Mosquito control method
By using isoxazolamide as a mosquito control agent, the problem of mosquito species' resistance to existing mosquito control agents is solved, and a long-term and safe mosquito control solution is provided, ensuring public health safety and reducing environmental and human health is achieved. risk.
Patent Information
- Application Number
- CN202380040219.1
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Priority Date
- 2022-05-16
- Filing Date
- 2023-05-16
- Publication Date
- 2024-12-27
AI Technical Summary
Existing mosquito control agents, such as pyrethroids, face the problem of resistance developed by mosquito species, resulting in a decrease in their effectiveness and lack of effective alternatives, especially in resistant mosquito species such as Anopheles Gambia and Aedes aegypti. Threat to public health.
Isoxazolamide is used as the active ingredient for mosquito killing. Through its biological effects against the biological effects of mosquito species, combined with its environmental safety and durability, it is used to prepare mosquito nets, sprays and other media control products to ensure long-term effectiveness and multiple wash stability.
Isoxazolamide significantly improves the killing effect of counteracting mosquito species, provides a long-term mosquito control solution, ensures public health security, and reduces potential harm to the environment and humans.
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Abstract
Description
[0001] The present invention relates to the technical field of mosquito control using certain isoxazoline compounds. More particularly, the present invention relates to methods of controlling mosquitoes, including mosquito vectors of pathogenic diseases and mosquitoes with developed insecticide resistance, such as resistance to pyrethroids, each method comprising an isoxazoline compound having mosquitoicidal activity.
[0002] Mosquito control manages mosquito populations to reduce their damage to human health, economy, and recreation. Mosquito control is a vital public health practice throughout the world, and especially in tropical regions, because mosquitoes transmit many diseases, such as malaria (Wikipedia contributors, "Mosquito control", Wikipedia [Wikipedia contributors, "Mosquito control", Wikipedia]).
[0003] Many infectious diseases (e.g., malaria, dengue and yellow fever, lymphatic filariasis and leishmaniasis) that cause debilitation or even death in humans and animals in many countries, especially in tropical countries, are transmitted by insect vectors. For example, the mosquito parasite Plasmodium falciparum accounts for more than 25% of child mortality outside the neonatal period. In some parts of Africa, malaria has been ranked first by the World Bank in terms of disability-adjusted life years lost. Many drugs can be used to treat and / or prevent some insect-borne diseases. However, not all mosquito-borne diseases can be effectively treated. For example, there are currently no chemotherapeutic drugs or vaccines for dengue virus. In addition, for antimalarial drugs, the therapeutic effects of currently available drugs are declining due to the increased resistance of some Plasmodium strains. Plasmodium enters the human bloodstream due to insect bites and causes malaria. Therefore, one of the most effective ways to prevent mosquito-borne diseases is to reduce the mosquito population in areas with high incidence of pathogen transmission and / or prevent mosquito bites in the first place. Recently, people have focused their efforts on controlling the mosquitoes that spread.
[0004] Three medically important genera of insects that transmit diseases are Anopheles, Culex, and Aedes. Culex and Aedes belong to the subfamily Culexinae, while Anopheles belongs to the subfamily Anophelesinae. Examples of diseases or pathogens transmitted by keystone mosquitoes are: Anopheles: malaria, filariasis; Culex: Japanese encephalitis, other viral diseases, filariasis; and Aedes: yellow fever, dengue, chikungunya, other viral diseases (e.g., Zika virus), and filariasis.
[0005] In an attempt to reduce the problems associated with disease-transmitting mosquitoes, a wide variety of insecticides and insect repellents have been developed. Insecticides can be used to specifically kill mosquitoes when they are in the larval stage or once they have developed into adults. Thus, insecticides that kill larvae are called larvicides, while insecticides that specifically kill adult mosquitoes are called adulticides. Most insecticides that are commonly used to prevent the spread of disease target adult mosquitoes, and in particular, female adult mosquitoes.
[0006] The organochlorine DDT was the compound most widely used as an adulticide worldwide until its use was banned in most areas. Since then, organophosphates such as malathion, carbamates and propoxur have been widely used in vector control programs in most parts of the world and have been steadily replaced by pyrethroids, which have become the most commonly used adulticides. Organophosphates such as pirimiphos-methyl are now being used again due to the development of pyrethroid resistance in many important vector species.
[0007] One of the most important problems associated with pyrethroids, as with their predecessors, is that resistance has developed in many insect species in multiple regions of the world. Pyrethroid resistance, caused by specific detoxification enzymes or altered target mechanisms (kdr-type mutations in sodium channels), has been reported in most medically important mosquito species on most continents, such as Anopheles gambiae in Africa and Aedes aegypti in Asia. If resistance continues to develop and spread at the current rate, existing forms of this class of insecticides may become ineffective in the near future. Such a situation could have potentially devastating consequences in terms of public health, as there are no obvious alternatives for many uses of pyrethroids.
[0008] Therefore, insecticides for controlling mosquitoes, especially mosquitoes with developing resistance, such as resistance to pyrethroids, are continually sought.
[0009] Certain isoxazoline derivatives having insecticidal properties are disclosed, for example, in WO 2011 / 067272. One specific isoxazoline having insecticidal properties is isoxathiapiprolin.
[0010] Isotrione is an insecticidal agricultural chemical having the following CAS number: 2061933-85-3, and is represented by chemical formula (I):
[0011]
[0012] Isoxafenamide may include isomer (5S, 4R), which is 4-[(5S)-5-(3,5-dichloro-4-fluoro-phenyl)-5-(trifluoromethyl)-4H-isoxazol-3-yl]-N-[(4R)-2-ethyl-3-oxo-isoxazolidin-4-yl]-2-methyl-benzamide (CAS No.: 1309959-62-3), and at least one isomer optionally selected from isomer (5S, 4S), isomer (5R, 4R), isomer (5R, 4S), and any combination thereof. In the present invention, the isomer (5S, 4S) is 4-[(5S)-5-(3,5-dichloro-4-fluoro-phenyl)-5-(trifluoromethyl)-4H-isoxazol-3-yl]-N-[(4S)-2-ethyl-3-oxo-isoxazolidin-4-yl]-2-methyl-benzamide; the isomer (5R, 4R) is 4-[(5R)-5-(3,5-dichloro-4-fluoro-phenyl)-5-(trifluoromethyl)- isomer (5R,4S) is 4-[(5R)-5-(3,5-dichloro-4-fluoro-phenyl)-5-(trifluoromethyl)-4H-isoxazol-3-yl]-N-[(4S)-2-ethyl-3-oxo-isoxazolidin-4-yl]-2-methyl-benzamide. When isoxathiapiprolin further comprises at least one isomer selected from isomer (5S, 4S), isomer (5R, 4R), isomer (5R, 4S), and any combination thereof, isoxathiapiprolin may comprise a molar proportion of isomer (5S, 4R) greater than 50%, for example at least 55%, 60%, 65%, 70%, 75%, 80%, 85%, 90%, 95%, 96%, 97%, 98% or 99%, relative to the total amount of isomers (5S, 4R), (5S, 4S), (5R, 4R) and (5R, 4S).
[0013] Isoxafenamide has been found to be particularly useful against mosquitoes, including mosquito vectors of pathogenic diseases and mosquitoes that are resistant to insecticides such as pyrethroids.
[0014] Thus, the present invention provides a method for controlling nuisance, disease-carrying or pyrethroid-resistant mosquito pests, the method comprising applying a mosquitocidally effective amount of isoxathiapyr to such mosquito pests or to a locus where such control is desired.
