DESC:FORM 2

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

COMPLETE SPECIFICATION
(Section 10 and Rule 13)

SYNERGISTIC FUNGICIDAL COMPOSITION CONTAINING BOSCALID

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 a synergistic fungicidal composition for agriculture use. Particularly, the present invention relates to a synergistic fungicidal composition comprising (a) Boscalid, (b) at least one strobilurin selected from Azoxystrobin, Picoxystrobin, Pyraclostrobin, or Trifloxystrobin, and (c) at least one triazole selected from Cyproconazole, Prothioconazole, or Tebuconazole along with suitable agrochemical additives.

BACKGROUND OF THE INVENTION
In the field of crop protection, the use of a particular active substance for the control of specific fungi may become increasingly difficult in time, because of the adaptation of the mentioned fungi to the fungicide being used. This leads to the loss of effectiveness in the control of the pathogen, and, consequently, downfall in crop production and profitability.

Fungicides are compounds, of natural or synthetic origin, which act to protect plants against damage caused by fungi. Current methods of agriculture rely heavily on the use of fungicides. In fact, some crops cannot be grown usefully without the use of fungicides. Using fungicides allows a grower to increase the yield and the quality of the crop, and consequently, increase the value of the crop. In most situations, the increase in value of the crop is worth at least three times the cost of the use of the fungicide.

A very well-known and widely used form of approaching this problem is by using a combination of different active substances presenting different mechanisms of action.

The present invention is related to a synergistic fungicidal composition consisting of boscalid, a strobilurin fungicide, and a triazole fungicide in effective amounts, along with suitable agrochemical additives, and a process thereof.
Boscalid (2-chloro-N-(4'-chloro[1,1'-biphenyl]-2-yl)-3-pyridinecarboxamide) is a member of the fungicide group succinate dehydrogenase inhibitors (SDHI) and is used worldwide in several crops for the control of a broad range of important pathogens. Boscalid is active against different fungal stages both on the plant surface and in the plant tissue. After application to the plant, the active ingredient is taken up via the leaf and then translocated via the transpiration flow. Due to its mobility, it shows local systemic and translaminar activity. By that, it can control fungal stages, which have already become established in deeper tissue layers. As a result, Boscalid has preventative and curative activity.
Strobilurin fungicide have been widely used in agricultural fields for decades. These pesticides are designed to manage fungal pathogens, although their broad-spectrum mode of action also produces non-target impacts. They present rapid and highly efficient germicidal activities, are cost effective and rapidly degrade during plant metabolism, and these benefits have contributed to the large-scale use of these fungicides. The strobilurin fungicides used in the present invention is selected from the group consisting of azoxystrobin, picoxystrobin, pyraclostrobin, and trifloxystrobin.

Triazole fungicides are widely used in agricultural fields. They are potent inhibitors of ergosterol synthesis, the major membrane sterol of fungi. They block the cytochrome P450-dependent enzyme C-14 alpha-demethylase, which is needed to convert lanosterol to ergosterol. The triazole fungicide used in the present invention is selected from the group consisting of cyproconazole, prothioconazole, and tebuconazole.

There is also a requirement of a stable fungicidal composition combining more than one active ingredient that has a synergistic effect and thereby reduce the need for multiple individual applications while providing better fungicidal activity. Further requirement also includes a combination product having synergistic effect which can be extensively applied in the field of agricultural for controlling wide spectra of fungi which also exhibits good physical and chemical stability.

The combinations of fungicides are often used to facilitate disease control, to broaden spectrum of control and to retard resistance development.

WO2009/040397A1 discloses ternary fungicidal compositions comprising as active components 1) boscalid, 2) chlorothalonil and 3) at least one active compound III, selected from groups A) to F): A) azoles; B) strobilurin; C) carboxamides; D) heterocyclic compounds; E) carbamates; F) other fungicides.

WO 2020/012445A1 discloses a eutectic mixture of boscalid and strobilurin fungicide selected from the group comprising azoxystrobin, picoxystrobin, trifloxystrobin and fluoxastrobin.

Various compositions have been developed to control fungi and in practice have been used as a single or a mixed agent. Practical agricultural experience has shown that the repeated and exclusive application of an individual active compound in the control of harmful fungi leads in many cases to a rapid selection of those fungus strains which have developed natural or adapted resistance against the active compound in question. Effective control of these fungi with the active compound in question is very difficult in such cases. Active compounds having different mechanisms of action are combined to delay the generation of resistance and reduce the application amount and prevention and treatment costs. Consequently, research is being conducted to produce fungicides and combinations of fungicides that are safer, that have better performance, that require lower dosages, that are easier to use, and that cost less.

