Stable synergistic pesticidal composition
A synergistic pesticidal composition of 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4-chloropyridazin-3(2H)-one, Hexythiazox, and Dinotefuran addresses pest resistance and environmental concerns, offering enhanced efficacy and stability for broad-spectrum pest control with improved crop yield and safety.
Patent Information
- Authority / Receiving Office
- WO · WO
- Patent Type
- Applications
- Current Assignee / Owner
- RANI PRIYA
- Filing Date
- 2025-11-27
- Publication Date
- 2026-06-04
AI Technical Summary
Existing pesticidal compositions face challenges such as pest resistance, environmental impact, phytotoxicity, and ineffectiveness against all stages of sucking pests, necessitating a stable and synergistic formulation with enhanced efficacy and reduced toxicity.
A synergistic pesticidal composition combining 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4-chloropyridazin-3(2H)-one, Hexythiazox, and Dinotefuran in specific weight percentages, optionally with additives, to enhance stability, penetration, and broad-spectrum pest control.
The composition provides superior pest control, reduces resistance development, minimizes toxicity, and promotes plant health with improved yield and environmental safety, while maintaining stability across various conditions.
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Abstract
Description
[0001] STABLE SYNERGISTIC PESTICIDAL COMPOSITION
[0002] FIELD OF THE INVENTION
[0003] The present invention relates to a stable synergistic pesticidal composition comprising A) a compound of Formula I, i.e., 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4-chloropyridazin-3(2H)-one or its agrochemically acceptable salts, isomers, esters and derivatives; B) Hexythiazox or its agrochemically acceptable salts, isomers, esters and derivatives; and C) Dinotefuran or its agrochemically acceptable salts, isomers, esters or its derivatives for effective control of various pests including but not limited to insects-pests, mites, arachnid, etc. and wide range of diseases caused by such pests. The present invention also relates to a process for preparation of such pesticidal composition for synergistic and efficacious control of various pests including insects-pests, mites, arachnid, etc and associated diseases.
[0004] BACKGROUND OF THE INVENTION
[0005] In a quest of improving the product performance, every novel combination has to surpass various criteria linked to desirous agrochemical traits. Among these, the most critical factors include high biological efficacy, profitability, and long-lasting protection, profitability, yield, storage, handling, application, effectiveness and safety to the applicator and the environment. Improvement in the formulation technologies plays a key role in enhancing product performance and meeting modern agricultural demands. Continuous use of conventional formulations has resulted in accumulated challenges such as increased toxic effect, ecological effect, resistance to specific target bugs / insect-pest population and disruption of biodiversity, but also, they basically influence their metabolism and productivity, requiring effective adversary of developing responses for ensure ideal crop yield and quality.
[0006] The driving force for new product developments is related to limitations of existing compositions and formulations leading to pest resistance; negative environmental impact such as plants phytotoxicity, staining of leaves; frequently adversely affect non-target pests impacting biodiversity and the climate. Solving these challenges, the standard developing of plant influences different physiological and biochemical cycles, provoking reduced advancement, lessened security from biological weights, and diminished by and large prosperity and effectiveness. Prior arts are known disclosing the pesticidal composition which comprises insecticidal and acaricidal components. However, existing insecticidal or acaricidal combinations shows adverse effect on plants and crops such as discoloration of plant leaves, resistance against sucking pests complex and are ineffective against control of all stages of sucking pests complex such as thrips, white fly, aphids etc.
[0007] Reference can be made to CN 102273481, which discloses a combination of compound of Dinotefuran and Compound of Formula I in a ratio of (1 to 80): (80 to 1), and the dinotefuran and the Compound of Formula I account for 20% of the effective components.
[0008] Further references can be made to CN 103843809, which discloses insecticidal composition containing dinotefuran and Compound of Formula I in a ratio of 1-80:80: 1.
[0009] Thus, there is a need to overcome these challenges mentioned herein above. In view of the same, the present objectives to develop a stable synergistic pesticidal composition having an enhanced efficacy, reduce the likelihood of resistance development, reduce toxicity, increase residual activity, reduced dosages, offers broader crop protection, improved and healthy foliage, improved crop yield, saves labour, mitigate environmental impact and economical and is yet cost effective to the end user.
[0010] The stable synergistic pesticidal composition of the present invention will thereby targets multiple biological pathways in pest, thereby increasing mortality rates and reduces the probability of resistance and where actives in the novel composition are mutually compatible and also resulting in stable composition also.
[0011] Therefore, the aim of the present invention is to provide a stable synergistic pesticidal composition that addresses these needs by providing a novel composition that combines active ingredients and that too in specific weight percentage ranges. Composition of present invention has demonstrated superior efficacy in controlling a broad spectrum of pests while being environmentally sustainable.
[0012] A compound of Formula I chemically known as 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4-chloropyridazin-3(2H)-one, is a non-systemic insecticide and acaricide with rapid knock down action and long residual activity. It is a mitochondrial complex I electron transport inhibitor and delivers rapid knockdown against motile stages of mites. It is used for the control of aphids, mites, thrips and leaf hoppers in various crops and trees such as cucumbers, tomatoes & peppers; strawberries; ornamentals; vegetables etc.
[0013] Further, Hexythiazox is a non-systemic insecticide and acaricide with contact and stomach action. It pertains to a mite growth inhibitor affecting CHS 1. It also acts as a selective growth regulator preventing emergence of new pests. It is an acaricide used for the control of eggs and larvae of many mites on a wide variety of fruit and crops such as apples, pears, stone fruit, citrus, grapes; nuts; turf; cotton; cucumber, etc.
[0014] Moreover, Dinotefuran is an isomeric mixture with systemic as well as contact and stomach action insecticide. It pertains to nicotinic acetylcholine receptor (nAChR) channel blocker and provide systemic control of sucking pests such as whiteflies; mealybugs; thrips; plant hoppers; leafminers; aphids in various plants such as vegetables; fruit; turf; rice crops etc.
[0015] In view of the drawbacks associated with the prior arts, there exists a need to provide a stable synergistic pesticidal composition for synergistic and effective control of pests including insectpest and sucking pests’ complex, mites and arachnids, etc.
[0016] The present invention satisfies the existing needs, as well as others, and generally overcomes the deficiencies found in the prior art. The present invention composition is synergistic, efficacious, environmentally friendly, simple to formulate, stable and is safe to use.
[0017] Thus, a 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 of A) a compound of Formula I, i.e., 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4-chloropyridazin-3(2H)-one or its agrochemically acceptable salts, isomers, esters and derivatives; B) Hexythiazox or its agrochemically acceptable salts, isomers, esters and derivatives; and C) Dinotefuran or its agrochemically acceptable salts, isomers, esters or its derivatives.
[0018] The present invention also provides a novel method of preparing composition of present invention, which is stable as well as provide desired bio-efficacy, synergy. Embodiments of the present invention may therefore ameliorate one or more of the above-mentioned problems. OBJECTIVES AND ADVANTAGES OF THE INVENTION
[0019] The principal objective of the present invention is to provide a novel and effective stable synergistic pesticidal composition demonstrating high efficacy and to provide complete protection to crops, plants against pests including but not limited to insect-pests, mites, flies, arachnid and diseases associated with them.
[0020] It is another objective of the present invention to provide improved, stable and ready to use pesticidal composition having synergistic and superior efficacious properties compared to prior art formulations or mixtures or compositions.
[0021] It is yet another objective of the present invention to provide a novel and effective stable synergistic pesticidal composition demonstrating high efficacy and high selectivity. It is yet another objective of the present invention to provide improved combination of insecticides and acaricides for broad spectrum control of pests.
[0022] It is yet another objective of the present invention to provide a method and a stable synergistic pesticidal composition for controlling pests including insect-pests, mites and arachnid, etc. and diseases associated with such pests.
[0023] Yet another objective of the present invention to provide a novel and effective stable synergistic pesticidal composition which has both preventive and curative action and is active against all life stages of major plant pathogens and that promotes plant health, growth and increases plant, crop yield in the field.
[0024] Yet another objective of the present invention is to provide a composition and method for controlling wide range of pests including insectpests, sucking pests and pests induced diseases affecting plants, crops and plant propagation materials, etc.
[0025] 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. 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.
[0026] It is another objective of the present invention to provide a novel and effective stable synergistic pesticidal composition which further optionally comprises additives 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.
[0027] Another objective of the present invention is to provide a stable synergistic pesticidal composition comprising A) a compound of Formula I, i.e., 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4-chloropyridazin-3(2H)-one or its agrochemically acceptable salts, isomers, esters and derivatives; B) Hexythiazox or its agrochemically acceptable salts, isomers, esters and derivatives; and C) Dinotefuran or its agrochemically acceptable salts, isomers, esters or its derivatives.
[0028] Yet another objective of the present invention is to provide a process for the preparation of a stable synergistic pesticidal composition comprising A) a compound of Formula I, i.e., 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4-chloropyridazin-3(2H)-one or its agrochemically acceptable salts, isomers, esters and derivatives; B) Hexythiazox or its agrochemically acceptable salts, isomers, esters and derivatives; and C) Dinotefuran or its agrochemically acceptable salts, isomers, esters or its derivatives.
[0029] Some or all these and other objects of the invention can be achieved by way of the invention described hereinafter.
[0030] ADVANTAGES:
[0031] 1. The stable synergistic pesticidal composition of the present invention resulted in significantly lower incidence of pesticidal diseases in various crops such as field crops; fruit including apples, pears, stone fruit, citrus, grapes, turf, nuts; cotton; cucumber; greenhouse crops including cucumbers, pepper & tomato; fruit trees; strawberries; ornamentals; vegetables; rice crops, etc.
[0032] 2. The stable synergistic pesticidal composition of the present invention results in significant lowering the count of insect pest such as of mites; spider mites; rust mites; tetranychid mites, mealybugs; thrips; plant hoppers; leaf-miners; aphids, pear psylla; whiteflies, etc.
[0033] 3. The stable synergistic pesticidal composition of the present invention shows no phytotoxicity effect and provide a stable synergistic pesticidal composition that shows technical advancement over the existing combination of insecticides and also shows to has an improved rain fastness.
[0034] 4. The stable synergistic pesticidal composition of the present invention decreases the chances of resistance against pesticidal diseases and shows to have an improved stability during the desired shelf life and promotes plant health and increases plant yield in the field.
[0035] SUMMARY OF THE INVENTION
[0036] Accordingly, the main aspect of the present invention is to provide a synergistic pesticidal composition having high insect pests control efficacy.
