DESC:FORM 2

THE PATENTS ACT, 1970
(SECTION 39 OF 1970)
&
The Patents Rules, 2003

COMPLETE SPECIFICATION
(Section 10 and Rule 13)

SYNERGISTIC STROBILURIN COMBINATION FORMULATIONs, PROCESS FOR PREPARING AND USE THEREOF

We, COROMANDEL INTERNATIONAL LIMITED,
an Indian company incorporated under Companies Act of 1956, having its principal place of business at Coromandel House, Sardar Patel Road, Secunderabad – 500 003, Telangana, India.

The following specification particularly describes the invention and the manner in which it is to be performed:
FIELD OF THE INVENTION
The present invention relates to synergistic composition comprising combination of dithiolane fungicide and strobilurin fungicide.

The present invention also relates to synergistic composition comprising combination of dithiolane fungicide, strobilurin fungicide and agrochemical auxiliaries.

The present invention also relates to synergistic composition comprising combination of a dithiolane fungicide, strobilurin fungicide, and agrochemical auxiliaries, wherein said dithiolane fungicide is Isoprothiolane and said strobilurin fungicide is selected form Picoxystrobin or Pyraclostrobin.

The present invention specifically relates to emulsifiable concentrate (EC) composition comprising combination of Isoprothiolane and strobilurin fungicide at a weight in the ratio of 1 : 10 to 10 : 1 of first active ingredient to the second active ingredient, more preferably in the ratio of 1 : 5 to 5 : 1, wherein said second active ingredient is selected from Picoxystrobin or Pyraclostrobin.

The present invention specifically relates to emulsifiable concentrate composition comprising combination of Isoprothiolane, Picoxystrobin and agrochemical auxiliaries.

The present invention specifically relates to emulsifiable concentrate (EC) composition comprising combination of Isoprothiolane, Pyraclostrobin and agrochemical auxiliaries.

The present invention also relates to a process for the preparation of emulsifiable concentrate composition comprising combination of Isoprothiolane and strobilurin fungicide, wherein the composition is prepared by simple blending and milling process.

BACKGROUND OF THE INVENTION
Isoprothiolane is a systemic fungicide with curative and protective effects. The active ingredient is used in rice cultivation to combat various fungal diseases such as ice blight, rice stem rot and Fusarium leaf spot on rice, also reducing plant-hopper populations following foliar applications. Isoprothiolane inhibits the penetration and elongation of infecting hyphae by inhibiting formation of infecting peg or cellulase secretion. The product is also used to treat fatty liver syndrome in cattle.

Isoprothiolane is chemically known as diisopropyl 1,3-dithiolan-2-ylidenemalonate or bis(1-methylethyl) 2-(1,3-dithiolan-2-ylidene)propanedioate and has the following structure:

Picoxystrobin is a fungicide belonging to the strobilurin group of chemicals. It is a preventative and curative fungicide with systemic and translaminar movement, acting by inhibition of mitochondrial respiration by blocking electron transfer at the Qo centre of cytochrome Bc1. It is used for control of a range of fungal diseases, including brown rust, tan spot, powdery mildew, and net blotch in cereals, pulses and oilseeds.

Picoxystrobin is a systemic and trans-laminar, Quinone outside Inhibitor (QoI) fungicide with preventive, curative and systemic activity for use on Canola, Cereal grains, dried peas, corn and soybeans. It is applied by ground equipment, aerially or via chemigation methods for control of foliar and soil-borne plant diseases. It inhibits mitochrondial respiration by blocking electron transfer at the Qo center of cytochrome bcl. The formulated product is a suspension concentrate (SC).

Picoxystrobin is chemically, methyl (E)-3-methoxy-2-[2-(6-trifluoromethyl-2- pyridyloxymethyl)phenyl]acrylate and has the following structure:

EP 0 278 595 B1 claims compositions of Picoxystrobin and the family patents claims Picoxystrobin.

Pyraclostrobin is a fungicide belonging to the group which is collectively known as strobilurins, which inhibit mitochondrial respiration. This leads to a reduction of energy-rich ATP that is available to support a range of essential processes in the fungal cell. Pyraclostrobin is a fungicide used to control major plant pathogens in cereals and other crops such as Cereals including wheat, barley, oats; forage & grain maize, triticale; Sugarbeet; Potatoes; Vegetables including brassicas, carrot; beans, vining peas; Fruit including strawberry, blackcurrants.