The present invention aims to provide one such combination of boscalid, a strobilurin fungicide, and a triazole fungicide to provide broader control spectrum at lower dosages.
OBJECT OF THE INVENTION
One object of the present invention is to provide a synergistic fungicidal composition comprising of boscalid, a strobilurin fungicide and a triazole fungicide.

Another object of the present invention is to provide a synergistic fungicidal composition comprising of (a) Boscalid, (b) at least one strobilurin fungicide selected from Azoxystrobin, Picoxystrobin, Pyraclostrobin, or Trifloxystrobin, and (c) at least one triazole fungicide selected from Cyproconazole, Prothioconazole, or Tebuconazole along with suitable agrochemical additives.

In yet another object of the present invention may provide combinations of fungicides that possess an enhanced efficacy over the individual fungicides used in isolation.

In yet another object of the present invention is to provide a fungicidal combination that results into reduced fungal disease incidence in the crops to which it is applied.

SUMMARY OF THE INVENTION
The present invention is to provide a synergistic fungicidal composition comprising of (a) Boscalid, (b) at least one strobilurin fungicide selected from Azoxystrobin, Picoxystrobin, Pyraclostrobin, or Trifloxystrobin, and (c) at least one triazole fungicide selected from Cyproconazole, Prothioconazole, or Tebuconazole along with suitable agrochemical additives.

In another aspect, the Boscalid is present in a range from 5% (w/w) to 15% (w/w); a strobilurin fungicide is selected from Azoxystrobin, Picoxystrobin, Pyraclostrobin, or Trifloxystrobin present in a range from 5% (w/w) to 15% (w/w); and a triazole fungicide selected from Cyproconazole, Prothioconazole, or Tebuconazole present in a range from 5% (w/w) to 15% (w/w) along with suitable agrochemical additives.

In another aspect, the present invention provides a synergistic fungicidal composition comprising of:
(a) Boscalid present in an amount of 5% to 15%,
(b) Azoxystrobin present in an amount of 5% to 15%,
(c) Cyproconazole present in an amount of 5% to 15%, and
(d) Agrochemical additives.

In another aspect, the present invention provides a synergistic fungicidal composition comprising of,
(a) Boscalid present in an amount of 5% to 15%,
(b) Trifloxystrobin present in an amount of 5% to 15%,
(c) Cyproconazole present in an amount of 5% to 15%, and
(d) Agrochemical additives.

According to the present invention the suitable agrochemical additives are selected from wetting agents, dispersing agents, disintegrating agents, anti-foaming agents, anti-freezing agents, deformers, bactericides, emulsifiers, rheology modifiers, solvents, and fillers.

In yet another aspect, the synergistic fungicidal composition of the present invention is formulated as Water dispersible granule (WG or WDG), Suspension concentrate (SC), Wettable powder (WP), and Suspo emulsions (SE).

In yet another aspect, the present invention is to provide a process for preparation of different types of composition; wherein, these compositions are prepared by mixing appropriate quantity of active ingredients with agrochemically acceptable excipients under certain appropriate conditions.

In yet another aspect, the present invention is to provide a method of effectively controlling fungal infestation/diseases, improving crop health, and increasing crop yield by applying synergistic fungicidal composition of the present invention on infected areas of different varieties of crops, fruits, and vegetables.

In yet another aspect, the present invention is to provide a synergistic fungicidal composition which is active against all life stages of major plant pathogens, and it controls disease severity on different varieties of crops, fruits, and vegetables without showing any phytotoxic effect.

In yet another aspect, the present invention is to provide a fungicidal combination that results into reduced fungal disease incidence in the crops to which it is applied.

In yet another aspect, the present invention is to provide a synergistic fungicidal composition that is stable at higher temperature conditions without affecting the suspensibility and content of actives, thereby increasing shelf life and storage stability of the composition.

In yet another aspect, the present invention is to provide a synergistic fungicidal composition with an improved stability and ready to use fungicidal composition, having superior bio-efficacy compared to the individual formulations.

DETAILED DESCRIPTION OF THE INVENTION
The terms "comprise," "comprises," and "comprising" are to be interpreted inclusively rather than exclusively. Likewise, the terms "include," "including" and "or" should all be construed to be inclusive, unless such a construction is clearly prohibited from the context. However, the embodiments provided by the present disclosure may lack any element that is not specifically disclosed herein. Thus, a disclosure of an embodiment defined using the term "comprising" is also a disclosure of embodiments "consisting essentially of” and "consisting of” the disclosed components. Where used herein, the term "example," particularly when followed by a listing of terms, is merely exemplary and illustrative, and should not be deemed to be exclusive or comprehensive. Any embodiment disclosed herein can be combined with any other embodiment disclosed herein unless explicitly indicated otherwise.