[0015] In addition to the biological efficacy of isoxathiapiprole against mosquitoes and resistant strains of such mosquitoes, other embodiments of the present invention include its safety to the environment (including to users of vector control programs) (e.g., its toxicity, persistence); its suitability for use in the manufacture of vector control program products (whether indoor residual spray formulations, mosquito nets, or other types), its suitability for adhering to and remaining effective on surfaces over time (in the case where the program is an indoor residual spray), and its suitability for incorporation into polymeric products (e.g., nets) so that the compound can readily control mosquitoes on the surface of the nets over time (and these nets can withstand multiple washings).
[0016] In one embodiment, a method for controlling nuisance, disease-carrying or insecticide-resistant mosquito pests, particularly pyrethroid insecticide-resistant mosquito pests, according to the present invention comprises a method of controlling, limiting or eliminating mosquito pests that transmit disease pathogens.
[0017] In one embodiment, the isoxathiapiprolin according to the methods and other aspects of the invention is useful in controlling mosquitoes, particularly mosquitoes that are vectors of disease pathogens, more particularly mosquitoes that are resistant to insecticides (including pyrethroid-resistant insecticides), 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 quinquefasciatus, atroparvus), Anopheles balabacensis, Anopheles coluzzii, Anopheles culicifacies, Anopheles darlingi, Anopheles dirus, Anopheles farauti, Anopheles flavirostris, Anopheles fluviatilis, Anopheles freeborni, Anopheles funestus, Anopheles gambiae sl), 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 punctipennis, punctulatus), Anopheles quadrimaculatus, Anopheles sacharovi, Anopheles sergentii, Anopheles sinensis, Anopheles stephensi, Anopheles subpictus, Anopheles sundaicus, Anopheles superpictus, and Mansonia titillans, Ochlerotatus stimulans, Ochlerotatus japonicas (each of which is an example of a mosquito capable of carrying or acting as a vector for a pathogenic disease).
[0018] By control it is meant that isoxathiapiprole is used in a manner to kill or repel mosquitoes so that bites do not occur, or in a manner to reduce the mosquito population so that bites are not as frequent as before, or in a manner to inhibit target mosquitoes from feeding on blood.
[0019] In another embodiment, isoxathiapyr is useful in controlling one or more mosquitoes selected from the genera Anopheles, Culex and Aedes, particularly one or more of the following genera: Aedes aegypti, Aedes albopictus, Aedes japonicus, Aedes harassing, Culex harassing, Culex pipiens pallens, Culex pipiens sharp, Culex pipiens quinquefasciatus, Culex relict, Culex annularis, Anopheles pallens, Anopheles arabiensis, Anopheles kuruzi, Anopheles dabryanus, Anopheles dire, Anopheles sl, Anopheles gambiae ss (Ifakara strain), Anopheles gambiae Tiassale (An. gambiae Tiassale); Anopheles gambiae Kisumu (An. gambiae Kisumu), Anopheles gambiae KisKDR (An. gambiae KisKDR), Anopheles gambiae M'Bé (An. gambiae M'Bé), Anopheles melas (Anopheles melas), Anopheles minimus (Anopheles minimus), Anopheles sinensis (Anopheles sinensis), Anopheles stephensi and Mansoniatitillans.
[0020] In another embodiment, isoxathiapiprolid is useful in the methods and other aspects of the invention to control adult mosquitoes.
[0021] Insecticide-resistant mosquito species have also been detected, and thus in another embodiment, isoxathiapiprole is useful for controlling insecticide-resistant mosquitoes, such as pyrethroid- and / or carbamate-resistant mosquitoes.
[0022] Pyrethroids are the only insecticides recommended by the WHO for use against malaria vectors on indoor residual sprays (IRS) and durable insecticide mosquito nets (LLINs) in the form of α-cypermethrin, bifenthrin, cyfluthrin, permethrin, deltamethrin, λ-cyfluthrin and efenprox. Over the past decades, it has been the preferred chemical class in agricultural and public health applications because of its relatively low toxicity to humans, rapid knockdown effect, relative durability (3 to 6 months as IRS) and low cost. However, the extensive use of pyrethroids in agricultural applications and vector control has led to resistance in major malaria and dengue vectors. For example, strong resistance to the pyrethroid deltamethrin (and permethrin) has been reported in the Anopheles gambiae Tiassalé (from Southern Côte d'Ivoire) strain (Constant VAEdi et al., Emerging Infectious Diseases; Vol. 18, No. 9, September 2012). Pyrethroid resistance has also been reported for the Cayman Island strain of Aedes aegypti to permethrin, deltamethrin, and lambda-cyfluthrin (Angela F. Harris et al., Am. J. Trop. Med. Hyg., 83(2), 2010) and for some Anopheles strains to alpha-cypermethrin, permethrin, and lambda-cyfluthrin (Win Van Bortel, Malaria Journal, 2008, 7:102).
[0023] In another embodiment of the present invention, isoxathiapiprolin is suitable for use against insecticide-resistant mosquitoes selected from Anopheles gambiae RSPH, Anopheles gambiae Tiassalé, Anopheles gambiae Akron, Anopheles gambiae Kisumi Rdl, Anopheles Arabian NDjamina, Anopheles Kuruzzi VK7, Anopheles FUMOZ, Aedes aegypti GrandCayman, Culex pipiens strain POO and Anopheles Arabian (Kingani strain) highly resistant to pyrethroids.
[0024] In another embodiment, the methods of the invention are useful against resistant mosquitoes, such as those listed below:
[0025] Anopheles gambiae, strain RSPH is a multi-resistant mosquito (target site and metabolic resistance) described in the Malaria Research and Reference Reagent Resource Center reagent catalog (www.MR4.org; MR4 number: MRA-334).
[0026] Anopheles gambiae, Tiassalé strain is a multi-resistant mosquito (target and metabolic resistant strain) that shows cross-resistance between carbamates, organophosphates and pyrethroids and is described in: Constant VAEdi et al., Emerging Infectious Diseases; Vol. 18, No. 9, September 2012 and Ludovic P Ahoua Alou et al., Malaria Journal 9:167, 2010.
[0027] Anopheles gambiae, Akron strain is a multi-resistant mosquito (target and metabolic resistance strain) and is described in Djouaka F Rousseau et al., BMC Genomics, 9:538; 2008.
[0028] Anopheles kuruzii, strain VK7 is the resistant target mosquito and is described in Dabire Roch Kounbobr et al., Malaria Journal, 7:188, 2008.
[0029] The Anopheles gambiae, FUMOZ strain, is a metabolically resistant strain and is described in Hunt et al., Med Vet Entomol. 2005 Sep;19(3):271-5). In this article it has been reported that in South Africa, Anopheles gambiae, one of the main malaria vector mosquitoes in Africa, shows resistance to pyrethroid and carbamate insecticides.
[0030] Anopheles arabiensis (Kingani strain), a highly pyrethroid-resistant strain, originated from Ifakara and colonized in Bagamoyo.
[0031] Anopheles gambiae, Kisumi Rdl strain, a dieldrin-resistant strain from Kenya.
[0032] Anopheles arabiensis, strain NDjamina, a pyrethroid-resistant strain from Chad.
[0033] Aedes aegypti, Grand Cayman strain is the resistant target mosquito and is described in Angela F. Harris, Am. J. Tro. Med. Hyg. [American Journal of Tropical Medicine and Hygiene] 83(2), 2010.
[0034] Culex pipiens quinquefasciatus (strain P00 metabolically resistant to DDT); obtained from Texchem, Penang, Malaysia.
[0035] Koffi, AA, Ahoua, Alou, LP, Adja, MA, et al., Insecticide resistance status of Anopheles gambiae s.s population from M'Bé: a WHOPES-labelled experimental hut station, 10 years after the political crisis in d'Ivoire [Insecticide resistance status of Anopheles gambiae ss populations from M'Bé: a WHOPES-labeled experimental hut station, 10 years after the political crisis in Ivory Coast]. Malar J 12, 151 (2013).
