Stable synergistic pesticidal composition and process of preparation thereof
A synergistic pesticidal composition of Dinotefuran, Formula I, and Fluxametamide addresses pest resistance and toxicity issues, offering enhanced pest control and environmental safety.
Patent Information
- Authority / Receiving Office
- WO · WO
- Patent Type
- Applications
- Current Assignee / Owner
- RANI SANGEETA
- Filing Date
- 2026-01-23
- Publication Date
- 2026-07-30
AI Technical Summary
Conventional pesticides face challenges such as pest resistance, adverse effects on non-target organisms, ecological disruption, and environmental contamination, necessitating the development of sustainable and effective pest management strategies.
A stable synergistic pesticidal composition combining Dinotefuran, a compound of Formula I, and Fluxametamide, which leverages multiple modes of action to enhance pest control efficacy, reduce resistance, and minimize toxicity to non-target organisms.
The composition provides broad-spectrum pest control with reduced toxicity, improved stability, and longer shelf life, effectively managing resistant pest populations while promoting ecological balance and crop health.
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Abstract
Description
[0001] STABLE SYNERGISTIC PESTICIDAL COMPOSITION AND PROCESS OF PREPARATION THEROF
[0002] FIELD OF THE INVENTION
[0003] The present invention relates to a stable synergistic pesticidal composition comprising A) Dinotefuran or its agrochemically acceptable salts, isomers, esters and derivatives; B) a compound of Formula I, i.e., N-[2,6-bis(l-methylethyl)-4-phenoxyphenyl]-N'-(l,l-dimethylethyl)thiourea or its agrochemically acceptable salts, isomers, esters and derivatives; and C) Fluxametamide or its agrochemically acceptable salts, isomers, esters or its derivatives for effective control of various insect, pests, and wide range of pesticidal diseases. Further, the present invention also relates to a process for preparation of such pesticidal composition for synergistic and efficacious control of various pests including but not limited to insects-pests.
[0004] BACKGROUND OF THE INVENTION
[0005] Exponential demand for agricultural yields has driven the need for effective pest management strategies to safeguard crops from various detrimental insects and pests. Traditional pest control methods have often face challenges such as the emergence of resistance in target pest populations and adverse effects on nontarget species that can disrupt ecological balance.
[0006] Use of pesticides is one of the vital tools in modern agriculture, enabling farmers to protect crops from a variety of pests, including insects, etc. Despite their effectiveness, conventional pesticides have raised significant concerns regarding their environmental impact, human health risks, and the development of pest resistance. These issues have compensated researchers and agricultural professionals to seek alternative solutions that are not only efficacious but also sustainable and environmentally friendly. Pesticides are often associated with a range of adverse effects, including toxicity to non-target organisms, including beneficial insects, wildlife, and humans. Furthermore, the persistence of many synthetic pesticides in the environment can lead to soil and water contamination, posing long-term risks to ecosystems and public health. In addition, the continuous use of the same chemical classes has resulted in the emergence of resistant pest populations, necessitating the development of new and innovative pest management strategies.
[0007] The present invention addresses these challenges by providing a novel pesticidal composition that imparts an enhanced efficacy as compared to the existing pesticidal combinations. This composition is designed to target a broad spectrum of agricultural pests while minimizing toxicity to non-target organisms and reducing the risk of resistance development. Furthermore, the formulation ensures enhanced stability and longer shelf life, ensuring that it remains effective under various storage conditions and application scenarios.Various prior arts in pesticidal compositions are tailored based on the active ingredients are used along with their intended applications. However, existing pesticidal combinations shows adverse effect on plants and crops such as discoloration of plant leaves, resistance to complex pests and are ineffective against various stages of insect pests and diseases.
[0008] Reference can be made to CN103380781 which discloses an insecticidal mixture comprising lambda cyhalothrin in an effective amount ranging between 0.5% and 12% and Diafenthiuron in an effective amount ranging between 15% and 70%, wherein the lambda cyhalothrin and Diafenthiuron are present in a ratio ranging from 1:4 to 1:35, and at least one pesticidal excipient.
[0009] Further reference can be made to CN103053587 which discloses the composite insecticidal and bactericidal composition containing dinotefuran and azoxystrobin is characterized in that the insecticidal and bactericidal composition takes dinotefuran and azoxystrobin as effective components, wherein the weight ratio of dinotefuran to azoxystrobin is 1: 30 or 1: 20.
[0010] In view of the factors discussed, there is a pressing need for novel pesticidal formulations that capitalize on the distinctive properties and mechanisms of action. By emphasizing combinations that enhance pest control effectiveness while mitigating resistance and non-target toxicity, the advance sustainable agricultural practices can be followed. This approach not only supports the economic viability of farmers but also contributes to the health of ecosystems and promotes sustainable agricultural development. Consequently, the present invention pertains to a stable synergistic pesticidal composition that demonstrates long-lasting effects and reduced toxicity compared to existing pesticidal formulations.
[0011] Thus, formulating a pesticidal composition that combines dinotefuran, a compound of Formula I, and Fluxametamide presents an innovative approach to enhance pest control effectiveness. By leveraging multiple modes of action, this composition aims to reduce the risk of resistance development and improve the overall efficacy of pest management strategies. Specifically, the synergistic effects of these components may facilitate improved control over a wider range of pests as compared to the solo compositions, thereby promoting the sustainability of agricultural practices.
[0012] The present disclosure is a solution to the aforementioned problems and provides a stable synergistic pesticidal composition including A) Dinotefuran or its agrochemically acceptable salts, esters and derivatives; B) a compound of Formula I, i.e., N-[2,6-bis(l-methylethyl)-4-phenoxyphenyl]-N'-(l,l-dimethylethyl)thiourea or its agrochemically acceptable salts, esters and derivatives; and C) Fluxametamide or its agrochemically acceptable isomers,salts, esters or its derivatives. Accordingly, this invention discloses the specific compounds used in this innovative ternary composition.
[0013] Through extensive research and development, the inventor of the present invention has successfully combined pesticidal compounds to create a novel pesticidal composition with a broad-spectrum activity and improved efficacy. This composition exhibits synergistic effects and demonstrates significantly enhanced efficacy as compared to the solo compositions. Accordingly, the present invention outlines the specific compounds involved in this innovative formulation and the process to formulate the composition. Dinotefuran, is an insecticide that belongs to nitroguanidine or nitroguanidine neonicotinoid class of chemical compounds. Dinotefuran shows contact and Systemic and stomach action. It effects the nervous system of insects by blocking on Nicotinic acetylcholine receptor (nAChR) channels. It is used to control a wide range of sucking pests including Whiteflies; Mealybugs; Thrips; Plant hoppers; Leafminers; Aphids; etc. It is effectively used for crops such as Vegetables; Fruit; Turf; Rice crops; etc.
[0014] Further a compound of Formula I chemically known as N-[2,6-bis(l-methylethyl)-4-phenoxyphenyl]-N'-(1,1 -dimethylethyl)thiourea, is an insecticide, acaricide and miticide. Diafenthiuron is a thiourea insecticide and acaricides, which shows broad spectrum, contact and stomach action with some ovicidal activity. It acts by inhibiting oxidative phosphorylation by inhibiting mitochondrial ATP synthase. It is effective against sucking pests including Aphids; Whiteflies; Diamond back moth; thrips; Jassids; etc. It is suitable to use for crops such as Cotton; Fruit trees; Ornamentals; Soybeans; etc.
[0015] Further, Fluxametamide is a broad-spectrum isooxazoline insecticide, belongs to the amide class of insecticides. Fluxametamide is a racemate comprising equimolar amounts of (R)- and (S)-fluxametamide. It operates through a unique mechanism involving the modulation of insect ion channels, ultimately leading to paralysis and death. Incorporating fluxametamide into pest management strategies offers an additional mode of action, which is vital for managing resistance in pest populations that have become accustomed to conventional insecticides. It is effective against a broad spectrum of pests including insects such as Houseflies; Spider mite; Leafhoppers to prevent the harms to crops such as Strawberries, Aubergine, Tea, etc.
[0016] The present invention satisfies the existing needs, as well as others, and generally overcomes the deficiencies found in the prior art. The pesticidal composition of the present invention is synergistic, efficacious, environmentally friendly, cost-effective, simple to formulate, stable and is safe and easy to use. Thus, a stable synergistic pesticidal composition of the present invention aims to overcome the problems of the prior art and provides a stable synergistic pesticidal composition comprising bioactive amounts ofcomprising pesticidal composition comprising A) Dinotefuran or its agrochemically acceptable salts, esters and derivatives; B) a compound of Formula I, i.e., N-[2,6-bis(l-methylethyl)-4-phenoxyphenyl]-N'-(l,l-dimethylethyl)thiourea or its agrochemically acceptable salts, esters and derivatives; and C) Fluxametamide or its agrochemically acceptable isomers, salts, esters or its derivatives for effective control of various pests, insect-pests and a wide range of pesticidal diseases.
[0017] OBJECTIVES AND ADVANTAGES OF THE INVENTION
[0018] The main objective present invention is to introduce a novel and effective stable synergistic pesticidal composition that demonstrates high efficacy and stability, offering broad spectrum of action against a diverse array of pests, including sucking and chewing insect pests -pests, and diseases.
[0019] Another object of the invention is to provide a composition that delivers synergistic or enhanced pesticidal efficacy by combining active ingredients having different modes of action, thereby ensuring rapid knockdown, prolonged residual activity, and improved overall pest management.
[0020] A further object of the invention is to provide a pesticidal composition that is effective against resistant insect-pests populations, particularly those that have developed resistance to single-mode or conventional insecticides, thus contributing to resistance management strategies.
[0021] Yet another object of the invention is to provide a composition that is effective at lower application doses, thereby reducing chemical load on the environment while maintaining high levels of pest control.
[0022] Another object of the present invention is to provide a pesticidal composition that is safe to crops (non-phytotoxic) when applied at recommended doses and suitable for use in foliar, soil, or seed treatment applications, depending on formulation type.
[0023] A further object of the invention is to provide a composition that enhances crop health, vigor, and yield by minimizing pest-induced stress and damage during critical growth stages.
[0024] Another object of the invention is to provide a cost-effective and farmer-friendly pesticidal solution with improved stability, ease of handling, and longer shelf life.
[0025] Another objective of the present invention delivers an improved, stable, and ready-to-use pesticidal composition that showcases superior synergistic efficacy compared to existing formulations, mixtures, or compositions, ensuring enhanced pest control.Another objective of the present invention is to provide selective effectiveness while significantly reducing adverse effects on non-target organisms, particularly beneficial species, thus promoting ecological balance.
[0026] Yet another objective of the present invention is to provide improved, stable and ready to use pesticidal composition that demonstrates superior synergistic efficacy compared to existing formulations, mixtures or compositions ensuring improved insects-pests control.
[0027] Yet another objective of the present invention to provide a novel and effective stable synergistic pesticidal composition effectively targeting all life stages of major plant pathogens and promoting overall plant health and crop yield.
[0028] It is yet another objective of the present invention to provide a method and a stable synergistic pesticidal composition for controlling pests including insects.
[0029] Yet another objective of the present invention is to provide a composition and method for controlling various pests including sucking pests including pesticidal and insect diseases in plants, crops and plant propagation materials.
[0030] Another objective of the present invention is to provide one shot application of novel and effective stable synergistic pesticidal composition for killing / controlling highly resistant pests at lower application rates.
[0031] Yet another objective of the present invention is to provide an improved formulation that ensures uniform spray-ability, enhanced stability, permeability & flowability.
[0032] It is another objective of the present invention to provide a novel and effective stable synergistic pesticidal composition which is environmentally safe, possesses broad spectrum bio-efficacy, is non-phytotoxic and has improved stability during the desired shelf life at various temperature and pH conditions and has enhanced efficacy and penetration capacity and is economically more beneficial.
[0033] It is another objective of the present invention to provide a novel and effective stable synergistic pesticidal composition which further comprises additives, inert ingredients and / or adjuvants, for providing the enhanced stability, enhanced permeability, improved penetration capacity, uniform spray-ability, improved rain-fastness, enriched biotic factors, better flowability, enhanced spreading or coverage effect, effective storage stability, longer residual effect, improved uptake of active ingredients, and safer to the environment attributes to the composition of present invention.It is another objective of the present invention is to provide a stable synergistic pesticidal composition that protects crop and the environmental damage.
[0034] Another main objective of the present invention is to provide a novel and effective stable synergistic pesticidal composition that is environmentally safe, exhibits broad-spectrum bio-efficacy, is non-phytotoxic, and maintains improved stability throughout its intended shelf life across various temperature and pH conditions, while also enhancing efficacy, penetration capacity, and economic viability.
[0035] Yet another objective of present invention is to provide a stable synergistic pesticidal composition that improves germination rate, increased plants stand count and plant health, which results in higher yield.
[0036] Another objective of the present invention is to provide a stable synergistic pesticidal composition comprising A) Dinotefuran or its agrochemically acceptable salts, esters and derivatives; B) a compound of Formula I, i.e., N-[2,6-bis(l-methylethyl)-4-phenoxyphenyl]-N'-(l,l-dimethylethyl)thiourea or its agrochemically acceptable salts, esters and derivatives; and C) Fluxametamide or its agrochemically acceptable isomers, salts, esters or its derivatives.
[0037] Yet another objective of the present invention is to provide a process for the preparation of a stable synergistic pesticidal composition comprising A) Dinotefuran or its agrochemically acceptable salts, esters and derivatives; B) a compound of Formula I, i.e., N-[2,6-bis(l-methylethyl)-4-phenoxyphenyl]-N'-(l,l-dimethylethyl)thiourea or its agrochemically acceptable salts, esters and derivatives; and C) Fluxametamide or its agrochemically acceptable isomers, salts, esters or its derivatives.
[0038] Some or all these and other objects of the invention can be achieved by way of the invention described hereinafter.
[0039] ADVANTAGES:
[0040] 1. The stable synergistic pesticidal composition is effective in protecting a wide range of crops, including fruits, vegetables, cereals, ornaments, flowers and seeds against major plant diseases including foliar, stem and root diseases and shows no phytotoxicity effect and provide a stable synergistic pesticidal composition that shows technical advancement over the existing combination of pesticides and also proves to has an improved rain fastness.
[0041] 2. The stable synergistic pesticidal composition ensures better control of plant / crop in a shorter period of time and shows to have decrease chances of resistance against pesticidal diseases and shows tohave an improved stability during the desired shelf life and promotes plant health and increases plant yield in the field.
[0042] 3. The stable synergistic pesticidal composition improves germination rate, increased plant stand count, lower cost of application, better cost-benefit ratio to the end user, reduced wear of equipment and loss caused by mechanical damage to the crop and soil.