It is to be noted that, as used in the specification, the singular forms "a", "an" and "the" include plural referents unless the context clearly dictates 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.

As used herein, the terms "crops" and "vegetation" can include, for instance, dormant seeds, germinant seeds, emerging seedlings, plants emerging from vegetative propagules, immature vegetation, and established vegetation.

As used herein, immature vegetation may be understood to include small vegetative plants prior to reproductive stage, and mature vegetation may be understood to include vegetative plants during and after the reproductive stage.

As used herein, the terms “fungicide” may be understood as a chemical substance that is used to destroy the parasitic fungi and their spores.

As used herein, a "fungicidally effective amount" may be understood to include an amount of an active ingredient that causes a "fungicidal effect," i.e., an adversely modifying effect including, for instance, a deviation from natural growth or development, killing, regulation, desiccation, growth inhibition, growth reduction, and retardation of fungi.

As used herein, the term “synergistic composition” may be understood to include effective combination of more than one agrochemical that allows the application of the said agrochemical in a much lower dosage, which results in a less dosage treatment for the crops.

As used herein, the term “agrochemical additives” may be understood to include a range of surfactants, dispersing agents, pigments, solvents, co-solvents, defoamers, emulsions, crystallization inhibitors, viscosity modifiers, suspending agents, dyes, antioxidants, light absorbers, mixing aids, neutralizers or pH adjusting substances and buffers, corrosion inhibitors, fragrances, wetting agents, absorption enhancers, micronutrients, plasticizers, lubricants, thickeners, anti-freezing agents, sterilization agents, biocide, adjuvant among others.

The present invention provides a synergistic fungicidal composition comprising of (a) Boscalid, (b) at least one strobilurin fungicide selected from Azoxystrobin, Picoxystrobin, Pyraclostrobin, or Trifloxystrobin, and (c) at least one triazole fungicide selected from Cyproconazole, Prothioconazole, or Tebuconazole along with suitable agrochemical additives.

In an embodiment, the synergistic fungicidal composition comprising Boscalid present in a range from 5% (w/w) to 15% (w/w); a strobilurin fungicide selected from Azoxystrobin, Picoxystrobin, Pyraclostrobin, or Trifloxystrobin present in a range from 5% (w/w) to 15% (w/w); and a triazole fungicide selected from Cyproconazole, Prothioconazole, or Tebuconazole present in a range from 5% (w/w) to 15% (w/w) along with suitable agrochemical additives.

The agrochemically acceptable excipients of the present synergistic fungicidal composition are selected from wetting agents, dispersing agents, disintegrating agents, anti-caking agents, anti-freezing agents, deformers, bactericides, emulsifiers, rheology modifiers solvents, and fillers.

Examples of wetting agents include but not limited to aliphatic alcohol ethoxylates, sodium alkyl naphthalene sulphonate blend, sodium dioctyl sulphosuccinate, sodium isopropyl naphthalene sulfonate, naphthalene sulfonic acid and phenol sulphonic acid sodium salt, tristyrylphenol ethoxylate, and alkyl phenol ethoxylates, either alone or mixtures thereof, present in a range from 1% to 5% (w/w).

Examples of dispersing agents include but not limited to acrylic copolymer, polyaryl phenol ethoxylated phosphate ester, sodium salt of naphthalene sulphonate formaldehyde condensate, potassium salt of polycarboxylates, modified polyacrylate, naphthalene sulfonic acid condensate, condensed methyl naphthalene sulphonate sodium salt, polyaryl phenyl ether phosphate, sodium ligno sulphonates, and tristyryl phenol ethoxylate phosphate esters, either alone or mixtures thereof, present in a range from 1% to 10% (w/w).

Examples of disintegrating agents include but not limited to ammonium sulphate, and sodium sulphate anhydrous, either alone or mixtures thereof, present in a range from 10% to 25% (w/w).

Examples of anti-caking agent include but not limited to silicon dioxide, precipitated silica powder, polydimethylsiloxane, silicon-based agents, either alone or mixtures thereof, present in a range from 0.1% to 5% (w/w).

Examples of anti-freezing agent include but not limited to glycol, polyethylene glycols, mono ethylene glycol, glycerine, diethylene glycol, Propylene glycol, methoxy polyethylene glycols, polypropylene glycols, polybutylene glycols, glycerine, and ethylene glycol, either alone or mixtures thereof, present in a range from 1% to 10% (w/w).

Examples of defoamer include but not limited to silicon emulsion, precipitated silica, fumed silica, modified phyllosilicate, either alone or mixtures thereof, present in a range from 0.1% to 2% (w/w).

Examples of bactericide include but not limited to 1,2-benzisothiazol-3(2H)-one, formaldehyde, sodium benzoate, and 5-chloro-2-methyl-4-isothiazolin-3-one, either alone or mixtures thereof, present in a range from 0.05% to 0.5% (w/w).

