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    • 专利摘要:
    abstract patent of invention: "synergistic fungicidal mixtures for fungal control in cereals". the present invention relates to a fungicidal composition containing a fungicidally effective amount of (a) the compound of formula i, (3s, 6s, 7r, 8r) -8-benzyl-3- (3 - ((isobutyryloxy ) methoxy) -4-methoxypolinolinido) -6-methyl-4,9-dioxo-1,5-dioxonan-7-yl, and (b) fluxpyroxade, and provides synergistic control of selected fungi.
    公开号:BR112015015351B1
    申请号:R112015015351-8
    申请日:2013-12-23
    公开日:2020-06-16
    发明作者:David G. Ouimette；J. Todd Mathieson；Gregory M. Kemmitt
    申请人:Dow Agrosciences Llc；
    IPC主号:
    专利说明:

    Descriptive Report of the Invention Patent for SYNERGIC FUNGICIDE MIXTURE, FUNGICIDE COMPOSITION, AND METHOD FOR TREATING A PLANT.
    CROSS REFERENCE TO RELATED DEPOSIT REQUESTS
    [001] This application claims the benefit of Patent Application
    Provisional Serial No. US 61 / 747,094, filed on December 28, 2012, which is expressly incorporated by reference in this document.
    FIELD
    [002] This description refers to a synergistic fungicidal composition containing (a) the compound of Formula I and (b) fluxpyroxade. BACKGROUND
    [003] Fungicides are compounds, of natural or synthetic origin, that act to protect plants against damage caused by fungi. Current farming methods are highly dependent on the use of fungicides. In fact, some crops cannot be usefully grown without the use of fungicides. The use of fungicides allows a grower to increase the yield and quality of the crop and, consequently, to increase the value of the crop. In most situations, the increase in the value of the crop is worth at least three times the cost of using the fungicide.
    [004] However, no fungicide is useful in all situations and the repeated use of a single fungicide often results in the development of resistance to that and related fungicides. Consequently, research has been carried out to produce fungicides and combinations of fungicides that are safer, that perform better, that require lower dosages, that are easier to use, and that cost less.
    [005] Synergism occurs when the activity of two or more
    Petition 870190095737, of 09/25/2019, p. 4/30
    2/20 compounds exceed the activities of the compounds when used individually.
    summary
    [006] One purpose of this description is to provide synergistic compositions that comprise fungicidal compounds. Another objective of this description is to provide processes that use these synergistic compositions. Synergistic compositions are able to prevent or cure, or both, diseases caused by fungi of the class Ascomycetes. In addition, synergistic compositions have increased efficacy against Ascomycete pathogens, including wheat leaf spot. According to this description, synergistic compositions are provided together with methods for their use.
    [007] Some embodiments include a synergistic fungicidal mixture comprising a fungicidally effective amount of the compound of Formula I and fluxpyroxade.
    [008] Some embodiments include a mixture of the compound of Formula I and fluxpyroxade in which the weight ratios of the compound of Formula I to fluxpyroxade is from about 1: 1 to about 16: 1. In some particular embodiments, the weight ratio is about 1: 2 to about 16: 1, about 1: 4 to about 16: 1, or about 1: 8 to 16: 1. In other more particular embodiments, the weight ratio is from about 1: 1 to about 8: 1, from about 1: 1 to about 4: 1, or about 1: 1 to about 1: 2.
    Petition 870190095737, of 09/25/2019, p. 5/30
    3/20
    [009] Some embodiments include a mixture of the Formula I compound and fluxpyroxade in which the weight ratios of the Formula I compound to fluxpyroxade include ratios selected from the group of ratios consisting of: about 1: 1, about 1 : 2, about 1: 3, about 1: 4, about 1: 5, about 1: 6, about 1: 7, about 1: 8, about 1: 9, about 1:10 , about 1:11, about 1:12, about 1:13, about 1:14, about 1:16, about 2: 1, about 3: 1, about 4: 1, about about 5: 1, about 6: 1, about 7: 1, about 8: 1, about 9: 1, about 10: 1, about 11: 1, about 12: 1, about 13 : 1, about 14: 1, and about 16: 1, or within any defined range between any two previous values.