[0043] 4. The stable synergistic pesticidal composition of the present invention results in significant effective control against various pest and insects-pests diseases including but not limited to wide range of pests including sucking pests, Whiteflies; Mealybugs; Thrips; Fruit borer, Plant hoppers; Leafminers; Aphids; Whiteflies; Diamondback moth; thrips; Jassids; Houseflies; Leafhoppers; etc.
[0044] 5. The stable synergistic pesticidal composition can be applied to various crops and plants including but not limited to Vegetables; Fruit; Turf; Rice crops; Cotton; Fruit trees; Ornamentals; Soybeans; Strawberries, Aubergine, Tea, etc.
[0045] SUMMARY OF THE INVENTION
[0046] Accordingly, the main aspect of the present invention is to provide a stable synergistic pesticidal composition having high pests control efficacy.
[0047] Accordingly, the present invention relates to a stable synergistic pesticidal composition comprising:
[0048] A) Dinotefuran or its agrochemically acceptable isomers, salts, esters and derivatives;
[0049] B) Compound of Formula I, i.e., N-[2,6-bis(l-methylethyl)-4-phenoxyphenyl]-N'-(l,l- dimethylethyl)thiourea or its agrochemically acceptable salts, esters and derivatives; and
[0050] C) Fluxametamide or its agrochemically acceptable isomers, salts, esters or its derivatives.
[0051] In another aspect, the present invention provides a stable synergistic pesticidal composition comprising:
[0052] A) Dinotefuran or its agrochemically acceptable isomers, salts, esters and derivatives;
[0053] B) Compound of Formula I, i-e., N-[2,6-bis(1-methylethyl)-4-phenoxyphenyl]-N′-(1,1-dimethylethyl)thiourea or its agrochemically acceptable salts, esters and derivatives;C) Fluxametamide or its agrochemically acceptable isomers, salts, esters or its derivatives; andD) One or more agrochemically acceptable excipients.
[0054] In one another aspect, the present invention provides a stable synergistic pesticidal composition comprising:A) Dinotefuran or its agrochemically acceptable isomers, salts, esters and derivatives;
[0055] B) Compound of Formula I, i.e., N-[2,6-bis(l-methylethyl)-4-phenoxyphenyl]-N'-(l,l- dimethylethyl)thiourea or its agrochemically acceptable salts, esters and derivatives;
[0056] C) Fluxametamide or its agrochemically acceptable isomers, salts, esters or its derivatives; and D) At least one or more additive.
[0057] In one another aspect, the present invention provides a stable synergistic pesticidal composition comprising:
[0058] A) Dinotefuran or its agrochemically acceptable isomers, salts, esters and derivatives;
[0059] B) Compound of Formula I, i.e., N-[2,6-bis(l-methylethyl)-4-phenoxyphenyl]-N'-(l,l- dimethylethyl)thiourea or its agrochemically acceptable salts, esters and derivatives;
[0060] C) Fluxametamide or its agrochemically acceptable isomers, salts, esters or its derivatives; and D) At least one or more additive selected from urea clathrate, Siloxane Polyalkyleneoxide copolymer, tallow amine ethoxylate, ammonium sulphate, and epoxide soybean oil either alone or in combination thereof
[0061] In one another aspect, the present invention provides a stable synergistic pesticidal composition comprising:
[0062] A) Dinotefuran or its agrochemically acceptable isomers, salts, esters and derivatives;
[0063] B) Compound of Formula I, i.e., N-[2,6-bis(l-methylethyl)-4-phenoxyphenyl]-N'-(l,l- dimethylethyl)thiourea or its agrochemically acceptable salts, esters and derivatives;
[0064] C) Fluxametamide or its agrochemically acceptable isomers, salts, esters or its derivatives;
[0065] D) At least one or more additive selected from urea clathrate, Siloxane Polyalkyleneoxide copolymer, tallow amine ethoxylate, ammonium sulphate, and epoxide soybean oil either alone or in combination thereof; and
[0066] E) One or more agrochemically acceptable excipients.
[0067] In one another aspect, the present invention provides a stable synergistic pesticidal composition comprising:
[0068] A) Dinotefuran or its agrochemically acceptable isomers, salts, esters and derivatives, in the range of 0.001-90% by weight of the composition;B) Compound of Formula I, i.e., N-[2,6-bis(l-methylethyl)-4-phenoxyphenyl]-N'-(l,l- dimethylethyl)thiourea or its agrochemically acceptable salts, esters and derivatives, in the range of 0.001-90% by weight of the composition; and
[0069] C) Fluxametamide or its agrochemically acceptable isomers, salts, esters or its derivatives in the range of 0.001-90% by weight of the composition.
[0070] In one another aspect, the present invention provides a stable synergistic pesticidal composition comprising:
[0071] A) Dinotefuran or its agrochemically acceptable isomers, salts, esters and derivatives, in the range of 0.001-90% by weight of the composition;
[0072] B) Compound of Formula I, i.e., N-[2,6-bis(l-methylethyl)-4-phenoxyphenyl]-N'-(l,l- dimethylethyl)thiourea or its agrochemically acceptable salts, esters and derivatives, in the range of 0.001-90% by weight of the composition;
[0073] C) Fluxametamide or its agrochemically acceptable isomers, salts, esters or its derivatives in the range of 0.001-90% by weight of the composition; and
[0074] D) One or more agrochemically acceptable excipients.
[0075] In one another aspect, the present invention provides a stable synergistic pesticidal composition comprising: A) Dinotefuran or its agrochemically acceptable isomers, salts, esters and derivatives, in the range of 0.001-90% by weight of the composition;
[0076] B) Compound of Formula I, i.e., N-[2,6-bis(l-methylethyl)-4-phenoxyphenyl]-N'-(l,l- dimethylethyl)thiourea or its agrochemically acceptable salts, esters and derivatives, in the range of 0.001-90% by weight of the composition;
[0077] C) Fluxametamide or its agrochemically acceptable isomers, salts, esters or its derivatives in the range of 0.001-90% by weight of the composition;
[0078] D) At least one or more additive selected from urea clathrate, Siloxane Polyalkyleneoxide copolymer, tallow amine ethoxylate, ammonium sulphate, and epoxide soybean oil either alone or in combination thereof, in the range of 0.001-20% by weight of the composition; and
[0079] E) One or more agrochemically acceptable excipients.
[0080] In yet another aspect, the present invention provides a process for preparation of the stable synergistic pesticidal composition comprising:A) Dinotefuran or its agrochemically acceptable isomers, salts, esters and derivatives;
[0081] B) Compound of Formula I, i.e., N-[2,6-bis(l-methylethyl)-4-phenoxyphenyl]-N'-(l,l- dimethylethyl)thiourea or its agrochemically acceptable salts, esters and derivatives; and
[0082] C) Fluxametamide or its agrochemically acceptable isomers, salts, esters or its derivatives.
[0083] In an aspect of the present invention, the present invention provides a stable synergistic pesticidal composition which further comprises additives and / or adjuvants, for providing the following attributes to the composition of present invention:
[0084] a) reduced phytotoxicity, target specificity, improved compatibility
[0085] b) enhanced stability, permeability, and spreading or coverage effect,
[0086] c) improved penetration capacity, and improved rain-fastness,
[0087] d) uniform spray-ability, storage stability, and longer residual effect,
[0088] e) enriched biotic factors, and better flowability,
[0089] f) improved uptake of active ingredients, and safer to the environment,
[0090] g) improved shelf life of formulations.
[0091] In another aspect, the present synergistic pesticidal composition is stable and has enhanced shelf life and effectively control wide range of pests including insects-pests diseases in various crops. In another aspect, the present invention provides a stable synergistic pesticidal composition which has enhanced efficacy and penetration capacity.
[0092] DETAILED DESCRIPTION OF THE INVENTION
[0093] In describing the embodiments of the invention, specific terminology is resorted for sake of clarity. However, it is not intended that the invention be limited to specific terms so selected and it is to be understood that each specific term includes all technical equivalents that operate in a similar manner to accomplish a similar purpose.
[0094] Discussed below are some representative embodiments of the present invention. The invention in its broader aspects is not limited to the specific details and representative methods.
[0095] All technical and scientific terms used herein have the same meanings as commonly understood by someone ordinarily skilled in the art to which the present subject matter belongs.The terminology used, in the present disclosure, is only for the purpose of explaining a particular embodiment and such terminology shall not be considered to limit the scope of the present disclosure.
[0096] As used in the present disclosure, the forms "a,” "an," and "the" may be intended to include the plural forms as well, unless the context clearly suggests otherwise. Thus, for example, reference to a composition containing “a compound” includes a mixture of two or more compounds. It should also be noted that the term “or” is generally employed in its sense including “and / or” unless the content clearly dictates otherwise.
[0097] The terms "comprises", "comprising", “including”, and “having” are open ended transitional phrases and therefore specify the presence of stated features, integers, steps, operations, elements, but do not forbid the presence or addition of one or more other features, integers, steps, operations, elements, components, and / or groups thereof. The particular order of steps disclosed in the method and process of the present disclosure is not to be construed as necessarily requiring their performance as described or illustrated. It is also to be understood that additional or alternative steps may be employed.
[0098] Variations or modifications to the composition of this invention, within the scope of the invention, may occur to those skilled in the art upon reviewing the disclosure herein. Such variations or modifications are well within the spirit of this invention.
[0099] The expression of various quantities in terms of “% w / w” or “%” means the percentage by weight, relative to the weight of the total solution or composition unless otherwise specified.
[0100] The term “active ingredient” (a.i.) or “active agent” or “active” used herein refers to that component of the composition responsible for control of various insects-pests and diseases at the same time.
[0101] The term “crop” shall include a multitude of desired crop plants or an individual crop plant growing at a locus.
[0102] The term “synergistic”, as used herein, refers to the combined action of two or more active agents blended together and administered conjointly that is greater than the sum of their individual effects.
[0103] “Bioactive amounts” as mentioned herein means that amount which, when applied for treatment of crops, is sufficient to give effect in such treatment.The term “control” means to inhibit the ability of insect pests to survive, grow, feed and / or reproduce, or to limit the insect pests’ related damage or loss in crop plants. To “control” insect pests may or may not mean killing the insects although, it preferably means killing the insect pests.
[0104] The term “health of a plant” or “plant health” is defined as a condition of the plant and / or its products. As a result of the improved health; yield, plant vigour, quality and tolerance to abiotic or biotic stress is increased. As a result, the health of a plant is increased even in the absence of pest pressure.
[0105] Accordingly, in an especially preferred embodiment according to the invention, the health of a plant is increased both in the presence and absence of biotic or abiotic stress factors. An increase in plant vigor may for example result in an increased yield and / or tolerance to abiotic or biotic stress.
[0106] One indicator for the condition of the plant is the yield. “Yield” is to be understood as any plant product of economic value that is produced by the plant such as grains, fruits, vegetables, nuts, grains, seeds, wood (e.g., in the case of silviculture plants) or even flowers (e.g., in the case of gardening plants, ornamentals). The plant products may in addition be further utilized and / or processed after harvesting.
[0107] In another preferred embodiment of the invention, the yield of the plants treated according to the method of the invention, is increased synergistically.
[0108] In another especially preferred embodiment of the invention, the plant vigour of the treated plant is increased. In another preferred embodiment of the invention, the plant vigour of the plants treated according to the composition of the present invention is increased synergistically.
[0109] Another indicator for the condition of the plant is the “quality” of a plant and / or its products.
[0110] In an especially preferred embodiment of the invention, the quality of the treated plant is increased.
[0111] In another preferred embodiment of the invention, the quality of the plants treated according to the method of the invention, is increased synergistically.
[0112] The term rain fastness refers to the ability of a substance to remain effective after being applied to a surface and then exposed to rainfall or irrigation. In other words, it measures how well the substance adheres to the target surface and resists being washed away by water. A low rain fastness indicates that it may be washed off or diluted by rainfall, reducing its efficacy.
[0113] The term " Increased uptake of active ingredient" refers to the enhanced absorption or penetration of the active component of a substance into the target organism or plant. This increased uptake can lead to greater effectiveness of the product in controlling various insects-pests and wide range of diseases at the same time.It may occur through various mechanisms, such as improved formulation, adjuvants that enhance penetration, or modifications to the active ingredient itself to facilitate absorption. Overall, increased uptake of the active ingredient results in improved performance of the product in achieving its intended purpose.
[0114] The term “benefit: cost” refers to a ratio used in a cost-benefit analysis to summarize the overall relationship between the relative costs and benefits of a proposed composition. If a treatment has a benefit-cost ratio greater than 1.0, the treatment is expected to deliver a positive and better outcome.
[0115] In one embodiment of the present invention, the yield of the treated plant is increased.
[0116] In another embodiment of the present invention, there is synergistic and efficacious control of various insect-pests and diseases affecting the plants and crops.
[0117] Another embodiment of the present invention, includes within its scope, all possible salts, esters and derivatives of the active ingredients of the composition.
[0118] It is also to be understood that the terminology used herein is for the purpose of describing particular embodiments of the invention only and is not intended to limit the scope of the invention in any manner. The use of examples anywhere in this specification including examples of any terms discussed herein is illustrative only, and in no way limits the scope and meaning of the invention or of any exemplified term. Likewise, the invention is not limited to various embodiments given in this specification.
[0119] Unless otherwise defined, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention pertains. In the case of conflict, the present document, including definitions will control.
[0120] The composition or formulation according to the present invention has a reduced or zero phytotoxicity with respect to agricultural crops. This results in the present invention effective and possible in the selective control of diseases including insects-pest’s control.
[0121] In an embodiment, the stable synergistic pesticidal composition or formulation has a reduced or zero phytotoxicity with respect to important agricultural crops. This results in the present invention effective and possible in the selective control of diseases.Unless otherwise defined, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this disclosure belongs. Although methods and materials similar or equivalent to those described herein can be used in the practice or testing of the disclosure, suitable methods and materials are described herein.
[0122] Unless otherwise stated, and as discussed further below, the term isomers as used herein refers to but not limited to enantiomers of chiral compound or a mixture thereof.
[0123] It has been observed by the inventors of the present invention that the composition of present invention not only provides synergistic effect but also provides anti-aging effect to the crops or plants to which it is applied. In addition, the stable synergistic pesticidal composition of the present invention is effective against all developmental stages of insects including egg, nymph, larva, pupa, and adult.
[0124] In an embodiment, the present invention provides a stable synergistic pesticidal composition comprising:
[0125] A) Dinotefuran or its agrochemically acceptable isomers, salts, esters and derivatives;
[0126] B) Compound of Formula I, i.e., N-[2,6-bis(1-methylethyl)-4-phenoxyphenyl]-N′-(1,1-dimethylethyl)thioureaor its agrochemically acceptable salts, esters and derivatives; and
[0127] C) Fluxametamide or its agrochemically acceptable isomers, salts, esters or its derivatives.