Examples of emulsifiers include but not limited to tristyryl phenyl ethoxylate, calcium alkyl benzene sulfonate, either alone or mixtures thereof, present in a range from 1% to 5% (w/w).

Examples of rheology modifier include but not limited to xanthan gum, and aluminium magnesium silicate, either alone or mixtures thereof, present in a range from 5% to 25% (w/w).

Example of solvent include but not limited to aromatic solvent (Solven C9), di-methyl formamide, N-methyl pyrrolidone, heavy aromatic naphtha, either alone or mixtures thereof, present in a range from 10% to 20% (w/w).

Examples of filler include but not limited to distilled water, china-clay, kaolin, and starch, either alone or mixtures thereof, present in Q.S.

In another embodiment, the present invention is formulated into various formulations such as Granular composition (GR), Capsule suspension (CS), Dispersible concentrate (DC), Dustable powder (DP), Powder for dry seed treatment (DS), Emulsifiable concentrate (EC), Emulsifiable granule (EG), Emulsifiable water-in-oil (EO), Emulsifiable powder (EP), Emulsifiable for seed treatment (ES), Emulsifiable oil-in-water, 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), a mixed formulation of CS and SE (ZE), a mixed formulation of CS and EW (ZW).

In another embodiment, the synergistic fungicidal composition of the present invention is formulated as Water dispersible granule (WG or WDG), Suspension concentrate (SC), Wettable powder (WP), and Suspo emulsions (SE).

In yet another embodiment, the present invention discloses the process for preparation of different formulations such as Water dispersible granule (WG or WDG), Suspension concentrate (SC), Wettable powder (WP), and Suspo emulsions (SE); wherein these formulations/compositions prepared by mixing required quantity of active ingredients with agrochemical additives/excipients under certain appropriate conditions. The process for preparation of each composition is provided in the example section.

The present invention provides a synergistic fungicidal composition that is useful as plant disease control agents. The present invention therefore further comprises a method for effectively controlling plant diseases caused by fungal plant pathogens comprising applying to the plant or portion thereof to be protected, or to the plant seed or seedling to be protected, an effective amount of a mixtures of the invention or a fungicidal composition containing said mixture.

In yet another embodiment, the present invention provides a synergistic fungicidal composition that provide control of diseases caused by a broad spectrum of fungal plant pathogens in the Basidiomycete, Ascomycete, Oomycete and Deuteromycete classes. They are effective in controlling a broad spectrum of plant diseases, particularly foliar pathogens of ornamental, vegetable, field, cereal, and fruit crops.

In yet another embodiment, the present invention provides a synergistic fungicidal composition to provide effective control over the diseases caused by abroad spectrum of fungal pathogens preventatively or curatively by applying an effective amount of present mixture or composition either pre-or post-infection, to the portion of the plant to be protected such as the roots, stems, foliage, fruit, seeds, tubers or bulbs, or to the media (soil or sand) in which the plants to be protected are growing, or can also be applied to the seed to protect the seed and seedling.

The composition of the present invention and method provided may be utilized to control fungi and their spores such as Phakopsora pachyrhizi, Magnaporthe oryzae, Botrytis cinerea, Puccinia spp, Fusarium graminearum, Fusarium oxysporum, Blumeria graminis, Mycosphaerella graminicola, Colletotrichum spp.Usti, lago maydis, Melampsora lini, and Rhizoctonia solani among others. in crops or other settings, including but not limited to cereal crops, market gardening, ornamental cultures, vineyards, tree nuts, vegetables, turfgrasses among others.

Examples:
The examples illustrating different embodiments of the present invention are provided herein. However, these are exemplary only and should not be regarded as limiting the elements of the present invention.

Example-1: Boscalid 10% + Azoxystrobin 7.5%+ Cyproconazole 7.5% WDG
S. No. Composition Function % (w/w)
1. Boscalid Active ingredient 10.0
2. Azoxystrobin Active ingredient 7.5
3. Cyproconazole Active ingredient 7.5
4. Sodium Dioctyl Sulphosuccinate Wetting agent 2.0
5. Potassium salt of Polycarboxylates Dispersing agent 3.0
6. Ammonium sulphate Disintegrating Agent 15.0
7. Silicon emulsion Defoamer 0.5
8. Silicon dioxide Anti caking agent 3.0
9. China clay Filler Q.S.