    [0010] Some embodiments include a mixture in which the ratio of the Formula I compound to fluxpyroxade is about 1 to about 1. Some modalities include a mixture in which the ratio of the Formula I compound to fluxpyroxade is about 1 to about of 2. Some modalities include a mixture in which the ratio of the Formula I compound to fluxpyroxade is about 1 to about 3. Some modalities include a mixture in which the ratio of the Formula I compound to fluxpyroxade is about 1 to about of 4. Some modalities include a mixture in which the ratio of the Formula I compound to fluxpyroxade is about 1 to about 5. Some modalities include a mixture in which the ratio of the Formula I compound to fluxpyroxade is about 1 to about of 6. Some modalities include a mixture in which the ratio of the Formula I compound to fluxpyroxade is about 1 to about 7. Some modalities include a mixture in which the ratio of the Formula I compound to fluxpyroxade is about 1 to about 8. Some modalities include a mixture in which the ratio of the Formula I compound to fluxpyroxade is about 1 to about 9. Some modalities include a mixture in which the ratio of the Formula I compound to fluxpyroxade
    Petition 870190095737, of 09/25/2019, p. 6/30
    4/20 xade is about 1 to about 10. Some embodiments include a mixture in which the ratio of the Formula I compound to fluxpyroxade is about 1 to about 11. Some embodiments include a mixture in which the ratio of the compound to Formula I for fluxpyroxade is about 1 to about 12. Some modalities include a mixture in which the ratio of the compound of Formula I to fluxpyroxade is about 1 to about 13. Some modalities include a mixture in which the ratio of the compound of Formula I for fluxpyroxade is about 1 to about 14. Some embodiments include a mixture wherein the ratio of the compound of Formula I to fluxpyroxade is about 1 to about 16. Still other modalities include a fungicidal composition comprising a fungicidally amount efficacy of the fungicidal mixture and an agriculturally acceptable adjuvant or vehicle.
    [0011] Still other modalities include methods for treating a plant, which comprises the step of: applying a fungicidally effective amount of a mixture that includes the compound of Formula 1 and fluxpyroxade to a surface selected from at least one surface selected from of the surface group consisting of: at least a portion of a plant, soil adjacent to a plant, soil in contact with a plant, seeds, and equipment used in contact with a plant or a surface adjacent to a plant. In some embodiments, the fungicidally effective amount of the mixture is applied in the range of about 30 grams / hectare (g / ha) to about 200 g / ha of fluxpyroxade and about 35 g / ha to about 300 g / ha of Formula 1 compound.
    Detailed Description
    [0012] The present description relates to a synergistic fungicidal mixture comprising a fungicidally effective amount (a) of the compound of Formula I, (3 S, 6 S, 7 R, 8 R) -8-benzyl-3- (3 - (((isobutyryloxy) methoxy) -4-methoxypicolinamido) -6-methyl-4,9-dioxo-1,5-dioxonan-7-yl isobutiPetition 870190095737, of 25/09/2019, p. 7/30
    5/20 rat, and (b) fluxpyroxade, 3- (difluoromethyl) -1-methyl-N- (3 ', 4', 5'-trifluorobiphenyl 1-2-1) pi razol-4-carboxamide.
    [0013] The compound of Formula I is described in US No. 6,861,390 (which is hereby incorporated by reference in its entirety for reference).
    [0014] Fluxapiroxade is described in The e-Pesticide Manual,
    Version 5.2, 2011. The structure of fluxpyroxade is as follows:
    [0015] In the composition described in this document, the weight ratios of the compound of Formula I for fluxpyroxade in which the fungicidal effect is synergistic include ratios in the ranges of about 1: 1, about 1: 2, about 1: 3 , about 1: 4, about 1: 5, about 1: 6, about 1: 7, about 1: 8, about 1: 9, about 1:10, about 1:11, about 1:12, about 1:13, about 1:14, about 1:16, about 2: 1, about 3: 1, about 4: 1, about 5: 1, about 6 : 1, about 7: 1, about 8: 1, about 9: 1, about 10: 1, about 11: 1, about 12: 1, about 13: 1, about 14: 1 , and about 16: 1. Except where clearly noted or clearly implied otherwise, the term about,
    Petition 870190095737, of 09/25/2019, p. 8/30
    6/20 as used in this document, refers to a range of plus or minus 10%, for example, about 1 includes the range of values from 0.9 to 1.1.
    [0016] The rate at which the synergistic composition is applied will depend on the particular type of fungus that will be controlled, the degree of control required and the time and method of application. In general, the composition of the description can be applied at an application rate between about 50 grams per hectare (g / ha) and about 1500 g / ha based on the total amount of active ingredients in the composition. In other embodiments, the composition of the description can be applied at an application rate between about 65 grams per hectare (g / ha) and about 500 g / ha based on the total amount of active ingredients in the composition. Fluxapyroxade is applied at a rate between about 30 g / ha and about 200 g / ha and the Formula I compound is applied at a rate between about 35 g / ha and about 300 g / ha.