[0128] In another embodiment, the present invention provides a stable synergistic pesticidal composition comprising:
[0129] A) Dinotefuran or its agrochemically acceptable isomers, salts, esters and derivatives;
[0130] B) Compound of Formula I, i.e., N-[2,6-bis(1-methylethyl)-4-phenoxyphenyl]-N′-(1,1-dimethylethyl)thiourea or its agrochemically acceptable salts, esters and derivatives;C) Fluxametamide or its agrochemically acceptable isomers, salts, esters or its derivatives; andD) One or more agrochemically acceptable excipients
[0131] In one another embodiment, the present invention provides a stable synergistic pesticidal composition comprising:
[0132] A) Dinotefuran or its agrochemically acceptable isomers, salts, esters and derivatives;
[0133] B) Compound of Formula I, i.e., N-[2,6-bis(l-methylethyl)-4-phenoxyphenyl]-N'-(l,l- dimethylethyl)thiourea or its agrochemically acceptable salts, esters and derivatives;C) Fluxametamide or its agrochemically acceptable isomers, salts, esters or its derivatives; and D) At least one or more additive.
[0134] In one another embodiment, the present invention provides a stable synergistic pesticidal composition comprising:
[0135] A) Dinotefuran or its agrochemically acceptable isomers, salts, esters and derivatives;
[0136] B) Compound of Formula I, i.e., N-[2,6-bis(l-methylethyl)-4-phenoxyphenyl]-N'-(l,l- dimethylethyl)thiourea or its agrochemically acceptable salts, esters and derivatives; and
[0137] C) Fluxametamide or its agrochemically acceptable isomers, salts, esters or its derivatives;
[0138] D) At least one additive selected from urea clathrate, Siloxane Polyalkylene oxide copolymer, tallow amine ethoxylate, ammonium sulphate, and epoxide soybean oil either alone or in combination thereof; and
[0139] E) One or more agrochemically acceptable excipients.
[0140] In one another embodiment, the present invention provides a stable synergistic pesticidal composition comprising:
[0141] A) Dinotefuran or its agrochemically acceptable isomers, salts, esters and derivatives, in the range of 0.001-90% by weight of the composition;
[0142] B) Compound of Formula I, i.e., N-[2,6-bis(l-methylethyl)-4-phenoxyphenyl]-N'-(l,l- dimethylethyl)thiourea or its agrochemically acceptable salts, esters and derivatives, in the range of 0.001-90% by weight of the composition; and
[0143] C) Fluxametamide or its agrochemically acceptable isomers, salts, esters or its derivatives in the range of 0.001-90% by weight of the composition.
[0144] In one another embodiment, the present invention provides a stable synergistic pesticidal composition comprising:
[0145] A) Dinotefuran or its agrochemically acceptable isomers, salts, esters and derivatives, in the range of 0.001-90% by weight of the composition;B) Compound of Formula I, i.e., N-[2,6-bis(l-methylethyl)-4-phenoxyphenyl]-N'-(l,l- dimethylethyl)thiourea or its agrochemically acceptable salts, esters and derivatives, in the range of 0.001-90% by weight of the composition;
[0146] C) Fluxametamide or its agrochemically acceptable isomers, salts, esters or its derivatives in the range of 0.001-90% by weight of the composition; and
[0147] D) One or more agrochemically acceptable excipients.
[0148] In one another embodiment, the present invention provides a stable synergistic pesticidal composition comprising:
[0149] A) Dinotefuran or its agrochemically acceptable isomers, salts, esters and derivatives, in the range of 0.001-90% by weight of the composition;
[0150] B) Compound of Formula I, i.e., N-[2,6-bis(l-methylethyl)-4-phenoxyphenyl]-N'-(l,l- dimethylethyl)thiourea or its agrochemically acceptable salts, esters and derivatives, in the range of 0.001-90% by weight of the composition;
[0151] C) Fluxametamide or its agrochemically acceptable isomers, salts, esters or its derivatives in the range of 0.001-90% by weight of the composition;
[0152] D) At least one additive selected from urea clathrate, Siloxane Polyalkyleneoxide Copolymer, tallow amine ethoxylate, ammonium sulphate, and epoxide soybean oil either alone or in combination thereof, in the range of 0.001-20% by weight of the composition; and
[0153] E) One or more agrochemically acceptable excipients.
[0154] In yet another embodiment, the present invention provides a process for preparation of the stable synergistic pesticidal composition comprising:
[0155] A) Dinotefuran or its agrochemically acceptable isomers, salts, esters and derivatives;
[0156] B) Compound of Formula I, i.e., N-[2,6-bis(l-methylethyl)-4-phenoxyphenyl]-N'-(l,l- dimethylethyl)thiourea or its agrochemically acceptable salts, esters and derivatives; and
[0157] C) Fluxametamide or its agrochemically acceptable isomers, salts, esters or its derivatives.
[0158] In accordance with an embodiment of the present invention, there is provided a stable synergistic pesticidal composition comprising active ingredients present in the weight % range as given below:Dinotefuran or its Compound of Formula I, i.e., N-[2,6- Fluxametamide or its agrochemically acceptable bis(l-methylethyl)-4- agrochemically acceptable isomers, salts, esters and phenoxyphenyl]-N'-(l,l- isomers, salts, esters or its derivatives dimethylethyljthiourea or its derivatives agrochemically acceptable salts,
[0159] esters and derivatives
[0160] 0.001-90% 0.001-90% 0.001-90%
[0161]
[0162] In one embodiment of the present invention, the stable synergistic pesticidal composition results in an increased yield of the treated plant. In another embodiment of the invention, there is synergistic and efficacious control of various insects-pests diseases affecting the plants and crops. The present invention includes within its scope, all possible salts, esters and derivatives of the active ingredients of the composition. In one of the embodiments, the stable synergistic pesticidal composition or formulation according to the present invention has a reduced or zero phytotoxicity with respect to important agricultural crops. This enables the present invention to render effective and selective control of pesticidal diseases.
[0163] In an embodiment of the present invention, the stable synergistic pesticidal composition further optionally comprises additives, inert ingredients and / or adjuvants, for providing the following attributes to the composition of present invention:
[0164] a) enhanced stability, permeability, and spreading or coverage effect
[0165] b) improved penetration capacity, and storage stability,
[0166] c) uniform spray-ability, and improved rain-fastness,
[0167] d) enriched biotic factors, and better flowability,
[0168] e) longer residual effect, and improved uptake of active ingredients, and safer to the environment, improved shelf life of the formulation
[0169] In another embodiment of the present invention, the stable synergistic pesticidal composition of the present invention further comprises one or more agrochemically acceptable excipients including but not limited to the group comprising surfactant(s), dispersing agent(s), co-dispersant, anti-freezing agent(s), emulsifier(s) (anionic and non-ionic), anti-foaming agent / defoamer(s), wetting agent(s), antimi crobial / anti -bacterial agent(s), anti-caking agent, thickening agentZthickener(s), quick coating agent(s) or sticking agents / sticker(s), spreader(s), binder(s), pH-adjusting agent(s), anti-caking agent(s), adjuvant(s), filler(s) / suspension aid(s), colorant(s), carrier(s), buffering agent(s), polymer(s) rheology modifier(s), solvent(s), co-solvent(s), biocide or a combination thereof. Additional components may also be included,
[0170] Y1e.g., protective colloids, carriers, adhesives, thixotropic agents, penetration agents, stabilizers, sequestering agents. More generally, the active materials can be combined with any solid or liquid carrier / additive, which complies with usual formulation techniques.
[0171] An adjuvant used in the present Invention is any material that is added to an agrochemical formulation to enhance or modify the performance of the formulation. An adjuvant used in the present invention to make it a safer to ecological environmental, having low toxicity and having no phyto toxicity effects on any part of the plant.
[0172] Examples of surfactant(s) and / or dispersing agent and / or co-dispersant used herein include but not limited to polymeric anionic dispersant, polyarylphenyl ether phosphate, tristyryl phenol ethoxylate, Polymethyl methacrylate-polyethylene glycol graft copolymer, acrylate copolymer, Graft Comb copolymer, Sodium Napthalene Formmaldehyde condensate, acrylic copolymer, polymeric dispersant, Calcium salt of alkyl benzene sulphonate, Non-ionic surfactant, polyalkoxylated butyl ether, acrylic graft copolymer, Sodium methyl oleoyl taurate, non-ionic proprietary surfactant, Methyl naphthalene sulfonic acid, polymer with formaldehyde, sodium salt, ethoxylated tristryl phenol Sulphate, alkyl naphthalene formaldehyde condensate, naphthalene sulfonic acid, phenol sulfonic acid-formal dehyde polycondensation as sodium salt, sodium salt condensate with formaldehyde, ethoxylated oleyl cetyl alcohol, Sodium Alkyl Naphthalene Sulfonate Blend, styrenated phenol ethoxylate, polyalkelene glycol ether, Sodium Isopropyl Naphthalene Sulfonate, Dialkyl naphthalene sulphonate sodium salt, Naphthalene Sulphonic Acid, Formaldehyde, Acrylate graft Copolymer, Ethoxylated fatty glyceride, Ethoxylated Polyarylphenol Phosphate Ester, Lignosulfonic Acid, Sodium Salt, Sulfomethylated, ethoxylated fatty alcohol, methyl naphthalene sulfonic acid, polymer with formaldehyde sodium salt, Sodium Alkylnaphthalene Sulfonate Formaldehyde Condensate, Sodium polymethyl methacrylate, sodium polyacrylate, alkyl naphthalene sulfonate formaldehyde condensate or its sodium salt, Sodium Naphthalene Sulfonate formaldehyde condensate, sodium lignosulphonate, calcium lignosulphonate, Sodium Alkyl Naphthalene Sulfonate, Naphthalene Sulphonic Acid, Formaldehyde, alkylphenol polyoxyethylene ether, sodium salt of naphthalene sulfonate condensate, alkyl naphthalene sulfonate condensate blend, polymeric surfactant, sodium salt of alkyl naphthalene sulfonate, sodium salt of methyl naphthalene sulfonate, polycarboxylate, naphthalene sulfonic acid-branched and linear derivative sodium salts, fatty alcohol polyoxyethylene ether, alcohol polyglycol ether, non-aqueous dispersant – non-ionic polymeric surfactant, aqueous dispersant - polymeric amphoteric aqueous dispersant or mixtures thereof and present in the range of 0.001-20% by weight of the composition.Examples of wetting agent used herein include but not limited to tristyrylphenol ethoxylate non-ionic emulsifier, mixture of non-ionic surfactants, Blend of Anionic and Non-ionic, alkoxylated alcohol, block copolymer, alcohol polyglycol ether, alkyl olefin sulphates, dioctyl sulpho succinate, alkyl naphthalene sulphate, Di-isopropyl Napthalene sulphonate, Benzenesulfonic acid, Hydroxy polymer with formaldehyde, Phenol and Urea sodium salt, Polyalkoxy ethers, alkyl phenol ethoxylates, tri-styrenated phenol ethoxylate, EO / PO block co-polymers, butyl polyalkylene oxide block copolymer, sodium lauryl sulphonate, Alpha olefin sulphonate, sodium sulphates or mixtures thereof and present in the range of 0.01-20% by weight of the total composition.
[0173] Examples of defoamer or antifoaming agent used herein include but not limited to silicon emulsion based anti-foam agents, Siloxane polyalkyleneoxide, Polydimethylsiloxane, Polyalkyleneoxide-modified Polydimethylsiloxane, trisiloxane ethoxylates, silicone oil, silicone compound, C10~C20 saturated fat acid compounds or C8~C10 aliphatic alcohols compound, vegetable oil based antifoam, tallow based fatty acids, polyalkyleneoxide polydimethylsiloxane emulsion and mixtures thereof and present in the range of 0.01-5.0 % by weight of the composition.
[0174] Examples of anti-freezing agent used herein include but not limited to glycol, propylene glycol, mono ethylene glycol, glycerine, diethylene glycol, sorbitol, urea, mannitol, polyethylene glycol or mixtures thereof and present in the range of 0.01-20% by weight of the composition.
[0175] Examples of fillers used herein include but not limited to silicon dioxide, china-clay, kaolin, starch, bentonite, precipitated silica, fumed silica, lactose monohydrate, talcum powder, lactose, ammonium sulphate, water, sodium Sulphate, magnesium sulphate, sodium citrate, sodium chloride, potassium chloride and mixtures thereof and present in the range of 0.1-60 % by weight of the composition.
[0176] Examples of anti-caking agent used herein include but not limited to group of talc, hydrous magnesium silicate, magnesium carbonate, calcium carbonate, precipitate silica, silica powder, hydrophobic fumed silica and mixtures thereof and present in the range of 0.1-10% by weight of the composition.
[0177] Examples of carrier used herein include but not limited to silicon dioxide, china clay, kaolin, starch, bentonite, precipitated silica, silica powder, fumed silica, ppt silica powder, lactose monohydrate, talcum powder, lactose, ammonium sulpha or mixture thereof and present in the range of 1.0-45 % by weight of the composition.Examples of biocide or anti -microbial agent used herein include but not limited to 1, 2,- Benzisothiazolin -3-one, blends of 1,2,- benzisothiazolin-3-one and 2-methyl-4-isothiazolin-3-one, 5-chloro-2-methyl-4-isothiazolin-3-one, blends of 5-chloro-2-methyl-4-isothiazolin-3-one and 2-methyl-4-isothiazolin-3-one, zinc l-hydroxy-2(lH)-pyridinethione, blends of zinc l-hydroxy-2(lH)-pyridinethione and zinc oxide, and 2-n-octyl-4- isothiazolin-3-one or mixture thereof and present in the range of 0.01 to 10 % by weight of the composition.
[0178] Examples of rheology modifier or thickeners or thickening agents or suspending agents used herein include but not limited to polysaccharides, carboxymethyl cellulose, bentonite clay, aluminium magnesium silicate, hydroxy propyl cellulose, xanthan gum, gum arabic, Silica powder, gaur gum, carbomer, chitosan, precipitated silica or mixtures thereof and present in the range of 0.01-5.0 % by weight of the composition.
[0179] Examples of emulsifier(s) used herein include but not limited to araliphatic or aliphatic non-ionic oil emulsifier-ethoxylated sorbitol hexaester derived from oleic acid, emulsifier such as ethoxylated mono-, di- and trialkylphenols, ethoxylates of long-chain alcohols and polyethylene oxide / polypropylene oxide homo- and copolymers, Polymeric emulsifier (Nonionic polyalkylene oxide block copolymer), Ethoxylates of long-chain alkanols, Castor oil ethoxylate, ethoxylated monoalkylphenol, ethoxilates of cetyl alcohol and / or stearyl alcohol; Tri styrylphenol ethoxylate -20 mole, Ethoxylated Tristyrylphenol,and Anionic emulsifier such as alkali metal and ammonium salts of alkyl sulfates, of hemisulfates of ethoxylated alkanols and ethoxylated alkylphenols, alkylsulfonic acids, bis(phenylsulfonic acid) ethers and their alkali metal or ammonium salts, sodiumlaurylsulfate, sodium (cetyl / stearyl) sulfate or mixture thereof and present in the range of 0.01 -20 % by weight of the composition.