Pyraclostrobin is chemically, methyl N-{2-[1-(4-chlorophenyl)pyrazol-3-yloxymethyl]phenyl}(N-methoxy)carbamate and has the following structure:

US 5,869,517 A claims Pyraclostrobin generically.

WO 2013/126947A1 discloses an emulsifiable concentrate (EC) formulation comprising a least one agrochemical active ingredient, at least one surfactant emulsifier; optionally, a stabiliser; and a primary solvent system, wherein the solvent system comprises a combination of benzyl acetate and a sufficient amount of at least one polar, substantially water-miscible co-solvent. However, composition comprising combination of dithiolane fungicide and strobilurin fungicide is not disclosed.

The combinations with fungicidal active substances for widening the spectrum of action and/or for protecting the crop plants are also known. Though, the ability of these combination compounds to efficiently control diseases varies with a large number of the parameters including, but not limited, the type of the formulations of combination fungicide, the type of phytopathogenic fungi to be controlled, the type of the plant to be protected and ambient conditions, such as temperature, precipitations, humidity, length of the day, biological diversity of the micro environment, the like.

Though, conventionally each of these active ingredients are used individually, combination product is not approved which has applications compared to the mono product. Hence, there is increased interest in the use of Active ingredients in combination to give synergistic results.

Therefore, formulations of fungicidal active substances in combinations should generally have good chemical and physical stability, good application properties, user friendliness, having good biological activity and enhanced efficacy combined with high selectivity. Proper formulation and efficient delivery systems of combinations fungicides are the key elements in the performance of different products.

Accordingly, there is a need in the art to provide pesticidal synergistic compositions which are environmentally safer and stable pesticidal compositions having two active ingredients with different physical and chemical properties, which are environmentally safe, easy and effective combination formulation of two active with enhanced efficacy and stable product during storage.

It was surprisingly and unexpectedly found by the present inventors that a selective combination composition of two active ingredients comprising Isoprothiolane, strobilurin fungicide, and agrochemical auxiliaries, possesses enhanced efficacy, improved penetration and long duration control of phytopathogens as compared to its other traditional formulations with long storage stability across a wide temperature range and having no adverse impact on photosynthetic activity in plant and seed quality.

OBJECTIVE OF INVENTION
The main objective of the present invention is to provide synergistic composition comprising combination of dithiolane fungicide and strobilurin fungicide.

Another objective of the present invention is to provide synergistic composition comprising combination of dithiolane fungicide, strobilurin fungicide and agrochemical auxiliaries.

Another objective of the present invention is to provide synergistic composition comprising combination of a dithiolane fungicide, strobilurin fungicide, and agrochemical auxiliaries, wherein said dithiolane fungicide is Isoprothiolane and strobilurin fungicide is selected form Picoxystrobin or Pyraclostrobin.

Another objective of the present invention is to provide emulsifiable concentrate composition comprising combination of Isoprothiolane and strobilurin fungicide at a weight in the ratio of 1 : 10 to 10 : 1 of first active ingredient to the second active ingredient, more preferably in the ratio of 1 : 5 to 5 : 1, wherein said second active ingredient is selected from Picoxystrobin or Pyraclostrobin.

Another objective of the present invention is to provide emulsifiable concentrate composition comprising combination of Isoprothiolane, Picoxystrobin and agrochemical auxiliaries

The present invention specifically relates to emulsifiable concentrate composition comprising combination of Isoprothiolane and Pyraclostrobin and agrochemical auxiliaries.

Another objective of the present invention is to provide a process for the preparation of emulsifiable concentrate composition comprising combination of Isoprothiolane and strobilurin fungicide, wherein the composition is prepared by simple blending and milling process.

SUMMARY OF INVENTION
Accordingly, the present invention provides a synergistic composition comprising combination of dithiolane fungicide and strobilurin fungicide.

In one embodiment, the present invention provides a synergistic composition comprising combination of dithiolane fungicide, strobilurin fungicide and agrochemical auxiliaries.