    [0017] The components of the synergistic mixture of the present description can be applied separately or as part of a multi-part fungicidal system. The synergistic blend of the present description can be applied in conjunction with one or more other fungicides to control a wider range of unwanted diseases. When used in conjunction with other fungicide (s), the currently claimed compounds can be formulated with the other fungicide (s), mixed in tank with the other fungicide (s) ) or applied sequentially with the other fungicide (s). Such other fungicides may include (RS) -N- (3,5-dichlorophenyl) -2- (methoxymethyl) succinimide, 1,2-dichloropropane, 1,3-dichloro-1,1,3,3-tetrafluoroacetone hydrate, 1-chloro-2,4-dinitronaphthalene, 1-chloro-2-nitropropane, 2 (2-heptadecyl-2-imidazolin-1-yl) ethanol, 2,3-dihydro-5-phenyl-1,4- diti-ina
    1,1,4,4-tetraoxide, 2-methoxyethylmercury acetate, 2-methoxyethylmercury chloride, 2-methoxyethylmercury silicate, 3- (4-chlorophenyl) -5
    Petition 870190095737, of 09/25/2019, p. 9/30
    7/20 methylrodanine, 4- (2-nitroprop-1-enyl) phenyl thiocyanate, N-3, 5-dichlorophenyl-succinimide, N-3-nitrophenylitaconimide, 2- (thiocyanatomethylthio) -benzothiazole, (3-ethoxypropyl) bromide mercury, 2-methoxyethylmercury chloride, 2-phenylphenol, 8-hydroxyquinoline sulphate, 8-phenylmercurioxiquinoline, acibenzolar, acibenzolar-S-methyl, acypetacs, acypetacscobre, acypetacs-zinc, albendazole, aldimide, aldimide, aldimide , amobam, Ampelomices quisqualis, ampropylfos, anilazine, antimycin, asomato, aureofungin, azaconazole, azitiram, azoxystrobin, Bacillus subtilis, Bacillus subtilis QST713 strain, barium polysulphide, Baier 32394, benalaxyl, benaloxyl, benaloxyl, benaloxyl, benaloxyl, , bentiavalicarb, isopropyl bentiavalicarb, bentiazole, benzamacril, benzamacryl-isobutyl, benzamorph, benzohydroxamic acid, benzovindiflupir, benzylaminobenzene sulfonate salt (BABS), berberine, berberine chloride, betoxhi, bicarbonate, bicarbonate, bicarbonate, bicarbonate napacril, biphenyl, bismertiazole, bis (methylmercury) sulphate, bis (tributyltin) oxide, bitertanol, bitionol, bixafen, blasticidin-S, borax, Bordeaux mixture, boscalide, bromotalonil, bromuconazole, bupyrimide, bupyrimide, buttered butylamine, cadmium sulfate, calcium, copper, zinc, chromate, calcium polysulfide, Candida oleofila, captafol, captan, carbamorph, carbendazim, carbendazim benzenesulfonate, carbendazim sulfite, carboxamide, carpropamide, carvacrol, carvone, ECSC, Chesh mix , quinomethionate, chitosan, clazafenone, clobentiazone, chloraniformethane, chloranil, chlorphenazole, chlorodinitronaphthalenes, chlorquinox, chloroneb, chloropicrin, chlorotalonil, clozolinate, climbazol, clotrimazole, Coniotirium minitans, copper acetate, copper oxide acetate , basic, copper hydroxide, copper naphthenate, copper octanoate, copper oleate, copper oxychloride, copper silicate, copper sulphate, copper sulphate (tribasi co), copper and zinc chromate, cumoxystrobin, cresol, cufraneb, cupric hydrazinium sulfate, cuprobam, oxide
    Petition 870190095737, of 09/25/2019, p. 10/30
    8/20 of cuprous, cyzofamide, cyclamfuramide, cycloheximide, cyflufenamide, cymoxanil, cyipendazole, cyproconazole, cyprodinil, ciprofuram, dazomet, sodium dazomet, DBCP, debacarb, decafentin, dehydroacetic acid, dichlorobonide, dichlorobonide, dichlorobonide (dichlorobonide), dichlorobonide, dichlorobonide, dichlorobone. , dichloran, dichlorophen, diclozoline, diclobutrazol, diclocimet, diclomezine, sodium diclomezine, dietofencarb, diethyl pyrocarbonate, diphenoconazole, iron difenzoquat, diflumetorim, dimethaclone, dimethyrimol, dimetomorine, dinoxobox, dinoxobox, dinoxyazone , dinocap-4, dinocap-6, dinocton, dinopenton, dinosulfon, dinoterbon, diphenylamine, dipyrithione, disulfiram, ditalimphos, dithianon, dithioether, DNOC, ammonium DNOC, potassium DNOC, sodium DNOC, dodemorph, dodemorph acetate, dodemorph , dodicin hydrochloride, sodium dodicin, dodine, dodine-free base, drazoxolon, EBP, edifenfos, enestrobin, enestroburin, enoxastrobin, epoxiconazole, ESBP, etaconazole, etem, and taboxam, ethirim, etirimol, ethoxyquin, ethirimol, ethylmercury 2,3- dihydroxypropyl mercaptide, ethylmercury acetate, ethylmercury bromide, ethylmercury chloride, ethylmercury phosphate, etridiazole, famoxadone, phenoxyphenol, phenoxyphenol, phenamino, , fenbuconazole, fenfuram, fenexamide, fenitropan, fenjuntong, fenoxanil, fenpiclonil, fenpropidina, fenpropimorf, fenpirazamina, fentina, fentina acetate, fentina chloride, fentina hydroxide, ferbam, ferimzone, fluazinam, flofoxyfluid, fludioxide, fludioxide , fluopiram, fluoroimide, fluotrimazole, fluoxastrobin, fluquinconazole, flusilazole, flusulfamide, methyl flutiacet, flutianyl, flutolanil, flutriafol, folpet, formaldehyde, fosetil, aluminum fosetil, fuberidazole, furalaxil, furamet, furamol, furamol, furamol, furamol , furmeciclox, furofanato, Fusarium oxisporum, Gliocladium spp., gliodine, griseofulvin, guazatin, guazatin acetates, GY -81, halachrinate, Hercules 3944, hexachlorobenzene, hexachlorobutadiene, hexachlorophene, hexaconazole, hexylthiophos, huanjunzuo, hydrar