[0180] Examples of solvent(s) and co-solvent(s) used herein include but not limited to polar and non-polar solvent from the group comprising heavy aromatic hydrocarbon, N methyl pyrollidone (NMP), Solvent Naphtha (Solvent C-9), Di methyl sulfoxide (DMSO), Dimethylformamide (DMF), N- alcohol, 2-ethyl hexanol, alkyl amide, vegetable oil, mineral oil, distilled water, aromatic solvents, water or mixtures thereof and present in the range of 1.0 to 20% by weight of the composition.
[0181] Examples of colouring pigment(s) / dye(s) used herein include but not limited to red dye FGR03, Permanent Rubin L5-B-01, pigment blue 15:4, pigment blue 15:3, pigment blue 15:2, pigment blue 15:1, pigment blue 80, pigment yellow 1, pigment yellow 13, pigment red 112, pigment red 48:2, pigment red 48:1, pigment red 57: 1, pigment red 53:1, pigment orange 43, pigment orange 34, pigment orange 5, pigment green 36, pigment green 7, pigment white 6, pigment brown 25, basic violet 10, basic violet 49, violet 23,acid red 51, acid red 52, acid red 14, acid blue 9, acid yellow 23, basic red 10, basic red 108 or mixtures thereof and present in the range of 0.01- 10.0 % by weight of the composition.
[0182] Examples of polymer(s) used herein include but not limited to isocyanate, polyisocyanate used is toluene-2, 4-diisocyanate (TDI), diethylenetriamine (DETA),ethylene diamine (EDA), triethylenetetramine (TETA), and / or hexamethylene diamine (HMDA), diethanolglycine sodium salt, ethanoldiglycine disodium salt, hydroxymonocarboxylic acid compounds, hydroxydicarboxylic acid compounds, tetrasodium N, N-bis(carboxylatomethyl)-L-glutamate (GLDA), methylene diisocyanate (MDI), and / or low molecular weight polydiisocynates or mixtures thereof and present in the range of 0.01- 5.0 % by weight of the composition.
[0183] Examples of binder(s) used herein include but not limited to polyvinylpyrrolidone, polyvinyl alcohol, methyl cellulose, and carboxymethyl cellulose, polyisocyanate, polyterpene resin or mixtures thereof and present in the range of 0.01- 40 % by weight of the composition
[0184] Examples of preservative(s) used herein include but not limited to Methyl paraben (Methyl p-hydroxybenzoate), Propyl paraben (Propyl p-hydroxybenzoate), Methylisothiazolinone (MIT), Chloromethylisothiazolinone (CMIT), Benzisothiazolinone (BIT), DMDM Hydantoin, Imidazolidinyl Urea, Phenol, Cresol, Chlorocresol, Benzoic acid, Sorbic acid, Salicylic acid, Thymol (natural preservative), Sodium benzoate, Potassium sorbate, Bronopol (2-bromo-2-nitropropane-l,3-diol), Propyl para-hydroxy-benzoate or mixture thereof and present in the range of 0.01- 35 % by weight of the composition.
[0185] Examples of stabilizer(s) used herein include but not limited to butylated copolymer, Butylated Hydroxy Toluene (BHT), Butylated Hydroxyanisole (BHA), Ascorbic Acid (Vitamin C), a benzotriazole UV absorber, Hindered Amine Light Stabilizers (HALS), Oxanilide derivatives, Ethoxylated Alkylphenols (e.g., nonylphenol ethoxylates), Block copolymers, Polyvinyl alcohol (PVA), Acrylic or Butylated Copolymers, Citric acid / Sodium citrate, Phosphates (e.g., Sodium or Potassium phosphate), Acetates (e.g., Sodium acetate), EDTA (Ethylenediaminetetraacetic acid), Citric acid (dual role: pH and chelation), NTA (Nitrilotriacetic acid), Xanthan gum, Attapulgite clay, Bentonite, Hydroxypropyl methylcellulose (HPMC) or mixture thereof and present in the range of 0.01- 35 % by weight of the composition.
[0186] Examples of pH adjusting agent(s) / buffering agent(s) used herein include but not limited to Citric Acid, Citric Acid Monohydrate, Citric Acid Dihydrate, Sodium Citrate, Potassium Citrate, Tartaric Acid,Potassium Hydrogen Tartrate, Lactic Acid, Sodium Phosphate (Monobasic or Dibasic), Potassium Phosphate (Monobasic / Dibasic), Sodium Bicarbonate, Sodium Carbonate, Ammonium Acetate / Ammonium Hydroxide, Acetic Acid, Sodium Acetate, Borax (Sodium Borate) or mixture thereof and present in the range of 0.01- 25 % by weight of the composition.
[0187] In further embodiment, depending on the formulation type, they comprise one or more liquid or solid carriers, appropriate surfactants (such as dispersants, protective colloids, emulsifiers, wetting agents and tackifiers), and appropriate further excipients which are customary for formulating agrochemical compositions.
[0188] Suitable carriers include liquid and solid carriers. Liquid carriers include e.g. non-aqueous solvents such as cyclic and aromatic hydrocarbons, e.g. paraffins, tetrahydronaphthalene, alkylated naphthalenes and their derivatives, alkylated benzenes and their derivatives, alcohols such as methanol, ethanol, propanol, butanol and cyclohexanol, ketones such as cyclohexanone, strongly polar solvents, e.g. amines such as N-methylpyrrolidone, and water as well as mixtures thereof. Solid carriers include e.g. mineral earths such as silicas, silica gels, silicates, talc, kaolin, limestone, lime, chalk, bole, loess, clay, dolomite, diatomaceous earth, calcium sulfate, magnesium sulfate, magnesium oxide, ground synthetic materials, fertilizers such as ammonium sulfate, ammonium phosphate, ammonium nitrate, ureas, and products of vegetable origin such as cereal meal, tree bark meal, wood meal and nutshell meal, cellulose powders, or other solid carriers.
[0189] In yet another embodiment of the present invention, the present stable synergistic pesticidal composition can be formulated as one or more of Flowable concentrate for seed treatment (FS), Capsule suspension (CS), Dispersible concentrate (DC), Dustable powder (DP), Powder for dry seed treatment (DS), Emulsifiable concentrate (EC), Emulsifiable granule (EG), Emulsion water-in-oil (EO), Emulsifiable powder (EP), Emulsion for seed treatment (ES), Emulsion oil-in-water (EW), Granules (GR), Microemulsion (ME), Oil-dispersion (OD), Oil miscible flowable concentrate (OF), Oil miscible liquid (OL), Oil dispersible powder (OP), Suspension concentrate (SC), Suspension concentrate for direct application (SD), Suspo-emulsion (SE), Water soluble granule (SG), Soluble concentrate (SL), Spreading oil (SO), Water soluble powder (SP), Water soluble tablet (ST), Ultra-low volume (ULV) suspension, Tablet (TB), Ultralow volume (ULV) liquid, Water dispersible granules (WG), Wettable powder (WP), Water dispersible powder for slurry seed treatment (WS), Water dispersible tablet (WT), a mixed formulation of CS and SC (ZC) or a mixed formulation of CS and SE (ZE) or a mixed formulation of CS and EW (ZW).In yet another preferred embodiment of the present invention, the present stable synergistic pesticidal composition can be formulated as but not limited to Suspension Concentrate (SC), Wettable Powder (WP), Water dispersible granules(WG) etc.
[0190] In yet another embodiment of the present invention, the invention further provides the process for preparation of the said pesticidal composition, wherein the said composition can be one or more of Flowable concentrate for seed treatment (FS), Capsule suspension (CS), Dispersible concentrate (DC), Dustable powder (DP), Powder for dry seed treatment (DS), Emulsifiable concentrate (EC), Emulsifiable granule (EG), Emulsion water-in-oil (EO), Emulsifiable powder (EP), Emulsion for seed treatment (ES), Emulsion oil-in-water (EW), Granules (GR), Micro-emulsion (ME), Oil-dispersion (OD), Oil miscible flowable concentrate (OF), Oil miscible liquid (OL), Oil dispersible powder (OP), Suspension concentrate (SC), Suspension concentrate for direct application (SD), Suspo-emulsion (SE), Water soluble granule (SG), Soluble concentrate (SL), Spreading oil (SO), Water soluble powder (SP), Water soluble tablet (ST), Ultralow volume (ULV) suspension, Tablet (TB), Ultra-low volume (ULV) liquid, Water dispersible granules (WG), Wettable powder (WP), Water dispersible powder for slurry seed treatment (WS), Water dispersible tablet (WT), a mixed formulation of CS and SC (ZC) or a mixed formulation of CS and SE (ZE) or a mixed formulation of CS and EW (ZW).
[0191] In one embodiment, in the present invention compositions, additives such as urea clathrate, Siloxane Polyalkyleneoxide copolymer or organosilicone based powder adjuvant, tallow amine ethoxylate, ammonium sulphate, and epoxide soybean oil (ESO) serve distinct yet complementary functions, both individually and synergistically. Urea clathrate stabilizes volatile active ingredients by encapsulating them, thereby improving shelf life and enabling controlled release. Siloxane Polyalkyleneoxide copolymer or organosilicone based powder adjuvant, which are trisiloxane-based superspreaders, reduce surface tension significantly and enhance the spreading, wetting, and penetration of the formulation on plant surfaces, improving bioavailability. Tallow amine ethoxylate, a non-ionic surfactant, aids in emulsification and acts as a strong adjuvant, enhancing the uptake of systemic active ingredients. Ammonium sulphate is commonly used as a water conditioner to prevent antagonism from hard water ions like calcium and magnesium; it also enhances the absorption of pesticides. Epoxide soybean oil (ESO) contributes as a stabilizer and plasticizer, protecting active ingredients from UV and oxidative degradation while improving formulation compatibility.
[0192] In another embodiment, when used in combination in pesticidal composition, these additives enhance the overall efficacy, stability, and environmental safety of the agrochemical composition. For instance, the combined use of Siloxane Polyalkyleneoxide copolymer and ammonium sulphate can significantly boost pesticide performance, while ESO and urea clathrate together offer enhanced protection and sustainedrelease of active ingredients. Thus, their synergistic interaction leads to improved performance and consistency under varying environmental and application conditions.
[0193] In one embodiment, additives such as urea clathrate, Siloxane Polyalkyleneoxide Copolymer or organosilicone-based powder adjuvant, tallow amine ethoxylate, ammonium sulphate, and epoxide soybean oil either alone or in combination thereof, present in the range of 0.01 - 20% by weight of the composition.
[0194] In one embodiment, additives such as urea clathrate, Siloxane Polyalkyleneoxide copolymer or organosilicone basedsuper-wetter, tallow amine ethoxylate, ammonium sulphate, and epoxide soybean oil either alone or in combination thereof, present in the range of 0.001 - 20% by weight of the composition. In yet another embodiment of the present invention, the present stable synergistic pesticidal composition can be applied to various crops and plants including but not limited to Vegetables; Fruit; Turf; Rice; Rice (Paddy); Cotton; Brinjal; Fruit trees; Ornamentals; Soybeans; Strawberries, Aubergine; Tea; Potato; Soyabean; Cabbage; Chilli; Okra; Redgram; Tomato; etc. It is also applied as a ready to use household pesticide.
[0195] In yet another embodiment of the present invention, the present stable synergistic pesticidal composition provides synergistic and effective control against various pests including insects-pests diseases including but not limited to wide range of pests including sucking pests, Mealybugs; Plant hoppers; Leafminers; Aphids; Diamond back moth; Houseflies; Spider mite; Leafhoppers; Brown plant hopper; White Backed Plant Hopper; Green leaf Hopper; Thrips; Thrips (Thrips palmi), Jassids; Jassids (Amrasca bigutulla bigutulla), Whiteflies; Whiteflies (Bemisia tabaci), American cockroach (Periplaneta americana) and German Cockroach (Blattella germanica); Fruit and shoot borer; Tobacco caterpillar, Semi looper; Spotted pod Borer, Pod Borer; etc.
[0196] In yet another embodiment, the composition according to the invention can be applied to any and all developmental stages of pests, insects including egg, nymph, larva, pupa, and adult; including spore, germ, hypha, mature mycelium. The pests may be controlled by contacting the target pest, habitat, breeding ground or its locus with a bioactive amount of the novel and inventive composition of the present invention.
[0197] In yet another embodiment, the present stable synergistic pesticidal composition of the present invention can be applied to a plant / crop / soil by spraying, rubbing, atomizing, irrigating, evaporating, dusting, fogging, broadcasting, pouring, mist blowing, soil mixing, foaming, painting, spreading-on, drenching, dipping or drip irrigation, etc.In yet another embodiment, the composition of the present invention can also comprise or may be applied together and / or sequentially with further active compounds. These further compounds can be selected from fertilizers or micronutrient donors or microorganisms or other preparations that influence plant growth, such as inoculants (e.g., a strain of nitrogen-fixing bacteria), and plant inducers.
[0198] Thus, before describing the present invention in detail, it is to be understood that this invention is not limited to particularly exemplified systems or process parameters that may of course, vary. It is also to be understood that the terminology used herein is for the purpose of describing particular embodiments of the invention only and is not intended to limit the scope of the invention in any manner. The use of examples anywhere in this specification including examples of any terms discussed herein is illustrative only, and in no way limits the scope and meaning of the invention or of any exemplified term. Likewise, the invention is not limited to various embodiments given in this specification. Unless otherwise defined, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention pertains. In the case of conflict, the present document, including definitions will control.
