Agrochemical composition

Abstract

The present invention relates to an agrochemical composition comprising kasugamycin or a salt thereof. The invention also relates to a soluble concentrate comprising kasugamycin, wherein the pH of the composition ranges from 2 to 4.

Description

Technical Field

[0002] This invention relates to an agricultural chemical composition. More specifically, this invention relates to an agricultural chemical composition comprising kasugamycin or a salt thereof. Background Technology

[0004] Kasugamycin is an aminoglycoside antibiotic that inhibits translation by binding to ribosomes and is widely used in agriculture and medicine to combat microbial pathogens. As an agricultural antibiotic and fungicide, kasugamycin primarily targets the ribosome, interfering with bacteria's ability to synthesize new proteins, thereby inhibiting bacterial proliferation. This substance possesses both antibacterial and bactericidal properties and has been widely applied. Its mechanism of action involves interfering with the esterase system of pathogen amino acid metabolism, disrupting protein biosynthesis, inhibiting hyphal growth, and inducing cell granulation, thus rendering the pathogen unable to reproduce and infect.

[0005] Kasugamycin is produced by aerobic fermentation of *Streptomyces kasugaensis*. Its active ingredient, kasugamycin hydrochloride hydrate, is isolated from the fermentation products. Compared to free alkali, this component exhibits significantly enhanced stability, remaining stable even after 10 days of storage at 50°C. It shows good resistance to weak acids, slowly decomposing at pH 7, but decomposes within weeks in alkaline solutions even at room temperature. Therefore, the industry urgently needs a stable agrochemical.

[0006] The present invention aims to develop a stable agricultural composition comprising ingredients such as kasugamycin or its salts to overcome the shortcomings of existing agricultural compound formulations. This composition provides broad-spectrum antimicrobial properties, such as antifungal and antibacterial properties, while reducing the dosage required. Summary of the Invention

[0008] This invention provides an agricultural chemical composition containing kasugamycin and a method for preparing the same.

[0009] In one aspect, the present invention provides an agricultural chemical composition comprising kasugamycin or a salt thereof, wherein the composition has a low pH.

[0010] In one aspect, the present invention provides a soluble concentrate composition comprising kasugamycin or a salt thereof, wherein said composition has a low pH.

[0011] In another aspect, the present invention provides a soluble concentrate composition comprising kasugamycin hydrochloride, wherein the pH range of the composition is 2 to 4.

[0012] In one aspect, the present invention provides an agricultural chemical composition comprising:

[0013] a) Kasugamycin hydrochloride,

[0014] b) Nonionic surfactants, and

[0015] c) Agrochemically acceptable excipients

[0016] The pH range of the composition is 2 to 4.

[0017] In one respect, the ratio of kasugamycin hydrochloride to nonionic surfactant ranges from 0.1:1 to 5:1.

[0018] In another aspect, the present invention provides the application of agricultural chemical compositions for controlling pathogenic infections in crops.

[0019] In another aspect, the present invention provides a method for controlling or inhibiting plant pathogens, comprising applying a composition to a site of pathogen infection, a plant, a plant part, or plant propagation material, the composition comprising:

[0020] (i) Kasugamycin or its salts, and

[0021] (ii) Nonionic surfactants,

[0022] The weight ratio of kasugamycin or its salt to nonionic surfactant ranges from 0.1:1 to 5:1, and the pH ranges from 2 to 4. Detailed Implementation

[0024] The following is a detailed description of embodiments of the present invention. These embodiments are detailed enough to clearly convey the invention. However, the amount of detail provided is not intended to limit the contemplative variations of the embodiments; rather, it is intended to cover all modifications, equivalents, and alternatives that fall within the spirit and scope of the invention as defined by the appended claims.

[0025] Unless the context otherwise requires, throughout the following instruction manual, the word “comprise” and its variations, such as “comprises / comprising” and “includes / including”, shall be interpreted in an open, inclusive sense, meaning “including but not limited to”.

[0026] Throughout this specification, references to "one embodiment" or "some embodiments" mean that a particular feature, structure, or characteristic described in connection with that embodiment is included in at least one embodiment. Therefore, the phrases "in one embodiment" or "in some embodiments" appearing throughout this specification do not necessarily refer to the same embodiment. Furthermore, a particular feature, structure, or characteristic may be combined in any suitable manner in one or more embodiments.

[0027] As used in this specification and in the following numbered embodiments or claims, the terms "a," "an," and "the" include plural references unless the context clearly specifies otherwise. Furthermore, as used in this specification, "in" includes both "in" and "on" unless the context clearly specifies otherwise.

[0028] As used herein, the terms “comprising,” “including,” “having,” “containing,” “involving,” etc., should be understood as open-ended, meaning including but not limited to. The terms “preferred” and “preferred” refer to embodiments of the invention that may provide certain benefits in certain circumstances.

[0029] The aspects and implementation schemes described herein should also be interpreted as using "consisting of" or "substantially consisting of" instead of the clause "comprising".

[0030] Given the measurements under discussion and the errors associated with the measurement of a particular quantity (i.e., limitations of the measurement system), the terms "about" or "approximately" as used herein include the stated value and the average of the values ​​within an acceptable range of deviations determined by one of ordinary skill in the art. For example, "about" may mean within one or more standard deviations, or within ±10% or ±5% of the stated value. Unless otherwise stated herein, descriptions of numerical ranges are intended only as a shorthand method for individually referring to each individual value falling within the range, and each individual value is incorporated into the specification as if it were individually described herein. The endpoints of all ranges are included within the range and can be combined independently. It should be understood that, where a parameter range is provided, all integers within that range and their tenths are also provided. For example, "0.1-80%" includes 0.1%, 0.2%, 0.3%, etc., up to 80%.