In another embodiment, the present invention provides a synergistic composition comprising combination of a dithiolane fungicide, strobilurin fungicide, emulsifiers, solvents and optionally other agrochemical auxiliaries.

In another embodiment, the present invention provides a synergistic composition comprising combination of a dithiolane fungicide, strobilurin fungicide, emulsifiers, solvents and optionally other agrochemical auxiliaries, wherein said dithiolane fungicide is Isoprothiolane and strobilurin fungicide is selected form Picoxystrobin or Pyraclostrobin.

In another embodiment, the present invention provides a synergistic composition comprising combination of a dithiolane fungicide and strobilurin fungicide, wherein said composition is an emulsifiable concentrate.

In another embodiment, the present invention provides an emulsifiable concentrate composition comprising combination of Isoprothiolane, Picoxystrobin and agrochemical auxiliaries.

In another embodiment, the present invention provides an emulsifiable concentrate composition comprising combination of Isoprothiolane, Pyraclostrobin and agrochemical auxiliaries.

In another embodiment, the present invention provides an emulsifiable concentrate composition comprising combination of Isoprothiolane and strobilurin fungicide at a weight in the ratio of 1 : 10 to 10 : 1 of first active ingredient to the second active ingredient, more preferably in the ratio of 1 : 5 to 5 : 1, wherein said second active ingredient is selected from Picoxystrobin or Pyraclostrobin.

In another embodiment, the present invention provides an emulsifiable concentrate composition comprising:
a. 1% to 50% (w/w) of Isoprothiolane,
b. 1% to 30% (w/w) of strobilurin fungicide selected from Picoxystrobin or Pyraclostrobin,
c. 1% to 30% (w/w) of emulsifiers, and
d. 0.1% to 70% (w/w) of other agrochemical auxiliaries.

In another embodiment, the present invention provides an emulsifiable concentrate composition comprising:
a. 1% to 50% (w/w) of Isoprothiolane,
b. 1% to 30% (w/w) of strobilurin fungicide selected from Picoxystrobin or Pyraclostrobin,
c. 1% to 30% (w/w) of emulsifier,
d. 1% to 70% (w/w) of solvent and optionally
e. 1% to 15% (w/w) of stabiliser.

In another embodiment, the present invention provides an emulsifiable concentrate composition comprising:
a. 1% to 50% (w/w) of Isoprothiolane,
b. 1% to 30% (w/w) of Picoxystrobin.
c. 1% to 30% (w/w) of mixture of calcium dodecyl benzene sulphonate, isobutanol and tristyrylphenol ethoxylate,
d. 1% to 20% (w/w) of N-methyl-2-pyrrolidone,
e. 1% to 50% (w/w) of aromatic solvent C-12, and
f. 1% to 15% (w/w) of epoxidised soybean oil.

In another embodiment, the present invention provides an emulsifiable concentrate composition comprising:
a. 1% to 50% (w/w) of Isoprothiolane,
b. 1% to 30% (w/w) of Pyraclostrobin.
c. 1% to 30% (w/w) of mixture of calcium dodecyl benzene sulphonate, isobutanol and tristyrylphenol ethoxylate,
d. 1% to 20% (w/w) of N-methyl-2-pyrrolidone, and
e. 1% to 50% (w/w) of solvent C-9.
In another embodiment, the present invention provides a process for the preparation of emulsifiable concentrate composition comprising combination of Isoprothiolane and strobilurin fungicide, wherein the composition is prepared by simple blending and milling process.

In another embodiment, the present invention provides a process for preparing emulsifiable concentrate comprising the steps of:
a. weighing and mixing active ingredients and auxiliaries,
b. filtering the obtained material and packing.

In another embodiment, the present invention provides a process for preparing emulsifiable concentrate comprising the steps of:
a. weighing and mixing Isoprothiolane, Picoxystrobin, Epoxidised soybean oil, mixture of calcium dodecyl benzene sulphonate, isobutanol and tristyrylphenol ethoxylate, N-methyl-2-pyrrolidone and aromatic solvent C-12.
b. filtering the obtained material and packing.