    Petition 870190095737, of 09/25/2019, p. 11/30
    9/20 gafen, himexazole, ICIA0858, imazalil, imazalil nitrate, imazalil sulfate, imibenconazole, iminoctadine, iminoctadine triacetate, iminoctadine tris (albesylate), inezin, iodocarb, iodine, iodine, iodine, ipodam, ipro , isoprothiolan, isopirazam, isothianil, isovaledione, jiaxiangjunzhi, casugamycin, hydrated casugamycin hydrochloride, kejunlin, cresoxim-methyl, laminarine, lvdingjunzhi, mancopper, mancozeb, mandipropamid, maneb, chlorinam, meben, meben, meben, , mercuric oxide, mercury chloride, metalaxyl, metalaxyl-M, metam, metam-ammonium, metam-potassium, metamsodium, metazoxolon, metconazole, metasulfocarb, metfuroxam, methyl bromide, methyl iodide, methyl isothiocyanate, methyl benzoate, methyl benzoate, methyl benzoate methylmercury, methylmercury pentachlorophenoxide, metamin, metominostrobin, metrafenone, metsulfovax, mildiomycin, milneb, moroxidine, hydrochloride that of moroxidine, mucochloric anhydride, myclobutanil, myclozoline, N-ethylmercury-4-toluenesulfonanilide, N- (ethylmercury) -p-toluenesulfonanilide, nabam, natamycin, bis (dimethyldithiocarbamate), nickel, nitro, nitro, nitro, nitro, nitro, nitro, nitro, nitro, nitro, nitro, nitro, nitro; ctilinone, ofurace, oleic acid (fatty acids), orisastrobin, ostol, oxadixyl, oxatiapiproline, oxine-copper, oxpoconazole fumarate, oxycarboxine, parinol, pefurazoate, penconazole, pencicuron, penflufen, pentachlorophenol, penturolene, penturolene, penturolene phenylmercury-urea, phenylmercury acetate, phenylmercury chloride, pyrocatechol phenylmercury derivative, dimethyldithiocarbamate phenylmercury, phenylmercury nitrate, phenylmercury salicylate, Phlebiopsis gigantea, phosdiphen, polycarbonate, phosphoric acid, polyphenoxide, phthaoxide, phthaxine polyoxorim zinc, potassium azide, potassium bicarbonate, potassium hydroxyquinoline sulphate, polysulfide potassium, potassium thiocyanate, probenazole, prochloraz, prochloraz-manganese, procymidone,
    Petition 870190095737, of 09/25/2019, p. 12/30
    10/20 propamidine, propamidine dihydrochloride, propamocarb, propamocarb hydrochloride, propiconazole, propineazole, proquinazid, protiocarb, protiocarb hydrochloride, protioconazole, piracarbolide, pyraclostrobin, pirametostrobin, pyroxybitrate, pyroxybitrate, pyroxybitrate, pyroxybitrate, pyroxybitrate, pyroxybitrate, pyroxybitrate, pyroxybitrate, pyroxybitrate, pyroxybitrate, pyroxybitrate, pyroxybitrate, pyroxybitrate, pyroxybitrate, pyroxybitrate, pyroxybitrate. , pyrisoxazole, piroquilon, piroxiclor, piroxifur, quinacetol, quinacetol sulphate, quinazamide, quinoclamine, quinconazole, quinoxifene, quintozene, rabenzazole, Reinoutria sacalinensis extract, saisentong, salicylanilide, silicon, silicon, 2 sodium azide, sodium bicarbonate, sodium orthophenylphenoxide, sodium pentachlorophenoxide, sodium polysulphide, spiroxamine, Streptomices griseoviridis, streptomycin, streptomycin sesquisulfate, SSF-109, sulfur, sultropen, SYP-Z048, tungsten, , keyboard software, tecnazene, tecoram, tetraconazole, thiabendazole, tiadifluor, tici ofen, tifluzamide, thioclorfenfim, thiodiazol-copper, thiomersal, thiophanate, thiophanatomethyl, thioquinox, tiram, thiadinyl, thioximid, tolclofos-methyl, tolylfluanide, tolylmercury acetate, triadimefon, triadimia, triadimide, triadimide, triadimide, triadimide, triadimide, triadimide triclamide, triclopiricarb, Tricoderma spp., tricyclazole, tridemorf, trifloxystrobin, triflumizole, triforin, triticonazole, uniconazole, uniconazole-P, urbacid, validamycin, valiphenalate, valifenal, vangard, vinclozanamide, zinc, zinc, zinc zinc, ziram, and zoxamide, and any combinations thereof.
    [0018] The compositions described in this document are preferably applied in the form of a formulation comprising a composition (a) of the compound of Formula I and (b) fluxpyroxade, together with a phytopathologically acceptable carrier.