[0031] All methods described herein may be performed in a suitable order unless otherwise stated herein or clearly contradicted by the context. Unless otherwise required, the use of any and all exemplary or demonstrative language (e.g., “such as”) is intended only to better illustrate the invention and not to limit its scope. No language in the specification should be construed as indicating that any unclaimed element is necessary for the practice of the invention as used herein.

[0032] As used herein, the term "plant" or "crop" refers to a whole plant, plant organs (such as leaves, stems, shoots, roots, trunks, branches, buds, fruits, etc.), plant cells, or plant seeds. The term also covers plant crops, such as fruits. The term "plant" can also include its propagation material, which can include all reproductive parts of a plant, such as seeds and asexual plant material, such as cuttings and tubers, which can be used for plant propagation. This includes seeds, tubers, spores, bulbs, rhizomes, buds, basal buds, stolons, and other parts of the plant, including seedlings and young plants that are transplanted after germination or emergence from the soil.

[0033] As used herein, the term "site" refers to a designated vicinity or area for the growth of a desired crop, where the growth and / or spread of undesirable vegetation needs to be controlled. A site includes the vicinity of the desired crop plants, where undesirable vegetation growth has occurred, is most likely to occur, or has not yet occurred.

[0034] As used herein, the term "stable" refers to the chemical and / or physical stability of an active compound.

[0035] The salt mentioned in this article is agriculturally acceptable salt. As used in this article, "agriculturally acceptable salt" means salt that is acceptable for use in agriculture or horticulture.

[0036] As used herein, the term "ratio" refers to a weight ratio. Within the range of said ratio, the active ingredient (i.e., kasugamycin) and the nonionic surfactant (i.e., ethoxylated isotretinoin) effectively prevent the degradation of the active ingredient in the liquid composition and maintain high stability during the preparation, storage, and application of the composition.

[0037] In some embodiments, numerical values ​​representing the amount of ingredients, properties (such as concentrations), used to describe and claim certain embodiments of the invention should be understood to be modified by the term "about" in some cases. Therefore, in some embodiments, the numerical parameters listed in the written description are approximate values ​​and may vary depending on the desired properties expected to be obtained in a particular embodiment. In some embodiments, numerical parameters should be interpreted in conjunction with the number of significant figures reported and with the application of conventional rounding techniques. Although the wide range of numerical ranges and parameters illustrating some embodiments of the invention are approximate values, the values ​​described in specific examples should still be reported as accurately as practically practicable.

[0038] The list of ranges of values ​​in this document is intended only as a shorthand for individually referring to each individual value falling within that range. Unless otherwise stated herein, each individual value is incorporated herein as if it were listed separately. The headings and abstracts of the invention provided herein are for convenience only and are not intended to define the scope or meaning of the embodiments.

[0039] All methods described herein may be performed in any suitable order unless otherwise stated herein or the context clearly contradicts it. The use of any and all embodiments or exemplary language (e.g., “such as”) provided herein with respect to certain implementations is intended only to better illustrate the scope of the invention and does not constitute a limitation on the scope of the invention as otherwise claimed. The language in this specification should not be construed as indicating that any unclaimed element is necessary for the practice of the invention as used herein.

[0040] This invention is based on the inventors' accidental discovery that agrochemical compositions containing kasugamycin exhibit superior stability under low pH conditions compared to kasugamycin formulations reported in the literature. Furthermore, the inventors aim to demonstrate that combinations of kasugamycin with preservatives can provide enhanced antibacterial and antifungal properties. The inventors also provide a suitable surfactant to improve the stability of kasugamycin formulations.

[0041] Therefore, the present invention provides an agricultural composition comprising kasugamycin or a salt thereof, which exhibits antifungal and antibacterial properties. Furthermore, various aspects of the present invention relate to an aqueous premixed agricultural formulation and a method for its preparation.

[0042] In one embodiment, the present invention provides an agricultural chemical composition comprising kasugamycin.

[0043] In one embodiment, the present invention provides an agricultural chemical composition comprising:

[0044] a) Kasugamycin or its salts,

[0045] b) Nonionic surfactants, and

[0046] c) Agrochemically acceptable excipients

[0047] The pH range of the composition is 2 to 4.

[0048] In one embodiment, the present invention provides an agricultural chemical composition comprising:

[0049] a) Kasugamycin hydrochloride,

[0050] b) Nonionic surfactants, and

[0051] c) Agrochemically acceptable excipients

[0052] The pH range of the composition is 2 to 4.

[0053] In one embodiment, the ratio of kasugamycin hydrochloride to nonionic surfactant ranges from 0.1:1 to 5:1.

[0054] In a preferred embodiment, the ratio of kasugamycin hydrochloride to nonionic surfactant ranges from 0.1:1 to 3:1.

[0055] In a preferred embodiment, the ratio of kasugamycin hydrochloride to nonionic surfactant ranges from 0.1:1 to 2:1.

[0056] In one embodiment, the agrochemical composition of the present invention is a liquid formulation.

[0057] In one embodiment, the stable agrochemical composition is selected from soluble concentrates (SL), capsule suspensions (CS), dispersible concentrates (DC), emulsions, water-in-oil (EO), emulsions, oil-in-water (EW), oil dispersions (OD), oil-miscible flowable concentrates, oil-miscible suspensions (OF), oil-miscible liquids (OL), suspension concentrates (SC), and suspension-emulsions (SE).

[0058] In one embodiment, the agrochemical composition is a soluble concentrate formulation.

[0059] In one embodiment, the present invention provides a soluble concentrate composition comprising kasugamycin or a salt thereof, wherein the pH range of the composition is 2 to 4.