In another embodiment, the present invention provides a process for preparing emulsifiable concentrate comprising the steps of:
a. weighing and mixing Isoprothiolane, Pyraclostrobin, mixture of calcium dodecyl benzene sulphonate, isobutanol and tristyrylphenol ethoxylate, N-methyl-2-pyrrolidone and aromatic solvent C-9.
b. filtering the obtained material and packing.

DETAILED DESCRIPTION OF THE INVENTION
The term "comprising", which is synonymous with "including", "containing", or "characterized by" here is defined as being inclusive or open-ended, and does not exclude additional, unrecited elements or method steps, unless the context clearly requires otherwise.
The present invention provides synergistic composition comprising combination of 1 : 10 to 10 : 1 of first active ingredient to the second active ingredient, more preferably in the ratio of 1 : 5 to 5 : 1. However, variables of the ratios of each of the active ingredients can be used and the selection of the particular amount is dependent upon many factors including, for example, type of formulations, the crop, disease sought to be controlled and environmental conditions. The selection of the proper quantity of active agent to be applied, however, is within the expertise of one skilled in the art.

The composition of the present invention could be applied to plants, seeds, fruits, soil as preventive and curative state.

ECs are versatile formulations that can be applied with many types of sprayers. EC composition enables spontaneous emulsification upon dilution and are easy to handle and measure. Very little agitation is required to mix them with water, and will not separate; Little visible residue on the plant; Do not wear sprayer parts or plug screens or nozzles; Seldom leaves visible residue

The emulsifier used in the composition allows the active ingredient in the solvent to mix with water, these form an emulsion. The emulsifying surfactant system enabling the EC to form an oil-in-water emulsion when the formulation is added to water is typically a mixture of two or more surfactants, at least one of which is a nonionic surfactant and optionally at least one of which is an anionic surfactant.

The surfactants customarily employed in formulation technology, which are described, inter alia, in “Mc Cutcheon's Detergents and Emulsifiers Annual” MC Publishing Corp., Ridgewood N.J., 1981, Stache, H., “Tensid-Taschenbuch”, Carl Hanser Verlag, Munich Nienna, 1981 and M. and J. Ash, “Encyclopedia of Surfactants”, Vol I-III, Chemical Publishing Co., New York, 1980-81, are also suitable for preparation of the herbicidal compositions according to the invention.
The surfactant is required to maintain the particles in emulsion and prevent them from agglomerating in the emulsion formation. The surfactant employed in the formulation composition is selected from the group consisting of non-ionic surfactants, anionic surfactant and a mixture of anionic and non-ionic surfactant and polymeric surfactant. Among these preferred surfactants is mixture of anionic and non-ionic surfactants.

The anionic and non-ionic surfactants as used herein are selected from and not limited to C1-C16-alkyl benzene sulfonates, C1-C16-alkyl naphthalene sulfonates, lignosulfonates, naphthalene sulfonate-formaldehyde condensates, C1-C16-alkyl naphthalene sulfonate-formaldehyde condensates, polyoxy-C2-C3-alkylene C8-C22-alkyl ether sulfates, polyoxy-C2-C3-alkylene C8-C22-alkyl ether phosphates, polyoxy- C2-C3-alkylene C1-C16-alkylbenzene ether sulfates, polyoxy-C2-C3-alkylene C1-C16-alkylbenzene ether phosphates, C8-C22-alkyl sulfates, C4-C18-dialkyl sulfosuccinates, polyoxy- C2-C3-alkylene mono-, di- or tristyryl phenyl ether sulfates, polyoxy- C2-C3-alkylene mono-, di- or tristyryl phenyl etherphosphates, polyoxyethylene polycarboxylates, polyphosphates, fatty acid alkanolamides, calcium dodecylbenzene sulfonate in combination with 2-methylpropan-1-ol, poly (oxy-1, 2-ethanediyl),.alpha.-[tris(1-phenylethyl)phenyl]-.omega.-hydroxy- (mixture of calcium dodecyl benzene sulphonate, isobutanol and tristyrylphenol ethoxylate) (Geronil FF4 and Geronil FF6), the condensation products of fatty acid esters, fatty alcohols, fatty acid amides or fatty amines with ethylene and/or propylene oxide, alkyl- , alkenyl or polyaryl-substituted phenols with ethylene and/or propylene oxide, fatty esters of polyhydric alcohol esters e.g. sorbitan fatty acid esters, polyoxy-C2-C3-alkylene mono-, di- or tristyryl phenyl ethers, condensation product of such esters with ethylene oxide, e.g. polyoxyethylene sorbitan fatty acid esters, block copolymers of ethylene oxide and propylene oxides, ethoxylated lanolin alcohols or ethoxylated lanolin acids from the group consisting of homo- or copolymers of C2-C3-alkylene oxides, polyoxy-C2-C3-alkylene C8-C22-alkyl ethers, polyoxy-C2-C3-alkylene C1-C16-alkylbenzene ethers, polyoxy- C2-C3-alkylene mono-, di- or tristyryl phenyl ethers, polyoxy-C2-C3-alkylene mono- or distyryl phenyl ether-formaldehyde condensates, and acetylene glycols, Calcium dodecyl benzene sulphonate, 2-methylpropan-1-ol, Poly(oxy-1,2-ethanediyl), .alpha.-[tris(1-phenylethyl)phenyl]-.omega.-hydroxy- with molecular ranges (mixture of calcium dodecyl benzene sulphonate, isobutanol and tristyrylphenol ethoxylate) (Geronil FF4 and Geronil FF6).