    [0019] Concentrated formulations can be dispersed in water, or other liquid, for application, or the formulations can be similar to powder or granular, these can then be applied without
    Petition 870190095737, of 09/25/2019, p. 13/30
    11/20 additional treatment. The formulations are prepared according to the procedures that are conventional in the chemical technique, but these are innovative and important due to the presence of a synergistic composition in these.
    [0020] The formulations that are most commonly applied are aqueous suspensions or emulsions. Such water-soluble, water-suspendable or emulsifiable formulations are solids, generally known as wettable powders, or liquids, generally known as emulsifiable concentrates, aqueous suspensions, or suspension concentrates. The present description covers all vehicles through which synergistic compositions can be formulated for delivery and use as a fungicide.
    [0021] As will be easily assessed, any material to which these synergistic compositions can be added can be used, provided that they obtain the desired utility without significant interference in the activity of these synergistic compositions as antifungal agents.
    [0022] Wettable powders, which can be compacted to form water-dispersible granules, comprise an intimate mixture of the synergistic composition, an agriculturally acceptable vehicle and surfactants. The concentration of the synergistic composition in the wettable powder is generally from about 10% to about 90% by weight, more preferably about 25% to about 75% by weight, based on the total weight of the formulation. In the preparation of wettable powder formulations, the synergistic composition can be combined with any of the finely divided solids, such as pyrophyllite, talc, chalk, plaster, Fuller's earth, bentonite, atapulgite, starch, casein, gluten, montmorillonite clays, earth diatoms, purified silicates or similar. In such operations, the finely divided vehicle is ground or mixed with the synergistic composition in a volatile organic solvent. Surfactants
    Petition 870190095737, of 09/25/2019, p. 14/30
    Effective 12/20, comprising from about 0.5% to about 10%, by weight, of the wettable powder, include sulfonated lignins, naphthalenesulfonates, alkylbenzenesulfonates, alkyl sulfates, and non-ionic surfactants, such as ethylene oxide adducts. alkyl phenols.
    [0023] The emulsifiable concentrates of the synergistic composition comprise a convenient concentration, such as from about 10% to about 50%, by weight, in a suitable liquid, based on the total weight of the emulsifiable concentrate formulation. The components of the synergistic compositions, together or separately, are dissolved in a vehicle, which is a water-miscible solvent or a mixture of water-immiscible organic solvents, and emulsifiers. The concentrates can be diluted with water and oil to form spray mixtures in the form of oil-in-water emulsions. Useful organic solvents include aromatics, especially naphthalenic and olefinic portions of high oil boiling point like heavy aromatic naphtha. Other organic solvents can also be used, such as terpenic solvents, including rosin derivatives, aliphatic ketones, such as cyclohexanone, and complex alcohols, such as 2-ethoxyethanol.
    [0024] The emulsifiers that can be advantageously used in this document can be easily determined by the elements skilled in the art and include various nonionic, anionic, cationic and amphoteric emulsifiers, or a blend of two or more emulsifiers. Examples of non-ionic emulsifiers useful in the preparation of emulsifiable concentrates include polyalkylene glycol ethers and condensation products of alkyl and aryl phenols, aliphatic alcohols, aliphatic amines or fatty acids with ethylene oxide, propylene oxides such as ethoxylated alkyl phenols and carboxylic esters solubilized with the polyol or polyoxyalkylene. Cationic emulsifiers include quaternary ammonium compounds and amine salts
    Petition 870190095737, of 09/25/2019, p. 15/30
    13/20 grease. Anionic emulsifiers include the oil-soluble salts (e.g., calcium) of alkylaryl sulfonic acids, oil-soluble salts or sulfated polyglycol ethers and appropriate salts of phosphate polyglycol ether.
    [0025] Representative organic liquids that can be used to prepare the emulsifiable concentrates of the present description are aromatic liquids like xylene, propyl benzene fractions, or mixed naphthalene fractions, mineral oils, aromatic organic liquids substituted like dioctyl phthalate, kerosene, dialkyl amides of various fatty acids, particularly the dimethyl amides of fatty glycols and glycol derivatives such as on-butyl ether, ethyl ether or diethylene glycol methyl ether, and triethylene glycol methyl ether. Mixtures of two or more organic liquids are also generally used to prepare the emulsifiable concentrate. Preferred organic liquids are xylene, and propyl benzene fractions, with xylene being more preferred. Surface active dispersing agents are generally employed in liquid formulations and the amount from 0.1 to 20 weight percent of the combined weight of the dispersing agent with the synergistic compositions. The formulations can also contain other compatible additives, for example, plant growth regulators and other biologically active compounds used in agriculture.
    [0026] Aqueous suspensions comprise suspensions of one or more water-insoluble compounds, dispersed in an aqueous vehicle in a concentration in the range of about 5% to about 70% by weight, based on the total weight of the suspension formulation watery. The suspensions are prepared by finely grinding the components of the synergistic combination together or separately, and vigorously mixing the ground material in a vehicle comprised of water and surfactants selected from the same types discussed
    Petition 870190095737, of 09/25/2019, p. 16/30
    14/20 of the above. Other ingredients, such as inorganic salts and synthetic or natural gums, can also be added to increase the density and viscosity of the aqueous vehicle. It is generally more effective to grind and mix at the same time when preparing the aqueous mixture and homogenizing it in an implement such as a sand mill, ball mill, or piston-type homogenizer.