The process for manufacture of composition is as follows: 10.0 gm of Boscalid, 7.5 gm of Azoxystrobin, 7.5 gm of Cyproconazole, 2.0 gm of Sodium Dioctyl Sulphosuccinate, 3.0 gm of Potassium salt of Polycarboxylates, 15.0 gm of ammonium sulphate, 0.5 gm of silicon emulsion, 3.0 gm of silicon dioxide, and required quantity of china clay were weighed in the pre-blender reactor and mixed for 1 hour. The mixture was milled through air jet mill instrument (Inlet pressure 2-3 kg/cm2, grinding pressure 6 kg/ cm2) to obtain the desired particle size (D90 < 12 microns). Collecting the milled material and post blending the material for 1 hour. Extruding the granule at 35 rpm (1.0 mesh), collecting the water dispersible granules, and drying at 50 °C for 30 min (moisture content it should be < 5%) followed by 5 packing the material in a suitable package.

Example-2: Boscalid 10% + Picoxystrobin 7.5% + Cyproconazole 7.5% WDG
S. No. Composition Function % (w/w)
1. Boscalid Active ingredient 10.0
2. Picoxystrobin Active ingredient 7.5
3. Cyproconazole Active ingredient 7.5
4. Sodium Dioctyl Sulphosuccinate Wetting agent 2.0
5. Potassium salt of Polycarboxylates Dispersing agent 3.0
6. Ammonium sulphate Disintegrating Agent 15.0
7. Silicon emulsion Defoamer 0.5
8. Silicon dioxide Anti caking agent 3.0
9. China clay Filler Q.S.

Manufacturing process is similar to the procedure described in Example 1.

Example-3: Boscalid 10% + Trifloxystrobin 7.5% + Cyproconazole 7.5%WDG
S. No. Composition Function % (w/w)
1. Boscalid Active ingredient 10.0
2. Trifloxystrobin Active ingredient 7.5
3. Cyproconazole Active ingredient 7.5
4. Sodium Dioctyl Sulphosuccinate Wetting agent 2.0
5. Potassium salt of Polycarboxylates Dispersing agent 3.0
6. Ammonium sulphate Disintegrating Agent 15.0
7. Silicon emulsion Defoamer 0.5
8. Silicon dioxide Anti caking agent 3.0
9. China clay Filler Q.S.

Manufacturing process is similar to the procedure described in Example 1.

Example-4: Boscalid 10% + Azoxystrobin 7.5% + Cyproconazole 7.5% SC
S. No. Composition Function % (w/w)
1. Boscalid Active ingredient 10.0
2. Azoxystrobin Active ingredient 7.5
3. Cyproconazole Active ingredient 7.5
4. Acrylic Copolymer Dispersing Agent 3.0
5. Alcohol ethoxylates Wetting Agent 2.0
6. 1, 2-Benzisothiazol-3(2H)-one Bactericide 0.1
7. Silicone emulsion Defoamer 0.5
8. Precipitated Silica Powder Anti caking agent 1.0
9. Xanthan Gum Rheology Modifier 15.0
10. Propylene Glycol Anti-freezing agent 5.0
11. Distilled Water Filler Q.S.

2% gum solution was prepared by charging 2 gm of xanthan gum into require quantity of distilled water and homogenizing 12-18 hours prior to use. Charging DM water, 5.0 gm of 1,2-propylene glycol and 0.5 gm of silicone emulsion into designated vessel and mixed thoroughly. Added 3.0 gm of acrylic copolymer, 2.0 gm of alcohol ethoxylates and 1.0 gm of precipitated silica into the vessel having water and homogenize the contents for 45 – 60 minutes using high shear homogenizer. Then add 10 gm of Boscalid technical, 7.5 gm of Azoxystrobin technical and 7.5 gm of Cyproconazole technical to this premix slowly and homogenize to get uniform slurry ready for grinding. The material was subjected to grinding in Dyno mill till desired particle size was achieved. Finally add 2% xanthan gum solution to above milled slurry under stirring condition to achieve SC formulation.

Example-5: Boscalid 10% + Picoxystrobin 7.5% + Cyproconazole 7.5% SC
S. No. Composition Function % (w/w)
1. Boscalid Active ingredient 10.0
2. Picoxystrobin Active ingredient 7.5
3. Cyproconazole Active ingredient 7.5
4. Acrylic Copolymer Dispersing Agent 3.0
5. Alcohol ethoxylates Wetting Agent 2.0
6. 1, 2-Benzisothiazol-3(2H)-one Bactericide 0.1
7. Silicone emulsion Defoamer 0.5
8. Silicon dioxide Anti caking agent 1.0
9. Xanthan Gum Rheology Modifier 15.0
10. Propylene Glycol Anti-freezing agent 5.0
11. Distilled Water Filler Q.S.

Manufacturing process is similar to the procedure described in Example 4.

