic agent inside the dwelling.

11. The method according to claim 9, wherein the mosquito pest is a disease vector.

12. The method according to claim 9, wherein the mosquito pest is a malaria vector.

13. The method according to claim 9, wherein the mosquito pest is an insecticide-resistant mosquito.

14. The method according to claim 9, wherein the mosquito pest is a pyrethroid insecticide-resistant mosquito.

15. The method according to claim 9, wherein the mosquito pest is selected from the genera Anopheles, Culex, and Aedes.

16. The aforementioned mosquito pests include Aedes aegypti, Aedes albopictus, Aedes japonicas, Aedes vexans, Culex molestus, Culex pallens, Culex pipiens, Culex quinquefasciatus, Culex restuans, Culex tarsalis, and Anopheles albimanas. Anopheles alabiensis, Anopheles coluzzii, Anopheles darlingi, Anopheles dirus, Anopheles funestus, Anopheles gambiae s. l., Anopheles gambiae s. s. The method according to claim 9, selected from (Ifakara strain), Anofeles gambiae Tiassale; Anofeles gambiae Kisumu, Anofeles gambiae KisKDR, Anofeles gambiae M'Be, Anofeles melas, Anofeles minimus, Anofeles sinensis, Anofeles stephensi, and Mansonia titilans.

17. A mesh incorporating isocycloceram, which, after 20 washes, exhibits WHOPES-guideline bioactivity resulting in 95-100% knockdown at 60 minutes and / or 80-100% mortality at 24 hours.

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