[0036] Vector control programs are means of controlling vectors such as mosquitoes. Examples of such means are compositions, products and treated articles, which include substrates or non-living materials incorporated with (e.g., coated with or impregnated with) isoxathiapyr, spray products (e.g., indoor residual sprays and aerosol products) containing isoxathiapyr, coating compositions containing isoxathiapyr, and products or treated articles containing isoxathiapyr.
[0037] Examples of integrated mosquito vector management or control programs of the present invention (e.g., programs for controlling mosquito bites, blood sucking, or reducing related mosquito populations) include using such compositions, products, treated articles, and substrates of the present invention at locations where there is potential or known interaction between mosquito vectors and animals (including humans) susceptible to pathogenic diseases transmitted by such vectors. Suitable integrated programs 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 these sites.
[0038] Examples of substrates or non-living materials of the present invention are self-supporting films / sheets (e.g., screens), threads, fibers, yarns, pellets, fabrics (or textiles (e.g., for clothing)), nets, tents, and curtains incorporating (e.g., coated with or impregnated with) isoxathiacarb, which can be used to protect against mosquito bites and reduce blood sucking. Specifically, it is well known that humans can be protected from mosquito bites during their sleep by insecticide-coated sleeping nets. The coated or impregnated fabrics of the present invention can also be used as curtains in front of windows, door openings or vents to control mosquito entry into residences.
[0039] The compounds are used in substrates (e.g., nets and fabrics) of the present invention to achieve at least one of the following objectives:
[0040] ●Good insecticide effect
[0041] ●Fast-acting insecticide effect
[0042] ●Long-lasting insecticidal effect
[0043] ●Even release of active ingredients
[0044] ● Durability (including long-term resistance to multiple washings)
[0045] ●Simple production
[0046] ●Safe for users
[0047] The net and fabric (or textile) of the present invention that merge (for example, be coated with or be impregnated with) isoxathiazole are made of various natural and synthetic fibers, and can also be used as textile blend forms of woven or non-woven forms, such as knitwear or fibers. Natural fibers are for example cotton, raffia leaf fibers, jute, flax, sisal, burlap, wool, silk or hemp. Synthetic fibers can be made of polyamide, polyester, polyacrylonitrile, polyolefin (for example polypropylene or polyethylene), polytetrafluoroethylene and fiber mixture (for example mixture of synthetic fibers and natural fibers). Polyamide, polyolefin and polyester are as preferred fiber materials. Polyester, such as polyethylene terephthalate is particularly preferred. Most preferably, the net made of polyethylene and / or polypropylene.
[0048] The art discloses methods suitable for incorporating compounds (by coating methods) into nets and fabrics (see, for example, WO 2003 / 034823, WO 2008 / 122287, WO 01 / 37662, US2009036547, WO 2007 / 036710), including dipping or immersing them in a formulation of an insecticide, or spraying the formulation onto their surface. After treating the nets and fabrics of the present invention, they can be simply dried at ambient temperature (see below for more background information). Such methods are also suitable for incorporating (by coating) isoxathiapyr.
[0049] Also disclosed in the art is a method for combining a compound with a net or fabric by dipping, the method comprising preparing a polymer material in the presence of isoxazole wormamide, which is then extruded into fibers, lines or yarns for use in making nets and fabrics (see, for example, WO 08004711, WO 2009 / 121580, WO 2011 / 128380, WO 2011 / 141260, WO 2010 / 118743). Such nets and fabrics can obtain an effective amount of compound on the net and fabric surface to control mosquito bites. Typically, the compound is mixed with a molten polymer. Such methods are also suitable for combining (by dipping) isoxazole wormamide.
[0050] In the context of the compounds, additives and other insecticides of the present invention, the term "incorporating" or "incorporated" means that the substrate or non-living material comprises or contains the respectively defined compound, additive and / or insecticide (eg by coating or impregnation).
[0051] Preferably, the substrate of the present invention is a net, preferably a durable net, which is combined with isoxathiapiprolin by coating the net with a composition comprising isoxathiapiprolin, or by manufacturing a polymeric material in the presence of such isoxathiapiprolin and then processing the resulting polymeric material into the net of the present invention.
[0052] According to the present invention, when isoxathiapiprolin is used within a polymer, then during use of the resulting net or fabric made from the polymer, such isoxathiapiprolin is released to the surface of the net to control mosquito bites - this control is maintained at sufficient levels and for sufficient time.
[0053] Examples of suitable polymers are polyamides, polyesters, polyacrylonitrile, polyolefins, such as polyethylene compositions that can be made from different polyethylene polymers; these can be LDPE, LLDPE, MDPE and HDPE. LLDPE (Linear Low Density Polyethylene) is basically a linear polymer (polyethylene) with a large number of short chain branches, usually made by copolymerization of ethylene with long chain olefins. MDPE is a medium density polyethylene, basically a linear polymer of polyethylene with a shorter chain length than HDPE. HDPE (High Density Polyethylene) or Polyethylene High Density (PEHD) is a polyethylene thermoplastic. HDPE has almost no branches, so it has stronger intermolecular forces and tensile strength than low density polyethylene. It is also harder and more opaque, and can withstand slightly higher temperatures (120 degrees Celsius / 248 degrees Fahrenheit for short periods of time, 110 degrees Celsius / 230 degrees Fahrenheit continuously). HDPE yarn is stronger than LDPE mixed polyethylene yarn. Due to the absence of long chain branches, LLDPE is structurally different from traditional low density polyethylene (LDPE). These polyethylene compositions (HDPE, LDPE, LLDPE and mixtures thereof) are commonly used to prepare yarns and polyethylene-based textile products. Methods for incorporating insecticide compounds into polymers without impairing the resulting properties are known in the art, such as using mixtures of HDPE and LDPE. Such methods can also be used to incorporate isoxathiapiprolin into polymers.
[0054] An example of a spray product of the present invention is an indoor residual spray or space spray containing isoxathiapiprolin. Indoor residual spray (IRS) technology is to apply residual deposits of insecticides to indoor surfaces where media stay, such as walls and ceilings. The main goal of indoor residual spraying is to reduce the life span of mosquito vectors, thereby reducing or interrupting disease transmission. The secondary effect is to reduce the density of mosquitoes in the treatment area. IRS is a recognized, proven and cost-effective intervention method for controlling malaria, and it is also used to manage Leishmaniasis and Chagas disease. Many malarial mosquito vectors are home-dwelling and stay in houses after feeding on blood. These mosquitoes are particularly easy to control by indoor residual spray (IRS) containing isoxathiapiprolin. As its name implies, IRS involves coating the walls and other surfaces of houses with post-effect insecticides. Within a few months, isoxathiapiprolin will kill mosquitoes that come into contact with these surfaces. IRS does not directly prevent people from being bitten by mosquitoes. Instead, they typically kill mosquitoes after they feed, if they rest on the sprayed surface. Thus, IRS prevents the spread of infection to other people. To achieve this goal, IRS must be applied to a high percentage (usually greater than 70%) of households in a certain area. Although communities play a passive role in IRS programs, cooperation with IRS is the key to success. Community participation in IRS usually consists of cooperating with the spray team, removing food and covering surfaces before spraying, and avoiding covering treated surfaces with new paint or plaster. However, community or individual householder opposition to IRS has become a serious problem in some areas due to odor, mess, possible chemical exposure or sheer hassle. Therefore, sprays with good residual efficacy and acceptable odor according to the present invention are particularly suitable as components of an integrated mosquito vector management or control program.