[0199] Representative examples of the present composition of this invention are provided below and are not to be construed as limiting in any manner:
[0200] %(w / w) of the S. No. Ingredients
[0201] composition 1 Dinotefuran Technical 0.001-90 2 Compound of Formula I Technical 0.001-90 3 Fluxametamide Technical 0.001-90
[0202] Additive(s)- Urea Clatharate, Siloxane Polyalkyleneoxide Copolymer, tallow
[0203] 4 amine ethoxylate, ammonium sulphate, and Epoxide soybean oil either alone or 0.001-20 in combination thereof
[0204] Surfactant / Dispersing agent(s) / Co-dispersant(s)- polymeric anionic
[0205] dispersant, polyarylphenyl ether phosphate, tristyryl phenol ethoxylate, Polymethyl methacrylate-polyethylene glycol graft copolymer, acrylate
[0206] 5 copolymer, Graft Comb copolymer, Sodium Napthalene Formmaldehyde 0.001-20 condensate, acrylic copolymer, polymeric dispersant, Calcium salt of alkyl
[0207] benzene sulphonate, Non-ionic surfactant, polyalkoxylated butyl ether, acrylic
[0208] graft copolymer, Sodium methyl oleoyl taurate, non-ionic proprietary
[0209]
[0210] surfactant, Methyl naphthalene sulfonic acid, polymer with formaldehyde, sodium salt, ethoxylated tristryl phenol Sulphate, alkyl naphthalene formaldehyde condensate, naphthalene sulfonic acid, phenol sulfonic acid- formaldehyde polycondensation as sodium salt, sodium salt condensate with formaldehyde, ethoxylated oleyl cetyl alcohol, Sodium Alkyl Naphthalene Sulfonate Blend, styrenated phenol ethoxylate, polyalkelene glycol ether, Sodium Isopropyl Naphthalene Sulfonate, Dialkyl naphthalene sulphonate sodium salt, Naphthalene Sulphonic Acid, Formaldehyde, Acrylate graft Copolymer, Ethoxylated fatty glyceride, Ethoxylated Polyarylphenol Phosphate Ester, Lignosulfonic Acid, Sodium Salt, Sulfomethylated, ethoxylated fatty alcohol, methyl naphthalene sulfonic acid, polymer with formaldehyde sodium salt, Sodium Alkylnaphthalene Sulfonate Formaldehyde Condensate, Sodium polymethyl methacrylate, sodium polyacrylate, alkyl naphthalene sulfonate formaldehyde condensate or its sodium salt, Sodium Naphthalene Sulfonate formaldehyde condensate, sodium lignosulphonate, calcium lignosulphonate, Sodium Alkyl Naphthalene Sulfonate, Naphthalene Sulphonic Acid, Formaldehyde, alkylphenol polyoxyethylene ether, sodium salt of naphthalene sulfonate condensate, alkyl naphthalene sulfonate condensate blend, polymeric surfactant, sodium salt of alkyl naphthalene sulfonate, sodium salt of methyl naphthalene sulfonate, polycarboxylate, naphthalene sulfonic acid-branched and linear derivative sodium salts, fatty alcohol polyoxyethylene ether, alcohol polyglycol ether, non-aqueous dispersant – non-ionic polymeric surfactant, aqueous dispersant - polymeric amphoteric aqueous dispersant or mixtures thereof
[0211] Wetting agent(s)- tristyrylphenol ethoxylate non-ionic emulsifier, polyalkoxylated butyl ether, mixture of non-ionic surfactants, Blend of Anionic and Non-ionic, alkoxylated alcohol, block copolymer, alcohol polyglycol ether, alkyl olefin sulphates, dioctyl sulpho succinate, alkyl naphthalene sulphate biisopropyl Napthalene sulphonate, Benzenesulfonic acid, Hydroxy polymer with 0.01-20 formaldehyde, Phenol and Urea sodium salt, Polyalkoxy ethers, alkyl phenol ethoxylates, tri-styrenated phenol ethoxylate, EO / PO block co-polymers, butyl polyalkylene oxide block copolymer, sodium lauryl sulphate, sodium sulphates or mixtures thereof
[0212]
[0213] Defoamer / Anti-foaming agent- silicon emulsion based anti-foam agents, Siloxane polyalkyleneoxide, Polydimethylsiloxane, trisiloxane ethoxylates, silicone oil, silicone compound, C10~C20 saturated fat acid compounds or C8 0.01-5.0 ~C10 aliphatic alcohols compound, tallow based fatty acids, polyalkyleneoxide polydimethylsiloxane emulsion and mixtures thereof
[0214] Anti-freezing agent(s)- glycol, propylene glycol, mono ethylene glycol, glycerine, di ethylene glycol, sorbitol, urea, mannitol, polyethylene glycol, 0.01-20 polypropylene glycol or mixtures thereof
[0215] Filler(s)- silicon dioxide, china-clay, kaolin, starch, bentonite, precipitated silica, fumed silica, lactose monohydrate, talcum powder, lactose, ammonium
[0216] 0.1-60 sulphate, water, sodium Sulphate, magnesium sulphate, sodium citrate, sodium chloride, potassium chloride and mixtures thereof
[0217] Anti-caking agent(s)- group of talc, hydrous magnesium silicate, magnesium carbonate, calcium carbonate, precipitate silica, silica powder, hydrophobic 0.1-10 fumed silica and mixtures thereof
[0218] Carrier(s)- silicon dioxide, china clay, kaolin, starch, bentonite, precipitated silica, silica powder, fumed silica, ppt silica powder, lactose monohydrate, 1.0-45 talcum powder, lactose, ammonium sulpha or mixture thereof
[0219] Biocide / Anti-microbial agent (s)- 1, 2,- Benzisothiazolin -3-one, blends of 1,2,- benzisothiazolin-3-one and 2-methyl-4-isothiazolin-3-one, 5-chloro-2- methyl-4-isothiazolin-3-one, blends of 5-chloro-2-methyl-4-isothiazolin-3-one 0.01-10 and 2-methyl-4-isothiazolin-3-one, zinc 1 -hydroxy -2(1 H)-pyridinethione, blends of zinc l-hydroxy-2(lH)-pyridinethione and zinc oxide, and 2-n-octyl-4- isothiazolin-3-one or mixture thereof
[0220] Rheology modifier / Thickening agent(s)- polysaccharides, carboxymethyl cellulose, bentonite clay, aluminium magnesium silicate, hydroxy propyl 0.01-5.0 cellulose, xanthan gum, gum arabic, Silica powder, gaur gum, carbomer, chitosan, precipitated silica or mixtures thereof
[0221] Emulsifier(s)- Non-ionic emulsifiers- Araliphatic or aliphatic non-ionic oil emulsifier - ethoxylated sorbitol hexaester (derived from oleic acid), Ethoxylated mono-, 0.01-20 di- and trialkylphenols, Ethoxylates of long-chain alcohols, Polyethylene oxide / polypropylene oxide homo- and copolymers, EO / PO block copolymers,
[0222]
[0223] Polymeric emulsifier (Nonionic polyalkylene oxide block copolymer), Ethoxylates of long-chain alkanols, Castor oil ethoxylate, Ethoxylated monoalkylphenol, Ethoxylates of cetyl alcohol and / or stearyl alcohol, Tristyrylphenol ethoxylate, Ethoxylated Tristyrylphenol, Ethoxylated alcohols, Ethoxylated castor oil, Alkylaryl ethoxylates or a mixture thereof.
[0224] Ionic emulsifiers:
[0225] Alkali metal and ammonium salts of alkyl sulfates, Hemisulfates of ethoxylated alkanols and ethoxylated alkylphenols, Alkylsulfonic acids, Bis (phenylsulfonic acid) ethers and their alkali metal or ammonium salts, Sodium lauryl sulfate, Sodium (cetyl / stearyl) sulfate, or a mixture thereof
[0226] Solvent or co-solvent(s) - polar and non-polar solvent from the group comprising heavy aromatic hydrocarbon, N-methyl pyrollidone (NMP), Solvent Naphtha (Solvent C-9), Di methyl sulfoxide (DMSO), 1.0-20 Dimethylformamide (DMF), N- alcohol, 2-ethyl hexanol, alkyl amide,, mineral oil, distilled water, aromatic solvents, water or mixtures thereof
[0227] Colouring pigment(s) / dye(s)- red dye FGR03, Permanent Rubin L5-B-01, pigment blue 15:4, pigment blue 15:3, pigment blue 15:2, pigment blue 15:1, pigment blue 80, pigment yellow 1, pigment yellow 13, pigment red 112, pigment red 48:2, pigment red 48:1, pigment red 57: 1, pigment red 53:1,
[0228] 0.01-10 pigment orange 43, pigment orange 34, pigment orange 5, pigment green 36, pigment green 7, pigment white 6, pigment brown 25, basic violet 10, basic violet 49, violet 23, acid red 51, acid red 52, acid red 14, acid blue 9, acid yellow 23, basic red 10, basic red 108 or mixtures thereof
[0229] Polymer(s)- isocyanate, polyisocyanate used is toluene-2, 4-diisocyanate (TDI), diethylenetriamine (DETA),ethylene diamine (EDA), triethylenetetramine (TETA), and / or hexamethylene diamine (HMDA), diethanolglycine sodium salt, ethanoldiglycine disodium salt,
[0230] 0.01-5.0 hydroxymonocarboxylic acid compounds, hydroxydicarboxylic acid compounds, tetrasodium N, N-bis(carboxylatomethyl)-L-glutamate (GLDA), methylene diisocyanate (MDI), and / or low molecular weight polydiisocynates or mixtures thereof
[0231] Binder(s)- polyvinylpyrrolidone, polyvinyl alcohol, methyl cellulose, and
[0232] 0.01-40 % carboxymethyl cellulose, polyisocyanate, polyterpene resin or mixtures thereof
[0233]
[0234] Preservative(s)- Methyl paraben (Methyl p-hydroxybenzoate), Propyl paraben (Propyl p-hydroxybenzoate), Methylisothiazolinone (MIT), Chloromethylisothiazolinone (CMIT), Benzisothiazolinone (BIT), DMDM
[0235] 19 Hydantoin, Imidazolidinyl Urea, Phenol, Cresol, Chlorocresol, Benzoic acid, 0.01-35% Sorbic acid, Salicylic acid, Thymol (natural preservative), Sodium benzoate, Potassium sorbate, Bronopol (2-bromo-2-nitropropane-l,3-diol), Propyl parahydroxy -benzoate or mixture thereof
[0236] Stablizer(s)- butylated copolymer, Butylated Hydroxy Toluene (BHT), Butylated Hydroxyanisole (BHA), Ascorbic Acid (Vitamin C), Tocopherol (Vitamin E), Tinuvin® (e.g., Tinuvin 1130 - a benzotriazole UV absorber), Hindered Amine Light Stabilizers (HALS), Oxanilide derivatives, Ethoxylated Alkylphenols (e.g., nonylphenol ethoxylates), Block copolymers (e.g.,
[0237] 20 Pluronic® types), Polyvinyl alcohol (PVA), Acrylic or Butylated Copolymers, 0.01-35% Citric acid / Sodium citrate, Phosphates (e.g., Sodium or Potassium phosphate), Acetates (e.g., Sodium acetate), EDTA (Ethylenediaminetetraacetic acid), Citric acid (dual role: pH and chelation), NTA (Nitrilotriacetic acid), Xanthan gum, Attapulgite clay, Bentonite, Hydroxypropyl methylcellulose (HPMC) or mixture thereof
[0238] pH adjusting agent(s) / Buffering agent(s) - Citric Acid, Citric Acid Monohydrate, Citric Acid Dihydrate, Sodium Citrate, Potassium Citrate, Tartaric Acid, Potassium Hydrogen Tartrate, Lactic Acid, Sodium Phosphate
[0239] 21 0.01-25% (Monobasic or Dibasic), Potassium Phosphate (Monobasic / Dibasic), Sodium Bicarbonate, Sodium Carbonate, Ammonium Acetate / Ammonium Hydroxide, Acetic Acid, Sodium Acetate, Borax (Sodium Borate) or mixture thereof
[0240] 22 DM water / China Clay QS Total 100
[0241]
[0242] Example A: Dinotefuran 3.2 %+ Compound of formula I 20 % + Fluxametamide 3.2 % SC Sr. Ingredients % W / W No.
[0243] 1 Dinotefuran Technical 3.2 2 Compound of formula I Technical 20 3 Fluxametamide Technical 3.2
[0244]
[0245] 4 Acrylic Graft Copolymer 5.00
[0246] 5 Polyalkoxy ethers 3.00
[0247] 6 Methyl naphthalene sulfonic acid, polymer with
[0248] formaldehyde, sodium salt 4.00 7 Propylene Glycol 7.00
[0249] 8 1,2-Benzisothiazolin-3-one 0.10
[0250] 9 Polydimethylsiloxane emulsion 1.00
[0251] 10 Xanthum Gum 0.15
[0252] 11 D M water QS to make 100%
[0253]
[0254] TOTAL 100.0
[0255] FORMULATION PROCESS
[0256] A. Pre-Mixing
[0257] 1. Into a clean reactor charge D M Water and start the stirring.
[0258] 2. Add Propylene glycol, Acrylic Graft Copolymer, Polyalkoxy ethers, Methyl naphthalene sulfonic acid, polymer with formaldehyde, sodium salt. Polydimethyl siloxane, and 1,2- Benzisothiazolin-3-one. Mix well to make a homogeneous solution.
[0259] 3. To this add Dinotefuran technical, Compound of formula I technical and Fluxametamide technical and mix well to form a homogeneous slurry.
[0260] B. Wet-Milling process
[0261] 1. Allow to pass the premix through the bead mill at 400 to 500 Ltr / hr feed rate so as get a desired particle size.
[0262] 2. The grinded material is collected in post blender.
[0263] C. Post Mixing
[0264] 1. The milled slurry is collected into the post blender and to this pre hydrated xanthum gum is added.
[0265] 2. Mix well till the slurry attains right viscosity.
[0266] 3. Pack the formulation into HDPE bottles.
[0267] STABILITY DATA: Dinotefuran 3.2 %+ Compound of formula I 20% + Fluxametamide 3.2 %
[0268] SC
[0269] Sr. Test Parameter
[0270]
[0271] Observation
[0272]
[0273] Cold Test at
[0274]
[0275] HST at 54 °CNO 0°C 7 days 14 days 1. Off-white coloured
[0276] suspension free from Complies Appearance Complies Complies any lumps or extraneous
[0277] matter
[0278] 2. Dinotefuran Technical
[0279] (%w / w) 3.2 % (+ 10 %, -5%) 3.31 3.29 3.38 3. Compound of formula I 20.27
[0280] technical (% w 20 % (+5 %, -5%) 20.29 20.34
[0281] / w))
[0282] 4. Fluxametamide
[0283] 3.32 3.37 Technical (% w / w) 3.2 % (+10 %, -5%)
[0284] 3.29
[0285] 5. Suspensibility 98.62
[0286] Min 80%
[0287] Dinotefuran, %w / w 98.66 98.85 6. Suspensibility Compound Min 80% 98.51
[0288] 98.56 98.60 of formula I, %w / w
[0289] 7. Suspensibility Min 80% 98.12
[0290] Fluxametamide, %w / w 98.25 98.75 8. Persistant Foaming, mL Max. 60 8 9 7 9. Wet Sieve, material
[0291] passing through 45- Min 98 % 99.5 99.6 99.7 micron sieve
[0292] 10. pH of 1% aqueous
[0293] 7.0 - 10.0 7.55 7.35 7.4 emulsion
[0294] 11. Pourability, Rinse residue,
[0295] Max. 1.5 1.11
[0296] % by mass 1.28 1.10
[0297]
[0298] 12. Density @ 25 °C, g / mL 1.150 - 1.250 1.21 1.22 1.19
[0299] Example B. Dinotefuran 10 %+ Compound of formula I 30% + Fluxametamide 0.1 % WG
[0300] Sr. No. Ingredients % W / W
[0301] 1 Dinotefuran Technical 10.00 2 Compound of formula I Technical 30.00 3 Fluxametamide Technical 0.1 4 Sodium Isopropyl Naphthalene Sulfonate 2.5 5 Sodium Lignosulphonate 4.0 6 Sodium salt of naphthalene sulfonate formaldehyde condensate 4.5 7 Sodium Polycarboxylate 3.0 8 Lactose monohydrate 8.0 9 Polydimethylsiloxane emulsion 0.5 10 Silica ppt 3.0 11 China clay QS to make 100%
[0302]
[0303] TOTAL 100.0
[0304] MANUFACTURING PROCESS:China clay was taken in the ribbon blender for mixing. To this, Silica ppt, Sodium Isopropyl Naphthalene Sulfonate, Sodium Lignosulphonate, Sodium salt of naphthalene sulfonate formaldehyde condensate, Sodium Polycarboxylate, Lactose monohydrate, Dinotefuran technical, Compound of formula I technical, Fluxametamide technical were added and mixed well.