Geronil FF4 and Geronil FF6 comprise of same components but in different concentrations.

Geronil FF4 comprising blend of:
calcium dodecylbenzene sulphonate >40% to < 50%,
2-methylpropan-1-ol (isobutanol) >30% to < 40%,
poly(oxy-1,2-ethanediyl), .alpha.-[tris(1- phenylethyl)phenyl]-.omega.-hydroxy- (tristyrylphenol ethoxylate) >15% to < 20%.

Geronil FF6 comprising blend of:
calcium dodecylbenzene sulphonate > 10% to < 15%,
2-methylpropan-1-ol (isobutanol) >5% to < 10%,
poly(oxy-1,2-ethanediyl), .alpha.-[tris(1-phenylethyl)phenyl]-.omega.-hydroxy- (tristyrylphenol ethoxylate) >70% to < 80%.

The emulsifier is present in the composition in a range of about 1 to 30%, more preferably 2 to 20% of the total weight of the composition.

Stabiliser as used herein is also an emulsifier used herein above or epoxylates vegetable oils such as Epoxidized soybean oil (ESO), Butylated hydroxytoluene (BHT), polyethyleneglycol, polypropyleneglycol chain, an ethylene glycol-propylene glycol copolymeric chain, or a mixture thereof.

The stabiliser is present in the composition in a range of about 1 to 15%, more preferably 1 to 10% of the total weight of the composition.

Solvent as used herein is a suitable water-immiscible solvents selected from the group consisting of aromatic hydrocarbons, aliphatic hydrocarbons, dialkylene glycol dialkyl ethers (diethylene glycol dimethyl ether), ketones, alkyl esters of acetic acid or mixtures thereo. Aromatic and aliphatic hydrocarbons such as hexane, cyclohexane, benzene, toluene, xylene, mineral oil or kerosene or substituted naphthalenes, polar aprotic solvents such as DMSO, DMF, NMP (N-methyl-2-pyrrolidone) etc, mixtures of mono- and polyalkylated aromatics are commercially available under the registered trademarks Solvesso® and Shellsol® and Petrol Spezial®.

The solvents present in the composition in a range of about 1 to 70%, more preferably 10 to 70% of the total weight of the composition.

Isoprothiolane and strobilurin fungicide may be present in the composition or applied in any amounts relative to each other, to provide the enhanced or synergistic effect of the mixture. Isoprothiolane and strobilurin fungicide may be present in the synergistic pesticidal composition in any suitable amount, and is generally present in an amount of from 1% to 50% by weight of the composition, preferably from 1% to 40% by weight of the composition. However, variables of the ratios of each of the active ingredients can be used and the selection of the particular amount is dependent upon many factors including, for example, type of formulations, the crop, disease sought to be controlled and environmental conditions. The selection of the proper quantity of active agent to be applied, however, is within the expertise of one skilled in the art.