[0037] Accordingly, the present invention relates to a synergistic pesticidal composition comprising A) Compound of Formula I, i.e., 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4-chloropyridazin- 3(2H)-one or its agrochemically acceptable salts, isomers, esters and derivatives;
[0038] B) Hexythiazox or its agrochemically acceptable salts, isomers, esters and derivatives; and C) Dinotefuran or its agrochemically acceptable salts, isomers, esters or its derivatives.
[0039] In another aspect, the present invention provides a stable synergistic pesticidal composition comprising:
[0040] A) Compound of Formula I, i.e., 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4-chloropyridazin- 3(2H)-one or its agrochemically acceptable salts, isomers, esters and derivatives;
[0041] B) Hexythiazox or its agrochemically acceptable salts, isomers, esters and derivatives;
[0042] C) Dinotefuran or its agrochemically acceptable salts, isomers, esters or its derivatives; and D) At least one or more agrochemically acceptable excipients.
[0043] In another aspect, the present invention provides a stable synergistic pesticidal composition comprising:
[0044] A) Compound of Formula I, i.e., 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4-chloropyridazin- 3(2H)-one or its agrochemically acceptable salts, isomers, esters and derivatives;
[0045] B) Hexythiazox or its agrochemically acceptable salts, isomers, esters and derivatives;
[0046] C) Dinotefuran or its agrochemically acceptable salts, isomers, esters or its derivatives; and
[0047] D) At least one or more agrochemically acceptable additives.
[0048] In one another aspect, the present invention provides a stable synergistic pesticidal composition comprising:
[0049] A) Compound of Formula I, i.e., 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4-chloropyridazin- 3(2H)-one or its agrochemically acceptable salts, isomers, esters and derivatives;
[0050] B) Hexythiazox or its agrochemically acceptable salts, isomers, esters and derivatives;
[0051] C) Dinotefuran or its agrochemically acceptable salts, isomers, esters or its derivatives;
[0052] 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
[0053] E) One or more agrochemically acceptable excipients.
[0054] In one another aspect, the present invention provides a stable synergistic pesticidal composition comprising:
[0055] A) Compound of Formula I, i.e., 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4-chloropyridazin- 3(2H)-one or its agrochemically acceptable salts, isomers, esters and derivatives, in the range of 0.1-90% by weight of the composition;
[0056] B) Hexythiazox or its agrochemically acceptable salts, isomers, esters and derivatives, in the range of 0.1-90% by weight of the composition; and C) Dinotefuran or its agrochemically acceptable salts, isomers, esters or its derivatives, in the range of 0.1-90% by weight of the composition;
[0057] In yet another aspect, the present invention provides a process for preparation of the stable synergistic pesticidal composition comprising:
[0058] A) Compound of Formula I, i.e., 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4-chloropyridazin- 3(2H)-one or its agrochemically acceptable salts, isomers, esters and derivatives;
[0059] B) Hexythiazox or its agrochemically acceptable salts, isomers, esters and derivatives; and
[0060] C) Dinotefuran or its agrochemically acceptable salts, isomers, esters or its derivatives.
[0061] In an aspect of the present invention, the present invention provides a stable synergistic pesticidal composition which further optionally comprises additives and / or adjuvants, for providing the following attributes to the composition of present invention:
[0062] a) improved penetration capacity,
[0063] b) enhanced spreading or coverage effect,
[0064] c) uniform spray-ability,
[0065] d) enhanced stability and permeability
[0066] e) improved rain-fastness,
[0067] f) enriched biotic factors,
[0068] g) better flowability,
[0069] h) effective storage stability,
[0070] i) longer residual effect,
[0071] j) improved uptake of active ingredients, and
[0072] k) safer to the environment.
[0073] In another aspect, the present synergistic pesticidal composition is stable and has enhanced shelf life and effectively control wide range of pests including insect pests, mites, arachnid, etc. in various crops.
[0074] In another aspect, the present invention provides a stable synergistic pesticidal composition which has enhanced efficacy and penetration capacity. DETAILED DESCRIPTION OF THE INVENTION
[0075] 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.
[0076] 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.
[0077] 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.
[0078] 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.
[0079] 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.
[0080] The terms “comprise / 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. 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.
[0081] The expression of various quantities in terms of “% w / w” or “% w / v” means the percentage by weight, relative to the weight or the volume of the total solution or composition unless otherwise specified.
[0082] 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 pests including but not limited to insects-pests, arachnids and mites, etc. at the same time.
[0083] The term “crop” shall include a multitude of desired crop plants or an individual crop plant growing at a locus.
[0084] 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. “Bioactive amounts” as mentioned herein means that amount which, when applied for treatment of crops, is sufficient to give effect in such treatment.
[0085] 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. 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.
[0086] 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.
[0087] 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.
[0088] In another preferred embodiment of the invention, the yield of the plants treated according to the method of the invention, is increased synergistically.
[0089] 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.
[0090] Another indicator for the condition of the plant is the “quality” of a plant and / or its products. In an especially preferred embodiment of the invention, the quality of the treated plant is increased. In another preferred embodiment of the invention, the quality of the plants treated according to the method of the invention, is increased synergistically.
[0091] 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.
[0092] 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 including sucking pests 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. 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.
[0093] According to embodiments of the present invention, the yield of the treated plant is increased.
[0094] In another embodiment of the present invention, there is synergistic and efficacious control of various pests affecting the plants and crops.
[0095] Another embodiment of the present invention, includes within its scope, all possible salts, isomers, esters and derivatives of the active ingredients of the composition.
[0096] 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.
[0097] 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.
[0098] 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 pests including but not limited to insects-pests, mites, arachnids, etc.
[0099] It has been observed 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 insect pests including egg, nymph, larva, pupa, and adult.
[0100] In an embodiment, the present invention provides a stable synergistic pesticidal composition comprising:
[0101] A) Compound of Formula I, i.e., 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4-chloropyridazin- 3(2H)-one or its agrochemically acceptable salts, isomers, esters and derivatives;
[0102] B) Hexythiazox or its agrochemically acceptable salts, isomers, esters and derivatives; and
[0103] C) Dinotefuran or its agrochemically acceptable salts, isomers, esters or its derivatives.
[0104] In another embodiment, the present invention provides a stable synergistic pesticidal composition comprising:
[0105] A) Compound of Formula I, i.e., 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4-chloropyridazin- 3(2H)-one or its agrochemically acceptable salts, isomers, esters and derivatives;
[0106] B) Hexythiazox or its agrochemically acceptable salts, isomers, esters and derivatives;
[0107] C) Dinotefuran or its agrochemically acceptable salts, isomers, esters or its derivatives; and
[0108] D) At least one or more agrochemically acceptable excipients.
[0109] In another embodiment, the present invention provides a stable synergistic pesticidal composition comprising:
[0110] A) Compound of Formula I, i.e., 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4-chloropyridazin- 3(2H)-one or its agrochemically acceptable salts, isomers, esters and derivatives;
[0111] B) Hexythiazox or its agrochemically acceptable salts, isomers, esters and derivatives;
[0112] C) Dinotefuran or its agrochemically acceptable salts, isomers, esters or its derivatives; and
[0113] D) At least one or more additives.
[0114] In one another embodiment, the present invention provides a stable synergistic pesticidal composition comprising: A) Compound of Formula I, i.e., 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4-chloropyridazin- 3(2H)-one or its agrochemically acceptable salts, isomers, esters and derivatives;
[0115] B) Hexythiazox or its agrochemically acceptable salts, isomers, esters and derivatives;
[0116] C) Dinotefuran or its agrochemically acceptable salts, isomers, esters or its derivatives;
[0117] D) At least one or additive selected from Urea clathrate, Siloxane Polyalkyleneoxide Copolymer, tallow amine ethoxylate, ammonium sulphate, and Epoxide soybean oil either alone or in combination thereof; and
[0118] E) At least one or more agrochemically acceptable excipients.
[0119] In one another embodiment, the present invention provides a stable synergistic pesticidal composition comprising:
[0120] A) Compound of Formula I, i.e., 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4-chloropyridazin- 3(2H)-one or its agrochemically acceptable salts, isomers, esters and derivatives, in the range of 0.1-90% by weight of the composition;
[0121] B) Hexythiazox or its agrochemically acceptable salts, isomers, esters and derivatives, in the range of 0.1-90% by weight of the composition; and
[0122] C) Dinotefuran or its agrochemically acceptable salts, isomers, esters or its derivatives, in the range of 0.1 -90% by weight of the composition.
[0123] In one another embodiment, the present invention provides a stable synergistic pesticidal composition comprising:
[0124] A) Compound of Formula I, i.e., 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4-chloropyridazin- 3(2H)-one or its agrochemically acceptable salts, isomers, esters and derivatives, in the range of 0.1-90% by weight of the composition;
[0125] B) Hexythiazox or its agrochemically acceptable salts, isomers, esters and derivatives, in the range of 0.1-90% by weight of the composition;
[0126] C) Dinotefuran or its agrochemically acceptable salts, isomers, esters or its derivatives, in the range of 0.1-90% by weight of the composition; and D) At least one or more agrochemically acceptable excipients.
[0127] In one another embodiment, the present invention provides a stable synergistic pesticidal composition comprising:
[0128] A) Compound of Formula I, i.e., 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4-chloropyridazin- 3(2H)-one or its agrochemically acceptable salts, isomers, esters and derivatives, in the range of 0.1-90% by weight of the composition;
[0129] B) Hexythiazox or its agrochemically acceptable salts, isomers, esters and derivatives, in the range of 0.1-90% by weight of the composition;
[0130] C) Dinotefuran or its agrochemically acceptable salts, isomers, esters or its derivatives, in the range of 0.1-90% by weight of the composition; and
[0131] D) At least one or more agrochemically acceptable additives.
[0132] In one another embodiment, the present invention provides a stable synergistic pesticidal composition comprising:
[0133] A) Compound of Formula I, i.e., 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4-chloropyridazin- 3(2H)-one or its agrochemically acceptable salts, isomers, esters and derivatives, in the range of 0.1-90% by weight of the composition;
[0134] B) Hexythiazox or its agrochemically acceptable salts, isomers, esters and derivatives, in the range of 0.1-90% by weight of the composition;
[0135] C) Dinotefuran or its agrochemically acceptable salts, isomers, esters or its derivatives, in the range of 0.1-90% by weight of the composition;
[0136] D) At least an 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 0.01-20% by weight of the composition; and
[0137] E) At least one or more agrochemically acceptable excipients.