[0060] In another embodiment, the present invention provides a soluble concentrate composition comprising kasugamycin hydrochloride, wherein the pH range of the composition is 2 to 4.

[0061] In one embodiment, the present invention provides a soluble concentrate composition comprising: a) kasugamycin or a salt thereof,

[0062] b) Nonionic surfactants, and

[0063] c) Excipients that are acceptable in agricultural chemistry.

[0064] In one embodiment, the present invention provides a soluble concentrate composition comprising: a) kasugamycin hydrochloride,

[0065] b) Nonionic surfactants, and

[0066] c) Excipients that are acceptable in agricultural chemistry.

[0067] In one embodiment, the present invention provides a soluble concentrate composition comprising: a) kasugamycin or a salt thereof,

[0068] b) Nonionic surfactants,

[0069] c) Antimicrobial agents, and

[0070] d) Excipients that are acceptable in agricultural chemistry.

[0071] In one embodiment, the present invention provides a soluble concentrate composition comprising: a) kasugamycin hydrochloride,

[0072] b) Nonionic surfactants,

[0073] c) Antimicrobial agents,

[0074] d) pH adjusters, and

[0075] e) Excipients that are acceptable in agricultural chemistry.

[0076] In one embodiment, the present invention provides a soluble concentrate composition comprising: a) kasugamycin or a salt thereof,

[0077] b) Nonionic surfactants, and

[0078] c) Agrochemically acceptable excipients

[0079] The pH range of the composition is 2 to 4.

[0080] In one embodiment, the nonionic surfactant does not carry a molecular charge (positive or negative) and does not form ions in water. Non-limiting examples of nonionic surfactants include: polymeric surfactants such as block copolymers, random copolymers, graft copolymers, and star polymers; amine ethoxylates, alkanolamides, and ethoxylated alkanolamides; alkoxylated triglycerides (such as ethoxylated soybean oil, castor oil, and rapeseed oil); polyethoxylated esters such as polyethoxylated sorbitan fatty acid esters, polyethoxylated sorbitan fatty acid esters, and polyethoxylated glycerol fatty acid esters; alkylphenol alkoxylates (e.g., octyl- (such as trinitropropylene oxide, butene oxide, or mixtures thereof); amine ethoxylates, alkanolamides, and ethoxylated alkanolamides; alkoxylated triglycerides (such as ethoxylated soybean oil, castor oil, and rapeseed oil); alkylphenol alkoxylates (e.g., octylphenol (such as trinitropropylene oxide)). Butene oxide or mixtures thereof); sugar derivatives such as sucrose esters, alkyl polyglycosides and alkyl polysaccharides; amine ethoxylates, alkanolamides and ethoxylated alkanolamides; alkoxylated triglycerides (such as ethoxylated soybean oil, castor oil and rapeseed oil); alkylphenol alkoxylates (e.g. octylphenol alkoxylates, nonylphenol alkoxylates, dinonylphenol alkoxylates or dodecylphenol alkoxylates); fatty acid ethoxylates; ethoxylates of fatty acid esters and oils; fatty acid esters, ethoxylated methyl esters; glycerides, lanolin derivatives, other sorbitan derivatives such as sorbitan esters; fatty acid ethoxylates, PEG (polyethylene glycol) resins, alkyd copolyesters; polyethylene glycol (PEG); polyethylene glycol fatty acid esters; silicone surfactants; and combinations thereof.

[0081] In one embodiment, the nonionic surfactant is preferably selected from alcohol alkoxylates, more preferably alcohol ethoxylates.

[0082] In a preferred embodiment, the nonionic surfactant is ethoxylated isotridecyl alcohol.

[0083] In one embodiment, the weight ratio of kasugamycin hydrochloride to ethoxylated isothiazol ranges from 0.1:1 to 5:1.

[0084] In a preferred embodiment, the weight ratio of kasugamycin hydrochloride to ethoxylated isothiazol ranges from 0.1:1 to 3:1.

[0085] In a preferred embodiment, the weight ratio of kasugamycin hydrochloride to ethoxylated isothiazol ranges from 0.1:1 to 2:1.

[0086] In one embodiment, the antimicrobial agent is selected from: chlorphenesin, benzoic acid or its salts or esters (e.g., sodium benzoate), propionic acid or its salts, salicylic acid or its salts, sorbic acid or its salts (e.g., potassium sorbate), formaldehyde, paraformaldehyde, zinc pyrithione, inorganic sulfites, bisulfites, chlorobutanol, 4-hydroxybenzoic acid or its salts or esters (e.g., methylparaben, ethylparaben, propylparaben), dehydroacetic acid and / or its salts (e.g., sodium dehydroacetate), formic acid or its salts, dibromohexamethylene ethanesulfonate, thimerosal, phenylmercuric acid, undecenoic acid or its salts, hexocide, bromonitrazepam. Diols, 5-bromo-5-nitro-1,3-dioxane, dichlorobenzyl alcohol, benzyl alcohol, triclocarban, chlorocresol, triclosan, chloroxylenol, imidazolidinyl urea, polyaminopropyl biguanide, phenoxyethanol, hexamethylenetetramine, quaternary ammonium salt-15, clomiphene, DMDM ​​hydantoin, 1-hydroxy-4-methyl-6-(2,4,4-trimethylpentyl)-2-pyridone, piroctone ethanolamine, bromochlorofen, o-cymene-5-ol, methylchloroisothiazolinone, methylisothiazolinone, mixtures of methylchloroisothiazolinone and methylisothiazolinone, chlorophenol, chloroacetamide, phenoxyisopropanol, alkyl (C 12 -C 22 Trimethylammonium bromide, alkyl (C 12 -C 22 Trimethylammonium chloride, dimethyloxazolidine, diazolidinyl urea, hexamidine, hexamidine dihydroxyethanesulfonate, hexamidine p-hydroxybenzoate, hexamidine p-hydroxybenzoate, glutaraldehyde, 7-ethylbicyclooxazolidine, sodium hydroxymethylaminoacetate, silver chloride, benzyl chloride, benzalkonium chloride, benzalkonium bromide, benzyl saccharin, benzyl hemiacetal, iodopropynyl butyl methylamine, silver citrate, or combinations thereof.