Formulation includes water soluble concentrate (SL), an emulstifiable concentrate (EC), an emulsion (EW), a microemulsion (ME), a suspension concentrates (SC), an oil-based suspension concentrates (OD), a flowable suspension (FS), water soluble powder (WS), water-dispersible granule (WDG), water-soluble granule (SG), a water-dispersible powder (WP), a water soluble powder (SP), a granule (GR), an encapsulated granule (CG), a fine granule (FG), a macrogranule (GG), an aqueous suspoemulsion (SE), capsule suspension (CS) and a microgranule (MG).

Preferably, the synergistic pesticide composition can be formulated as Emulfiable concentrate (EC).

The EC compositions of the present invention can be diluted with water or water solutions of agronomic compounds before use to produce a sprayable suspension composition which is used in treating plants or increasing plant growth, Dilution in water usually results in suspensions, emulsions, suspoemulsions or solutions of the agrochemical active ingredient at a concentration of at least 0.001 g/l.

A particular mode of administering the composition of the present invention is the administration to the aboveground parts of plants, in particular to the leaves thereof (leaf-application). The number of applications and the administered doses are chosen in accordance with the biological and climatic conditions of life of the causative agent. The antifungal compositions though, can also be applied to the soil and get into the plants through the root system (systemic activity), in case the locus of the plants is sprayed with a liquid composition or if the components are added to the soil in a solid formulation e.g. in the form of wettable powder (soil application).

When using the active compound combinations according to the invention, the application rate can be varied within a relatively wide range, depending on the kind of application. For the treatment of parts of plants, the active-compound combination application rates are generally between 0.1 and 10000 g/ha, preferably between 100 and 2500 g/ha. For seed dressing, the active compound combination application rates are generally between 0.001 and 50 g per kilogram of seed, preferably between 0.01 and 20 g per kilogram of seed. For the treatment of the soil, the active-compound combination application rates are generally between 0.1 and 10000 g/ha preferably between 1 and 5000 g/ha.

The following examples describe the nature of the invention which are given only for the purpose of illustrating the present invention in more detail and are not limitative.

EXAMPLES
Example 1: Composition of Isoprothiolane 25% + Picoxystrobin 10% EC:
S. No. Ingredients/Raw Materials Quantity (% w/w)
1. Isoprothiolane technical (a) 98.61% (b) 25% 25.35
2. Picoxystrobin technical (a) 98.59% (b) 10% 10.14
3. Mixture of calcium dodecyl benzene sulphonate, isobutanol and tristyrylphenol ethoxylate (Geronol FF4) 3.60
4. Mixture of calcium dodecyl benzene sulphonate, isobutanol and tristyrylphenol ethoxylate (Geronol FF6) 8.40
5. N-methyl-2-pyrrolidone (NMP) 10.00
6. aromatic solvent C-12 (Solvesso 200) 41.51
7. Epoxidised soybean oil 1.00
Total 100

Manufacturing process

N-methyl-2-pyrrolidone solvent was charged to a clean reactor vessel under stirring according to the batch size, followed by Picoxystrobin technical and continue to stir for 15 minutes. Aromatic solvent C-12 charged under continuous stirring and Isoprothiolane technical was charged to the above step and continue to stir for 30 mins. ESO was charged to the above mixture and stir for 10 mins. Geronol FF4 and Geronol FF6 were charged and the contents stirred for 1 hour. The mixture was passed through 10µ sieve filter paper and the material was collected and packed.

Example 2: Composition of Isoprothiolane 25% + Pyraclostrobin 10% EC:
S. No. Ingredients/Raw Materials Quantity (% w/w)
1. Isoprothiolane technical (a)98.6%(b)25% 25.35
2. Pyraclostrobin technical (a)98% (b)10% 10.20
3. Mixture of calcium dodecyl benzene sulphonate, isobutanol and tristyrylphenol ethoxylate (Geronol FF4) 3.60
4. Mixture of calcium dodecyl benzene sulphonate, isobutanol and tristyrylphenol ethoxylate (Geronol FF6) 8.40
5. N-methyl-2-pyrrolidone (NMP) 10.00
6. Solvent C9 QS
Total 100

Manufacturing process

N-methyl-2-pyrrolidone solvent was charged to a clean reactor vessel under stirring according to the batch size, followed by Pyraclostrobin technical and continues to stir for 15 minutes. Solvent C-IX was charged under continuous stirring and Isoprothiolane technical was charged to the above step and continue to stir for 30 mins. Geronol FF4 and Geronol FF6 were charged and the contents stirred for 1 hour. The mixture was passed through 10µ sieve filter paper and the material was collected and packed.