    [0027] The synergistic composition can also be applied as a granular formulation, which is particularly useful for soil applications. Granular formulations generally contain from about 0.5% to about 10%, by weight, of the compounds, based on the total weight of the granular formulation, dispersed in a vehicle that consists entirely or in large part of coarsely divided atapulgite, bentonite , diatomite, clay or similar economic substance. Such formulations are generally prepared by dissolving the synergistic composition in a suitable solvent and applying it to a granular carrier that has been preformed in the appropriate particle size, in the range from about 0.5 to about 3 mm. Such formulations can also be prepared by mixing a mass or paste of the carrier and the synergistic composition, and grinding and drying to obtain the desired granular particle.
    [0028] Powders containing the synergistic composition are prepared simply by intimately mixing the powdered synergistic composition with a suitable powdery agricultural vehicle, such as, for example, kaolin clay, ground volcanic rock, and the like. The powders may suitably contain from about 1% to about 10%, by weight, of the synergistic composition / vehicle combination.
    [0029] The formulations may contain agriculturally acceptable adjuvant surfactants to increase the deposition, wetting and penetration of the synergistic composition on the target culture and organism. These adjuvant surfactants can optionally be used
    Petition 870190095737, of 09/25/2019, p. 17/30
    15/20 as a component of the formulation or as a tank mixture. The amount of adjuvant surfactant will vary from 0.01 percent to 1.0 percent volume / volume (v / v) based on a spray volume of water, preferably 0.05 to 0.5 per cent. Suitable adjuvant surfactants include ethoxylated nonyl phenols, ethoxylated synthetic or natural alcohols, salts of sulfosuccinic esters or acids, ethoxylated organosilicones, ethoxylated fatty amines and blends of surfactants with mineral or vegetable oils.
    [0030] Formulations may optionally include combinations that may comprise at least 1%, by weight, of one or more synergistic compositions with another pesticidal compound. Such additional pesticidal compounds may be fungicides, insecticides, nematocides, miticides, arthropodicides, bactericides or combinations thereof which are compatible with the synergistic compositions of the present description in the medium selected for application, and not antagonistic to the activity of the present compounds. Consequently, in such embodiments, the other pesticide compound is employed as a supplementary toxic product for the same pesticide or a different pesticide use. The pesticidal compound and the synergistic composition can generally be mixed in a weight ratio of 1: 100 to 100: 1.
    [0031] This description includes, within its scope, methods for the control or prevention of fungal attack. These methods include applying to the fungus or to the area adjacent to the fungus, or to a plant or area adjacent to a plant in which infestation will be prevented (for example, applying to wheat or barley plants), a fungically effective amount of the synergistic composition. The synergistic composition is suitable for treating various plants at fungicidal levels, while exhibiting low phytotoxicity. The synergistic composition is useful in a protective or eradicating way. Synergistic composition is applied using any one of a variety of techniques
    Petition 870190095737, of 09/25/2019, p. 18/30
    16/20 known, as the synergistic composition or as a formulation comprising the synergistic composition. For example, synergistic compositions can be applied to the roots, seeds or foliage of plants to control various fungi, without impairing the commercial value of the plants. The synergistic composition is applied in the form of any of the types of formulation generally used, for example, as solutions, dust, wettable powders, flowable concentrates, or emulsifiable concentrates. These materials are conveniently applied in several known ways.
    [0032] The synergistic composition was considered to have significant fungicidal effect particularly for agricultural use. The synergistic composition is particularly effective for use with agricultural crops and horticultural plants, or with wood, paint, leather or carpet lining.
    [0033] In particular, the synergistic composition is effective in controlling a variety of unwanted fungi that infect useful plant cultures. The synergistic composition can be used against a variety of Ascomycetes and Basidiomycetes fungi, including, for example, the following representative fungal species: brown wheat rust (Puccinia recondita; Bayer PUCCRT code); striped wheat field rust (Puccinia striiformis; Bayer PUCCST code); leaf spot of the wheat field (Mycosphaerella graminicola; anamorph: Septoria tritici; Bayer SEPTTR code); spot of wheat field glumas (Leptosphaeria nodorum; Bayer LEPTNO code; anamorph: Stagonospora nodorum) and banana black sigatoka disease (Mycosphaerella fijiensis; BAYER MYCOFI code). It will be understood by those skilled in the art that the effectiveness of synergistic compositions of one or more previous fungi establishes the general utility of synergistic compositions as fungicides.
    [0034] Synergistic compositions have a wide gram of effectiveness as a fungicide. The extinguished amount of the synergistic composition
    Petition 870190095737, of 09/25/2019, p. 19/30
    17/20 that will be applied depends not only on the relative quantities of the components, but also on the particular desired action, the fungal species that will be controlled, and the growth stage of the same, as well as the part of the plant or other product that will be contacted with synergistic composition. Thus, formulations containing the synergistic composition cannot be equally effective at similar concentrations or against the same fungal species.