[0305] Mixing was continued until the material became completely homogenized. The premix was then passed through the Airjet mill at 6 to 7 kg / cm2of grinding pressure and a feeding rate of 100 to 150 kg / hr so as to obtain a particle size of D90 less than 10 microns. The ground material was collected in the post blender.
[0306] Extrusion process
[0307] Into the post blender, the solution of water and Polydimethylsiloxane emulsion was added by means of spraying, and a dough was prepared. This dough was mixed well to obtain a well-hydrated mass for extrusion. The dough was then allowed to pass through the screw valve fitted with the post blender and subsequently passed through the basket extruder.
[0308] Drying Process
[0309] The wet extruded granules were passed through the VFBG (vibro fluid bed drier), which had been brought to a consistent temperature of 50 °C prior to drying. The granules were then checked for moisture content, which was required to be not more than 3%. Once the parameter was set, the process was continued.
[0310] The dried granules were passed through a vibro sieve machine to separate any lumps or dust, and the desired size granules were collected and packed.
[0311] STABILITY DATA: Dinotefuran 10 %+ Compound of formula I 30% + Fluxametamide 0.1 % WG
[0312] Sr. Test Parameter Specification Observation HST at 54 No. °C 14 days 1 Appearance Off-white coloured powder Complies Complies free from any lumps or
[0313] extraneous matter
[0314] 2 Active Content
[0315] 10.17 10.24 Dinotefuran, %w / w 10% (+5%, -5%)
[0316] 3 Active Content Compound
[0317] 30.72 of formula I, %w / w 30% (+5%, -5%) 30.61
[0318] 4 Active Content
[0319] 0.1% (+10%, -5%) 0.11 0.11 Fluxametamide, %w / w
[0320] 5 Suspensibility of Min 80% 98.35 98.55 Dinotefuran (% w / w)
[0321] 6 Suspensibility of Min 80% 98.36 98.82 Compound of formula I (%
[0322] w / w)
[0323] 7 Suspensibility of Min 80% 98.15 98.33 Fluxametamide (% w / w)
[0324] 8 Wet Sieve test (retained on Min 98 % 99.39 99.45
[0325] 45 micron sieve, %w / w
[0326]
[0327] 9 pH of 1% aqueous emulsion 5.0 to 8.0 6.57 6.6410 Persistent foam after 1min 60 Max 12 11
[0328] (ml)
[0329]
[0330] 11 Wettability 120 sec Max 20 18
[0331] EXAMPLE C: Dinotefuran 0.1 %+ Compound of formula I 40% + Fluxametamide 10 % WP Sr. No. Ingredients % W / W
[0332] 1 Dinotefuran Technical 0.1
[0333] 2 Compound of formula I Technical 40
[0334] 3 Fluxametamide Technical 10
[0335] 4 Sodium Lignosulphonate 10.0
[0336] 5 Sodium alkyl naphthalene sulfonate formaldehyde condensate 5.0
[0337] 6 Sodium lauryl sulphonate 3.0
[0338] 7 Silica ppt 2.0
[0339] 8 China clay Q. S. to make 100% TOTAL 100.0
[0340]
[0341] MANUFACTURING PROCESS:
[0342] 1. All required technicals, i.e., Dinotefuran technical, Compound of formula I technical, Fluxametamide technical and inert ingredients, were mixed and then ground in an air jet mill. 2. The particle size was checked after grinding to ensure that it was less than 10 microns (D90). 3. The ground powder was post-blended and mixed well.
[0343] STABILITY DATA: Dinotefuran 0.1 %+ Compound of formula I 40% + Fluxametamide 10 % WP
[0344] Sr. Test Parameter Specification Observation at HST at 54 °C No. Room 14 days
[0345] Temperature
[0346]
[0347] 1 Appearance White to off white Complies Complies powder free from
[0348] extraneous matter
[0349] 2 Dinotefuran Technical
[0350] 0.1 % (+ 10%, -5%) 0.11 0.11 (%w / w)
[0351] 3 Compound of formula I 40 % (+ 5%, -5%)
[0352] 40.54 40.67 technical (% w / w))
[0353] 4 Fluxametamide Technical
[0354] 10 % (+5%, -5%) 10.12 10.17 (% w / w)
[0355] 5 Suspensibility of Min 80% 98.33 98.56 Dinotefuran (% w / w)
[0356] 6 Suspensibility of Min 80% 98.38 98.81 Compound of formula 1
[0357] (% w / w)
[0358] 7 Suspensibility of Min 80% 98.12 98.23 Fluxametamide (% w / w)
[0359] 8 Persistent Foaming, mL Max. 60 after 1 minute 11 14 (1% solution in 342 ppm
[0360] hard water)
[0361] 9 Wet Sieve, material passing Min 98 % 98.82 98.90 through 45 -micron sieve
[0362] 10 pH of 1 % aqueous emulsion 5.0 to 8.0 6.56 6.63
[0363]
[0364] 11 Wettability 120 sec max 60 70
[0365] Evaluation of synergistic effect of pesticidal composition of the present invention
[0366] A synergistic effect of two or more products exists whenever the action of an active ingredient combination is greater than the sum of the actions of the individual components. Synergism was calculated by using Colby’s method (Weeds, vol. 15 No. 1 (Jan 1967), pp. 20-2).
[0367] The synergistic action expected for a given combination of two active components can be calculated as follows:
[0368] XY
[0369] E = (X + Y) - 100The synergistic action expected for a given combination of three active components can be calculated as follows:
[0370] (XY+YZ+XZ) (XYZ)
[0371] E = (X + Y + Z) - + - 100 10000
[0372] Where:
[0373] E represents expected percentage of pesticidal control for the combination of the two or three active ingredients at defined doses (for example equal to x, y and z, respectively).
[0374] X is the percentage of pesticidal control observed by the compound (Dinotefuran) at a defined dose (equal to x).
[0375] Y is the percentage of pesticidal control observed by the compound (Compound of formula I) at a defined dose (equal to y).
[0376] Z is the percentage of pesticidal control observed by the compound (Fluxametamide) at a defined dose (equal to z).
[0377] When the percentage of pesticidal control observed for the combination is greater than the expected percentage, there is a synergism effect.
[0378] Observed control (%)
[0379] Ratio = - Expected control (%)
[0380] Ratio of O / E > 1, synergism observed
[0381] The present invention is illustrated by way of examples, the examples are meant for illustrative purposes and should not be construed as limiting.
[0382] Experiment for Synergistic activity of stable synergistic pesticidal composition of present invention: Example 1- Details of experiment on Chilli crop:
[0383] Field experiment for synergistic activity of Dinotefuran + Compound of formula I + Fluxametamide for the control of fruit borer and thrips in Chilli crop was conducted.
[0384] To evaluate the synergistic effect, Chilli [Variety: Pusa Jwala] crop was sown in 5 m x 5 m plots maintaining 45 cm x 30 cm plant distance with three replications and in Randomized Block Design (RBD). The treatments were applied as foliar spray in the form of SC formulation @ 1250 ml / ha. Each active component was applied twice in different ternary and binary compositions. Solo compositions were also taken for comparison. The treatment details are as under:S. No Treatments (SC) Concentration (SC)
[0385] T1 Dinotefuran + Compound of formula I + Fluxametamide 10% + 30% + 0.1%
[0386] T2 Dinotefuran + Compound of formula I + Fluxametamide 6% + 0.1% + 6%
[0387] T3 Dinotefuran + Compound of formula I + Fluxametamide 3.2 + 20% + 3.2%
[0388] T4 Dinotefuran + Compound of formula I + Fluxametamide 0.1% + 40% + 10%
[0389] T5 Dinotefuran + Compound of formula I 10% + 30%
[0390] T6 Dinotefuran + Compound of formula I 6% + 0.1%
[0391] T7 Dinotefuran + Compound of formula I 3.2 + 20%
[0392] T8 Dinotefuran + Compound of formula I 0.1% + 40%
[0393] T9 Dinotefuran + Fluxametamide 10% + 0.1%
[0394] T10 Dinotefuran + Fluxametamide 6% + 6%
[0395] Til Dinotefuran + Fluxametamide 3.2 + 3.2%
[0396] T12 Dinotefuran + Fluxametamide 0.1% + 10%
[0397] T13 Compound of formula I + Fluxametamide 30% + 0.1%
[0398] T14 Compound of formula I + Fluxametamide 0.1% + 6%
[0399] T15 Compound of formula I + Fluxametamide 20% + 3.2%
[0400] T16 Compound of formula I + Fluxametamide 40% + 10%
[0401] T17 Dinotefuran 10%
[0402] T18 Dinotefuran 6%
[0403] T19 Dinotefuran 3.2%
[0404] T20 Dinotefuran 0.1%
[0405] T21 Compound of formula I 30%
[0406] T22 Compound of formula I 0.1%
[0407] T23 Compound of formula I 20%
[0408] T24 Compound of formula I 40%
[0409] T25 Fluxametamide 0.1%
[0410] T26 Fluxametamide 6.0%
[0411] T27 Fluxametamide 3.2%
[0412] T28 Fluxametamide 10%
[0413]
[0414] T29 Untreated Check -
[0415] The treatments T1 to T28 were used as foliar application whereas no treatment was done for T29 control treatment. Two applications of each treatment were carried out at 15-day intervals, initiated upon reaching the Economic Threshold Level (ETL) of the target insect population in the experimental plots. Observations on thrips (Scirtothrips dorsalis) were recorded before spraying and at 7 and 14 days after the first and second applications. For each of the 10 randomly selected Chilli plants per plot, three leaves: one each from the upper, middle and lower canopy were examined to assess the thrips population. Observations for fruit borer (Helicoverpa armigera)) were recorded before spraying and at 7 and 14 days after the first and second applications. On the same 10 randomly selected Chilli plants per plot, 10 plants were examined torecord per cent fruit damage. The number of infested and healthy fruits was counted and per cent fruit damage was calculated accordingly. The per cent reduction in insect population was calculated over control. Based on the per cent reduction at 14 days after second spray in insect population the Expected control was calculated and compared with Observed control. The results of the trial have been presented here under in Table 1.
[0416] Table 1: Synergistic effect of pesticidal composition of the present invention (Dinotefuran + Compound of formula I + Fluxametamide) against insect pest in Chilli crop
[0417] s. Treatments Formulation Per cent insect control No (SC)
[0418] Observ Expecte Colby ed d ratio Dinotefuran + Compound of formula I + 10% + 30% + 1.11 T1
[0419] Fluxametamide 0.1% 72.01 64.83 1 Dinotefuran + Compound of formula I + 6% + 0.1% + 1.21 T2
[0420] Fluxametamide 6% 79.84 65.52 9 Dinotefuran + Compound of formula I + 3.2 + 20% + 1.24 T3
[0421] Fluxametamide 3.2% 90.12 72.15 9 Dinotefuran + Compound of formula I + 0.1% + 40% + 1.17 T4
[0422] Fluxametamide 10% 78.43 66.69 6 0.83 T5
[0423] Dinotefuran + Compound of formula I 10% + 30% 46.92 56.45 1 0.74 T6
[0424] Dinotefuran + Compound of formula I 6% + 0.1% 33.15 44.46 6 0.85 T7
[0425] Dinotefuran + Compound of formula I 3.2 + 20% 47.19 55.48 1 0.79 T8
[0426] Dinotefuran + Compound of formula I 0.1% + 40% 36.83 46.16 8 0.74 T9
[0427] Dinotefuran + Fluxametamide 10% + 0.1% 34.20 45.7 8 0.88 T10
[0428] Dinotefuran + Fluxametamide 6% + 6% 51.19 57.83 5 0.92 Til
[0429] Dinotefuran + Fluxametamide 3.2 + 3.2% 53.25 57.45 7
[0430]
[0431] 0.83 T12
[0432] Dinotefuran + Fluxametamide 0.1% + 10% 40.02 48.05 3 0.77 T13
[0433] Compound of formula I + Fluxametamide 30% + 0.1% 37.02 47.71 6 0.83 T14
[0434] Compound of formula I + Fluxametamide 0.1% + 6% 41.18 49.22 7 0.89 T15
[0435] Compound of formula I + Fluxametamide 20% + 3.2% 52.71 59.06 2 0.84 T16
[0436] Compound of formula I + Fluxametamide 40% + 10% 51.20 60.32 9 T17 Dinotefuran 10% 32.75 - - T18 Dinotefuran 6% 32.09 - - T19 Dinotefuran 3.2% 31.98 - - T20 Dinotefuran 0.1% 16.05 - - T21 Compound of formula I 30.0% 35.24 - - T22 Compound of formula I 0.1% 18.22 - - T23 Compound of formula I 20.0% 34.55 - - T24 Compound of formula I 40.0% 35.87 - - T25 Fluxametamide 0.1% 19.25 - - T26 Fluxametamide 6.0% 37.91 - - T27 Fluxametamide 3.2% 37.45 - - T28 Fluxametamide 10% 38.12 - - T29 Untreated Check - - - -
[0437]
[0438] It is clearly evident from the data presented in Table 1 on per cent insect pest control in Chilli that the ternary pesticidal composition comprising Dinotefuran + Compound of formula I + Fluxametamide (treatments T1 to T4) exhibits a synergistic effect against insect pests, as indicated by a Colby’s ratio greater than 1. The Colby’s ratio here reflects the combined efficacy against thrips and fruit borer in Chilli. In contrast, the binary compositions involving any two of these insecticides (treatments T5 to T16) were found to be inefficacious and showed no synergistic effect for the control of both thrips and fruit borer when compared to the ternary stable synergistic pesticidal composition of the present invention.