[0055] In contrast to IRS (which requires the active ingredient isoxathiapiprolin to be combined with the surface of the residence (such as walls, ceilings), the spatial spray product of the present invention relies on the production of a large number of small insecticidal droplets, which are intended to be distributed through a certain volume of air over a given time. When these droplets hit the target mosquito, they will deliver a lethal dose of isoxathiapiprolin. Traditional methods for producing spatial sprays include thermal fogging (whereby a dense cloud of droplets of insecticide is produced, which looks like thick fog) and ultra-low volume (ULV) (whereby droplets are produced by cold, mechanical aerosol generators).
[0056] Since a large area can be treated at any one time, this method is a very effective way to quickly reduce the number of mosquitoes in a specific area. Since the residual activity after application is very limited, it must be repeated every 5 to 7 days in order to achieve full effect. This method is particularly effective in outbreaks where a rapid reduction in mosquito populations is required. Therefore, it can be used in urban dengue control activities.
[0057] Effective space spraying generally depends on the following specific principles:
[0058] Target insects usually fly through the spray cloud (or sometimes are struck when they land on exposed surfaces). Therefore, the contact efficiency between the spray droplets and the target insects is critical. This is achieved by ensuring that the spray droplets remain in the air for an optimal time and that they contain the appropriate dose of insecticide. Both of these issues are primarily addressed by optimizing the droplet size.
[0059] If the droplets are too large, they will fall to the ground too quickly and will not penetrate vegetation or other obstacles encountered during application (limiting the effective area of application). If one of these large droplets hits a single insect, this is also "overkill" because a high dose will be delivered to each insect.
[0060] • If the droplets are too small, they may not deposit on the target insect for aerodynamic reasons (no impact), or they may be carried upwards into the atmosphere by convective air currents.
[0061] • The optimum size of droplets for spatial spray applications are droplets with a volume median diameter (VMD) of 10 to 25 microns.
[0062] The composition of the present invention can be provided in the form of a spray product as an aerosol-based application, including atomized foam applications. Pressure cans are typical carriers for forming aerosols. Aerosol propellants compatible with the insecticide compound are used. Preferably, liquefied gas type propellants are used. Suitable propellants include compressed air, carbon dioxide, butane and nitrogen. The concentration of the propellant in the isoxazole insectamide composition is about 5% to about 40% by weight of the isoxazole insectamide composition, preferably about 15% to about 30% by weight of the isoxazole insectamide composition.
[0063] In one embodiment, the isoxathiapiprolin formulation of the present invention may also include one or more foaming agents. The foaming agents that can be used include sodium laureth sulfate, cocamide DEA and cocamidopropyl betaine. Preferably, sodium laureth sulfate, cocamide DEA and cocamidopropyl betaine are used in combination. The concentration of the one or more foaming agents in the isoxathiapiprolin composition is about 10% to about 25% by weight of the composition, more preferably 15% to 20% by weight.
[0064] When the isoxathiapiprolin formulation is used in an aerosol application without a blowing agent, the composition of the present invention can be used without direct mixing before use. However, aerosol formulations containing blowing agents need to be mixed (i.e., shaken) immediately before use. In addition, if the formulations containing blowing agents are used for long-term use, they may need to be regularly mixed additionally during use.
[0065] The residential area can also be treated with the isoxathiapiprolin composition of the present invention by using a combustion formulation containing the composition (such as a candle, cigarette or scented sheet). For example, the composition can be included in a household product, such as a "heated" air freshener, in which the insecticidal composition is released by heating (e.g., electric heating) or by combustion.
[0066] The composition containing isoxathiapiprole used in the method of the present invention may be provided as an aerosol, mosquito coil and / or a spray product for a vaporizer or a fogger.
[0067] The concentration of isoxathiapiprole in each polymer material, fiber, yarn, fabric, web or matrix of the present invention can vary within a relatively wide concentration range, for example from 0.05% to 15% by weight, preferably 0.2% to 10% by weight, more preferably 0.4% to 8% by weight, in particular 0.5% to 5% by weight, such as 1% to 3%.
[0068] The above percentages are based on the dry weight of the web or substrate or non-living material.
[0069] Similarly, the concentration of the compounds of the invention in the composition (whether for treating a surface or for coating a fiber, yarn, web, fabric) may vary within a relatively wide concentration range, for example from 0.1% to 70% by weight, such as 0.5% to 50% by weight, preferably 1% to 40% by weight, more preferably 5% to 30% by weight, in particular 10% to 20% by weight.
[0070] The concentration should be chosen according to the field of application in order to meet the requirements regarding insecticide efficacy, persistence and toxicity. The properties of the material can also be adjusted so that tailor-made textile fabrics can be obtained in this way.
[0071] When used in the IRS method of the present invention, isoxathiapiprolin (AI) is applied to the surface of the dwelling at a concentration of 0.01 g to 2 g of AI / m 2 , appropriately 0.05 g to 1 g of AI / m 2 , preferably 0.1 g to 0.7 g of AI / m 2 ; In particular, an AI of 100 mg to 200 mg / m 2 The amount of coverage exists.
[0072] Therefore, the effective amount of isoxathiapiprolin may depend on how it is used, the mosquitoes most desired to be controlled, and the environment in which it is used. Therefore, the effective amount of isoxathiapiprolin is sufficient to achieve control of mosquitoes; if:
[0073] ● For use as an IRS formulation, the effective amount is such that the coverage of the AI on the surface is 0.01 g to 2 g of AI / m 2 , preferably 0.05 g to 1 g of AI / m 2 , especially 0.1 g to 0.7 g of AI / m 2 , especially 100mg to 200mg AI / m 2 ;
[0074] ● For combined use within a web or matrix, an effective amount is 0.05% to 15% by weight, preferably 0.2% to 10% by weight, more preferably 0.4% to 8% by weight, especially 0.5% to 5% by weight, such as 1% to 3%.
[0075] Typically, when used in certain products of the invention, isoxathiapiprolin is distributed continuously in the thread, yarn, web or fabric, but may also be distributed partially or discontinuously in the thread, yarn, web or fabric. For example, a web may contain certain portions that are coated or made of impregnated fibers and other portions that are not coated or not made of impregnated fibers; alternatively, some of the fibers making up the web are impregnated or coated with the compound of the invention, while other fibers are not, or other fibers are impregnated or coated with another insecticide compound (see below).
[0076] The nets of the present invention impregnated or coated with isoxathiapiprole can meet the WHOPES standard of only 20 washes for long-lasting mosquito nets containing insecticides (see "Guidelines for laboratory and field testing of long-lasting insecticidal mosquito nets", 2005, http: / / www.who.int / whopes / guidelines / en / ), which means that the nets should not lose their biological activity after only approximately 20 wash cycles.
[0077] In one embodiment, the net of the present invention impregnated or coated with isoxathiapiprolin may have a biological activity in accordance with WHOPES guidelines, with a knockdown of between 95% and 100% after 60 minutes or a mortality of between 80% and 100% after 24 hours after at least 20, such as 25, preferably at least 30 and even more preferably at least 35 washes.
[0078] "WHOPES Directive" is to be understood as the Directive "Guidelines for laboratory and field testing of long-lasting insecticidal mosquito nets", 2005. This Directive is available at the following interactive address: http: / / www.who.int / whopes / guidelines / en / .
[0079] When the net is "impregnated" with isoxathiacarb to prepare the net of the present invention, the fibers constituting the net are made by melting the polymer, isoxathiacarb and optionally other compounds (such as other insecticides, additives, stabilizers). When the net is impregnated with such isoxathiacarb, the net of the present invention contains synthetic fibers; on the contrary, the net of the present invention coated with such isoxathiacarb contains synthetic fibers and / or natural fibers.
[0080] Polymeric materials useful in the compositions of the invention incorporating isoxathiapiprolin may be produced by mixing such isoxathiapiprolin with polymers in a liquid phase, and optionally other additives such as binders and / or synergists, and other insecticidal compounds.