[0138] In a specific embodiment, the present invention provides a stable synergistic pesticidal composition comprising: A) Compound of Formula I, i.e., 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4-chloropyridazin- 3(2H)-one or its agrochemically acceptable salts, isomers, esters and derivatives, in the range of 0.1-45% by weight of the composition;
[0139] B) Hexythiazox or its agrochemically acceptable salts, isomers, esters and derivatives, in the range of 0.1-25% by weight of the composition; and
[0140] C) Dinotefuran or its agrochemically acceptable salts, isomers, esters or its derivatives, in the range of 0.1-45% by weight of the composition.
[0141] In yet another embodiment, the present invention provides a process for preparation of the stable synergistic pesticidal composition comprising:
[0142] A) Compound of Formula I, i.e., 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4-chloropyridazin- 3(2H)-one or its agrochemically acceptable salts, isomers, esters and derivatives;
[0143] B) Hexythiazox or its agrochemically acceptable salts, isomers, esters and derivatives; and
[0144] C) Dinotefuran or its agrochemically acceptable salts, isomers, esters or its derivatives.
[0145] In accordance with an embodiment of the present invention, there is provided a synergistic pesticidal composition comprising active ingredients present in the weight % (w / w% or w / v%) range as given below:
[0146] Compound of Formula I herein pertain to 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4-chloropyridazin-3(2H)-one or its agrochemically acceptable salts, esters and derivatives
[0147] S. No Active Ingredient Weight % range (w / w% or w / v%)
[0148] 1 Compound of Formula I or its agrochemically acceptable 0.1-90%
[0149] salts, isomers, esters and derivatives
[0150] 2 Hexythiazox or its agrochemically acceptable salts, 0.1-90%
[0151] isomers, esters and derivatives
[0152] 3 Dinotefuran or its agrochemically acceptable salts, 0.1-90%
[0153] isomers, esters or its derivatives
[0154]
[0155] According to yet another embodiment, process for preparing the pesticidal composition involves selecting and weighing the active ingredients in predetermined synergistic weight % range, mixing the said active ingredients with one or more agrochemically acceptable carriers and / or excipients, and optionally incorporating one or more surfactants, dispersing agents, wetting agents, suspending agents, stabilizers, defoamers, or binders to obtain the stable synergistic pesticidal composition.
[0156] According to embodiments of the present invention, the synergistic pesticidal composition results in an increased yield of the treated plant. Accordingly, pesticidal composition of present invention shows synergistic and efficacious control of various pests including but not limited to insect-pests, mites, flies, arachnids, etc and their associated diseases affecting the plants and crops. The present invention includes within its scope, all possible salts, isomers, esters and derivatives of the active ingredients of the composition.
[0157] 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. Adjuvants used in the present invention to make it a safer to ecological environmental, having low toxicity and having no phytotoxicity effects on any part of the plant.
[0158] Examples of surfactant(s) and / or dispersing agent and / or co-dispersant used herein include but not limited polymeric anionic dispersant, polyarylphenyl ether phosphate, tristyryl phenol ethoxylate, Polymethyl methacrylate -polyethylene glycol graft copolymer, acrylate copolymer, 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-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 and present in the range of 0.1-20% by weight of the composition.
[0159] Examples of wetting agent used herein include but not limited to tristyrylphenol ethoxylate nonionic 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, 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 sulphate, sodium sulphates or mixtures thereof and present in the range of 0.1 -20% by weight of the total composition.
[0160] Examples of defoamer or antifoaming agent used herein include but not limited to silicon emulsion based anti-foam agents, Siloxane polyalkyleneoxide, 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.
[0161] 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 1.0-20% by weight of the composition. 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.
[0162] 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.
[0163] 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 0.1-45 % by weight of the composition.
[0164] 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 1-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.
[0165] Examples of rheology modifier or thickeners or thickening 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.
[0166] 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, EO / PO block 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; Tristyrylphenol 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.
[0167] Examples of solvent(s) and co-solvent(s) used herein include but not limited to polar and nonpolar 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.
[0168] 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.
[0169] 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.
[0170] 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.
[0171] 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-1,3-diol), Propyl para-hydroxy -benzoate or mixture thereof and present in the range of 0.01- 35 % by weight of the composition.
[0172] Examples of stabilizer(s) used herein include but not limited to 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., Pluronic® types), 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.
[0173] 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. According to embodiments of the present invention, the synergistic pesticidal composition or formulation according to the present invention 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 associated with pests such as insects, arachnids, mites, etc.
[0174] In an embodiment of the present invention, the stable synergistic pesticidal composition further optionally comprises additives and / or adjuvants, for providing the following attributes to the composition of present invention:
[0175] a) enhanced permeability and stability
[0176] b) improved penetration capacity, and uptake of active ingredients
[0177] c) effective storage stability,
[0178] d) longer residual effect,
[0179] e) improved rain-fastness,
[0180] f) enriched biotic factors,
[0181] g) uniform spray-ability,
[0182] h) better flowability,
[0183] i) enhanced spreading or coverage effect,
[0184] j) safer to the environment.
[0185] 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), 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 or a combination thereof. Additional components may also be included, e.g., protective colloids, carriers, adhesives, thixotropic agents, penetration agents, stabilisers, sequestering agents. More generally, the active materials can be combined with any solid or liquid carrier / additive, which complies with usual formulation techniques. In yet another embodiment of the present invention, the present stable synergistic pesticidal composition can be formulated as one or more 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). 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 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).
[0186] 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 composition. Further excipients include e.g. organic and inorganic thickeners, bactericides, antifreeze agents, antifoams, colorants and, for seed formulations, adhesives.
[0187] 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.
[0188] In one embodiment, additives such as Siloxane Polyalkyleneoxide Copolymer or Siloxane Polyalkyleneoxide Copolymer super-wetter is an organosilicone based powder adjuvant that can enhance the water absorption efficiency of hard-to-wet soils by increasing their water infiltration, drainage, water retention and hydrophilicity; tallow amine ethoxylate increases the biocompatibility in environmental applications and help in the interactions of active ingredients; ammonium sulphate help is resistant to leaching and helps the crop to utilize nitrogen efficiently; and epoxide soybean oil provides increased active ingredient uptake and improved rain fastness to the composition. The said additives are stable and hygroscopic resulting in an efficient uptake and functioning.
[0189] In one embodiment, Siloxane Polyalkyleneoxide Copolymer has superspreading ability, it significantly lowers the surface tension of spray solutions, allowing them to spread uniformly across plant surfaces, including waxy or hard-to-wet leaves. This enhances the penetration and absorption of insecticides, leading to improved efficacy. Siloxane Polyalkyleneoxide Copolymer is especially effective in low-volume spray applications and helps increase rainfastness and reduce runoff. Its use supports more efficient pesticide delivery, often allowing for reduced application rates. In one embodiment, the inclusion of both Siloxane Polyalkyleneoxide Copolymer, organosilicone-based powder adjuvant, and tallow amine ethoxylate in a formulation significantly enhances its surface activity and delivery efficiency. Siloxane Polyalkyleneoxide, a trisiloxane-based superspreader, dramatically reduces surface tension, enabling rapid and uniform spreading of the solution across plant surfaces, even on waxy or water-repellent leaves. In synergy, tallow amine ethoxylate, a non-ionic surfactant, acts as a powerful wetting and penetration agent, improving the absorption of active ingredients into plant tissues. This combination ensures maximum bioavailability and performance of agrochemical actives.
[0190] According to an another embodiment, additives such as Siloxane Poly alkyleneoxide Copolymer or super-wetter is an organosilicone based powder adjuvant that can enhance the water absorption efficiency of hard-to-wet soils by increasing their water infiltration, drainage, water retention and hydrophilicity; tallow amine ethoxylate increases the biocompatibility in environmental applications and help in the interactions of active ingredients; ammonium sulphate help is resistant to leaching and helps the crop to utilize nitrogen efficiently; urea clathrate provides superior wetting and spray retention properties and serves as an excellent nitrogen source for crops and epoxide soybean oil provides increased active ingredient uptake and improved rain fastness to the composition; and epoxide soybean oil provides increased active ingredient uptake and improved rain fastness to the composition. The said additives are stable and hygroscopic resulting in an efficient uptake and functioning. 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.
[0191] Siloxane Polyalkyleneoxide Copolymer or organosilicone-based powder adjuvant has superspreading ability, it significantly lowers the surface tension of spray solutions, allowing them to spread uniformly across plant surfaces, including waxy or hard-to-wet leaves. This enhances the penetration and absorption of insecticides, leading to improved efficacy. Organosilicone-based powder adjuvant is especially effective in low-volume spray applications and helps increase rainfastness and reduce runoff. Its use supports more efficient pesticide delivery, often allowing for reduced application rates. In one embodiment, the inclusion of both Siloxane Polyalkyleneoxide Copolymer or organosilicone -based powder adjuvant and tallow amine ethoxylate in a formulation significantly enhances its surface activity and delivery efficiency. Siloxane Polyalkyleneoxide Copolymer, a trisiloxane -based super-spreader, dramatically reduces surface tension, enabling rapid and uniform spreading of the solution across plant surfaces, even on waxy or water-repellent leaves. In synergy, tallow amine ethoxylate, a non-ionic surfactant, acts as a powerful wetting and penetration agent, improving the absorption of active ingredients into plant tissues. This combination ensures maximum bioavailability and performance of agrochemical actives.
[0192] In one embodiment, ammonium sulphate particularly as a water conditioner and adjuvant. It helps improve the efficacy of pesticides, by binding with hard water cations such as calcium and magnesium that would otherwise reduce pesticide absorption and activity. By preventing these ions from interacting with the active ingredient, ammonium sulphate enhances uptake into plant tissues. It may also act as a nitrogen source, supporting plant growth.
[0193] In one embodiment, Epoxide soybean oil, a bio-based plasticizer and solvent, improves formulation compatibility, reduces phytotoxicity, and enhances the dispersion of active compounds. Derived from renewable sources, both additives support sustainable agriculture by offering low toxicity, biodegradability, and improved formulation efficiency without compromising efficacy.
[0194] In one embodiment, Siloxane Polyalkyleneoxide Copolymer, tallow amine ethoxylate, ammonium sulphate, and epoxidie soybean oil are additives used individually or in combination to enhance the performance of agrochemical formulations. Siloxane Polyalkyleneoxide Copolymer, a superspreading organosilicone surfactant, reduces surface tension and improves leaf coverage and penetration of active ingredients. Tallow amine ethoxylates, as non-ionic surfactants, aid in emulsification and enhance pesticide uptake. Ammonium sulphate serves as a water conditioner, preventing hard water ions from reducing pesticide efficacy, while also acting as a nitrogen source. Epoxide soybean oil, a biodegradable solvent and plasticizer, improves formulation stability, compatibility, and reduces phytotoxicity. Used alone or synergistically, these additives optimize spray performance, improve bioavailability of actives, and support sustainable and effective crop protection. According toembodiments of the present invention, the present stable synergistic pesticidal composition can be applied to various crops and plants including but not limited to tea, cotton, chilli, brinjal, apple, grapes, rose, okra, rice, rice (paddy), etc.