[0439] Experiment for Bio-efficacy evaluation of stable synergistic pesticidal composition of present invention:For the ternary and binary pesticidal composition based on Dinotefuran + Compound of formula I + Fluxametamide evaluation under field conditions, the basic test composition as Dinotefuran 3.2% + Compound of formula I 20% + Fluxametamide 3.2% SC were manufactured specifically by the inventor. For ternary pesticidal composition, Dinotefuran 3.2% + Compound of formula I 20% + Fluxametamide 3.2% SC was used and for binary compositions, Dinotefuran 3.2% + Compound of formula I 20% SC, Dinotefuran 3.2% + Fluxametamide 3.2% SC and Compound of formula I 20% + Fluxametamide 3.2% SC were used. The solo formulations of Dinotefuran 3.2% SC, Compound of formula I 20% SC and Fluxametamide 3.2% SC were used for comparison. The other formulations namely Compound of formula I 18% + Fipronil 8% + Dinotefuran 5% w / w SC, Compound of formula I 50 % WP and Fluxametamide 10% w / w EC available in the market were also used for comparison.
[0440] Example 2: Evaluation of the stable synergistic pesticidal composition of the present invention on Chilli
[0441] The synergistic composition of the present invention Dinotefuran 3.2% + Compound of formula I 20% + Fluxametamide 3.2% SC was evaluated on Chilli crop [Variety: Pusa Jwala] at a farmer field. The crop sowing was done in Randomized Block Design (RBD) with three replications maintaining a distance of 45 cm x 30 cm between plants and rows.
[0442] The observations were recorded for the following objectives.
[0443] Objectives:
[0444] 1. Bio-efficacy evaluation against thrips on Chilli crop
[0445] 2. Bio-efficacy evaluation against fruit borer on Chilli crop
[0446] 3. Bio-efficacy evaluation based on percent reduction in thrips population
[0447] 4. Bio-efficacy evaluation based on percent reduction in fruit borer population
[0448] 5. Bio-efficacy evaluation based on Chilli crop yield.
[0449] 6. Phytotoxicity evaluation on Chilli crop
[0450] Treatment details:
[0451] S. No. Treatments (SC) a. i. dose Formulation (g / ha) Dose (g or ml / ha) Dinotefuran 3.2% + Compound of formula I
[0452] T1
[0453] 20% + Fluxametamide 3.2% 30 + 187.5 + 30 937.5 Dinotefuran 3.2% + Compound of formula I
[0454] T2 40 + 250 + 40
[0455] 20% + Fluxametamide 3.2% 1250 Dinotefuran 3.2% + Compound of formula I
[0456] T3
[0457]
[0458] 20% + Fluxametamide 3.2% 50 + 312.5 + 50 1562.5Dinotefuran 3.2% + Compound of formula I
[0459] T4
[0460] 20% 30 + 187.5 937.5 Dinotefuran 3.2% + Compound of formula I
[0461] T5 40 + 250
[0462] 20% 1250 Dinotefuran 3.2% + Compound of formula I
[0463] T6
[0464] 20% 50 + 312.5 1562.5
[0465] T7 Dinotefuran 3.2% + Fluxametamide 3.2% 30 + 30 937.5
[0466] T8 Dinotefuran 3.2% + Fluxametamide 3.2% 40 + 40 1250
[0467] T9 Dinotefuran 3.2% + Fluxametamide 3.2% 50 + 50 1562.5 Compound of formula I 20% + Fluxametamide
[0468] T10
[0469] 3.2% 187.5 + 30 937.5 Compound of formula I 20% + Fluxametamide
[0470] Til 250 + 40 1250
[0471] 3.2%
[0472] Compound of formula I 20% + Fluxametamide
[0473] T12 312.5 + 50 1562.5
[0474] 3.2%
[0475] T13 Dinotefuran 3.2% 40 1250
[0476] T14 Compound of formula I 20% 250 1250
[0477] T15 Fluxametamide 3.2% 40 1250 Compound of formula I 18% + Fipronil 8% +
[0478] T16 157.50 + 70.00 + 43.75 875 Dinotefuran 5% w / w SC
[0479] T17 Compound of formula I 50 % WP 300 600
[0480] T18 Fluxametamide 10% w / w EC 40 400
[0481] T19 Untreated check - - Dinotefuran 3.2% + Compound of formula I
[0482] T20 20% + Fluxametamide 3.2% (only for 80 + 500 + 80
[0483]
[0484] phytotoxicity analysis) 2500
[0485] Methodology:
[0486] The treatments T1 to T18 and T20 were used as foliar application whereas no treatment was done for T19 i.e., control treatment. All treatments were applied at the time of initiation of pest in the experimental plots. Observations on thrips (Scirtothrips dorsalis) were recorded before spraying and at 7 and 14 days after the first and second applications. For each of the 10 randomly selected Chilli plants per plot, three leaves: one each from the upper, middle and lower canopy were examined to assess the thrips population. Observations for fruit borer (Helicoverpa armigera)) were recorded before spraying and at 7 and 14 days after the first and second applications. On the same 10 randomly selected Chilli plants per plot, 10 plants were examined to record per cent fruit damage. The number of infested and healthy fruits were counted and per cent fruit damage was calculated accordingly. The per cent reduction in insect population was calculated over control. The crop yield was recorded at crop harvest. The observations for phytotoxicity on Chilli crop at 1, 3, 7, 10and 14 days after 1stspray were also recorded. The data were subjected to statistical analysis of variance. Results are presented in Table 2, 3, 4, 5 and 6.
[0487] Results:
[0488] Table 2: Field bio-efficacy evaluation of Dinotefuran 3.2% + Compound of formula I 20% + Fluxametamide 3.2% SC against fruit borer of Chilli crop
[0489] Per cent Fruit damage % Increase against Formal
[0490] control ation
[0491] S. No a.i. dose Pre- Treatments (SC) dose (g
[0492] (g / ha) treatme 14 DAS 14 DAS 1 2ndorst
[0493] nt (2nd) Spray Sp ml / ha) (1st) ray count
[0494] Dinotefuran 3.2%
[0495] + Compound of 13.57
[0496] 17.28 6.54
[0497] T1 formula I 20% + (21.62 42.13 76.57 Fl (24.56) (14.82) uxametamide 30 + 187.5 + )
[0498] 3.2% 30 937.5
[0499] Dinotefuran 3.2%
[0500] + Compound of 12.3
[0501] 17.37
[0502] T2 formula I 20% + 3.25
[0503] 40 + 250 + 40 (20.53 47.55 88.36 (24.63) (10.39) Fluxametamide )
[0504] 3.2% 1250
[0505] Dinotefuran 3.2%
[0506] + Compound of 12.07
[0507] 17.2 3.03
[0508] T3 formula I 20% + (20.33 89.14 ( (10.02) 48.53 24.5)
[0509] Fluxametamide 50 + 312.5 + )
[0510] 3.2% 50 1562.5
[0511] Dinotefuran 3.2% 17.79
[0512] 17.35 17.43 T4 + Compound of 24.14 (24.95 37.55 (24.62) (24.68)
[0513] formula I 20% 30 + 187.5 937.5 )
[0514] Dinotefuran 3.2% 16.68
[0515] 17.41 15.78
[0516] + Compound of (24.11 28.87 T5 40 + 250 43.46 (23.41) (24.66) formula I 20% 1250 )
[0517] Dinotefuran 3.2% 16.47
[0518] 17.19 15.48
[0519] + Compound of (23.94 29.77 44.54 T6
[0520] (23.17) (24.49)
[0521] formula I 20% 50 + 312.5 1562.5 )
[0522] Dinotefuran 3.2% 17.27
[0523] 16.32 17.16 T7 + Fluxametamide (24.56 26.35 41.53 (24.47) (23.83)
[0524] 3.2% 30 + 30 937.5 )
[0525] Dinotefuran 3.2%
[0526] 17.2 15.77 14.42
[0527] + Fluxametamide T8 40 + 40 32.75 48.33 (23.4) (22.32) (24.5) 3.2% 1250
[0528] Dinotefuran 3.2%
[0529] 17.44 15.65 14.18 + Fluxametamide T9 33.26 49.19 (22.12) (24.68) (23.3)
[0530] 3.2% 50 + 50 1562.5
[0531]
[0532] Compound of
[0533] 15.82
[0534] formula I 20% + 17.13 15
[0535] T10 (23.44 32.54 Fluxametamide 46.26 (24.45) (22.79)
[0536] 3.2% 187.5 + 30 937.5 )
[0537] Compound of
[0538] 14.67
[0539] formula I 20% + 17.29 12.43
[0540] Til (22.52 37.44
[0541] Flux 250 + 40 1250 55.46Fluxametamide (24.57) (20.64)
[0542] 3.2% )
[0543] Compound of
[0544] formula I 20% + 17.2 14.53
[0545] 12.13
[0546] T12 312.5 + 50 1562.5 (22.41 38.04 56.54 Fluxametamide (24.5) (20.38)
[0547] ) 3.2%
[0548] 20.79
[0549] Dinotefuran 3.2% 17.19 22.48
[0550] T13 40 (27.13 11.34 19.46 (24.49) (28.3)
[0551] 1250 )
[0552] 19.12
[0553] Compound of 18.7 17.26 T14 (25.93 18.46 32.99 formula I 20% (24.55) (25.33)
[0554] 1250 )
[0555] 18.63 Fluxametamide 17.15 17.43
[0556] (25.57 T15 40 20.55 37.55 3.2% (24.46) (24.68)
[0557] 1250 )
[0558] Compound of
[0559] formula I 18% +
[0560] 157.50 + 17.33 14.65 7.13
[0561] Fipronil 8% + T16 875 37.53 74.45
[0562] 70.00 + 43.75 (24.6) (22.5) (15.49) Dinotefuran 5%
[0563] w / w SC
[0564] Compound of
[0565] 17.41 18.8 18.1
[0566] T17 formula I 50 % 19.83 35.15 (25.7) (24.66) (25.18) WP
[0567] 18.73 Fluxametamide 17.44 16.93
[0568] (25.64 39.34 T18 40 400 20.13
[0569] 10% w / w EC (24.68) (24.3)
[0570] )
[0571] 23.45
[0572] 17.2 27.91
[0573] T19 (28.96
[0574] (24.5) (31.89) Untreated check )
[0575] SEm± 0.17 0.11
[0576] CD (p=0.05) 0.33 0.50
[0577]
[0578] Figures in parentheses are angular transformed values; NS= non-significant; DAS: Days after spray Table 3: Field bio-efficacy evaluation of Dinotefuran 3.2% + Compound of formula I 20% + Fluxametamide 3.2% SC against thrips of Chilli crop
[0579] Per cent Fruit damage % Increase Formula against control tion
[0580] S. No Pre14
[0581] Treatments a.i. dose (g / ha) dose (g 2nd14 DAS treatment IstSpray DAS
[0582] or Spray (1st) count (2nd)
[0583] ml / ha)
[0584]
[0585] Dinotefuran 3.2%
[0586] + Compound of 3.37
[0587] 9.84 7.84
[0588] T1 formula I 20% + (1.97 46.19 81.54
[0589] (3.22)
[0590] Fluxametamide (2.89)
[0591] 30 + 187.5 + )
[0592] 3.2% 30 937.5
[0593] Dinotefuran 3.2%
[0594] + Compound of 1.37
[0595] 6.98
[0596] T2 formula I 20% + 40 + 250 + 40 10 (3.24) (1.37 52.09 92.5
[0597] (2.73)
[0598] Fluxametamide )
[0599] 3.2% 1250
[0600] Dinotefuran 3.2%
[0601] + Compound of 1.27
[0602] 9.71 6.71
[0603] T3 formula I 20% + (1.33 53.95 93.04 Fluxametamide (3-2) (2-69)
[0604] 50 + 312.5 + )
[0605] 3.2% 50 1562.5
[0606] Dinotefuran 3.2% 10.06
[0607] T4 + Compound of 10.78 10.76
[0608] (3.25 26.15 44.91 formula I 20% (3.36) (3.36)
[0609] 30 + 187.5 937.5 )
[0610] Dinotefuran 3.2% 8.89
[0611] + Compound of 10.23 9.77
[0612] T5 40 + 250 (3.06 32.94 51.31 formula I 20% (3.28) (3-2)
[0613] 1250 )
[0614] Dinotefuran 3.2% 8.65
[0615] 10.16 9.7
[0616] T6 + Compound of (3.02 33.42 52.63
[0617] (3.26) (3-19)
[0618] formula I 20% 50 + 312.5 1562.5 )
[0619] Dinotefuran 3.2% 9.49
[0620] 10.81 9.83
[0621] T7 + Fluxametamide (3.16 32.53 48.03
[0622] (3.36) (3-21)
[0623] 3.2% 30 + 30 937.5 )
[0624] Dinotefuran 3.2% 7.85
[0625] 9.38 9.03
[0626] T + Fluxametamide 38.028 40 + 40 (2.89 57.01
[0627] (3-14) (3.09)
[0628] 3.2% 1250 )
[0629] Dinotefuran 3.2% 7.68
[0630] 10.23 8.91
[0631] T9 + Fluxametamide (2.86 38.85 57.94
[0632] 3.2% (3.28) (3.07)
[0633] 50 + 50 1562.5 )
[0634] Compound of
[0635] formula I 20% + 10.88 10.39 11.01
[0636] T10 (3.37 40.42 Fluxametamide 24.43
[0637] (3-3) (3-41)
[0638] 3.2% 187.5 + 30 937.5 )
[0639] Compound of
[0640] 9.95
[0641] formula I 20% + 10.13 10.43
[0642] Til 250 + 40 1250 (3.23 28.41 Fluxametamide 45.51
[0643] (3.26) (3.31)
[0644] ) 3.2%
[0645] Compound of
[0646] 9.69
[0647] formula I 20% + 10.27 10.26
[0648] T12 312.5 + 50 1562.5 (3.19 29.51 46.93 Fluxametamide (3.28) (3.28)
[0649] ) 3.2%
[0650] 11.39
[0651] 10.16 11.35 Dinotefuran 3.2% 22.1 37.62 T13 40 (3.45
[0652] (3.44) (3.26)
[0653] 1250 )
[0654]
[0655] 12.27
[0656] Compound of 10.29 12.02
[0657] T14 250 (3.57 17.5 32.8 formula I 20% (3.28) (3.54)
[0658] 1250 )
[0659] 12.1 Fluxametamide 9.41 11.81
[0660] T15 40 (3.55 18.94 33.73
[0661] 3.2% (3.15) (3.51)
[0662] 1250 )
[0663] Compound of
[0664] formula I 18% +
[0665] 157.50 + 9.61 7.88 3.92
[0666] T16 Fipronil 8% + 875 45.92 78.53 Dinotefuran 5% 70.00 + 43.75 (3.18) (2.89) (2-1)
[0667] w / w SC
[0668] Compound of 12.07
[0669] 10.33 11.73
[0670] T17 formula I 50 % 300 600 (3.55 19.49 33.9
[0671] WP (3.29) (3-5)
[0672] )
[0673] 12.02 Fluxametamide 10.42 11.8
[0674] T18 40 400 (3.54 19.01 34.17
[0675] 10% w / w EC (3-3) (3.51)
[0676] )
[0677] 18.26
[0678] 10.03 14.57
[0679] T19 (3.24) (4.33 - - (3.88)
[0680] Untreated check )
[0681] SEm± 0.03 0.10
[0682]
[0683] CD (p=0.05) 0.10 0.30
[0684] Figures in parentheses are square root transformed values; NS= non-significant; DAS: Days after spray Table 4: Field bio-efficacy evaluation of Dinotefuran 3.2% + Compound of formula I 20% + Fluxametamide 3.2% SC based on Chilli yield.