Field Bio-efficacy studies of Isoprothiolane + Picoxystrobin EC

Trial 1: Rice blast

The rice blast is caused by the fungal pathogen Magnaporthe oryzae. This is potentially devasting disease can infect rice foliage. The symptoms of rice blast include lesions that can be found on all parts of the plant, including leaves, leaf collars, necks, panicles, pedicels, and seed. Its major threat to rice crop and can also affect the crop stand and yield. Infection of rice occurs when conidia are deposited on rice tissues and germinate by producing a germ tube and an appressorium. The appressorium is a melanized structure, and from it develops an infection peg which penetrates the tissue. After penetration, the primary infection hypha grows rapidly and ramifies within susceptible tissues. Growth within tissues of resistant cultivars is often inhibited. Generally, rice blast is favoured by moderate temperatures (240C) and periods of high moisture that are 12 hours or longer, conditions readily attainable in flooded rice fields. Spores produced as the primary inoculum on the overwintering tissues produce the initial infections on young seedlings when the spores that are deposited on leaves, germinate, and invade leaf tissues.

The field trial was conducted to evaluate the efficacy of innovative mixtures of Isoprothiolane and Picoxystrobin against Magnaporthe oryzae fungus in rice crop. Trial was conducted with randomized block design with net plot size of 5m x 6m. Rice crop was raised with all standard agronomic practices. Spraying was done with manual operated backpack knapsack sprayer with 500 L of water spray volume per hectare at 45 days after transplanting. The visual observations were recorded for % disease control from ten hills per plot. The observations were recorded at before spraying, 7 DAA (Days after application) and 14 DAA (Days after application).

Table 1: blast disease control in rice:
Compositions Dose (gram active per hectare) % Rice Blast control
7 DAA 14 DAA
Isoprothiolane 25% + Picoxystrobin 10% EC 350 90 85
Isoprothiolane 25% EC 250 55 45
Picoxystrobin 10% SC 100 65 55
EC – Emulsion concentrates, SC– Suspension Concentrate and DAA - Days after application.
The trial results show excellent efficacy of Isoprothiolane 25% + Picoxystrobin 10% EC combinations against blast disease of rice. The solo application of two active ingredients tested here, were not able to provide satisfactory control of rice blast disease. The combination of Isoprothiolane 25% + Picoxystrobin 10% EC found very promising against rice blast in terms of efficacy as well as residual control.

Trial – 2 : Leaf spot complex
The leaf spot is caused by the fungal pathogens Helminthosporium spp., Cercospora spp. Magnaporthe oryzae. This is potentially devasting disease can infect rice foliage. It leads to premature death of leaves and leaf sheaths, premature ripening of grains, and in severe cases, lodging of plants. Its major threat to many crops and can also affect the crop stand and yield. Leaf spot complex fungus is cosmopolitan and widely distributed in tropical, subtropical regions of Asia and for its development required hot and humid environment. The disease usually occurs in potassium deficient soils, and in areas with temperature ranging from 25-28°C. It appears during the late growth stages of the rice crop, starting at heading stage. Plants are most susceptible during panicle initiation onwards, and damage becomes more severe as plants approach maturity.

The field trial was conducted to evaluate the efficacy of innovative mixtures of Isoprothiolane and Picoxystrobin against leaf spot complex fungus in rice crop. Trial was conducted with randomized block design with net plot size of 5m x 6m. rice crop was raised with all standard agronomic practices. Spraying was done with manual operated backpack knapsack sprayer with 500 L of water spray volume per hectare at 45 days after transplanting. The visual observations were recorded for % disease control from ten hills per plot. The observations were recorded at before spraying, 7 DAA (Days after application) and 14 DAA (Days after application).