[0195] According to embodiments of the present invention, the present pesticidal composition provides synergistic and effective control against pests including but not limited to insect-pest, sucking complex pests including brown plant hopper, leaf hopper, green leaf hopper, White backed plant hopper, red spider mite, red spider mite (Oligonychus cofeeaea), white fly, yellow mite (Polyphagotarsonemus latus), European red mite (Panonychus ulmi), scarlet mite (Brevipalpus phoenicis), red spider mite, jassids, Aphids & Thrips etc.
[0196] According to embodiments of the present invention, the composition can be applied to any and all developmental stages of pests, such as egg, nymph, larva, pupa, and adult. The insect pests may be controlled by contacting the target insect pest, habitat, breeding ground or its locus with a bioactive amount of the novel and inventive composition of the present invention.
[0197] According to embodiments the 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.
[0198] 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.
[0199] 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. The pesticidal composition of the present invention has very advantageous, curative, preventive and systemic insecticidal properties for protecting plants and crops.
[0200] The composition of the present invention also provides control of pests including insect-pests, arachnids, mites, etc. preventatively or curatively by applying an effective amount of the composition either pre-or post-infection.
[0201] 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. In one embodiment, the composition according to the present invention acts synergistically to control pests in various crops.
[0202] Representative examples of the present composition of this invention are provided below and are not to be construed as limiting in any manner:
[0203] EXAMPLES: GENERAL RECIPE OF COMPOSITION OF PRESENT INVENTION:
[0204] Compound of Formula I pertain to 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4-chloropyridazin-3(2H)-one or its agrochemically acceptable salts, isomers, esters and derivatives;
[0205] % (w / w) of S. No. Ingredients the composition 1 Compound of Formula I Technical 0.1-90 2 Hexythiazox Technical 0.1-90
[0206]
[0207] Dinotefuran Technical 0.1-90 Additive(s)- Siloxane Polyalkyleneoxide Copolymer, tallow amine ethoxylate, ammonium sulphate, and Epoxide soybean oil either alone or 0.01-20 in combination thereof
[0208] Surfactant / Dispersing agent(s) / Co-dispersant(s)- polymeric anionic dispersant, polyarylphenyl ether phosphate, tristyryl phenol ethoxylate, Polymethyl methacrylate -polyethylene glycol graft copolymer, Sodium lauryl sulphonate, Alpha olefin sulphonate, acrylate copolymer, 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-formaldehyde polycondensation as sodium salt, sodium salt condensate with formaldehyde, ethoxylated oleyl cetyl alcohol, Sodium Alkyl Naphthalene Sulfonate Blend, styrenated phenol 0.1-20 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,
[0209]
[0210] 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
[0211] - non-ionic polymeric surfactant, aqueous dispersant - polymeric amphoteric aqueous dispersant or mixtures thereof
[0212] 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, Di-isopropyl Napthalene sulphonate,
[0213] 0.1-20 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 sulphate, sodium sulphates or mixtures thereof
[0214] Defoamer / Anti-foaming agent- silicon emulsion based anti-foam agents, Siloxane poly alkyleneoxide, Polydimethylsiloxane, Polyalkyleneoxide -modified Polydimethylsiloxane, trisiloxane ethoxylates, silicone oil, silicone compound, C10~C20 saturated fat acid 0.01-5.0 compounds or C8~C10 aliphatic alcohols compound, vegetable oil based antifoam, tallow based fatty acids, polyalkyleneoxide polydimethylsiloxane emulsion and mixtures thereof
[0215] Anti-freezing agent(s)- glycol, propylene glycol, mono ethylene glycol, glycerine, diethylene glycol, sorbitol, urea, mannitol, polyethylene glycol 1.0-20 or mixtures thereof
[0216] Filler(s)- silicon dioxide, china-clay, kaolin, starch, bentonite,
[0217] 0.1-60 precipitated silica, fumed silica, lactose monohydrate, talcum powder,
[0218]
[0219] lactose, ammonium sulphate, water, sodium Sulphate, magnesium sulphate, sodium citrate, sodium chloride, potassium chloride and mixtures thereof
[0220] Anti-caking agent(s)- group of talc, hydrous magnesium silicate, magnesium carbonate, calcium carbonate, precipitate silica, silica 0.1-10 powder, hydrophobic fumed silica and mixtures thereof
[0221] Carrier(s)- silicon dioxide, china clay, kaolin, starch, bentonite, precipitated silica, silica powder, fumed silica, ppt silica powder, lactose
[0222] 1.0-45 monohydrate, talcum powder, lactose, ammonium sulpha or mixture thereof
[0223] 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- 0.01-10 isothiazolin-3-one and 2-methyl-4-isothiazolin-3-one, zinc 1 -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 Rheology modifier / Thickening agent(s)- polysaccharides, carboxymethyl cellulose, bentonite clay, aluminium magnesium silicate,
[0224] 0.01-5.0 hydroxy propyl cellulose, xanthan gum, gum arabic, Silica powder, gaur gum, carbomer, chitosan, precipitated silica or mixtures thereof Emulsifier(s)- Emulsifier(s)- Non-ionic emulsifiers- Araliphatic or aliphatic non-ionic oil emulsifier - ethoxylated sorbitol hexaester (derived from oleic acid), Ethoxylated mono-, di- and trialkylphenols, Ethoxylates of long-chain alcohols, Polyethylene oxide / polypropylene 0.01-20 oxide homo- and copolymers, EO / PO block copolymers, 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,
[0225]
[0226] Tristyrylphenol ethoxylate, Ethoxylated Tristyrylphenol or a mixture thereof.
[0227] Ionic emulsifiers including but not limited to 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.
[0228] Or a mixture of ionic or non-ionic.
[0229] 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),
[0230] 1.0-20 Dimethylformamide (DMF), N- alcohol, 2-ethyl hexanol, alkyl amide, vegetable oil, mineral oil, distilled water, aromatic solvents, water or mixtures thereof
[0231] 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
[0232] , pigment red 53:1, pigment orange 43, pigment orange 34, pigment 0.01-10 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
[0233] 52, acid red 14, acid blue 9, acid yellow 23, basic red 10, basic red 108 or mixtures thereof
[0234] Polymer(s)- isocyanate, polyisocyanate used is toluene -2, 4-diisocyanate (TDI), diethylenetriamine (DETA), ethylene diamine (EDA), triethylenetetramine (TETA), and / or hexamethylene diamine (HMDA),
[0235] 0.01-5.0 diethanolglycine sodium salt, ethanoldiglycine disodium salt, hydroxymonocarboxylic acid compounds, hydroxydicarboxylic acid compounds, tetrasodium N, N-bis(carboxylatomethyl)-L-glutamate
[0236]
[0237] (GLDA), methylene diisocyanate (MDI), and / or low molecular weight polydiisocynates or mixtures thereof
[0238] Binder(s)- polyvinylpyrrolidone, polyvinyl alcohol, methyl cellulose, and carboxymethyl cellulose, polyisocyanate, polyterpene resin or 0.01-40 % mixtures thereof
[0239] Preservative(s)- Methyl paraben (Methyl p-hydroxybenzoate), Propyl paraben (Propyl p-hydroxybenzoate), Methylisothiazolinone (MIT), Chloromethylisothiazolinone (CMIT), Benzisothiazolinone (BIT), DMDM Hydantoin, Imidazolidinyl Urea, Phenol, Cresol, Chlorocresol, 0.01-35% Benzoic acid, Sorbic acid, Salicylic acid, Thymol (natural preservative), Sodium benzoate, Potassium sorbate, Bronopol (2-bromo-2- nitropropane-1,3-diol), Propyl para-hydroxy -benzoate or mixture thereof 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
[0240] UV absorber), Hindered Amine Light Stabilizers (HALS), Oxanilide derivatives, Ethoxylated Alkylphenols (e.g., nonylphenol ethoxylates), Block copolymers (e.g., Pluronic® types), Polyvinyl alcohol (PVA),
[0241] 0.01-35% 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
[0242] (dual role: pH and chelation), NTA (Nitrilotriacetic acid), Xanthan gum, Attapulgite clay, Bentonite, Hydroxypropyl methylcellulose (HPMC) or mixture thereof
[0243] 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 0.01-25% Phosphate (Monobasic or Dibasic), Potassium Phosphate (Monobasic / Dibasic), Sodium Bicarbonate, Sodium Carbonate, Ammonium Acetate
[0244]
[0245] / Ammonium Hydroxide, Acetic Acid, Sodium Acetate, Borax (Sodium
[0246] Borate) or mixture thereof
[0247] 22 Distilled water / China Clay / DMF QS Total 100
[0248]
[0249] Example A: Compound of Formula I Technical 12.5% + Hexythiazox Technical 2% + Dinotefuran Technical 9.5% SC
[0250] Sr. No. Ingredients Concentration % w / w)
[0251] 1 Compound of Formula I Technical 12.5%
[0252] 2 Hexythiazox Technical 2%
[0253] 3 Dinotefuran Technical 9.5%
[0254] 4 Acrylic graft copolymer 5.0%
[0255] 5 Epoxide Soybean Oil 0.5%
[0256] 6 Propylene Glycol 5%
[0257] 7 Ethoxylated Fatty Alcohol 2.0%
[0258] Polyalkyleneoxide-modified
[0259] 8
[0260] Polydimethylsiloxane 1.0%
[0261] 9 1,2-Benzisothiazolin-3-one 0.1%
[0262] 10 Xanthan gum 0.2%
[0263] 11 Distilled Water Q. S. to make 100%
[0264] Total 100.0
[0265]
[0266] FORMULATION PROCESS
[0267] DM water and mixture of surfactants (Acrylic graft copolymer, Ethoxylated Fatty Alcohol), Epoxide Soybean Oil, Polyalkyleneoxide-modified Polydimethylsiloxane emulsion & Propylene Glycol (PG) were charged and further diluted with DM water. Then required Compound of Formula I Technical, Hexythiazox Technical, and Dinotefuran Technical were mixed to obtain homogeneous mass at high shearing stirring.
[0268] Obtained homogeneous mass was ground in Bead Mill. Grinding is carried out until a mean particle size of below 5 microns is obtained.
[0269] Preparations of 2% gum solution - Take 100 g DM water add 0.2 g of 1,2- Benzisothiazolin-3-one, then xanthan gum is added with gradual stirring.