[0081] Methods of preparing suitable polymeric materials and then processing them are described in the art - see for example WO09121580, WO 2011 / 141260.
[0082] For example, a net based on a polymer material containing an isoxathiapiprolin insecticide is produced by the following steps:
[0083] a) melting the polymer to be used and one or more insecticidal active ingredients together or separately at a temperature of 120°C to 250°C,
[0084] b) forming the melt of step a) into a yarn and cooling it,
[0085] c) optionally passing the yarns formed in step b) through a drawing system and drawing them, and then optionally finishing them,
[0086] d) weaving these threads into a web,
[0087] e) subjecting the web to a heat setting operation, wherein the temperature of the heat setting operation is selected to be 20 degrees Celsius below the melting temperature of the polymer used.
[0088] The heat setting in step e) of producing the web is preceded by a washing step. For this, water and a detergent are preferably used. The heat setting is preferably carried out in a dry environment.
[0089] Although the manufacture of the net combined with the insecticide compound can occur at a single location, it is also conceivable that different steps can occur at different locations. Thus, a composition comprising isoxathiacarb can be prepared and then processed into a polymer. Therefore, the present invention also provides a composition comprising isoxathiacarb in concentrated form, which composition may also contain additives (such as adhesives and / or synergists) and one or more other insecticidal compounds (the composition has been specifically prepared for the manufacture of polymer materials impregnated with isoxathiacarb (such compositions are generally referred to as "masterbatches")). The amount of isoxathiacarb in the masterbatch will depend on different circumstances, but can generally be 10% to 95% by weight, such as 20% to 90% by weight, preferably 30% to 85% by weight, more preferably 35% to 80% by weight, especially 40% to 75% by weight.
[0090] The present invention also provides compositions or preparations for coating walls, floors and ceilings inside buildings and for coating substrates or non-living materials, which compositions or preparations contain isoxathiacarb. For this purpose, known techniques can be used to prepare the compositions of the present invention, which may contain adhesives to promote the binding of the compound to surfaces or other substrates. Reagents useful for binding are known in the art and tend to be in polymer form. The adhesive type suitable for application to a composition having a specific porosity and adhesive properties is different from the type suitable for fibers, yarns, fabrics or nets-those skilled in the art can select a suitable adhesive based on known teachings.
[0091] Typical adhesives are polyvinyl alcohol, modified starch, polyvinyl acrylate, polyacrylic acid, polyvinyl acetate copolymer, polyurethane and modified vegetable oil. Suitable adhesives can include latex dispersions derived from various polymers and copolymers and combinations thereof. Suitable latex used as adhesive in the present composition comprises styrene, alkyl styrene, isoprene, butadiene, acrylonitrile lower alkyl acrylate, vinyl chloride, vinylidene chloride, vinyl esters of lower carboxylic acids and α, polymers and copolymers of β-ethylenically unsaturated carboxylic acids, these polymers and copolymers include polymers containing three or more different monomer species copolymerizations, and the rear dispersion suspension of siloxane or polyurethane. Polytetrafluoroethylene (PTFE) polymers are also suitable for active ingredients to be bonded to other surfaces.
[0092] The formulations according to the invention comprise at least one compound listed in Table 1 (or pesticide (A)) and a carrier, such as water (C), and optionally a polymeric binder or carrier (B) and further components (D).
[0093] The polymer binder binds the isoxathiapiprolin to the surface of the non-living material and ensures long-term action. The use of a binder reduces the elimination of the isoxathiapiprolin pesticide from the non-living material due to environmental influences (such as rainfall) or human influence on the non-living material (such as washing and / or cleaning). Other components can be additional insecticide compounds, synergists, UV stabilizers.
[0094] The composition of the present invention can have many different forms or formulation types, such as suspensions, capsule suspensions, and those skilled in the art can prepare relevant compositions based on the properties of isoxathiapiprole, its uses and also the type of application.
[0095] For example, the isoxathiapiprolin used in the methods and other aspects of the present invention can be encapsulated in a formulation. The encapsulated compound can provide improved wash fastness and longer active period. The formulation can be organic or aqueous, preferably aqueous.
[0096] The microencapsulated isoxathiapiprolin for use in the compositions and methods of the present invention is prepared using any suitable technique known in the art. For example, various methods for microencapsulation materials have been developed previously. These processes can be divided into three categories: physical methods, phase separation, and interfacial reactions. In the physical method category, the microcapsule wall material and the core particles are physically combined together, and the wall material flows to wrap the core particles to form microcapsules. In the phase separation category, microcapsules are formed by emulsifying or dispersing the core material in an immiscible continuous phase, dissolving the wall material in the immiscible continuous phase, and physically separating it from the continuous phase (such as by coagulation), and depositing it around the core particles. In the interfacial reaction category, microcapsules are formed by emulsifying or dispersing the core material in an immiscible continuous phase, and then interfacial polymerization occurs on the surface of the core particles. The concentration of isoxathiapiprolin present in the microcapsules can vary from 0.1% to 60% of the weight of the microcapsules.
[0097] The formulation according to the present invention can be formed by mixing all ingredients with water, optionally using a suitable mixing and / or dispersing aggregate. Typically, the formulation is formed at a temperature of 10 degrees Celsius to 70 degrees Celsius, preferably 15 degrees Celsius to 50 degrees Celsius, more preferably 20 degrees Celsius to 40 degrees Celsius.
[0098] It is possible to use the pesticide (A) (ie, isoxathiapiprole alone or in admixture with other suitable mosquito killer insects), the solid polymer (B), and optionally further additives (D) and disperse them in the aqueous component (C).
[0099] If a binder is present in the composition of the invention, preference is given to using a dispersion of the polymer binder (B) in water and an aqueous formulation of the pesticide (A) in water prepared separately beforehand. Such separate formulations may contain additional additives to stabilize (A) and / or (B) in the respective formulations and are commercially available. In a second process step, such a raw material formulation and optionally additional water (component (C)) are added.
[0100] It is also possible to combine, ie to use a preformed dispersion of (A) and / or (B) and mix it with the solids (A) and / or (B).
[0101] The dispersion of polymer binder (B) may be a pre-made dispersion that has been made by a chemical manufacturer.
[0102] However, it is also within the scope of the present invention to use a "hand-made" dispersion (i.e., a dispersion prepared on a small scale by an end user). Such a dispersion can be prepared by providing a mixture of about 20% binder (B) in water, heating the mixture to a temperature of 90 to 100 degrees Celsius and vigorously stirring the mixture for several hours.
[0103] The formulation can be manufactured as a final product so that it can be easily used by the end user in the method according to the invention. However, it is of course also possible to manufacture a concentrate, which can be diluted by the end user with further water (C) to the desired concentration for use.
[0104] In one embodiment, a composition suitable for IRS application or a coating formulation containing isoxathiapiprolin contains an active ingredient and a carrier (such as water), and may also contain one or more co-formulations selected from the following: a dispersant, a wetting agent, an antifreeze agent, a thickener, a preservative, an emulsifier, and a binder or sticker.
[0105] Furthermore, the formulation may be delivered to the end user in the form of a kit comprising at least:
[0106] A first component comprising at least one compound (A) listed in Table 1; and
[0107] • A second component comprising at least one polymeric binder (B).
[0108] • The further additive (D) may be a third separate component of the kit or may already be mixed with components (A) and / or (B).
[0109] The end user can prepare the formulation for use by adding water (C) to the components of the kit and mixing.
[0110] The components of the kit may also be formulations in water. Of course, an aqueous formulation of one component may be mixed with a dry formulation of one or more other components.
[0111] As an example, the kit may comprise
[0112] ● a formulation of a compound listed in Table 1 (A) and optionally water (C); and
[0113] • A second formulation, ie a separate formulation of at least one polymeric binder (B), water as component (C), and optionally component (D).