Example-6: Boscalid 10% + Trifloxystrobin 7.5% + Cyproconazole 7.5% SC
S. No. Composition Function % (w/w)
1. Boscalid Active ingredient 10.0
2. Trifloxystrobin Active ingredient 7.5
3. Cyproconazole Active ingredient 7.5
4. Acrylic Copolymer Dispersing Agent 3.0
5. Alcohol ethoxylates Wetting Agent 2.0
6. 1, 2-Benzisothiazol-3(2H)-one Bactericide 0.1
7. Silicone emulsion Defoamer 0.5
8. Silicon dioxide Anti caking agent 1.0
9. Xanthan Gum Rheology Modifier 15.0
10. Propylene Glycol Anti-freezing agent 5.0
11. Distilled Water Filler Q.S.

Manufacturing process is similar to the procedure described in Example 4.

Example-7: Boscalid 10% + Azoxystrobin 10% + Cyproconazole 10% WP
S. No. Composition Function % (w/w)
1. Boscalid Active ingredient 10.0
2. Azoxystrobin Active ingredient 10.0
3. Cyproconazole Active ingredient 10.0
4. Sodium Dioctyl Sulphosuccinate Wetting agent 2.0
5. Condensed methyl Naphthalene sulphonate sodium salt Dispersing Agent 3.0
6. Silicon dioxide Defoamer 0.5
7. Precipitated Silica Filler 3.0
8. China clay Filler Q.S.

Manufacturing Process: Charging required quantity of Boscalid, Azoxystrobin & Cyproconazole technical in ribbon blender. Then adding 2.0 gm of Sodium Dioctyl Sulphosuccinate, 3.0 gm of Condensed methyl Naphthalene sulphonate sodium salt, 3.0 gm of silica, 0.5 gm of Silicone dioxide and finally adding China clay in required quantity and homogenize it for 30 minutes. Pre-blended material was then ground through Jet mill/ air classifier mills. Finely ground material was blended in post blender till it became homogeneous (for approx. 1.5 hr).

Example-8: Boscalid 10% + Azoxystrobin 10% + Cyproconazole 10% SE
S. No. Composition Function % (w/w)
1. Boscalid Active ingredient 10.0
2. Azoxystrobin Active ingredient 10.0
3. Cyproconazole Active ingredient 10.0
4. Aromatic Solvent Naphtha (Solvent C9) Solvent 15.0
5. Tristyrylphenol Ethoxylates Emulsifier 3.0
6. Acrylic Copolymer Dispersing Agent 3.0
7. Alcohol ethoxylates Wetting Agent 2.0
8. 1, 2-Benzisothiazol-3(2H)-one Bactericide 0.1
9. Silicone emulsion Defoamer 0.5
10. Xanthan Gum Rheology Modifier 15.0
11. Propylene Glycol Anti-freezing agent 5.0
12. Distilled Water Filler Q.S.

Manufacturing Process: 2% gum solution was prepared by charging xanthan gum into require quantity of distilled water and homogenizing 12-18 hours prior to use. Charging DM water, 5.0 gm of 1,2-propylene glycol and 0.5 gm of silicone emulsion into designated vessel and mix thoroughly. Add 3.0 gm of acrylic copolymer, 2.0 gm of alcohol ethoxylates and 0.5 gm of silicon emulsion into the vessel having water and homogenize the contents for 45 – 60 minutes using high shear homogenizer. Then add 10 gm of Boscalid technical and 7.5 gm of Azoxystrobin technical to this premix slowly and homogenize to get uniform slurry ready for grinding. The material was subjected to grinding in Dyno mill till desired particle size was achieved. Charging 15.0 gm of aromatic solvent naphtha (Solvent C9) and adding 7.5 gm of Cyproconazole in mixing vessel and stirring till complete dissolution of Cyproconazole technical. Then adding 3.0 gm of tristyrylphenol ethoxylates and mixed properly to give EC premix.
Then mix SC and EC premix slowly into another vessel and homogenized the contents for 45 – 60 minutes using high shear homogenizer. Finally add 2% gum solution to this formulation to give the suspo-emulsion formulation.

Evaluation of synergistic effect of the fungicidal composition of the present invention:

A synergistic effect exists whenever the action of an active ingredient combination is greater than the sum of the actions of the individual components.

After calculating % disease control, the synergism was calculated by below formula:

The synergistic pesticidal action of the inventive mixtures calculated by Colby’s formula as follows:
Appropriate analysis of plant response to fungicide combination is critical in determining the type of activity observed. The most widely used model is the one Gowing* derived and Colby** modified. Gowing described a mathematical formula for calculating the predicting response values for pesticide mixtures. He suggested the expected (E) percent inhibition of growth induced by pesticide A plus pesticide B is as follows, *(Jerry Flint et al, 1988) ***

The synergistic action expected for a given combination of three active components can be calculated as follows:
(AB + AC + BC) ABC
Expected (E) = A + B + C - +
100 10000

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 A, B and C, respectively).
“A” is the percentage of fungicidal control observed by the compound at a defined dose.
“B” is the percentage of fungicidal control observed by the compound at a defined dose.
“C” is the percentage of fungicidal control observed by the compound at a defined dose.
The synergistic action expected for given combination of two active components can be calculated as follows:

AB
Expected (E) = A + B –
100
Where:
“A” is the percentage of fungicidal control observed by the compound at a defined dose.
“B” is the percentage of fungicidal control observed by the compound at a defined dose.