[0270] After grinding, 2% aqueous solution of xanthan gum was added with stirring. Mixing is carried out to obtain final homogenous mixture.
[0271] Obtained homogeneous mixture was checked for quality parameter.
[0272] STABILITY DATA: Compound of Formula I Technical 12.5% + Hexythiazox 2% + Dinotefuran 9.5% SC
[0273] Sr. No Test Parameter Specification Observation HST at 54 Cold Test °C 14 days at 0°C 7days
[0274] 1 Description White to off Complies Complies Complies white coloured
[0275] suspension liquid
[0276] 2 Compound of 12.5% (±5%) 12.78 12.54 12.18 Formula I
[0277] Technical (%w / w)
[0278] 3 Hexythiazox 2% (+10, -5%) 2.22 2.25 2.27 technical (% w / w))
[0279] 4 Dinotefuran 9.5% (±5%) 9.64 9.67 9.71 Technical (%
[0280] w / w)
[0281] 5 Suspensibility of Min 80% 92.23 92.72 92.21 Compound of
[0282] Formula I (% w / w)
[0283]
[0284] Suspensibility of Min 80% 92.32 92.56 92.31 Hexythiazox
[0285] technical (% w / w)
[0286] Suspensibility of Min 80% 92.18 92.84 92.54 Dinotefuran
[0287] Technical (% w / w)
[0288] Spontaneity of Min 80% 91.23 91.58 90.22 dispersion
[0289] Compound of
[0290] Formula I %w / w
[0291] Spontaneity of Min 80% 91.31 91.53 91.29 dispersion
[0292] Hexythiazox
[0293] Technical %w / w
[0294] Spontaneity of Min 80% 91.57 91.84 91.54 dispersion
[0295] Dinotefuran
[0296] Technical %w / w
[0297] pH 1.0% Aqueous 5.0 to 8.0 6.36 6.53 6.64 Solution
[0298] Viscosity @25°C 350 to 700 450 452 456 Spindle 63 60 rpm
[0299] (CPS)
[0300] Wet Sieve, Min 98 % 99.13 99.23 99.25 material passing
[0301] through 45 micron
[0302] sieve
[0303] Persistent foam 80ml Max 17 13 14 after 1min (ml)
[0304] Pourability (Rinse Max 2.0 0.39 0.41 0.42 residue)
[0305]
[0306] Example B: Compound of Formula I 24% + Hexythiazox 1.5%+ Dinotefuran 4.5% WP Sr. No. Ingredients % W / W
[0307] 1 Compound of Formula I Technical 24%
[0308] 2 Hexythiazox Technical 1.5%
[0309] 3 Dinotefuran Technical 4.5%
[0310] 4 Sodium alkyl naphthalene sulfonate blend 5.0%
[0311] 5 Sodium lauryl sulphonate / Alpha olefin sulphonate 3.0%
[0312] 6 Silica ppt 2.0%
[0313] 7 China clay Q. S. to make 100 TOTAL 100.0
[0314]
[0315] FORMULATION PROCESS:
[0316] All required Technicals.i.e. Compound of Formula I Technical, Hexythiazox Technical and Dinotefuran Technical and inert ingredients were mixed and then ground in air jet mill. Particle size was checked after grounding, to ensure that it is less than 10 microns(D90). Post blends the ground powder and then it was mixed well.
[0317] Stability Data: Compound of Formula I 24% + Hexythiazox 1.5%+ Dinotefuran 4.5% WP Sr. Test Parameter Specification Observation at HST at 54 °C No. Room 14 days
[0318] Temperature
[0319]
[0320] Appearance White to off white Complies Complies powder
[0321] Active Content 24% (±5%) 24.35 24.36 Compound of Formula I,
[0322] %w / w
[0323] Active Content 1.5% (+10, -5%) 1.51 1.56 Hexythiazox, %w / w
[0324] Active Content 4.5% (+10, -5%) 4.58 4.61 Dinotefuran, %w / w
[0325] Suspensibility Min 80% 92.12 92.18 Compound of Formula I
[0326] %w / w
[0327] Suspensibility Min 80% 92.16 92.67 Hexythiazox, %w / w
[0328] Suspensibility Min 80% 92.24 92.58 Dinotefuran %w / w
[0329] Persistant Foaming, mL Max. 60 after 1 11 14 (1% solution in 342 ppm minute
[0330] hard water)
[0331] Wet Sieve, material Min 98 % 98.82 98.72 passing through 45
[0332] micron sieve
[0333] pH of 1% aqueous 5.0 to 8.0 6.56 6.63 emulsion
[0334] Wettability 120 max 60 70
[0335]
[0336] EXAMPLE C: Compound of Formula I 7.5 % + Hexythiazox 0.1%+ Dinotefuran 18% EC Sr. No. Ingredients % W / W
[0337] 1 Compound of Formula I Technical 7.5 %
[0338] 2 Hexythiazox Technical 0.1%
[0339] 3 Dinotefuran Technical 18%
[0340] 4 Emulsifier (Blend of Anionic and Non-ionic) 15.00
[0341] 5 N-Methyl-2-pyrrolidone (NMP) Q. S.
[0342] TOTAL 100.00
[0343]
[0344] FORMULATION PROCESS
[0345] 1. Into a clean and dry reactor, solvent N-Methyl-2-pyrrolidone was charged and stirring was started.
[0346] 2. Compound of Formula I Technical, Hexythiazox Technical, and Dinotefuran Technical were added, mixed well, and dissolved to obtain a clear solution.
[0347] 3. Emulsifier (blend of anionic and non-ionic) was added and mixed well to form an emulsifiable concentrate.
[0348] 4. The solution was filtered through a sparkler filter, and the filtrate was collected into another clean and dry vessel.
[0349] 5. The formulation was packed in QA-approved containers.
[0350] STABILITY DATA: Compound of Formula I 7.5 % + Hexythiazox 0.1%+ Dinotefuran 18% EC
[0351] Sr. Test Parameter Specification Observatio HST at 54 Cold Test N n °C at
[0352] O 14 days 0°C 7
[0353] days
[0354] 1. Yellowish to slightly
[0355] Appearance brown coloured clear Complies Complies Complies liquid
[0356] 2. Active Content 7.67 7.72 7.69 Compound of 7.5 % (+10%, -5%)
[0357] Formula I
[0358] 3. Active Content 0.11 0.105 0.11
[0359] 0.1 % (+10%, -5%)
[0360] Hexythiazox
[0361] 4. Active Content of 18% (±5%) 18.27 18.35 18.51 Dinotefuran
[0362] 5. Persistent
[0363] Max. 60 16 14 12 Foaming, mL
[0364] 6. pH of 1 % aqueous
[0365] 5.0-8.0 6.75 6.71 6.68
[0366]
[0367] emulsion 8. Flash Point, °C
[0368] Above 24.5°C 47°C 48°C 49°C (Closed cup Abel)
[0369] 9. Emulsion stability Emulsion stability and
[0370] re-emulsification
[0371] 0 h Initial
[0372] emulsification complete
[0373] 5 h " Cream",
[0374] maximum: 0.2
[0375] ml
[0376] Complies Complies Complies 2.0 h " Cream",
[0377] maximum: 2ml 'Oil’,
[0378] maximum: trace
[0379] 24 h Reemulsification complete
[0380] 24.5 h " Cream",
[0381] maximum: 2 ml "oil",
[0382]
[0383] maximum: trace
[0384] Evaluation of synergistic effect of pesticidal composition of the present invention
[0385] 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).
[0386] The synergistic action expected for a given combination of two active components can be calculated as follows:
[0387] XY
[0388] E = (X + Y) - - 100
[0389] The synergistic action expected for a given combination of three active components can be calculated as follows:
[0390] (XY+YZ+XZ) (XYZ)
[0391] E = (X + Y + Z) - + - 100 10000
[0392] Where: 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).
[0393] X is the percentage of pesticidal control observed by the compound (Compound of Formula I) at a defined dose (equal to x).
[0394] Y is the percentage of pesticidal control observed by the compound (Hexythiazox) at a defined dose (equal to y).
[0395] Z is the percentage of pesticidal control observed by the compound (Dinotefuran) at a defined dose (equal to z).
[0396] When the percentage of pesticidal control observed for the combination is greater than the expected percentage, there is a synergism effect.
[0397] Observed control (%)
[0398] Ratio = - Expected control (%)
[0399] Ratio of O / E > 1, synergism observed
[0400] The present invention is illustrated by way of examples, the examples are meant for illustrative purposes and should not be construed as limiting.
[0401] Experiment for Synergistic activity of stable synergistic composition of present invention: Example 1- Details of experiment on brinjal crop:
[0402] Field experiment for synergistic activity of Compound of Formula I + Hexythiazox + Dinotefuran for the control of mite and jassids in brinjal crop was conducted.
[0403] To evaluate the synergistic effect, brinjal [Variety: Pusa Hybrid 5] crop was sown in 5 m x 5 m plots maintaining 75 cm x 45 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 @ 625 ml / ha. Each active component was applied twice in different ternary and binary combinations. Solo components were also taken for comparison. The treatment details are as under:
[0404] S. No. Treatment Concentration % (SC)
[0405]
[0406] T1 Compound of Formula I + Hexythiazox + Dinotefuran 1% + 5% + 1%
[0407] T2 Compound of Formula I + Hexythiazox + Dinotefuran 24% + 1.5% + 4.5% T3 Compound of Formula I + Hexythiazox + Dinotefuran 12.5% + 2% + 9.5% T4 Compound of Formula I + Hexythiazox + Dinotefuran 7.5% + 0.1% + 18% T5 Compound of Formula I + Hexythiazox 1% + 5%
[0408] T6 Compound of Formula I + Hexythiazox 24% + 1.5%
[0409] T7 Compound of Formula I + Hexythiazox 12.5% + 2%
[0410] T8 Compound of Formula I + Hexythiazox 7.5% + 0.1%
[0411] T9 Compound of Formula I + Dinotefuran 1% + 1%
[0412] T10 Compound of Formula I + Dinotefuran 24% + 4.5%
[0413] Til Compound of Formula I + Dinotefuran 12.5% + 9.5%
[0414] T12 Compound of Formula I + Dinotefuran 7.5% + 18%
[0415] T13 Hexythiazox + Dinotefuran 5% + 1%
[0416] T14 Hexythiazox + Dinotefuran 1.5% + 4.5%
[0417] T15 Hexythiazox + Dinotefuran 2% + 9.5%
[0418] T16 Hexythiazox + Dinotefuran 0.1% + 18%
[0419] T17 Compound of Formula I 1%
[0420] T18 Compound of Formula I 24%
[0421] T19 Compound of Formula I 12.5%
[0422] T20 Compound of Formula I 7.5%
[0423] T21 Hexythiazox 5.0%
[0424] T22 Hexythiazox 1.5%
[0425] T23 Hexythiazox 2.0%
[0426] T24 Hexythiazox 0.1%
[0427] T25 Dinotefuran 1.0%
[0428] T26 Dinotefuran 4.5%
[0429] T27 Dinotefuran 9.5%
[0430] T28 Dinotefuran 18%
[0431]
[0432] T29 Untreated -
[0433] 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 pests (Red spider mites and Jassids).