[0685] % Formulation
[0686] Yield Increase S. No Treatments a.i. dose (g / ha) dose (g or
[0687] (q / ha) against ml / ha)
[0688] control Dinotefuran 3.2% +
[0689] T1 Compound of formula I 69.43
[0690] 20% + Fluxametamide 3.2% 30 + 187.5 + 30 937.5 41.55 Dinotefuran 3.2% +
[0691] T2 Compound of formula I 40 + 250 + 40 72.67
[0692] 20% + Fluxametamide 3.2% 1250 48.15 Dinotefuran 3.2% +
[0693] T3 Compound of formula I 73.11
[0694] 20% + Fluxametamide 3.2% 50 + 312.5 + 50 1562.5 49.05 Dinotefuran 3.2% +
[0695] T4 Compound of formula I 59.13
[0696] 20% 30 + 187.5 937.5 20.55 Dinotefuran 3.2% +
[0697] T5 Compound of formula I 40 + 250 60.41
[0698] 20% 1250 23.16 Dinotefuran 3.2% +
[0699] T6 Compound of formula I 60.76
[0700]
[0701] 20% 50 + 312.5 1562.5 23.87Dinotefuran 3.2% +
[0702] T7 61.67 Fluxametamide 3.2% 30 + 30 937.5 25.73 Dinotefuran 3.2% +
[0703] T8 Fluxametamide 3.2% 40 + 40 63.15
[0704] 1250 28.75 Dinotefuran 3.2% +
[0705] T9 Fluxametamide 3.2% 63.28
[0706] 50 + 50 1562.5 29.01 Compound of formula I
[0707] T10 20% + Fluxametamide 3.2% 60.88
[0708] 187.5 + 30 937.5 24.12 Compound of formula I
[0709] Til 61.97
[0710] 20% + Fluxametamide 3.2% 250 + 40
[0711] 1250 26.34 Compound of formula I
[0712] T12 62.27
[0713] 20% + Fluxametamide 3.2% 312.5 + 50 1562.5 26.95 T13 Dinotefuran 3.2% 40 10 52.65 7.34 Compound of formula I
[0714] T14 250 55.01
[0715] 20% 10 12.15 T15 Fluxametamide 3.2% 40 10 58.10 18.45 Compound of formula I
[0716] T16 18% + Fipronil 8% + 157.50 + 70.00 + 43.75 875 68.65 Dinotefuran 5% w / w SC 39.96 Compound of formula I 50
[0717] T17
[0718] % WP 300 600 56.36
[0719] 14.90 Fluxametamide 10% w / w
[0720] T18 400 57.42
[0721] EC 40 17.06 T19 Untreated check - - 49.05 - CD (p=0.05) 1.25 -
[0722]
[0723] S Em ± 0.42 - DAS - Days after crop sowing; q / ha: quintal per hectare
[0724] Table 6: Phytotoxicity evaluation of Dinotefuran 3.2% + Compound of formula I 20% + Fluxametamide 3.2% SC on Chilli crop
[0725] Phytotoxicity parameters observed* s. a.i. dose Formulation (Mean data recorded at 1, 3, 7, 10 and 14 days Treatment
[0726] No. (g / ha) dose (ml / ha) after 1stspray)
[0727] L w N V E H Dinotefuran 3.2% +
[0728] Compound of formula I
[0729] T1 30 +
[0730] 0 0 0 0 0 0 20% + Fluxametamide 187.5 +
[0731] 3.2% 30 937.5
[0732] Dinotefuran 3.2% +
[0733] Compound of formula I
[0734] T2 40 + 250
[0735] 0 0 0 0 0 0 20% + Fluxametamide + 40
[0736] 3.2% 1250
[0737] Dinotefuran 3.2% +
[0738] Compound of formula I 50 +
[0739] T3 20% + Fluxametamide 0 0 0 0 0 0
[0740] 312.5 +
[0741] 3.2% 50 1562.5
[0742] Dinotefuran 3.2% +
[0743] T4 Compound of formula I 30 + 0 0 0 0 0 0
[0744]
[0745] 20% 187.5 937.5Dinotefuran 3.2% +
[0746] T5 Compound of formula I 40 + 250 0 0 0 0 0 0 20% 1250
[0747] Dinotefuran 3.2% +
[0748] T6 Compound of formula I 50 + 0 0 0 0 0 0 20% 312.5 1562.5
[0749] Dinotefuran 3.2% +
[0750] T7
[0751] Fluxametamide 3.2% 0 0 0 0 0 0
[0752] 30 + 30 937.5
[0753] Dinotefuran 3.2% +
[0754] T8 Fluxametamide 3.2% 40 + 40 0 0 0 0 0 0
[0755] 1250
[0756] Dinotefuran 3.2% +
[0757] T9 Fluxametamide 3.2% 0 0 0 0 0 0
[0758] 50 + 50 1562.5
[0759] Compound of formula I
[0760] T10 20% + Fluxametamide 187.5 + 0 0 0 0 0 0 3.2% 30 937.5
[0761] Compound of formula I
[0762] Til 20% + Fluxametamide 250 + 40 1250 0 0 0 0 0 0 3.2%
[0763] Compound of formula I
[0764] 312.5 +
[0765] T12 20% + Fluxametamide 1562.5 0 0 0 0 0 0 3.2% 50
[0766] T13 Dinotefuran 3.2% 40 1250 0 0 0 0 0 0 Compound of formula I
[0767] T14 250 0 0 0 0 0 0 20% 1250
[0768] T15 Fluxametamide 3.2% 40 1250 0 0 0 0 0 0 Compound of formula I
[0769] 157.50 +
[0770] 18% + Fipronil 8% +
[0771] T16 70.00 + 875 0 0 0 0 0 0 Dinotefuran 5% w / w
[0772] 43.75
[0773] SC
[0774] Compound of formula I
[0775] T17 300 600 0 0 0 0 0 0 50 % WP
[0776] Fluxametamide 10%
[0777] T18 40 400 0 0 0 0 0 0 w / w EC
[0778] T19 Untreated check - - Dinotefuran 3.2% +
[0779] Compound of formula I 80 + 500
[0780] T20 20% + Fluxametamide 0 0 0 0 0 0
[0781] + 80
[0782] 3.2% 2500
[0783] L - Leaf injury on tips / surface, W - Wilting, N - Necrosis, V - Vein clearing, E - Epinasty, H - Hyponasty
[0784] *Based on 0-10 scale where: 0=0%, 1=1-10%, 2=11-20%, 3=21-30%, 4=31-40%, 5=41-50%, 6=51-60%,
[0785] 7=61-70%, 8=71-80%, 9=81-90%, 10=91-100%
[0786]
[0787] From the examples above, it is clearly seen that the stable synergistic pesticidal composition of the present invention is superior for controlling the 14 days after 1st& 2ndspray (Table 2) and for controlling fruit borer population at 7 & 14 days after 1st& 2ndspray (Table 3) in Chilli crop as compared to the solo and composition applied at same dosage and other pesticides such as Compound of formula I 18% + Fipronil8% + Dinotefuran 5% w / w SC, Compound of formula I 50 % WP and Fluxametamide 10% w / w EC available in the market. The yield of Chilli crop also improved in the ternary pesticidal composition of Dinotefuran 3.2% + Compound of formula I 20% + Fluxametamide 3.2% SC as compared to binary and solo compositions (Table 4).
[0788] The disclosed stable synergistic pesticidal composition Dinotefuran 3.2% + Compound of formula I 20% + Fluxametamide 3.2% @ 937.5ml, 1250 ml, 1562.5 ml and 2500 ml / ha further showed no phytotoxicity in the Chilli crop even after 1, 3, 7, 10 and 14 days after 1stspray (Table 5).
[0789] It is evident from the above data that the stable synergistic pesticidal composition of the present invention i.e., Dinotefuran 3.2% + Compound of formula I 20% + Fluxametamide 3.2% SC resulted in good control of thrips and fruit borer in Chilli with higher respective yields as compared to the reference standard products (binary compositions and solo products). Further, the composition of present invention is resulted synergistic.
[0790] Through the pesticidal composition of present invention, the number of applications to control wide range of pests appearing at the same time is minimised. The composition of present invention is highly safe to the user and to the environment. The composition offers the user a single homogenous application eliminating the need for tank mix. The composition also is cost-effective as it provides much greater simultaneous control and can be used in a variety of crops with a broader spectrum of protection.
[0791] In particular, it has now been found, surprisingly that, for example, the pesticidal activity of the composition of present invention, compared with the pesticidal activity of individual components, is synergistic. In fact, various advantageous properties associated with the compositions according to the invention, include but are not limited to: a broadening of the spectrum of pesticidal activity to other pests, for example to resistant strains; a reduction in the rate of application of the active ingredients; adequate control of the pests at a rate of application at which the individual compounds are not very effective, advantageous behaviour during formulating and / or upon application, improved stability, improved crop characteristics including crop yields, more developed root system, increase in plant health including height, improved plant vigor, less plant verse (lodging), and other advantages familiar to a person skilled in the art.
[0792] From the above investigations, it will be observed that numerous modifications and variations can be effectuated without departing from the true spirit and scope of the novel concepts of the present invention. It is to be understood that no limitations with respect to the specific embodiments illustrated is intended or should be inferred. It should be understood that all such modifications and improvements have been deleted herein for the sake of conciseness and readability but are properly within the scope of the following claims.
Claims
I CLAIM
1. . A stable synergistic pesticidal composition comprising:A) Dinotefuran or its agrochemically acceptable isomers, salts, esters and derivatives;B) Compound of Formula I, i.e., N-[2,6-bis(l-methylethyl)-4-phenoxyphenyl]-N'-(l,l- dimethylethyl)thiourea or its agrochemically acceptable salts, esters and derivatives; andC) Fluxametamide or its agrochemically acceptable isomers, salts, esters or its derivatives.
2. , The stable synergistic pesticidal composition as claimed in claim 1, comprising:A) Dinotefuran or its agrochemically acceptable isomers, salts, esters and derivatives, in the range of 0.001-90% by weight of the composition;B) Compound of Formula I, i-e., N-[2,6-bis(l-methylethyl)-4-phenoxyphenyl]-N'-(l,l- dimethylethyl)thiourea or its agrochemically acceptable salts, esters and derivatives, in the range of 0.001-90% by weight of the composition; andC) Fluxametamide or its agrochemically acceptable isomers, salts, esters or its derivatives in the range of 0.001-90% by weight of the composition.
3. . A stable synergistic pesticidal composition comprising:A) Dinotefuran or its agrochemically acceptable isomers, salts, esters and derivatives;B) Compound of Formula I, i-e., N-[2,6-bis(l-methylethyl)-4-phenoxyphenyl]-N'-(l,l- dimethylethyl)thiourea or its agrochemically acceptable salts, esters and derivatives;C) Fluxametamide or its agrochemically acceptable isomers, salts, esters or its derivatives; and D) At least one or more additive.
4. . A stable synergistic pesticidal composition comprising:A) Compound of Formula I, i.e., 5,6-dihydro-2-methyl-l,4-oxathiin-3-carboxanilide or its agrochemically acceptable salts, esters and derivatives, in the range of 0.001-90% by weight of the composition;B) Compound of Formula II, i.e., 2,4,5,6-tetrachloro-l,3-benzenedicarbonitrile or its agrochemically acceptable salts, esters and derivatives, in the range of 0.001-90% by weight of the composition; C) At least one nitroguanidine insecticide selected from Imidacloprid or Clothianidin or its agrochemically acceptable salts, esters or its derivatives in the range of 0.001-90% by weight of the composition; andD) At least one or more additive selected from urea clathrate, Siloxane Polyalkyleneoxide Copolymer, tallow amine ethoxylate, ammonium sulphate, and epoxide soybean oil either alone or in combination thereof, in the range of 0.001-20% by weight of the composition.
5. . The stable synergistic pesticidal composition as claimed in claims 1-4, which further comprises one or more agrochemically acceptable excipients.
6. . The stable synergistic pesticidal composition as claimed in claim 1 to 5, wherein agrochemically acceptable excipients comprises surfactant(s), dispersing agent(s), co-dispersant, antifreezing agent(s), emulsifier(s) (anionic and non-ionic), anti-foaming agent / defoamer(s), wetting agent(s), antimicrobial / anti-bacterial agent(s), anti-caking agent, thickening agent / thickener(s), quick coating agent(s) or sticking agents / sticker(s), spreader(s), binder(s), pH-adjusting agent(s), anti-caking agent(s), adjuvant(s), filler(s) / suspension aid(s), colorant(s), carrier(s), buffering agent(s), polymer(s) rheology modifier(s), solvent(s), co-solvent(s), biocide(s), protective colloid(s), carrier(s), adhesive(s), thixotropic agent(s), penetration agent(s), stabiliser(s), sequestering agent(s) or a combination thereof.
7. . The stable synergistic pesticidal composition as claimed in any one of the claims 1 to 6, wherein the composition is in form of Capsule suspension (CS), Dispersible concentrate (DC), Dustable powder (DP), Powder for dry seed treatment (DS), Emulsifiable concentrate (EC), Emulsifiable granule (EG), Emulsion water-in-oil (EO), Emulsifiable powder (EP), Emulsion for seed treatment (ES), Emulsion oil-in-water (EW), Flowable concentrate for seed treatment (FS), Granules (GR), Micro-emulsion (ME), Oil-dispersion (OD), Oil miscible flowable concentrate (OF), Oil miscible liquid (OL), Oil dispersible powder (OP), Suspension concentrate (SC), Suspension concentrate for direct application (SD), Suspo-emulsion (SE), Water soluble granule (SG), Soluble concentrate (SL), Spreading oil (SO), Water soluble powder (SP), Water soluble tablet (ST), Ultra-low volume (ULV) suspension, Tablet (TB), Ultra-low volume (ULV) liquid, Water dispersible granules (WG), Wettable powder (WP), Water dispersible powder for slurry seed treatment (WS), Water dispersible tablet (WT), a mixed formulation of CS and SC (ZC) or a mixed formulation of CS and SE (ZE) or a mixed formulation of CS and EW (ZW).
8. . The stable synergistic pesticidal composition as claimed in claims 1 to 7, wherein the use of said composition promotes plant health, growth and increases plant, crop yield in the field.
9. . A process for preparing a stable synergistic pesticidal composition as claimed in claims 1-7.