When the percentage of fungicidal control observed for the combination is greater than the expected percentage, there is a synergistic effect. (Ratio of O/E > 1, means synergism observed.)

Reference:
*Gowing, D. P. 1960. Comments on tests of fungicide mixtures. Weeds 8:379–391.
**Colby, S. R. 1967. Calculating synergistic and antagonistic responses of fungicide combinations. Weeds 15:20–22
*** Jerry Flint et al, 1988. Analyzing Fungicide Interactions: A Statistical Treatment of Colby's Method. Weed Technology 2: 304-309

Field Bio-efficacy trials:
Asian soybean rust, caused by the fungus Phakopsora pachyrhizi, has been the most serious disease that affects soybean crops across the globe, causing losses of up to 80% if not controlled. It’s Infection under favourable temperature and moisture conditions takes place within 6 hours and uredinia can develop in lesions 5 to 8 days afterwards. The first uredinia spores can be produced as early as 9 days after infection, and spore production can continue a uredinium for up to 3 weeks.

The field trial was conducted to evaluate the efficacy of innovative mixtures of Boscalid + Cyproconazole + Strobilurin against Phakopsora pachyrhizi fungus in soybean 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 30-35 days after sowing.

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)

I. Synergistic effect of Boscalid + Cyproconazole + Azoxystrobin combination:

The field trials were carried out at various locations. The percentage efficacy was calculated after 14 days of application. The target weed was Asian Soybean Rust, and the results are recorded in the below table.
Table-1:
Compositions Dose
(GAH) % Asian Soybean Rust control
Expected Actual
Boscalid 25.2 WG 100 55
Cyproconazole 10% SL 75 65
Azoxystrobin 23% SC 75 45
Boscalid 25.2 WG + Cyproconazole 10% SL 100 + 75 84.25 82
Ratio of O/E 0.97
Cyproconazole 10% SL + Azoxystrobin 23% SC 75 + 75 80.75 75
Ratio of O/E 0.92
Boscalid 25.2 WG + Azoxystrobin 23% SC 100 + 75 75.25 72
Ratio of O/E 0.95
Boscalid 10% + Cyproconazole 7.5 % + Azoxystrobin 7.5% WDG 250 91.33 95
Ratio of O/E 1.04
The trial results in above table showed an excellent efficacy of Boscalid 10% + Cyproconazole 7.5 % + Azoxystrobin 7.5% WDG combinations against Asian rust of soybean. The solo application of three active ingredients also tested and were not able to provide satisfactory control of Asian soybean rust disease. The present combination of Boscalid 10% + Cyproconazole 7.5 % + Azoxystrobin 7.5% WDG was found to be very promising against Asian soybean rust in terms of efficacy as well as residual control.

II. Synergistic effect of Boscalid + Cyproconazole + Picoxystrobin combination:

The field trials were carried out at various locations. The percentage efficacy was calculated after 14 days of application. The target weed was Asian Soybean Rust, and the results are recorded in the below table.
Table-2:
Compositions Dose
(GAH) % Asian Soybean Rust control
Expected Actual
Boscalid 25.2 WG 100 55
Cyproconazole 10% SL 75 65
Picoxystrobin 22.52% SC 75 40
Boscalid 25.2 WG + Cyproconazole 10% SL 100 + 75 84.25 82
Ratio of O/E 0.97
Cyproconazole 10% SL + Picoxystrobin 22.52% SC 75 + 75 79 75
Ratio of O/E 0.94
Boscalid 25.2 WG + Picoxystrobin 22.52% SC 100 + 75 73 70
Ratio of O/E 0.95
Boscalid 10% + Cyproconazole 7.5 % + Picoxystrobin 7.5% WDG 250 90.55 95
Ratio of O/E 1.04
The trial results in above table showed an excellent efficacy of Boscalid 10% + Cyproconazole 7.5 % + Picoxystrobin 7.5% WDG combinations against Asian rust of soybean. The solo application of three active ingredients also tested and were not able to provide satisfactory control of Asian soybean rust disease. The present combination of Boscalid 10% + Cyproconazole 7.5 % + Picoxystrobin 7.5% WDG was found to be very promising against Asian soybean rust in terms of efficacy as well as residual control.