    [0035] Synergistic compositions are effective with plants in a disease-inhibiting and phytologically acceptable amount. The term disease inhibitory and phytologically acceptable amount refers to an amount of the synergistic composition that eliminates or inhibits the plant disease for which control is desired, but is not significantly toxic to the plant. The exact concentration of synergistic composition displayed varies with the fungal disease that will be controlled, the type of formulation used, the method of application, the particular plant species, climatic conditions, and the like.
    [0036] The present compositions can be applied to fungi or to the area adjacent to the fungus, or to a plant or area adjacent to the plant, through the use of conventional terrestrial sprayers, granule applicators, and by other conventional means known to those skilled in the art .
    [0037] The following examples are provided to further illustrate the description. These should not be construed as limiting the description.
    Examples
    [0038] Representative synergistic interactions, including application rates employed and disease control resulting from brown rust of the wheat field and leaf spot of the wheat field are shown in Table 1.
    [0039] For mixture studies with the compound of Formula I:
    Petition 870190095737, of 09/25/2019, p. 20/30
    18/20
    Treatments consist of fungicides, which include the compound of Formula I and fluxpyroxade. The technical grades of materials were dissolved in acetone to form stock solutions, these were then used to perform 4-fold dilutions in acetone for each individual fungicidal component or for the bidirectional mixture. The desired fungicide rates were obtained after mixing the dilutions with 9 volumes of water containing 110 parts per million (ppm) of Triton X-100. The fungicidal solutions (20 milliliters (mL)) were applied to 12 plant pots using an automatic sprayer, which used two 6218-1 / 4 JAUPM spray nozzles that operate at 20 pounds per square inch (psi) adjusted at opposite angles to cover both leaf surfaces. All sprayed plants were allowed to air dry before further handling. The control plants were sprayed in the same way with a blank solvent.
    Evaluation of Curative and Protective Activity of Fungicide Mixtures vs. Trigal leaf spot (Mycosphaerella graminicola; anamorph: Septoria tritici; Bayer code: SEPTTR).
    [0040] Wheat plants (variety Yuma) were developed from seed in a greenhouse in plastic pots with a surface area of 27.5 square centimeters (cm 2 ) containing 50% Metro mix of mineral soil / 50% without soil, with 8 to 12 seedlings per pot. The plants were used for testing when the first leaf fully emerged, this typically occurred 7 to 8 days after planting. The test plants were inoculated with an aqueous spore suspension of Septoria tritici (a) 3 days before fungicide treatments (3-day curative test, 3DC) or (b) 1 day after fungicide treatments (protective test of 1 day, 1DP). After inoculation, the plants were placed in a condensation environment from 1 to 3 days to allow the infection to occur. The plants were,
    Petition 870190095737, of 09/25/2019, p. 21/30
    19/20 then placed in the greenhouse to develop symptoms, which in the case of SEPTTR typically required 25 to 30 days.
    Evaluation of Curative Activity of Fungicide Mixtures vs. Brown rust of the rigid T (Puccinia recondita; Bayer code: PUCCRT).
    [0041] Yuma wheat seedlings were developed as described above and inoculated with an aqueous spore suspension of Puccinia recondita 3 days before treatment with fungicide (3DC). After inoculation, the plants were placed in a condensation environment for 1 day to allow infection to occur. The plants were then placed in the greenhouse to develop symptoms, which in the case of PUCCRT typically required 7 to 10 days.
    [0042] When disease severity reached 50 to 100% in control plants, infection levels were assessed visually in treated plants and scored on a 0 to 100 percent scale. The percentage of disease control was then calculated using the disease ratio in treated plants in relation to control plants.
    [0043] Colby's equation was used to determine the expected fungicidal effects of the mixtures. (See Colby, S. R. Calculation of the synergistic and antagonistic response of herbicide combinations. Weeds 1967, 15, 20 - 22.)
    [0044] The following equation was used to calculate the expected activity of mixtures containing two active ingredients, A and B:
    Expected = A + B - (A x B / 100)
    [0045] A = observed effectiveness of active component A at the same concentration used in the mixture;
    [0046] B = observed effectiveness of active component B at the same concentration used in the mixture.
    [0047] The treatments that have been evaluated, the application rates
    Petition 870190095737, of 09/25/2019, p. 22/30
    20/20 employed, the pathogens evaluated, and resulting diseases in both treated and control plants are shown in Table 1.
    Table 1: Synergistic interactions of compound I and fluxpyroxade in protective tests on Septoria tritici (SEPTTR) for 1 day (1DP) curative on Puccinia recondita (PUCCRT) for 3 days.