[0087] In one embodiment, the antimicrobial agent is sorbic acid, its calcium salt, potassium salt, and sodium salt.

[0088] In a preferred embodiment, the antimicrobial agent is potassium sorbate.

[0089] In one embodiment, the composition comprises 0.1% to 40% w / w kasugamycin or a salt thereof by weight of the formulation, and one or more excipients by weight of 5% to 99% w / w.

[0090] In one embodiment, the composition comprises 0.1% to 20% w / w kasugamycin or a salt thereof, and 10% to 70% w / w one or more excipients.

[0091] In one embodiment, the concentration of kasugamycin hydrochloride ranges from 0.1% w / w to 10% w / w.

[0092] In a preferred embodiment, the concentration of kasugamycin hydrochloride ranges from 0.5% w / w to 5% w / w.

[0093] In another preferred embodiment, the concentration of kasugamycin hydrochloride ranges from 0.5% w / w to 3% w / w.

[0094] In one implementation, the concentration of the nonionic surfactant ranges from 0.1% to 3% w / w.

[0095] In one implementation, the concentration of the nonionic surfactant ranges from 0.5% to 2% w / w.

[0096] In one embodiment, the concentration of the alcohol ethoxylate ranges from 0.1% to 3% w / w.

[0097] In one embodiment, the concentration of the alcohol ethoxylate ranges from 0.5% to 2% w / w.

[0098] In one embodiment, the concentration of ethoxylated isotretinoin ranges from 0.1% to 3% w / w.

[0099] In one embodiment, the concentration of ethoxylated isotretinoin ranges from 0.5% to 2% w / w.

[0100] In another embodiment, the composition further comprises at least one agrochemically acceptable excipient.

[0101] According to one embodiment of the present invention, the agrochemically acceptable excipient is selected from one or more of the following: emulsifiers, colorants, thickeners / binders, antifreeze agents, defoamers, antioxidants, solvents, preservatives, flow aids, anti-caking agents, pH adjusters, buffers, formulation aids, disintegrants, or combinations thereof.

[0102] In another embodiment, those skilled in the art can readily identify emulsifiers that can be advantageously used herein, including a variety of nonionic, anionic, cationic, and amphoteric emulsifiers, or mixtures of two or more emulsifiers. Examples of nonionic emulsifiers that can be used to prepare emulsifiable concentrates include polyalkylene glycol ethers and condensation products of alkyl and aryl phenols, aliphatic alcohols, aliphatic amines, or fatty acids with ethylene oxide or propylene oxide, such as ethoxylated alkylphenols and carboxylic acid esters solubilized with polyols or polyoxyethylenes. Cationic emulsifiers include quaternary ammonium compounds and fatty amine salts. Anionic emulsifiers include oil-soluble salts of alkyl aryl sulfonic acids (e.g., calcium), oil-soluble salts of sulfated polyglycol ethers, and suitable salts of phosphorylated polyglycol ethers.

[0103] In one embodiment, the colorant may be selected from: iron oxides, titanium oxides and Prussian blue, as well as organic dyes such as alizarin dyes, azo dyes or metal phthalocyanine dyes, and trace elements such as salts of iron, manganese, boron, copper, cobalt, molybdenum and zinc.

[0104] In another embodiment, the antifreeze added to the composition may be an alcohol selected from, but not limited to, the group consisting of: ethylene glycol, 1,2-propanediol, 1,3-propanediol, 1,2-butanediol, 1,3-butanediol, 1,4-butanediol, 1,4-pentanediol, 3-methyl-1,5-pentanediol, 2,3-dimethyl-2,3-butanediol, trimethylolpropane, mannitol, sorbitol, glycerol, pentaerythritol, 1,4-cyclohexanediol, xylenol, bisphenol such as bisphenol A, etc. In addition, ether alcohols such as diethylene glycol, triethylene glycol, tetraethylene glycol, polyoxyethylene or polyoxypropylene glycol with a molecular weight of up to about 4000, diethylene glycol monomethyl ether, diethylene glycol monoethyl ether, triethylene glycol monomethyl ether, butoxyethanol, butanediol monobutyl ether, dipentaerythritol, tripentaerythritol, tetrapentaerythritol, dipolyglycerol, tripolyglycerol, tetrapolyglycerol, pentapolyglycerol, hexapolyglycerol, heptapolyglycerol, and octapolyglycerol.

[0105] In a preferred embodiment, the antifreeze is monoethylene glycol.

[0106] According to one embodiment, the defoamer may be selected from polydimethoxysiloxane, polydimethylsiloxane, polyalkyl acrylate, castor oil, fatty acids, fatty acid esters, fatty acid sulfates, fatty alcohols, fatty alcohol esters, fatty alcohol sulfates, foot olive oil, mono- and diglycerides, paraffin oil, paraffin wax, polypropylene glycol, silicone oil, vegetable fats, vegetable fat sulfates, vegetable oils, vegetable oil sulfates, vegetable waxes, vegetable wax sulfates, and reagents based on silicon or magnesium stearate.