III. Synergistic effect of Boscalid + Cyproconazole + Trifloxystrobin combination:
The field trials were carried out at various locations. The percentage efficacy was calculated after 14 days of application. The target weed was Asian Soybean Rust, and the results are recorded in the below table.

Table-3:
Compositions Dose
(GAH) % Asian Soybean Rust control
Expected Actual
Boscalid 25.2 WG 100 55
Cyproconazole 10% SL 75 65
Trifloxystrobin 22% FS 75 50
Boscalid 25.2 WG + Cyproconazole 10% SL 100 + 75 84.25 82
Ratio of O/E 0.97
Cyproconazole 10% SL + Trifloxystrobin 22% FS 75 + 75 82.5 80
Ratio of O/E 0.96
Boscalid 25.2 WG + Trifloxystrobin 22% FS 100 + 75 77.5 75
Ratio of O/E 0.96
Boscalid 10% + Cyproconazole 7.5 % + Trifloxystrobin 7.5% WDG 250 92.12 98
Ratio of O/E 1.08

The trial results in above table showed an excellent efficacy of Boscalid 10% + Cyproconazole 7.5 % + Trifloxystrobin 7.5% WDG combinations against Asian rust of soybean. The solo application of three active ingredients also tested and were not able to provide satisfactory control of Asian soybean rust disease. The present combination of Boscalid 10% + Cyproconazole 7.5 % + Trifloxystrobin 7.5% WDG was found to be very promising against Asian soybean rust in terms of efficacy as well as residual control. ,CLAIMS:WE CLAIM:
1. A synergistic fungicidal composition comprising (a) Boscalid, (b) at least one strobilurin fungicide selected from Azoxystrobin, Picoxystrobin, Pyraclostrobin, or Trifloxystrobin, and (c) at least one triazole fungicide selected from Cyproconazole, Prothioconazole, or Tebuconazole along with suitable agrochemical additives.

2. The composition as claimed in claim 1, where in the Boscalid is present in a range from 5% (w/w) to 15% (w/w).

3. The composition as claimed in claim 1, where in the strobilurin fungicide is selected from Azoxystrobin, Picoxystrobin, Pyraclostrobin, or Trifloxystrobin, present in a range from 5% (w/w) to 15% (w/w).

4. The composition as claimed in claim 1, where in the triazole fungicide selected from Cyproconazole, Prothioconazole, or Tebuconazole, present in a range from 5% (w/w) to 15% (w/w).

5. The composition as claimed in claim 1, wherein the suitable agrochemical additives are selected from wetting agents, dispersing agents, disintegrating agents, anti-foaming agents, anti-freezing agents, deformers, bactericides, emulsifiers, rheology modifiers, solvents, and fillers.

6. The fungicidal composition as claimed in claim 1, wherein the composition is formulated as Suspension concentrate (SC), Water dispersible granule (WG or WDG), Wettable powder (WP), and Suspo emulsions (SE).

7. The fungicidal composition as claimed in claim 1, wherein the formulation is a suspension concentrate (SC) form comprising:
(a) Boscalid present in an amount of 10%, Azoxystrobin present in an amount of 7.5%, and Cyproconazole present in an amount of 7.5%,
(b) Boscalid present in an amount of 10%, Picoxystrobin present in an amount of 7.5%, and Cyproconazole present in an amount of 7.5%, and
(c) Boscalid present in an amount of 10%, Trifloxystrobin present in an amount of 7.5%, and Cyproconazole present in an amount of 7.5%.

8. The fungicidal composition as claimed in claim 1, wherein the formulation is a water dispersible granules (WDG or WG) form comprising:
(a) Boscalid present in an amount of 10%, Azoxystrobin present in an amount of 7.5%, and Cyproconazole present in an amount of 7.5%,
(b) Boscalid present in an amount of 10%, Picoxystrobin present in an amount of 7.5%, and Cyproconazole present in an amount of 7.5%, and
(c) Boscalid present in an amount of 10%, Trifloxystrobin present in an amount of 7.5%, and Cyproconazole present in an amount of 7.5%.

9. The fungicidal composition as claimed in claim 1, wherein the formulation is a suspo emulsion (SE) form comprising (a) Boscalid present in an amount of 10%, (b) Azoxystrobin present in an amount of 10%, (c) Cyproconazole present in an amount of 10%, and (d) agrochemical additives.

10. The fungicidal composition as claimed in claim 1, wherein the formulation is a wettable powder (WP) form comprising (a) Boscalid present in an amount of 10%, (b) Azoxystrobin present in an amount of 10%, (c) Cyproconazole present in an amount of 10%, and (d) agrochemical additives.

Date this Thirtieth (30th) day of May, 2024.

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