    Application Rate (ppm) _____________________________ SEPTTR 1DP PUCCRT 3DC Compound I Fluxapiroxade % DC Obs % DC Exp % DC Obs % DC Exp 6.25 0 93 - 98 - 1.56 0 2 - 12 - 0.39 0 0 - 0 - 0.1 0 0 - 2 - 0 6.25 94 - 100 - 0 1.56 0 - 86 - 0 0.39 0 - 0 - 0 0.1 0 - 0 - 1.56 1.56 26 2 - 87.7 1.56 0.39 9 2 48 12 1.56 0.1 12 2 52 12
    % DC Obs = Percentage of disease control observed% DC Exp = Percentage of disease control expected
    权利要求:
    Claims (6)
    [1]
    1. Synergistic fungicidal mixture, characterized by the fact that it comprises a fungicidally effective amount of:
    a compound of Formula I, (3S, 6S, 7R, 8R) -8-benzyl-3- (3 ((isobutyryloxy) methoxy) -4-methoxypicolinamido) -6-methyl-4,9-dioxo-1,5dioxonan- 7-yl isobutyrate, ch 3 O ^ Y CH3 H 3 C7 .0 od
    1 I o Ç H 3 ch 3
    Air 0 V Ãaá I H / 0 1 π ch 3
    ..... ü 0 °
    O (I), and
    Fluxapyroxade;
    the weight ratio of the compound of Formula I to fluxpyroxade is 1: 1 to 16: 1.
    [2]
    2. Mixture according to claim 1, characterized by the fact that the ratio of the compound of Formula I to fluxpyroxade is 1 to 1.
    [3]
    3. Mixture according to claim 1, characterized by the fact that the ratio of the compound of Formula I to fluxpyroxade is 1 to 16.
    [4]
    4. Fungicidal composition, characterized in that it comprises a fungicidally effective amount of the fungicidal mixture, as defined in any one of claims 1 to 3, and an agriculturally acceptable adjuvant or vehicle.
    [5]
    5. Method for treating a plant, characterized by the fact that it comprises the step of applying a fungicidally effective amount of a mixture, as defined in any one of claims 1 to 3, to a surface selected from at least
    Petition 870190095737, of 09/25/2019, p. 24/30
    2/2 nos a surface selected from the group of surfaces consisting of at least a portion of a plant, soil adjacent to a plant, soil in contact with a plant, seeds, and equipment used in contact with a plant or a surface adjacent to a plant.
    [6]
    6. Method, according to claim 6, characterized by the fact that the fungicidally effective amount of the mixture applied in the range of 30 g / ha to 200 g / ha of fluxpyroxade, and from 35 g / ha to 300 g / ha of compound of Formula (I).
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    同族专利:
    公开号 | 公开日
    US20140187587A1|2014-07-03|
    EP2938191B1|2018-01-31|
    AU2013370491B2|2016-10-06|
    KR102148190B1|2020-08-26|
    HUE038806T2|2018-11-28|
    MX2015008442A|2015-09-23|
    EP2938191A4|2016-07-27|
    TWI660671B|2019-06-01|
    IL239560A|2020-05-31|
    AR094305A1|2015-07-22|
    TWI586275B|2017-06-11|
    PT2938191T|2018-05-09|
    CN104883884A|2015-09-02|
    CA2894515C|2021-10-19|
    RU2015131103A|2017-01-31|
    ZA201504334B|2016-09-28|
    LT2938191T|2018-05-10|
    CA2894515A1|2014-07-03|
    DK2938191T3|2018-05-07|
    UA114661C2|2017-07-10|
    IL239560D0|2015-08-31|
    CN104883884B|2018-03-23|
    EP2938191A1|2015-11-04|
    ES2666144T3|2018-05-03|
    ECSP15032758A|2015-11-30|
    NZ708979A|2020-01-31|
    HK1215356A1|2016-08-26|
    AU2013370491A1|2015-07-02|
    TW201725987A|2017-08-01|
    CR20150304A|2015-08-24|
    RU2650402C2|2018-04-11|
    PH12015501475A1|2016-02-01|
    BR112015015351A2|2017-07-11|
    KR20150100865A|2015-09-02|
    JP6352302B2|2018-07-04|
    TW201427597A|2014-07-16|
    PL2938191T3|2018-07-31|
    CL2015001841A1|2015-10-02|
    UY35247A|2014-07-31|
    US10172354B2|2019-01-08|
    WO2014105842A1|2014-07-03|
    JP2016505606A|2016-02-25|
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    法律状态:
    2018-03-06| B06F| Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]|
    2018-03-13| B06F| Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]|
    2018-03-20| B06I| Publication of requirement cancelled [chapter 6.9 patent gazette]|Free format text: ANULADA A PUBLICACAO CODIGO 6.6.1 NA RPI NO 2462 DE 13/03/2018 POR TER SIDO INDEVIDA. |
    2019-05-07| B06T| Formal requirements before examination [chapter 6.20 patent gazette]|
    2019-09-03| B06A| Patent application procedure suspended [chapter 6.1 patent gazette]|
    2020-04-07| B09A| Decision: intention to grant [chapter 9.1 patent gazette]|
    2020-06-16| B16A| Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]|Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 23/12/2013, OBSERVADAS AS CONDICOES LEGAIS. |
    优先权:
    申请号 | 申请日 | 专利标题
    US201261747094P| true| 2012-12-28|2012-12-28|
    US61/747,094|2012-12-28|
    PCT/US2013/077537|WO2014105842A1|2012-12-28|2013-12-23|Synergistic fungicidal mixtures for fungal control in cereals|
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