[0107] Agricultural chemical compositions may also contain one or more antioxidants. Preferably, the agricultural chemical formulation contains an antioxidant.For example, antioxidants include: amino acids (e.g., glycine, histidine, tyrosine, tryptophan) and their derivatives; imidazoles and imidazole derivatives (e.g., uric acid); peptides (e.g., D,L-carnosine, D-carnosine, L-carnosine and their derivatives (e.g., anserine); carotenoids and carotenes (e.g., α-carotene, β-carotene, lycopene and their derivatives); lipoic acid and its derivatives (e.g., dihydrolipoic acid); glucosinolates, propylthiouracil and other sulfur compounds (e.g., thioglycerol, thiosorbitol, thioglycolic acid, thioredoxin, glutathione, cysteine, cystine, cystamine and their glycosylation, N-acetyl, methyl, ethyl, propyl, pentyl, butyl, lauryl, palmitoyl, oleoyl) Derivatives of β-linolenic acid, γ-linolenic acid, cholesterol esters, glycerides, etc., and their salts; dilaurate thiodipropionate, distearate thiodipropionate, thiodipropionic acid and their derivatives (esters, ethers, peptides, lipids, nucleotides, nucleosides and their salts); and low-tolerance doses (e.g., pmol / kg to pmol / kg) of sulfinimide compounds (e.g., sulfenyl butyrate, homocysteine ​​sulfinimide, sulfenyl butyrate sulfonate, pentyl, hexa-, and hepta-thionine sulfinimide); and metal chelators (e.g., α-hydroxy fatty acids, EDTA, EGTA, phytic acid, lactoferrin); α-hydroxy acids (e.g., citric acid, lactic acid, malic acid); humic acids; bile acids and bile extracts; gallic acid esters (e.g., β-linolenic acid, γ-linolenic acid, cholesterol esters, glycerides, etc.); β-linolenic acid, distearate, thiodipropionate and their derivatives (esters, ethers, peptides, lipids, nucleotides, nucleosides and their salts); and sulfinimide compounds (e.g., sulfenyl butyrate ... Propyl gallate, octyl gallate, and dodecyl gallate; flavonoids; catechins; bilirubin, biliverdin, and their derivatives; unsaturated fatty acids and their derivatives (e.g., gamma-linolenic acid, linoleic acid, arachidonic acid, oleic acid); folic acid and its derivatives; hydroquinone and its derivatives (e.g., arbutin); coenzyme Q (ubiquinone) and its reduced form (panthenol) and derivatives; vitamin C and its derivatives (e.g., ascorbate palmitate, stearate, dipalmitate, acetate, magnesium ascorbate phosphate, sodium ascorbate and magnesium salt, disodium ascorbate phosphate and sulfate, potassium ascorbate tocopherol phosphate, chitosan ascorbate); isoascorbic acid and its derivatives; tocopherol (vitamin E) and its derivatives (e.g., tocopherol acetate, linoleate, oleic acid, etc.). Esters and succinates, tocopherol polyethylene glycol-5, -10, -12, -18, -50 ethers, tocopherol polysorbate); vitamin A and its derivatives (e.g., retinyl palmitate); benzoin resin coniferyl benzoate; rutin and its derivatives (e.g., rutinic acid); disodium rutin disulfide; cinnamic acid and its derivatives (e.g., ferulic acid, ethyl ferulic acid, caffeic acid); kojic acid; chitosan glycolate and salicylate; butylated hydroxytoluene; butylated hydroxyanisole; nordihydroguaiac acid; nordihydroguaiac acid; trihydroxyphenylbutanone; uric acid and its derivatives; mannose and its derivatives; selenium and its derivatives (e.g., selenomethionine); stilbenes and their derivatives (e.g., stilbene oxide, trans-stilbene oxide), etc.

[0108] According to the present invention, a mixture of suitable derivatives (salts, esters, sugars, nucleotides, nucleosides, peptides, and lipids) containing these antioxidants, as well as these specific active ingredients or plant extracts (e.g., tea tree oil, rosemary extract, and rosmarinic acid), can be used. Typically, mixtures of the aforementioned antioxidants are possible.

[0109] According to one implementation scheme, water is an example of a suitable solvent. In principle, solvent mixtures can also be used.

[0110] In one embodiment, the soluble concentrate composition of the present invention can be stably stored at room temperature for 1 week to 24 months.

[0111] According to one embodiment of the present invention, after storing the stable agrochemical composition of the present invention for 24 months, the recovery rate of the residual amount of the active ingredient (i.e., kasugamycin) remains consistent with the initial concentration of kasugamycin in the composition.

[0112] In one embodiment, the present invention provides a method for preparing an agrochemical composition comprising kasugamycin hydrochloride.

[0113] According to one embodiment of the present invention, a stable agrochemical composition containing kasugamycin is used to control a variety of pathogenic pests.

[0114] According to one embodiment of the present invention, a stable agrochemical composition is used to control broad-spectrum microorganisms in the pre-emergence and post-emergence stages.

[0115] According to one embodiment of the present invention, the formulation of a stable agrochemical composition enables the active ingredient to be effectively absorbed by plants.

[0116] The combinations of the present invention can be developed into premixed compositions or kits, allowing the individual active substances to be mixed prior to application.

[0117] According to one embodiment of the present invention, a kit comprising a stable agrochemical composition is provided. The kit contains multiple components, including at least one of the components of the agrochemical composition comprising kasugamycin of the present invention.

[0118] According to one embodiment of the invention, the kit comprises kasugamycin or an agriculturally chemically acceptable salt thereof, and a nonionic surfactant in a ratio of 0.1:1 to 5:1.

[0119] In one embodiment of the invention, the kit may include at least one or all of the components used to prepare the stable agrochemical composition. For example, the kit may contain kasugamycin, a nonionic surfactant, an antimicrobial agent, a pH adjuster, and an agrochemically acceptable excipient.