[0114] Thus, in a further aspect, the present invention provides a kit for treating fibers, yarns, webs and fabrics by coating thereon an insecticide having wash-resistant properties, the kit comprising: a first sachet comprising a pre-measured amount of at least one compound listed in Table 1, and a second sachet comprising a pre-measured amount of at least one polymeric binder. The resulting treated fibers, yarns, webs and fabrics have been endowed with insecticidal properties desirable for vector control, such as control of vector-carrying mosquitoes.
[0115] The concentrations of components (A), (B), (C) and optionally (D) will be selected by a person skilled in the art depending on the technique used for coating / treatment.
[0116] Typically, the amount of pesticide (A) may be up to 50% by weight, preferably 5 to 50%, such as 10 to 40%, especially 15 to 30% by weight, based on the weight of the composition.
[0117] The amount of polymer binder (B) may range from 0.01 to 30% by weight, preferably from 0.5 to 15%, more preferably from 1 to 10%, especially from 1 to 5% by weight, based on the weight of the composition.
[0118] Typically, if present, the amount of additional component (D) is 0.1% to 20%, preferably 0.5% to 15% by weight, based on the weight of the composition. If present, suitable amounts of pigments and / or dyes are typically 0.01% to 5%, preferably 0.1% to 3%, more preferably 0.2% to 2% by weight, based on the weight of the composition.
[0119] Typical formulations ready for use comprise from 0.1% to 40%, preferably from 1% to 30%, of components (A), (B) and optionally (D), the remainder being water (C).
[0120] Typical concentrations of the concentrates to be diluted by the end user may contain 5% to 70%, preferably 10% to 60%, of components (A), (B) and optionally (D), the remainder being water (C).
[0121] The formulations of the invention may be applied to polymeric materials before they are formulated into the desired product (eg while still in yarn or sheet form), or after they have been formed into the relevant product.
[0122] In the case of a web and / or fabric, the method for coating the web and / or fabric comprises at least the following steps:
[0123] a) treating webs and / or fabrics with an aqueous formulation according to the invention by any process step selected from the group consisting of:
[0124] (a1) passing the material through the formulation; or
[0125] (a2) contacting the material with a roller which is partially or completely immersed in the preparation and drawing the preparation to the side of the material in contact with the roller, or
[0126] (a3) immersing the material into the formulation; or
[0127] (a4) spraying the preparation onto the material; or
[0128] (a5) applying the preparation onto or into a material; or
[0129] (a6) applying the formulation in the form of a foam; or
[0130] (a7) applying the formulation to a material.
[0131] b) removing excess formulation, optionally by squeezing the material between the rollers or by means of a scraper; and
[0132] c) drying the material.
[0133] If the raw material contains residues from previous production processes (eg sizing agents, spinning aids, other auxiliaries and / or impurities), a washing step prior to coating may be beneficial.
[0134] In particular, the following details are important for steps a), b), and c).
[0135] Step a1)
[0136] The formulation is applied by passing the material through the aqueous formulation. Said step is referred to as filling by those skilled in the art. In a preferred embodiment, the material is completely immersed in a tank containing the aqueous formulation or the material is passed through the formulation held between two horizontally oriented rollers. According to the present invention, the material can be passed through the formulation, or the formulation can be passed through the material. The amount of liquid absorbed by the formulation will be affected by the stability of the concentrated bath, the need for uniform distribution, the density of the material and the desire to save energy costs in the drying and curing steps. Typical liquid absorption can be 40% to 150% of the weight of the material. Those skilled in the art are familiar with determining the optimal value. Step a1) is preferably used for coating open width materials that are subsequently customized into a web.
[0137] For small-scale production or re-coating of untreated webs, a simple hand-held roller is sufficient.
[0138] Step a2)
[0139] The aqueous formulation can also be applied to the material by means of a roller which is partially immersed in the dispersion, so that the dispersion is applied to the side of the material which is in contact with the roller (kiss-rolling). In this way, only one side of the material can be coated, which is advantageous when, for example, direct contact of human skin with the insecticide-treated material should be avoided.
[0140] The coating of the material in step a1), a2) or a3) is usually carried out at a temperature of 10 to 70 degrees Celsius, preferably 15 to 50 degrees Celsius, more preferably 20 to 40 degrees Celsius.
[0141] Step a4)
[0142] The spray can be applied in a continuous process or in a batch process in a suitable textile machine equipped with a spray device (for example in an open washer / extractor). This device is particularly suitable for impregnating finished webs.
[0143] Step a6)
[0144] The foam contains less water than the above-mentioned dispersion. The drying process can therefore be very short. It can be treated by injecting a gas or a gas mixture (e.g. air) therein. It may be necessary to add a surfactant, preferably with film-forming properties. Suitable surfactants and the required technical equipment are known to those skilled in the art.
[0145] Step a7)
[0146] The coating process can preferably be carried out in a knife coating process. The process conditions are known to those skilled in the art.
[0147] Step b)
[0148] Excess emulsion is usually removed by squeezing the material, preferably by passing the material through rollers known in the art, so as to achieve a determined amount of liquid absorption. The squeezed liquid can be reused. Alternatively, excess aqueous emulsion or dispersion can be removed by centrifugation or vacuum suction.
[0149] Step c)
[0150] Drying can be carried out at ambient temperature. In particular, this passive drying can be carried out in hot dry climates. Of course, the application of elevated temperatures can accelerate the drying process. Usually an active drying process will be carried out during high-scale processing. Drying is usually carried out at a temperature below 200 degrees Celsius, preferably at a temperature of 30 degrees Celsius to 170 degrees Celsius, more preferably at room temperature. The choice of temperature is determined by the thermal stability of the insecticide in the formulation and the thermal stability of the impregnated non-living material.
[0151] For the method according to the invention, aqueous formulations comprising at least one pigment and / or at least one dye can be used so that the material is not only coated with the isoxathiapiprolin pesticide but is also dyed in the same time.
[0152] In another aspect, the present invention provides a method for treating fibers, yarns, webs and fabrics by applying an insecticide having wash-resistant properties, the method comprising (i) preparing a treatment composition comprising at least one compound listed in Table 1, (ii) treating the fibers, yarns, webs and fabrics, and (iii) drying the resulting treated fibers, yarns, webs and fabrics.
[0153] The polymer binder (B) may be dispersed in an aqueous formulation and comprises one or more fluorinated acrylic copolymers useful in water and oil resistant formulations, including copolymers prepared by polymerizing perfluoroalkyl acrylate monomers and comonomers, particularly acrylate monomers. The binder may also be a fluorocarbon resin (as described in WO 2006 / 128870).
[0154] Only water is used as solvent for the formulation. However, trace amounts of water-miscible organic solvents may be present. Examples of solvents include water-miscible alcohols, such as monohydric alcohols (such as methanol, ethanol or propanol), higher alcohols (such as ethylene glycol or polyether polyols) and ether alcohols (such as butyl glycol or methoxypropanol). Preferably, the content of organic solvent does not exceed 5% by weight (based on component (C)), more preferably does not exceed 1% by weight (based on component (C)), specifically does not exceed 0.1% by weight (based on component (C)).
[0155] Depending on the intended use of the non-living material to be treated, the formulation according to the invention may further comprise one or more components or additives (D) selected from the group consisting of preservatives, detergents, fillers, impact modifiers, antifogging agents, foaming agents, clarifiers, nucleating agents, coupling agents, fixatives, crosslinking agents, conductivity enhancers (antistatic agents), stabilizers such as antioxidants, carbon and oxygen radical scavengers and peroxide decomposers, etc., flame retardants, mold release agents, agents with UV protective properties, spreading agents, antiblocking agents, antimigration agents, foaming agents, antifouling agents, thickeners, additional biocides, wetting agents, plasticizers and film formers, adhesives or antiblocking agents, optical brighteners (fluorescent brighteners), pigments and dyes.