[0434] Observations of Tetranychus urticae (red spider mite) were recorded before spraying and at 14 days after the first and second applications. From each plot, five randomly selected brinjal plants were chosen, and three leaves from different canopy levels (top, middle and lower) were collected per plant. Mites (Red spider mites) on these leaves were counted using a hand lens and the average number of mites per plant was calculated. Observations of Amrasca biguttida biguttula (Jassids) were recorded before spraying and at 14 days after the first and second applications. Randomly selected 5-10 brinjal plants per plot and observed the top three fully opened leaves on each plant. The number of jassids (nymphs and adults) present on these leaves were count using the naked eye or a hand lens and the average number of jassids per plant was calculated. Based on the per cent reduction at 14 days after second spray in pest population, expected control was calculated and compared with observed control. The results of the trial have been presented here under in Table 1A.
[0435] Table 1A: Synergistic effect of stable synergistic pesticidal composition of the present invention (Compound of Formula I + Hexythiazox + Dinotefuran) against pest population mite and jassids in brinjal crop
[0436] Arthropod pests
[0437] S. N Concentration Colby Treatment
[0438] 0. (SC) Observe
[0439] Expected ratio d
[0440] Compound of Formula I + Hexythiazox + l% + 5% + 1% 64.12 42.6 1.51 T1 Dinotefuran
[0441] Compound of Formula I + Hexythiazox + 24% + 1.5% + 81.24 50.4 1.61 T2 Dinotefuran 4.5%
[0442] Compound of Formula I + Hexythiazox + 12.5% + 2% + 87.25 53.7 1.63 T3 Dinotefuran 9.5%
[0443] Compound of Formula I + Hexythiazox + 7.5% + 0.1% + 73.13 46.52 1.57 T4 Dinotefuran 18%
[0444] T5 Compound of Formula I + Hexythiazox l% + 5% 23.04 35.16 0.66 T6 Compound of Formula I + Hexythiazox 24% + 1.5% 37.01 40.65 0.91 T7 Compound of Formula I + Hexythiazox 12.5% + 2% 37.22 39.77 0.93 T8 Compound of Formula I + Hexythiazox 7.5% + 0.1% 23.78 26.6 0.89 T9 Compound of Formula I + Dinotefuran 1% + 1% 19.23 22.3 0.86 T10 Compound of Formula I + Dinotefuran 24% + 4.5% 38.32 40.77 0.94 T11 Compound of Formula I + Dinotefuran 12.5% + 9.5% 40.13 41.14 0.97 T12 Compound of Formula I + Dinotefuran 7.5% + 18% 36.13 39.84 0.91 T13 Hexythiazox + Dinotefuran 5% + 1% 27.12 34.6 0.78 T14 Hexythiazox + Dinotefuran 1.5% + 4.5% 27.14 30.01 0.90 T15 Hexythiazox + Dinotefuran 2% + 9.5% 38.12 39.53 0.96 T16 Hexythiazox + Dinotefuran 0.1% + 18% 33.01 35.23 0.93 T17 Compound of Formula I 1% 12.23 - - T18 Compound of Formula I 24% 29.13 - - T19 Compound of Formula I 12.5% 23.43 - - T20 Compound of Formula I 7.5% 17.43 - - Hexythiazox
[0445]
[0446] T21 5.0% 26.13 - - T22 Hexythiazox 1.5% 16.25 - - T23 Hexythiazox 2.0% 21.34 - - T24 Hexythiazox 0.1% 11.11 - - T25 Dinotefuran 1.0% 11.47 - - T26 Dinotefuran 4.5% 16.43 - - T27 Dinotefuran 9.5% 23.13 - - T28 Dinotefuran 18% 27.14 - - T29 Untreated - - - -
[0447]
[0448] 9
[0449] It is clearly evident from the data shown in above Table 1 A for percent pest control in brinjal crop that the stable synergistic pesticidal composition of the present invention comprising Compound of Formula I + Hexythiazox + Dinotefuran i.e. T1 to T4 are synergistic for pest population with > 1 Colby’s Ratio. The binary combination of two acaricide / insecticide (Compound of Formula I + Hexythiazox, Compound of Formula I + Dinotefuran and Hexythiazox + Dinotefuran) T5 to T16 is less efficacious and no synergistic effect is shown for the control of pest population, as compared to stable synergistic pesticidal composition of Compound of Formula I + Hexythiazox + Dinotefuran T1 to T4. The synergy data presented herein represent the cumulative efficacy against both pests (mites and jassids).
[0450] Experiment for Bio-efficacy evaluation of stable synergistic pesticidal composition of present invention:
[0451] For the ternary and binary compositions based on Compound of Formula I + Hexythiazox + Dinotefuran evaluation under field conditions, the basic test composition as Compound of Formula I 12.5% + Hexythiazox 2% + Dinotefuran 9.5% SC were manufactured. For stable synergistic pesticidal composition of present invention, Compound of Formula I 12.5% + Hexythiazox 2% + Dinotefuran 9.5% SC was used and for binary compositions, Compound of Formula I 12.5% + Hexythiazox 2% SC, Compound of Formula I 8% + Dinotefuran 9.5% SC and Hexythiazox 4% + Dinotefuran 9.5% SC were used. The solo formulations of Compound of Formula I 12.5% SC, Hexythiazox 2% SC and Dinotefuran 9.5% SC were used for comparison. The other formulations namely Compound of Formula I 20 % w / w WP, Hexythiazox 05.45 % w / w EC and Dinotefuran 70% WG available in the market were also used for comparison. Example 2: Evaluation of the stable synergistic pesticidal composition of the present invention on Brinjal
[0452] The synergistic composition of the present invention comprising Compound of Formula I 12.5% + Hexythiazox 2% + Dinotefuran 9.5% SC was evaluated on brinjal crop variety Pusa Hybrid 5 at a farmer field. The crop sowing was done in Randomized Block Design (RBD) with three replications maintaining a distance of 75 cm x 45 cm. The observations were recorded for the following objectives.
[0453] Objectives:
[0454] 1. Bio-efficacy evaluation against red spider mite on Brinjal crop.
[0455] 2. Bio-efficacy evaluation against jassids on Brinjal crop.
[0456] 3. Bio-efficacy evaluation based on per cent reduction in red spider mite population.
[0457] 4. Bio-efficacy evaluation based on percent reduction in jassids population.
[0458] 5. Bio-efficacy evaluation based on crop yield of Brinjal.
[0459] 6. Phytotoxicity evaluation on Brinjal crop.
[0460] Treatment details:
[0461] Formul ation S. N a.i. dose Treatment (SC) dose (g 0. (g / ha)
[0462] or ml / ha) Compound of Formula 1 12.5% + Hexythiazox 2% + Dinotefuran 58.59 + 9.37 +
[0463] T1 468.75 9.5% SC 44.53 Compound of Formula 1 12.5% + Hexythiazox 2% + Dinotefuran 78.12 + 12.5 +
[0464] T2 625 9.5% SC 59.37 Compound of Formula 1 12.5% + Hexythiazox 2% + Dinotefuran 97.65 + 15.62
[0465] T3 781.25 9.5% SC + 74.21
[0466] T4 Compound of Formula 1 12.5% + Hexythiazox 2% SC 58.59 + 9.37 468.75 T5 Compound of Formula 1 12.5% + Hexythiazox 2% SC 78.12 + 12.5 625 T6 Compound of Formula 1 12.5% + Hexythiazox 2% SC 97.65 + 15.62 781.25 T7 Compound of Formula 1 12.5% + Dinotefuran 9.5% SC 58.59 + 44.53 468.75 T8 Compound of Formula 1 12.5% + Dinotefuran 9.5% SC 78.12 + 59.37 625 T9 Compound of Formula 1 12.5% + Dinotefuran 9.5% SC 97.65 + 74.21 781.25 T1
[0467] 9.37 + 44.53 Hexythiazox 2% + Dinotefuran 9.5% SC 468.75 0
[0468] T1
[0469] 12.5 + 59.37
[0470] 1 Hexythiazox 2% + Dinotefuran 9.5% SC 625
[0471]
[0472] T1
[0473] 15.62 + 74.21 781.25 2 Hexythiazox 2% + Dinotefuran 9.5% SC
[0474] T1
[0475] 78.12 625 3 Compound of Formula 1 12.5% SC
[0476] T1
[0477] 4 Hexythiazox 2% SC 12.5 625 T1
[0478] 59.37
[0479] 5 Dinotefuran 9.5% SC 625 T1
[0480] 6 Compound of Formula 120 % w / w WP 100 500 T1
[0481] 7 25 500 Hexythiazox 05.45 % w / w EC
[0482] T1
[0483] 61.2 87 8 Dinotefuran 70 % WG
[0484] T1
[0485] 9 Untreated
[0486] T2 Compound of Formula 1 12.5% + Hexythiazox 2% + Dinotefuran 156.25+ 25 +
[0487] 1250
[0488]
[0489] 0 9.5% (for phytotoxicity analysis) 118.75
[0490] Methodology:
[0491] 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 when the pest population reached the economic threshold level in the experimental plots.
[0492] Observations of Tetranychus urticae (red spider mite) were recorded before spraying and at 14 days after the first and second applications. From each plot, five randomly selected brinjal plants were chosen, and three leaves from different canopy levels (top, middle and lower) were collected per plant. Mites on these leaves were counted using a hand lens and the average number of mites per plant was calculated. Observations of Amrasca biguttida biguttida (Jassids) were recorded before spraying and at 14 days after the first and second applications. 5-10 brinjal plants per plot were randomly selected and the top three fully opened leaves on each plant were observed. The number of jassids (nymphs and adults) present on these leaves were counted using the naked eye or a hand lens and the average number of jassids per plant was calculated. The per cent reduction in pest population was also calculated over control. The crop yield was recorded at crop harvest. The observations for phytotoxicity on Brinjal crop at 1, 3, 7, 10 and 14 days after 1stspray were also recorded. The data were subjected to statistical analysis of variance. Results are presented in Table 2A, 2B, 2C and 2D.