[0120] One or more components may have been combined or pre-formulated. In embodiments where the kit provides more than two components, the components may have been combined and packaged as is in individual containers such as vials, bottles, jars, pouches, bags, and / or cans. In other embodiments, the two or more components of the kit may be packaged separately, i.e., they are not pre-formulated. Thus, the kit may include one or more individual containers, such as vials, jars, bottles, pouches, bags, and / or cans, each containing a single component of the stable herbicide composition.

[0121] In both forms, the components of the kit can be applied separately or together with other components, or as components of a combined composition according to the invention, to prepare an agrochemical composition according to the invention.

[0122] In one embodiment, the composition of the present invention further comprises a herbicide, a fungicide, an insecticide, a nematicide, an acaricide, or a combination thereof.

[0123] The method of this invention can be used to control a wide range of plant diseases.

[0124] Rice diseases include: rice blast (Magnaporthe grisea), leaf spot (Cochliobolus miyabeanus), sheath blight (Rhizoctonia solani), and seedling blight (Gibberella fujikuroi).

[0125] Wheat diseases include: powdery mildew (Erysiphe graminis), Fusarium blight (Fusarium graminearum, Fusarium avenacerum, Fusarium culmorum, Microdochium nivale), rust (Puccinia striiformis, P. graminis, P. recondita), powdery mildew (Micronectriella nivale), snow mold (Typhula sp.), loose smut (Ustilago tritici), wheat grain blight (Tilletia caries), and eye spot (Pseudocercosporella). herpotrichoides), leaf spot (Mycosphaerella graminicola), glumpy spot (Stagonospora nodorum), black spot and yellow spot (Pyrenophora tritici-repentis).

[0126] Barley diseases include: powdery mildew (Erysiphe graminis), Fusarium graminearum (Fusarium graminearum), Fusarium avenacerum (F. avenacerum), Fusarium culmorum (F. culmorum), Microdochium nivale (Microdochium nivale), rust (Puccinia striiformis, P. graminis, P. hordei), loose smut (Ustilago nuda), scald (Rhynchosporium secalis), net blight (Pyrenophorateres), leaf spot (Cochliobolus sativus), and sheath blight (Pyrenophora). graminea) and Rhizoctonia solani rot (Rhizoctonia solani).

[0127] Maize diseases include: smut (Ustilago maydis), brown spot (Cochliobolus heterostrophus), copper spot (Gloeocercospora sorghi), southern rust (Puccinia polysora), gray spot (Cercosporazeae-maydis), white spot (Phaeosphaeria mydis and / or Pantoea ananatis), and Rhizoctonia solani rot.

[0128] Citrus diseases include: black spot (Diaporthe citri), scab (Elsinoe fawcetti), penicillium rot (Penicillium digitatum, P. italicum), and brown rot (Phytophthora parasitica, Phytophthora citrophthora).

[0129] Apple diseases include: blossom blight (Monilinia mali), canker (Valsa ceratosperma), powdery mildew (Podosphaera leucotricha), Alternaria alternatapple pathotype, scab (Venturia inaequalis), powdery mildew, bitter rot (Colletotrichumacutatum), crown rot (Phytophthora cactorum), spot disease (Diplocarpon mali), and ring rot (Botryosphaeria berengeriana).

[0130] Pear diseases include: scab (Venturia nashicola, V. pirina), powdery mildew, black spot (Alternaria alternata), rust (Gymnosporangium haraeanum), and Phytophthora cactorum.

[0131] Peach diseases include: brown rot (Monilinia fructicola), powdery mildew, scab (Cladosporium carpophilum), and pseudostem spot rot (Phomopsissp.).

[0132] Grape diseases include: anthracnose (Elsinoe ampelina), late rot (Glomerella cingulata), powdery mildew (Uncinula necator), rust (Phakopsora ampelopsidis), black rot (Guignardia bidwellii), gray mold, and downy mildew (Plasmopara vitícola).

[0133] Japanese persimmon diseases include: anthracnose (Gloeosporium kaki) and leaf spot (Cercospora kaki, Mycosphaerella nawae).

[0134] Gourd diseases include: anthracnose (Colletotrichum lagenarium), powdery mildew (Sphaerotheca fuliginea), vine blight (Mycosphaerella melononis), Fusarium oxysporum wilt, downy mildew (Pseudoperonosporacubensis), Phytophthora sp., and damping-off (Pythium sp.).

[0135] Tomato diseases include: early blight (Alternaria solani), leaf mold (Cladosporium fulvum), and late blight (Phytophthora infestans).

[0136] Eggplant diseases include: brown spot (Phomopsis vexans) and powdery mildew (Erysiphe cichoracearum).

[0137] Diseases of cruciferous vegetables include: Alternaria japonica leaf spot, Cercosporella brassicae white spot, Plasmodiophora brassicae clubroot, and Peronospora parasitica downy mildew.

[0138] Onion diseases include: rust (Puccinia allii) and downy mildew (Peronospora destructor).

[0139] Soybean diseases include: purple seed spot (Cercospora kikuchii), black bean disease (Elsinoe glycines), pod and stem blight (Diaporthe phaseolorum var. sojae), soybean black spot (Septoria glycines), gray spot (Cercospora sojina), rust (Phakopsora pachyrhizi), yellow rust, brown stem rot (Phytophthora sojae), and Rhizoctonia solani rot.

[0140] Kidney bean diseases include: anthracnose (from the fungus *Colletotrichum lindemthianum*).

[0141] Peanut diseases include: leaf spot (Cercospora personata), brown spot (Cercospora arachidicola), and white mold (Sclerotium rolfsii).