Table 2: Leaf spot complex control in rice:
Compositions Dose (gram active per hectare) % Leaf spot disease control
7 DAA 14 DAA
Isoprothiolane 25% + Picoxystrobin 10% EC 350 90 80
Isoprothiolane 25% EC 250 50 40
Picoxystrobin 10% SC 100 60 50
EC – Emulsion concentrates, SC– Suspension Concentrate and DAA - Days after application.

The trial results in Table 2 show excellent efficacy of Isoprothiolane 25% + Picoxystrobin 10% EC combinations against leaf spot complex disease of rice. The solo application of two active ingredients tested here, were not able to provide satisfactory control of leaf spot disease. The combination of Isoprothiolane 25% + Picoxystrobin 10% EC found very promising against rice leaf spot complex in terms of efficacy as well as residual control.

,CLAIMS:WE CLAIM

1. A synergistic composition comprising combination of dithiolane fungicide, strobilurin fungicide, emulsifiers, solvents and optionally other agrochemical auxiliaries.

2. The composition as claimed in claim 1, wherein said dithiolane fungicide is Isoprothiolane and strobilurin fungicide is selected form Picoxystrobin or Pyraclostrobin.

3. The composition as claimed in claim 1, wherein said composition is an emulsifiable concentrate.

4. The composition as claimed in claims 1-3, wherein said emulsifiable concentrate composition comprising:
a. 1% to 50% (w/w) of Isoprothiolane,
b. 1% to 30% (w/w) of strobilurin fungicide selected from Picoxystrobin or Pyraclostrobin,
c. 1% to 30% (w/w) of emulsifiers, and
d. 0.1% to 70% (w/w) of other agrochemical auxiliaries.

5. The composition as claimed in claims 4, wherein said emulsifiable concentrate composition comprising:
a. 1% to 50% (w/w) of Isoprothiolane,
b. 1% to 30% (w/w) of strobilurin fungicide selected from Picoxystrobin or Pyraclostrobin,
c. 1% to 30% (w/w) of emulsifier,
d. 1% to 70% (w/w) of solvent and optionally
e. 1% to 15% (w/w) of stabiliser.

6. The composition as claimed in claims 5, wherein said emulsifiable concentrate composition comprising:
a. 1% to 50% (w/w) of Isoprothiolane,
b. 1% to 30% (w/w) of Picoxystrobin.
c. 1% to 30% (w/w) of mixture of calcium dodecyl benzene sulphonate, isobutanol and tristyrylphenol ethoxylate,
d. 1% to 20% (w/w) of N-methyl-2-pyrrolidone,
e. 1% to 50% (w/w) of aromatic solvent C-12, and
f. 1% to 15% (w/w) of epoxidised soybean oil.

7. The composition as claimed in claims 5, wherein said emulsifiable concentrate composition comprising:
a. 1% to 50% (w/w) of Isoprothiolane,
b. 1% to 30% (w/w) of Pyraclostrobin.
c. 1% to 30% (w/w) of mixture of calcium dodecyl benzene sulphonate, isobutanol and tristyrylphenol ethoxylate,
d. 1% to 20% (w/w) of N-methyl-2-pyrrolidone, and
e. 1% to 50% (w/w) of solvent C-9.

8. The process for the preparation of composition as claimed in claims 1, wherein said process comprising the steps of:
c. weighing and mixing active ingredients and auxiliaries,
d. filtering the obtained material and packing.

9. The process for the preparation of composition as claimed in claims 6, wherein said process comprising the steps of:
a. weighing and mixing Isoprothiolane, Picoxystrobin, Epoxidised soybean oil, mixture of calcium dodecyl benzene sulphonate, isobutanol and tristyrylphenol ethoxylate, N-methyl-2-pyrrolidone and aromatic solvent C-12.
b. filtering the obtained material and packing.

10. The process for the preparation of composition as claimed in claims 7, wherein said process comprising the steps of:
a. weighing and mixing Isoprothiolane, Pyraclostrobin, mixture of calcium dodecyl benzene sulphonate, isobutanol and tristyrylphenol ethoxylate, N-methyl-2-pyrrolidone and aromatic solvent C-9.
b. filtering the obtained material and packing.

Dated this Twelfth (12th) day of August 2021

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Dr. S. Padmaja
Agent for the Applicant
IN/PA/883