[0493] Results: Table 2A: Field bio-efficacy evaluation of stable synergistic composition of present invention comprising Compound of Formula 112.5% + Hexythiazox 2% + Dinotefuran 9.5% SC against red spider mite (Tetranychus urticae of brinjal crop.
[0494] S. No Treatments a.i. dose Form Red spider mite / Per cent (g / ha) ulatio plant reduction over n dose control
[0495] (g or
[0496] ml / ha) Befo 14 14 14 14
[0497] re days days days days spra after after after I after y I II spray II spra spray spray y
[0498] T1 Compound of Formula I 58.59 + 468.75 5.01 4.79 1.93 46.66 84.4
[0499] 12.5% + Hexythiazox 9.37 + (2.35 (2-3) (1.56)
[0500] 2% + Dinotefuran 9.5% 44.53 )
[0501] SC
[0502] T2 Compound of Formula I 78.12 + 625 5.34 4.5 1.72 49.89 86.1
[0503] 12.5% + Hexythiazox 12.5 + (2.42 (2.24 (1-49)
[0504] 2% + Dinotefuran 9.5% 59.37 ) )
[0505] SC
[0506] T3 Compound of Formula I 97.65 + 781.25 5.22 4.39 1.59 51.11 87.15 12.5% + Hexythiazox 15.62 + (2.39 (2.21 (1-45)
[0507] 2% + Dinotefuran 9.5% 74.21 ) )
[0508] SC
[0509] T4 Compound of Formula I 58.59 + 468.75 4.96 6.8 7.55 24.28 38.97 12.5% + Hexythiazox 9.37 (2.34 (2-7) (2.84)
[0510] 2% SC )
[0511] T5 Compound of Formula I 78.12 + 625 5.2 6.65 7.37 25.95 40.42 12.5% + Hexythiazox 12.5 (2.39 (2.67 (2-81)
[0512] 2% SC ) )
[0513] T6 Compound of Formula I 97.65 + 781.25 5.54 6.58 7.29 26.73 41.07 12.5% + Hexythiazox 15.62 (2.46 (2.66 (2.79)
[0514] 2% SC ) )
[0515] T7 Compound of Formula I 58.59 + 468.75 5.57 7.1 7.99 20.94 35.41 12.5% + Dinotefuran 44.53 (2.46 (2.76 (2-91)
[0516] 9.5% SC ) )
[0517] T8 Compound of Formula I 78.12 + 625 5.37 6.96 7.85 22.49 36.54 12.5% + Dinotefuran 59.37 (2.42 (2.73 (2.89)
[0518] 9.5% SC ) )
[0519] T9 Compound of Formula I 97.65 + 781.25 5.65 6.91 7.79 23.05 37.03 12.5% + Dinotefuran 74.21 (2.48 (2.72 (2.88)
[0520] 9.5% SC ) )
[0521] T10 9.37 + 468.75 5.43 7.29 8.25 18.82 33.31 Hexythiazox 2% + 44.53 (2.44 (2.79 (2-96)
[0522]
[0523] Dinotefuran 9.5% SC ) ) T11 12.5 + 625 5.57 7.18 8.12 20.04 34.36 Hexythiazox 2% + 59.37 (2.46 (2.77 (2.94)
[0524] Dinotefuran 9.5% SC ) )
[0525] T12 15.62 + 781.25 5.73 7.11 8.1 20.82 34.52 Hexythiazox 2% + 74.21 (2-5) (2.76 (2.93)
[0526] Dinotefuran 9.5% SC )
[0527] T13 78.12 625 4.89 7.86 9.93 12.47 19.73 Compound of Formula I (2.32 (2.89 (3.23)
[0528] 12.5% SC ) )
[0529] T14 12.5 625 5.13( 8.01 10.35 10.8 16.33
[0530] 2.37) (2.92 (3.29)
[0531] Hexythiazox 2% SC )
[0532] T15 59.37 625 5.2 8.32 10.83 7.35 12.45 (2.39 (2.97 (3.37)
[0533] Dinotefuran 9.5% SC ) )
[0534] T16 Compound of Formula I 100 500 5.7 7.72 9.66 14.03 21.91 20 % w / w WP (2.49 (2.87 (3-19)
[0535] ) )
[0536] T17 Hexythiazox 05.45 % 25 500 5.58 7.89 10.14 12.14 18.03 w / w EC (2.47 (2-9) (3.26)
[0537] )
[0538] T18 Dinotefuran 70 % WG 61.2 87 5.06 8.26 10.7 8.02 13.5
[0539] (2.36 (2.96 (3.35)
[0540] ) )
[0541] T19 Untreated - 5.75 8.98 12.37 - - (2-5) (3.08 (3.59)
[0542] )
[0543] CD (p=0.05) NS 0.05 0.06
[0544]
[0545] SE(m) 0.02 0.02
[0546] Figures in parentheses are square root transformed values; NS= Non-significant
[0547] Table 2B: Field bio-efficacy evaluation of stable synergistic composition of present invention comprising Compound of Formula 112.5% + Hexythiazox 2% + Dinotefuran 9.5% SC against jassids (Amrasca biguttula biguttula) of brinjal crop.
[0548] S. N Treatments a.i. dose Form Jassids / plant Per cent
[0549] 0 (g / ha) ulatio reduction over n dose control
[0550] (g or
[0551] ml / ha) Befo 14 14 14 14
[0552] re days days days days spra after after after I after y I II spray II spra spray spray y
[0553] T1 Compound of Formula I 58.59 + 468.75 4.01 3.37 1.73 49.55 82
[0554] 12.5% + Hexythiazox 2% 9.37 + (2.12 (1.97 (1-49)
[0555]
[0556] + Dinotefuran 9.5% SC 44.53 ) ) T2 Compound of Formula I 78.12 + 625 4.14 3.23 1.44 51.65 85.02 12.5% + Hexythiazox 2% 12.5 + (2.15 (1.93 (1-39)
[0557] + Dinotefuran 9.5% SC 59.37 ) )
[0558] T3 Compound of Formula I 97.65 + 781.25 4 3.16 1.22 52.69 87.3 12.5% + Hexythiazox 2% 15.62 + (2.12 (1.91 (1-31)
[0559] + Dinotefuran 9.5% SC 74.21 ) )
[0560] T4 Compound of Formula I 58.59 + 468.75 4.43 5.53 7 17.22 27.16 12.5% + Hexythiazox 2% 9.37 (2.22 (2.46 (2.74)
[0561] SC ) )
[0562] T5 Compound of Formula I 78.12 + 625 5.19 5.4 6.78 19.16 29.45 12.5% + Hexythiazox 2% 12.5 (2.39 (2.43 (2.7)
[0563] SC ) )
[0564] T6 Compound of Formula I 97.65 + 781.25 4.78 5.37 6.71 19.61 30.18 12.5% + Hexythiazox 2% 15.62 (2-3) (2.42 (2-69)
[0565] SC )
[0566] T7 Compound of Formula I 58.59 + 468.75 4.42 5.21 6.27 22.01 34.76 12.5% + Dinotefuran 9.5% 44.53 (2.22 (2.39 (2-6)
[0567] SC ) )
[0568] T8 Compound of Formula I 78.12 + 625 5.24 5.07 6.07 24.1 36.84 12.5% + Dinotefuran 9.5% 59.37 (2-4) (2.36 (2.56)
[0569] SC )
[0570] T9 Compound of Formula I 97.65 + 781.25 4.39 4.99 5.78 25.3 39.85 12.5% + Dinotefuran 9.5% 74.21 (2.21 (2.34 (2-51)
[0571] SC ) )
[0572] T10 9.37 + 468.75 3.71 5.32 6.55 20.36 31.84 Hexythiazox 2% + 44.53 (2.05 (2.41 (2.66) Dinotefuran 9.5% SC ) )
[0573] T11 12.5 + 625 4.23 5.14 6.33 23.05 34.13 Hexythiazox 2% + 59.37 (2.17 (2.37 (2-61) Dinotefuran 9.5% SC ) )
[0574] T12 15.62 + 781.25 3.66 5.05 6.23 24.4 35.17 Hexythiazox 2% + 74.21 (2.04 (2.36 (2-59) Dinotefuran 9.5% SC ) )
[0575] T13 78.12 625 3.67 6.11 8.11 8.53 15.61 Compound of Formula I (2.04 (2.57 (2.93)
[0576] 12.5% SC ) )
[0577] T14 12.5 625 4.61 6.27 8.36 6.14 13.01
[0578] (2.26 (2.6) (2.98) Hexythiazox 2% SC )
[0579] T15 59.37 625 4.55 5.91 7.75 11.53 19.35
[0580] (2.25 (2.53 (2.87) Dinotefuran 9.5% SC ) )
[0581] T16 Compound of Formula I 20 100 500 4 6.02 7.91 9.88 17.69 % w / w WP (2.12 (2.55 (2-9)
[0582] ) )
[0583] T17 Hexythiazox 05.45 % w / w 25 500 3.78 6.15 8.25 7.93 14.15 EC (2.07 (2.58 (2-96)
[0584] ) )
[0585] T18 Dinotefuran 70 % WG 61.2 87 3.67 5.82 7.62 12.87 20.71
[0586]
[0587] (2.85) (2.04 (2.51
[0588] ) )
[0589] T19 Untreated - 3.97 6.68 9.61 - - (2.11 (2.68 (3.18)
[0590] ) )
[0591] CD (p=0.05) NS 0.03 0.09
[0592]
[0593] SE(m) 0.01 0.03
[0594] Figures in parentheses are square root transformed values; NS= Non-significant
[0595] Table 2C: Field bio-efficacy evaluation of stable synergistic composition of present invention comprising Compound of Formula 112.5% + Hexythiazox 2% + Dinotefuran 9.5% SC based on fruit yield of brinjal crop.