[0142] Pea diseases include: powdery mildew (Erysiphepisi) and root rot (Fusarium solani f. sp. pisi).

[0143] Potato diseases include: early blight (Alternaria solani), late blight (Phytophthora infestans), powdery rot (Phytophthora erythroseptica), and powdery scab (Spongospora subterranean f. sp. subterranea).

[0144] Strawberry diseases include: powdery mildew (sphaerotheca humuli) and anthracnose (Glomerella cingulata).

[0145] Tea tree diseases include: vesicular blight (Exobasidium reticulatum), white scab (Elsinoe leucospila), gray blight (Pestalotiopsis sp.), and anthracnose (Colletotrichum theae-sinensis).

[0146] Tobacco diseases include: brown spot (Alternaria longipes), powdery mildew (Erysiphe cichoracearum), anthracnose (Colletotrichum tabacum), downy mildew (Peronospora tabacina), and black shank (Phytophthora nicotianae).

[0147] Rapeseed diseases include: sclerotinia sclerotiorum rot and Rhizoctonia solani rot.

[0148] Cotton diseases include: Rhizoctonia solani rot (Rhizoctonia solani).

[0149] Beet diseases include: Cercospora beticola leaf spot, Thanatephorus cucumeris leaf blight, Thanatephorus cucumeris root rot, and Aphanomyces cochlioides root rot.

[0150] Rose diseases include: black spot (Diplocarpon rosae), powdery mildew (Sphaerotheca pannosa), and downy mildew (Peronospora sparsa).

[0151] Chrysanthemum and other Asteraceae plant diseases include: downy mildew (Bremia lactucae), leaf blight (Septoria chrysanthemi-indici), and white rust (Puccinia horiana).

[0152] Various diseases, including: diseases caused by Pythium fungi (Pythium aphanidermatum, Pythium debarianum, Pythium graminicola, Pythium irregulare, Pythium ultimum, gray mold (Botrytis cinerea) and sclerotinia sclerotiorum).

[0153] Japanese radish diseases include: Alternaria bassicicola leaf spot (Alternaria bassicicola).

[0154] Turfgrass diseases include: circular spot (Sclerotinia homeocarpa), brown spot, and large spot (Rhizoctonia solani).

[0155] Banana diseases include: black banana leaf spot (Mycosphaerella fijiensis) and yellow banana leaf spot (Mycosphaerella musicola).

[0156] Sunflower diseases include: downy mildew (Plasmopara halstedii).

[0157] Seed diseases or various early-stage plant diseases caused by Aspergillus spp., Penicillium spp., Fusarium spp., Gibberella spp., Tricoderma spp., Thieviopsis spp., Rhizopus spp., Mucor spp., Corticium spp., Phona spp., Rhizoctonia spp., and Diplodia spp.

[0158] Viral diseases of various plants mediated by species such as Polymixa spp. or Olpidium spp.

[0159] Most plant pathogenic bacteria belong to the following genera: Erwinia, Pectobacterium, Pantoea, Agrobacterium, Pseudomonas, Ralstonia, Burkholderia, Acidovorax, Xanthomonas, Clavibacter, Streptomyces, Xylella, Spiroplasma, and Phytoplasma.

[0160] In particular, the compositions of the present invention have significant control effects against *Pseudomonas syringae*, *Xanthomonas* spp., *Erwinia amylovora*, *Erwinia carotovora*, *Pyricularia oryzae*, *Xanthomonas axonopodispv. Vesicatoria*, *Burkholderia andropogonis*, and *Streptomyces scabies*.

[0161] Examples of crops to which the compositions of the present invention can be used include, but are not limited to, corn, rice, wheat, barley, rye, oats, sorghum, cotton, soybeans, peanuts, buckwheat, sugar beets, rapeseed, sunflowers, sugarcane, and tobacco; vegetables: Solanaceae vegetables, such as eggplant, tomato, bell pepper, black pepper, and potato; Cucurbitaceae vegetables, such as cucumber, pumpkin, zucchini, watermelon, cantaloupe, and squash; Cruciferous vegetables, such as radish, white radish, horseradish, kohlrabi, Chinese cabbage, cabbage, mustard greens, broccoli, and cauliflower; Asteraceae vegetables, such as burdock, wormwood, artichoke, and lettuce; Liliaceae vegetables, such as scallions, onions, garlic, and asparagus; Apiaceae vegetables, such as carrots, parsley, celery, and parsnips; Chenopodiaceae vegetables, such as spinach and lettuce; and Mintaceae vegetables, such as perilla. frutescens, mint, basil, etc.; strawberries, sweet potatoes, yams (Dioscorea japonica), taro, etc.; flowering and foliage plants, lawn grasses; fruits: pome fruits, such as apples, pears, citrus fruits, etc.; hard-fleshed fruits, such as peaches, plums, nectarines, apricots (Prunus mume), cherries, apricots, dried plums, etc.; citrus fruits, such as oranges, lemons, limes, grapefruits, etc.; nuts, such as chestnuts, walnuts, hazelnuts, almonds, pistachios, cashews, macadamia nuts, etc.; berries, such as blueberries, cranberries, blackberries, raspberries, etc.; grapes, persimmons, olives, plums, bananas, coffee, dates, coconuts, etc.; trees other than fruit trees; tea trees, mulberry trees, flowering plants; trees, such as ash trees, birch trees, dogwood, eucalyptus trees, ginkgo trees (Ginkgo biloba), lilac trees, maple trees, oak trees, poplar trees, Southern European redbud trees, sweetgum trees (Liquidambar formosana). (formosana), sycamore, beech, Japanese cypress, fir, hemlock, juniper, pine, spruce and yew, etc.