[0156] Typical amounts of polymeric binder (B) are from 0.01% to 10% by weight (dry weight) of the material (dry). As a general guideline, the weight ratio between insecticide and binder (B) should be approximately constant, its value depending on the insecticidal ability and migration ability of the insecticide, i.e. the higher the amount of insecticide, the higher the amount of binder (B). The preferred amount of binder (B) is from 0.1% to 5% by weight, more preferably 0.2% to 3% by weight of the weight (dry weight) of the material.
[0157] The coated material may contain at least one pigment and / or at least one dye. The amount of at least one dye is typically from 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 weight of the material (dry weight).
[0158] The method for coating or processing non-living material is not limited to specific technology. Can be coated by non-living substrate immersion bath or immersion in preparation or by spraying preparation on the surface of non-living material.After processing, can be by processed non-living substrate simply drying at ambient temperature.
[0159] Therefore, no complicated technology is required for the coating, and thus the coating process can be carried out by the end user himself on a small scale.
[0160] For example, a typical end-user may coat / treat the web himself, for example, in his home using a formulation according to the invention.For this purpose, the use of a kit as defined herein is particularly advantageous.
[0161] In one embodiment, the present invention provides a polymer, fiber, thread, yarn, web or fabric comprising one or more compounds of the present invention (listed in Table 1), wherein one or more other conventional materials for making such polymers may also be incorporated, and the polymer, fiber, thread, yarn, web or fabric may optionally further incorporate one or more other insecticides and / or synergists.
[0162] In one embodiment, the present invention provides a net or fabric in combination with one or more isoxathiapiprole (listed in Table 1), optionally further in combination with one or more other insecticides and / or synergists.
[0163] As described in the art, isoxathiapiprolin useful in the methods and other aspects of the invention can be used alone or in combination with another insecticide, synergist, repellent, chemical sterilant, flame retardant, UV protectant / absorber and / or additive for controlled release properties.
[0164] When used according to the present invention, isoxathiapiprole can be used alone to control mosquitoes, or in combination with one or other known insecticides and / or one or more additives (such as synergists) - in polymers for making non-living substrates (such as nets and fabrics), in formulations for treating non-living substrates (such as nets and fabrics), in IRS products and space spray products.
[0165] In one embodiment, the present invention provides a composition comprising one or more compounds of the present invention (which can be used to coat polymeric materials or products formed thereof, or is useful as a spray product), which composition optionally further comprises one or more other insecticides and / or synergists and one or more other additives.
[0166] Examples of synergists are piperonyl butoxide (PBO), sebacate esters, fatty acids, fatty acid esters, vegetable oils, esters of vegetable oils, alcohol alkoxylates and antioxidants.
[0167] 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-piperidyl) sebacate (BLS292).
[0168] Suitable fatty acids are (preferably monounsaturated or polyunsaturated) fatty acids with a chain length of 12 to 24 carbon atoms, for example palmitoleic acid, oleic acid, elaidic acid, octadecenoic acid, eicosenoic acid, cetylene acid, erucic acid, nervonic acid, linoleic acid, α-linolenic acid, γ-linolenic acid, arachidonic acid, eicosapentaenoic acid, docosapentaenoic acid and docosahexaenoic acid. Particularly preferred are oleic acid, linoleic acid, α-linolenic acid and γ-linolenic acid.
[0169] Suitable fatty acid esters are preferably methyl or ethyl esters of the above-mentioned fatty acids. Methyl esters are particularly preferred. Fatty acids and their esters may also each be present in a mixture.
[0170] Useful vegetable oils include all oils of plant origin that are usually available in agrochemical compositions. As examples, mention may be made of sunflower oil, rapeseed oil, olive oil, castor oil, colza oil, corn kernel oil, cottonseed oil and soybean oil. Rapeseed oil is preferred.
[0171] Suitable esters of vegetable oils are the methyl or ethyl esters of the above mentioned oils. The methyl esters are preferred.
[0172] Antioxidants useful as additives include, for example, butylated hydroxytoluene, butylated hydroxyanisole and L-ascorbic acid.
[0173] Plant essential oils can also be used in the indoor residual spray composition; examples are those selected from citronella, peppermint oil, d-limonene and Siberian fir. These plant essential oil materials are known and used for other purposes and can be prepared by the skilled artisan using known methods and are also commercially available.
[0174] In addition to isoxathiapiprole, the methods, compositions, polymers, products, matrices and / or integrated mosquito management programs according to the invention may contain one or more additional insecticidal active ingredients. Specifically, examples are one or more active ingredients from the following classes: organophosphates, pyrethroids, carbamates or neonicotinoids and DDT, indoxacarb, nicotine, sulfometuron, cartap, spinosad, camphechlor, chlordane, endosulfan, gamma-HCH, HCH, heptachlor, lindane, methoxychlor, acetoprole, ethiprole, fipronil, pyrafluprole, pyriprole, flupyrazole vaniliprole, avermectin, emamectin, avermectin benzoate, ivermectin, milbemycin, fenoxycarb, epofenonane, fenoxycarb, hydroprene, kinoprene, methoprene, pyriproxifen, triprene, chlorfenapyr, methoxyfenapyr, fenpyroxil, bistrifluan, chlofluazuron, diflubenzuron, fluazuron, flufenoxuron flucycloxuron, flufenoxuron, hexaflumuron, lufenuron, novaluron, noviflumuron, penfluoron, teflubenzuron, triflumuron, buprofezin, cyromazine, diafenthiuron, azocyclotin, cyhexatin tin), fenbutatin-oxide, chlorfenapyr, binapacyrl, dinobuton, dinocap, DNOC, fenazaquin, fenpyroximate, pyrimidifen, pyridaben, tebufenpyrad, tolfenpyrad, hydramethylnon, dicofol,Rotenone, acequinocyl, fluacrypyrim, Bacillus thuringiensis strains, spirodiclofen, spiromesifen, spirotetramat, ethyl 3-(2,5-dimethylphenyl)-8-methoxy-2-oxo-1-azaspiro[4.5]dec-3-en-4-yl acetate (alias: carbonic acid, 3-(2,5-dimethylphenyl)-8-methoxy-2-oxo-1-azaspiro[4.5]dec-3-en-4-yl ethyl ester, CAS Registry Number: 382608-10-8), flonicamid, amitraz, propargite, flubendiamide, chloranthraniliprol, thiocyclam oxalate, thiosultap-sodium, azadirachtin, Bacillus species, Beauveria species, Metarrhizium species, Paecilomyces species, Thuringiensin, Verticillium species, aluminum phosphide phosphide), bromomethyl, fluorosulfonyl, cryolite, flonicamid, pymetrozine, clofentezine, etoxazole, hexythiazox, amidoflumet, benclothiaz, benzoximate, bifenazate, bromopropylate, buprofezin, chinomethionate, chlordim eform), chlorobenzilate, chloropicrin, clothiazoben, cycloprene, cyflumetofen, dicyclanil, fenoxacrim, fentrifanil, flubenzimine, flufenerim, flutenzin, gossyplure, hydramethylnone, japonilure, metoxadiazone,Petroleum, piperonyl butoxide, kaliumoleat, pyridalyl, sulfluramid, tetradifon, tetrasul, triarathene and verbutin.
[0175] In another aspect, the present invention provides a method for protecting mammals (including humans) from mosquitoes, the method comprising applying to the mosquitoes or at a location where there is a potential or known interaction between mammals and mosquitoes a vector control regimen comprising a mosquitoicidally effective amount of a compound selected from the group consisting of isoxathiapyr.