[0596] S. N Treatments a.i. dose (g / ha) Formul Fruit % 0 ation Yield Increas dose (g Q / ha) e or against ml / ha) control T1 Compound of Formula 1 12.5% + 58.59 + 9.37 + 468.75 44.5 45.42 Hexythiazox 2% + Dinotefuran 9.5% SC 44.53
[0597] T2 Compound of Formula 1 12.5% + 78.12 + 12.5 + 625 45.39 48.33 Hexythiazox 2% + Dinotefuran 9.5% SC 59.37
[0598] T3 Compound of Formula 1 12.5% + 97.65 + 15.62 781.25 45.96 50.2 Hexythiazox 2% + Dinotefuran 9.5% SC + 74.21
[0599] T4 Compound of Formula 1 12.5% + 58.59 + 9.37 468.75 36.68 19.87 Hexythiazox 2% SC
[0600] T5 Compound of Formula 1 12.5% + 78.12 + 12.5 625 37.34 22.03 Hexythiazox 2% SC
[0601] T6 Compound of Formula 1 12.5% + 97.65 + 15.62 781.25 37.82 23.59 Hexythiazox 2% SC
[0602] T7 Compound of Formula 1 12.5% + 58.59 + 44.53 468.75 38.21 24.87 Dinotefuran 9.5% SC
[0603] T8 Compound of Formula 1 12.5% + 78.12 + 59.37 625 38.83 26.9 Dinotefuran 9.5% SC
[0604] T9 Compound of Formula 1 12.5% + 97.65 + 74.21 781.25 39.28 28.37 Dinotefuran 9.5% SC
[0605] T10 Hexythiazox 2% + Dinotefuran 9.5% SC 9.37 + 44.53 468.75 37.98 24.12 T11 Hexythiazox 2% + Dinotefuran 9.5% SC 12.5 + 59.37 625 38.53 25.92 T12 Hexythiazox 2% + Dinotefuran 9.5% SC 15.62 + 74.21 781.25 38.68 26.41 T13 Compound of Formula 1 12.5% SC 78.12 625 33.15 8.33 T14 Hexythiazox 2% SC 12.5 625 32.79 7.16 T15 Dinotefuran 9.5% SC 59.37 625 32.37 5.78 T16 Compound of Formula 120 % w / w WP 100 500 34.01 11.14 T17 Hexythiazox 05.45 % w / w EC 25 500 33.72 10.2 T18 Dinotefuran 70 % WG 61.2 87 33.6 9.8 T19 Untreated -
[0606]
[0607] 30.6 CD (p=0.05) 0.68
[0608]
[0609] SE(m) 0.23
[0610] Table 2D: Field bio-efficacy evaluation of stable synergistic composition of present invention comprising Compound of Formula I 12.5% + Hexythiazox 2% + Dinotefuran 9.5% SC on brinjal crop.
[0611] S. No Treatments a.i. dose Formu Phyto-toxicity parameters (g / ha) lation observed*
[0612] dose (g (mean data recorded at 1, 3, 7, or 10 and 14 days after 1st spray) ml / ha)
[0613] L w N V E H T1 Compound of Formula 1 12.5% + 58.59 + 9.37 468.75 0 0 0 0 0 0 Hexythiazox 2% + Dinotefuran + 44.53
[0614] 9.5% SC
[0615] T2 Compound of Formula 1 12.5% + 78.12 + 12.5 625 0 0 0 0 0 0 Hexythiazox 2% + Dinotefuran + 59.37
[0616] 9.5% SC
[0617] T3 Compound of Formula 1 12.5% + 97.65 + 15.62 781.25 0 0 0 0 0 0 Hexythiazox 2% + Dinotefuran + 74.21
[0618] 9.5% SC
[0619] T4 Compound of Formula 1 12.5% + 58.59 + 9.37 468.75 0 0 0 0 0 0 Hexythiazox 2% SC
[0620] T5 Compound of Formula 1 12.5% + 78.12 + 12.5 625 0 0 0 0 0 0 Hexythiazox 2% SC
[0621] T6 Compound of Formula 1 12.5% + 97.65 + 15.62 781.25 0 0 0 0 0 0 Hexythiazox 2% SC
[0622] T7 Compound of Formula 1 12.5% + 58.59 + 44.53 468.75 0 0 0 0 0 0 Dinotefuran 9.5% SC
[0623] T8 Compound of Formula 1 12.5% + 78.12 + 59.37 625 0 0 0 0 0 0 Dinotefuran 9.5% SC
[0624] T9 Compound of Formula 1 12.5% + 97.65 + 74.21 781.25 0 0 0 0 0 0 Dinotefuran 9.5% SC
[0625] T10 Hexythiazox 2% + Dinotefuran 9.37 + 44.53 468.75 0 0 0 0 0 0 9.5% SC
[0626] T11 Hexythiazox 2% + Dinotefuran 12.5 + 59.37 625 0 0 0 0 0 0 9.5% SC
[0627] T12 Hexythiazox 2% + Dinotefuran 15.62 + 74.21 781.25 0 0 0 0 0 0 9.5% SC
[0628] T13 Compound of Formula 1 12.5% 78.12 625 0 0 0 0 0 0 SC
[0629] T14 Hexythiazox 2% SC 12.5 625 0 0 0 0 0 0
[0630]
[0631] T15 Dinotefuran 9.5% SC 59.37 625 0 0 0 0 0 0 T16 Compound of Formula I 20 % 100 500 0 0 0 0 0 0 w / w WP
[0632] T17 Hexythiazox 05.45 % w / w EC 25 500 0 0 0 0 0 0 T18 Dinotefuran 70 % WG 61.2 87 0 0 0 0 0 0 T19 Untreated - T20 Compound of Formula 1 12.5% + 156.25+ 25 + 1250 0 0 0 0 0 0 Hexythiazox 2% + Dinotefuran 118.75
[0633] 9.5%
[0634] L - Leaf injury on tips / surface, W - Wilting, N - Necrosis, V - Vein clearing, E - Epinasty, H - Hyponasty
[0635] *Based on 0-10 scale where: 0=0%, 1=1-10%, 2=11-20%, 3=21-30%, 4=31-40%, 5=41-50%,
[0636]
[0637] 6=51-60%, 7=61-70%, 8=71-80%, 9=81-90%, 10=91-100%
[0638] From the example, it is clearly seen that the stable synergistic pesticidal composition of the present invention is superior for controlling the red spider mite (Tetranychus urticae) and jassids (Amrasca biguttula biguttula) in Brinjal at 14 days after 1st& 2ndspray (Table 2A and 2B) in Brinjal crop as compared to the other pesticides such as Compound of Formula 120 % w / w WP, Hexythiazox 05.45 % w / w EC and Dinotefuran 70 % WG available in the market. The yield of Brinjal crop also improved in the stable synergistic pesticidal composition comprising Compound of Formula I + Hexythiazox + Dinotefuran SC as compared to binary and solo compositions (Table 2C).
[0639] The disclosed stable synergistic pesticidal composition comprising Compound of Formula I + Hexythiazox + Dinotefuran SC @ 468.75, 625 and 781.25 ml / ha further showed no phytotoxicity in the Brinjal crop even after 1, 3, 7, 10 and 14 days after 1stspray (Table 2D).
[0640] It is evident from the above data that the stable synergistic pesticidal composition of the present invention comprising Compound of Formula I + Hexythiazox + Dinotefuran SC resulted in higher synergistic control in pest population of red spider mite (Tetranychus urlicae) and jassids (Amrasca biguttula biguttula) in Brinjal 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.
[0641] 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) Compound of Formula I, i.e., 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4- chloropyridazin-3(2H)-one or its agrochemically acceptable salts, isomers, esters and derivatives;B) Hexythiazox or its agrochemically acceptable salts, isomers, esters and derivatives; andC) Dinotefuran or its agrochemically acceptable salts, isomers, esters or its derivatives.
2. The stable synergistic pesticidal composition as claimed in claim 1, comprising:A) Compound of Formula I, i.e., 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4- chloropyridazin-3(2H)-one or its agrochemically acceptable salts, isomers, esters and derivatives, in the range of 0.1-90% by weight of the composition;B) Hexythiazox or its agrochemically acceptable salts, isomers, esters and derivatives, in the range of 0.1-90% by weight of the composition; andC) Dinotefuran or its agrochemically acceptable salts, isomers, esters or its derivatives, in the range of 0.1-90% by weight of the composition.
3. A stable synergistic pesticidal composition comprising:A) Compound of Formula I, i.e., 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4- chloropyridazin-3(2H)-one or its agrochemically acceptable salts, isomers, esters and derivatives;B) Hexythiazox or its agrochemically acceptable salts, isomers, esters and derivatives; andC) Dinotefuran or its agrochemically acceptable salts, isomers, esters or its derivatives.D) At least one or more additive.
4. A stable synergistic pesticidal composition comprising:A) Compound of Formula I, i.e., 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4- chloropyridazin-3(2H)-one or its agrochemically acceptable salts, isomers, esters and derivatives, in the range of 0.1-90% by weight of the composition;B) Hexythiazox or its agrochemically acceptable salts, isomers, esters and derivatives, in the range of 0.1-90% by weight of the composition; andC) Dinotefuran or its agrochemically acceptable salts, isomers, esters or its derivatives, in the range of 0.1-90% 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 0.01-20% 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, anti-freezing agent(s), emulsifier(s)( (anionic and non-ionic), anti-foaming agent / defoamer(s), wetting agent(s), biocide / antimicrobial / anti-bacterial agent(s), 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) / colouring agent(s) / dye(s), carrier(s), stabilizer, buffering agent(s), polymer(s), safener(s), rheology modifier(s), solvent(s), co-solvent(s), or mixtures thereof.
7. . The stable synergistic pesticidal composition as claimed in any one of the claims 1 to 5, wherein the composition is in form of Emulsifiable concentrate (EC), Capsule suspension (CS), Dispersible concentrate (DC), Dustable powder (DP), Powder for dry seed treatment (DS), 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 concentrate (MEC), 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 composition of CS and SC (ZC) or a mixed composition of CS and SE (ZE) and a mixed composition 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 yield in the field.
9. . A process for preparing a stable synergistic pesticidal composition comprising:A) Compound of Formula I, i.e., 2-tert-butyl-5-[(4-tert-butylbenzyl)thio]-4- chloropyridazin-3(2H)-one or its agrochemically acceptable salts, isomers, esters and derivatives;B) Hexythiazox or its agrochemically acceptable salts, isomers, esters and derivatives; andC) Dinotefuran or its agrochemically acceptable salts, isomers, esters or its derivatives.
10. . The process for preparing a stable synergistic pesticidal composition as claimed in claim 9, comprises the steps of:i) selecting and weighing the compounds of formula I, Hexythiazox, and Dinotefuran in predetermined synergistic proportions;ii) mixing the said active ingredients with one or more agrochemically acceptable carriers and / or excipientsiii) optionally incorporating one or more surfactants, dispersing agents, wetting agents, suspending agents, stabilizers, defoamers, or binders to obtain a homogeneous mixture; andiv) processing the resulting mixture into a desired formulation type selected from or Emulsifiable concentrate (EC), Suspension concentrate (SC), Suspo-emulsion (SE), Micro-emulsion (ME), Emulsion for seed treatment (ES), Wettable powder (WP), Wettable granules (WG), etc. by known techniques such as grinding, granulation, orhigh-shear homogenization, emulsification followed by drying, sieving, and packaging to obtain a physically and chemically stable synergistic composition suitable for agricultural application