[0162] In one embodiment, the present invention provides a method for controlling or inhibiting plant pathogens, comprising applying the composition described herein to the plant or plant part or plant propagation material or its site.

[0163] In one embodiment, the present invention provides a method for controlling or inhibiting plant pathogens, comprising applying a composition to a site of plant pathogen infection, a plant, a plant part, or plant propagation material, the composition comprising:

[0164] (i) Kasugamycin or its salts, and

[0165] (ii) Nonionic surfactants,

[0166] The weight ratio of kasugamycin or its salt to nonionic surfactant ranges from 0.1:1 to 5:1, and the pH ranges from 2 to 4.

[0167] In one embodiment, the present invention provides a method for controlling or inhibiting plant pathogens, comprising applying a composition to a site of plant pathogen infection, a plant, a plant part, or plant propagation material, the composition comprising:

[0168] (i) Kasugamycin hydrochloride, and

[0169] (ii) Nonionic surfactants,

[0170] The weight ratio of kasugamycin or its salt to nonionic surfactant ranges from 0.1:1 to 5:1, and the pH ranges from 2 to 4.

[0171] The combination of the present invention can be applied simultaneously as a tank mix or formulation, or sequentially. Application can be done to the soil before, before, or after plant emergence. Application can also be carried out as a foliar spray at different times during crop development, once or twice in the early or late stages after emergence.

[0172] The fungicidal combination according to the invention can be applied before or after the useful plant or its propagation material is infected by fungi, bacteria or other microorganisms. The soluble concentrate formulation significantly improves disease control efficacy, reduces the occurrence of microbial resistance, and increases crop yield.

[0173] The invention will now be described with reference to the following specific examples. It should be noted that the examples appended below are illustrative and not limiting of the invention, and those skilled in the art will be able to devise many alternative examples without departing from the scope of the invention.

[0174] Example

[0175] Example 1: Soluble Concentrate Composition

[0176]

[0177] Method: Add the required amount of water to a preparation tank, then add the amounts of kasugamycin hydrochloride, ethoxylated isotretinoin, potassium sorbate, and monoethylene glycol as shown in the table above, while stirring. Keep the system continuously stirred after each addition. Adjust the pH with an aqueous hydrochloric acid solution. If pH adjustment is required, continue stirring the mixture to obtain a soluble concentrate composition.

[0178] Example 2:

[0179] Stability data

[0180]

[0181] M refers to the month.

[0182] Table 2 above clearly demonstrates the stability of the agrochemical composition of this invention. The composition underwent stability evaluation at room temperature for over 24 months. As clearly shown in the table, the stability parameters at each time point met the corresponding requirements. Kasugamycin remained stable in monthly tests, exhibiting extremely low degradation rates. The system pH consistently remained within the low range of 2.80-3.10, which further promoted the stability of kasugamycin.

[0183] Example 3: Surfactant Screening Study

[0184] To screen the most suitable surfactant and its concentration for the stable kasugamycin soluble concentrate composition of this invention, a surfactant screening study was conducted. Accordingly, anionic surfactant, sodium dioctyl sulfosuccinate (soluble in propylene glycol), was used to formulate combinations A and B as shown in Table 3 below. The compositions of this invention use a nonionic surfactant, ethoxylated isotridecyl alcohol. All compositions underwent accelerated thermal stability (AHS) testing conditions, i.e., accelerated thermal stability testing conditions at 54°C for 14 days.

[0185] Table 3:

[0186]

[0187] Therefore, compositions A and B using anionic surfactants exhibited sedimentation under accelerated thermal stability testing conditions. However, the compositions of the present invention using ethoxylated isotrimetrol did not exhibit sedimentation and were used to prepare kasugamycin formulations.

Claims

1. An agricultural chemical composition comprising: a) Kasugamycin or its salts, b) Nonionic surfactants, and c) Agrochemically acceptable excipients The pH range of the composition is 2 to 4.

2. The composition according to claim 1, wherein, Kasugamycin is in the form of kasugamycin hydrochloride.

3. The composition according to claim 1, wherein, The composition is a soluble concentrate.

4. The composition according to claim 1, wherein, The nonionic surfactant includes alcohol alkoxylates, such as alcohol ethoxylates.

5. The composition according to claim 4, wherein, Alcohol ethoxylates include ethoxylated isotridecyl alcohol.

6. The composition according to claim 1, wherein, The weight ratio of kasugamycin to the nonionic surfactant ranges from 0.1:1 to 5:

1.

7. The composition according to claim 6, wherein, The weight ratio of kasugamycin hydrochloride to ethoxylated isothiazol ranges from 0.1:1 to 5:

1.

8. The composition according to claim 1, wherein, The agrochemically acceptable excipients are selected from the group consisting of surfactants, pH adjusters, buffers, preservatives, disintegrants, or combinations thereof.

9. The composition according to claim 1, wherein, The concentration range of kasugamycin is 0.1% to 20% w / w.

10. The composition according to claim 1, wherein, The concentration range of the nonionic surfactant is 0.1% to 3% w / w.

11. A soluble concentrate comprising: a) Kasugamycin or its salts, b) Nonionic surfactants, c) Antimicrobial agents, d) pH adjusters, and e) Excipients that are acceptable in agricultural chemistry.

12. The concentrate according to claim 11, wherein the pH range of the soluble concentrate is 2 to 4.

13. The composition according to claim 1, wherein the composition further comprises other pesticides selected from fungicides, herbicides, insecticides, and biostimulants.

14. A method for controlling pathogenic diseases of crops, comprising applying to a plant, plant part or plant propagation material a composition of an agrochemical containing kasugamycin or a salt thereof, said composition having a pH range of 2 to 4.

15. The use of the agrochemical composition according to claim 1 in controlling pathogenic infections in crops.

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