[0176] Another aspect of the invention is a method for controlling the spread of a vector-borne disease, the method comprising: identifying a mosquito vector; and contacting the mosquito vector or its environment with a vector control regimen comprising a mosquitoicidally effective amount of a compound selected from the group consisting of isoxathiapyr.
[0177] An aspect of the present invention also includes a method of controlling mosquitoes, the method comprising contacting a mosquito or its environment with a vector control regimen comprising a mosquitoicidally effective amount of a compound selected from the group consisting of isoxathiapyr.
[0178] The present invention also provides a method comprising: (i) identifying a location where there is potential or known interaction between mosquito vectors and mammals (including humans) susceptible to pathogenic disease infection when contacted by such vectors, and (ii) placing a vector control program at the location, wherein the program comprises a mosquitoicidally effective amount of a compound selected from the group consisting of isoxathiapyr.
[0179] The present invention will also be expected to control many viruses carried by such vectors by controlling mosquitoes. As an example, Zika virus infection may be controlled by controlling mosquitoes of the genus Aedes using one or more defined compounds (Table 1) as part of a vector control program. Examples of mosquitoes reported to spread Zika virus are Aedes, such as Aedes aegypti and Aedes albopictus. Therefore, on the one hand, the present invention provides a method for controlling Zika virus infection, wherein one or more defined compounds (Table 1) are present in mosquito-killing effective amounts near Aedes (such as Aedes aegypti and Aedes albopictus). Near mosquitoes means areas where mosquitoes may be present (such as in the general environment, particularly in a room) or positions where mosquitoes bite individuals or mammals (e.g., on the surface of the skin).
[0180] In each method according to the present invention, the vector control regimen is preferably one or more of a composition, a product and a treated article, each comprising a compound selected from the group consisting of isoxathiapiprolin.
[0181] As used herein, "fiber" simply refers to thin, thread-like pieces, usually made from natural materials such as cotton or jute.
[0182] In each aspect and each embodiment of the present invention, "consisting essentially of" and its inflections are preferred embodiments of "comprising" and its inflections, and "consisting of" and its inflections are preferred embodiments of "consisting essentially of" and its inflections.
[0183] The disclosure of the present application enables every combination of the embodiments disclosed herein to be achieved.
[0184] The following examples are provided to illustrate the present invention. They are not intended to limit the present invention.
[0185] Biological Examples:
[0186] Examples B1-B3: Bottle assays are based on the CDC Guidelines for Assessing Insecticide Resistance in Vectors Using Bottle Bioassays
[0187] 1 ml of acetone containing defined concentrations of test compounds, and 1500 ppm Mero (Bayer Crop Science) are added to 250 ml glass bottles and the bottles are placed on a rolling table so that the solvent coats the interior surfaces as it evaporates. Once dry, approximately 25 non-hematophagous adult female mosquitoes of the appropriate species and strain (two or three days old each) are aspirated from the stock culture and gently blown into the exposure bottle. The bottles are capped and placed upright under standard culture conditions, out of direct sunlight, at a nominal temperature of 28°C and a relative humidity of 60%-80%.
[0188] Start a stopwatch and assess knockdown after 60 minutes. A mosquito is considered knocked down if it cannot stand, as defined by the CDC.
[0189] After one hour, mosquitoes were carefully removed from the bottles using an insect extractor and placed in a recovery cup. The mosquitoes were provided with a 10% sucrose solution using cotton plugs and stored under culture conditions. Mortality was assessed after 24 and 48 hours.
[0190] Each treatment was replicated at least three times and the average knockdown or mortality was recorded. In each study, a group of bottles was infested with a known insecticide-susceptible mosquito strain from the same genus as the resistant strain. The results are shown in Tables B1-B3.
[0191] Table B1
[0192]
[0193] Table B2
[0194]
[0195] Table B3
[0196]
Claims
1. Use of isoxathiapiprolin in mosquito control.
2. Use of isoxathiapiprolin in controlling mosquito insects that are disease vectors.
3. Use of isoxathiapiprole in controlling mosquito insects that are vectors of malaria.
4. Use of isoxathiapiprole according to any one of the preceding claims, wherein the mosquito is an insecticide-resistant mosquito.
5. Use of isoxathiapiprole according to any one of the preceding claims, wherein the mosquito is a pyrethroid insecticide-resistant mosquito.
6. Use of isoxathiapiprole according to any one of the preceding claims, wherein the mosquito is selected from the genera Anopheles, Culex and Aedes.
7. The use of isoxathiapiprolin according to any one of the preceding claims, wherein the mosquito is selected from Aedes aegypti, Aedes albopictus, Aedes japonicus, Aedes harassing, Culex pipiens, Culex pipiens pallens, Culex pipiens sharp, Culex pipiens quinquefasciatus, Culex pipiens residual, Culex pipiens annularis, Anopheles pallens, Anopheles arabiensis, Anopheles kuruzi, Anopheles dabryanus, Anopheles dire, Anopheles catarrhalis, Anopheles gambiae sl, Anopheles gambiae ss (Ifakara strain), Anopheles gambiae Tiassale; Anopheles gambiae Kisumu, Anopheles gambiae KisKDR, Anopheles gambiae M'Bé, Anopheles milas, Anopheles minimus, Anopheles sinensis, Anopheles stephensi and Mansonia truncatula.
8. A method for preparing a polymer material impregnated with isoxathiapiprolin, which material can be used to make substrates or non-living materials such as threads, fibers, yarns, pellets, nets and fabrics, the method comprising mixing a polymer with isoxathiapiprolin at a temperature between 120°C and 250°C.
9. A method for controlling nuisance, disease-carrying or pyrethroid-resistant mosquito insect pests, the method comprising applying a mosquitocidally effective amount of isoxathiapyr to such mosquito pests or to a locus where such control is desired.
10. A method for mosquito insect control according to claim 9, comprising (a) applying an effective amount of a liquid composition comprising isoxathiapiprole, and optionally, a polymer binder or carrier, one or more other insecticides and / or synergists to a dwelling surface; and / or (b) placing a matrix or non-living material combined with isoxathiapiprole, and optionally, an additive, one or more other insecticides and / or synergists in a dwelling.
11. The method of any one of the preceding claims, wherein the mosquito insect is a disease vector.
12. The method according to any one of the preceding claims, wherein the mosquito insect is a malaria vector.
13. The method of any one of the preceding claims, wherein the mosquito insect is an insecticide-resistant mosquito.
14. The method according to any one of the preceding claims, wherein the mosquito insect is a pyrethroid insecticide-resistant mosquito.
15. The method according to any one of the preceding claims, wherein the mosquito insect is selected from the genera Anopheles, Culex and Aedes.
16. The method according to any one of the preceding claims, wherein the mosquito insect is selected from the group consisting of Aedes aegypti, Aedes albopictus, Aedes japonicus, Aedes harassing, Culex pipiens, Culex pipiens pallens, Culex pipiens quinquefasciatus, Culex pipiens relictus, Culex pipiens annularis, Anopheles pallens, Anopheles arabiensis, Anopheles kuruzi, Anopheles dabryanus, Anopheles dirus, Anopheles fascis, Anopheles gambiae sl, Anopheles gambiae ss (Ifakara strain), Anopheles gambiae Tiassale; Anopheles gambiae Kisumu, Anopheles gambiae KisKDR, Anopheles gambiae M'Bé, Anopheles milas, Anopheles minimus, Anopheles sinensis, Anopheles stephensi and Mansonia cutis.
17. A net combined with isoxathiapiprolin having a biological activity in accordance with WHOPES guidelines: between 95% and 100% knockdown after 60 minutes and / or between 80% and 100% mortality after 24 hours after 20 washes.
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