FIELD OF THE INVENTION
The present invention relates to a insecticidal compositions comprising first insecticide A, N-
(cyanomethyl)-4-(trifluoromethyl)-3-pyridinecarboxamide and a second insecticide B which is
selected from Abamectin, Chlorantraniliprole, Spirotetramat, Spiromesifen and a third
5 insecticide C different from insecticide A and B which is selected from Bifenthrin,
Deltamethrin, Diafenthiuron, Lambda-cyhalothrin, Pymetrozine and Thiacloprid, formulation
thereof and to a method of controlling undesired insects-pests in crops of useful plants.
BACKGROUND OF THE INVENTION
In economically important crops, higher crop efficiency is achieved by controlling the
10 invertebrate pests. Invertebrate pests cause damage to growing and stored agricultural crops
and thereby result in significant reduction in the crop productivity. Therefore, the control of
invertebrate pests is economically important for the enhanced crop productivity. Many
products are available as solo or in combinations of two or more active ingredients. However,
more economically efficient and ecologically safe insecticidal composition and methods are
15 still being sought.
In order to reduce the risk from increased number of resistant pest strains, mixtures of different
active compounds are nowadays employed for controlling harmful pests. By combining
different active compounds having different mechanism of action, it is possible to effectively
control pests of different groups over a relatively longer period of time and preventing
20 development of resistance. However, this requires continuous development of an effective
composition with different active compounds, so as to avoid selection to the particular
mechanism of action.
Therefore, there exist a need in the art to develop an insecticidal compositions, which are stable,
synergistic, broad spectrum, environmentally safe and effective in control of a wide spectrum
25 of insect pests in crops. The insecticidal compositions must show a broader scope of activity
to avoid or to prevent the development of resistant varieties of strains to the active ingredients
or to the mixtures of known active ingredients used by farmer while minimising the doses of
chemicals sprayed in the agriculture fields.
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As a solution to the above mentioned problems, the inventors of the present invention
surprisingly found that compositions comprising first insecticide A, N-(cyanomethyl)-4-
(trifluoromethyl)-3-pyridinecarboxamide and a second insecticide B which is selected from
Abamectin, Chlorantraniliprole, Spirotetramat, Spiromesifen and a third insecticide C different
5 from insecticide A and B which is selected from Bifenthrin, Diafenthiuron, Deltamethrin,
Lambda-cyhalothrin, Pymetrozine and Thiacloprid provides effective control of a wide
spectrum of insect pests.
SUMMARY OF THE INVENTION
Accordingly, the present invention provides a compositions comprising first insecticide A, N10 (cyanomethyl)-4-(trifluoromethyl)-3-pyridinecarboxamide and a second insecticide B which is
either selected from Abamectin, Chlorantraniliprole, Spirotetramat, Spiromesifen and a third
insecticide C different from insecticide A and B which is either selected from Bifenthrin,
Diafenthiuron, Deltamethrin, Lambda-cyhalothrin, Pymetrozine and Thiacloprid and
agriculturally acceptable excipient(s).
15 In one aspect, the compositions of the present invention comprises first insecticide A, N-
(cyanomethyl)-4-(trifluoromethyl) pyridine-3-carboxamide in the range of 1-20% w/w; a
second insecticide B which is selected from Abamectin in the range of 0.1-3%w/w or
Chlorantraniliprole in the range of 1-15%w/w or Spirotetramat in the range of 1-13%w/w or
Spiromesifen in the range of 3.6-28%w/w; a third insecticide C different from insecticide A
20 and B which is selected from Bifenthrin in the range of 5-27%w/w or Deltamethrin in the range
of 0.1-5%w/w or Diafenthiuron in the range of 14-33%w/w or Lambda cyhalothrin in the range
of 1-8%w/w or Pymetrozine in the range of 5-28%w/w or Thiacloprid in the range of 5-
30%w/w; and agriculturally acceptable excipient(s).
In another aspect, the compositions of the present invention is selected from a group
25 comprising:
a) first insecticide A, N-(cyanomethyl)-4-(trifluoromethyl)-3-pyridinecarboxamide a second
insecticide B, Abamectin and a third insecticide C which is selected from Bifenthrin,
Diafenthiuron, Deltamethrin, Lambda-cyhalothrin, Pymetrozine, Thiacloprid and
agriculturally acceptable excipient(s);
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b) first insecticide A, N-(cyanomethyl)-4-(trifluoromethyl)-3-pyridinecarboxamide a second
insecticide B, Chlorantraniliprole and a third insecticide C which is selected from Bifenthrin,
Diafenthiuron, Deltamethrin, Lambda-cyhalothrin, Pymetrozine, Thiacloprid and
agriculturally acceptable excipient(s);
5 c) first insecticide A, N-(cyanomethyl)-4-(trifluoromethyl)-3-pyridinecarboxamide a second
insecticide B, Spirotetramat and a third insecticide C which is selected from Bifenthrin,
Diafenthiuron, Deltamethrin, Lambda-cyhalothrin, Pymetrozine, Thiacloprid and
agriculturally acceptable excipient(s);
d) first insecticide A, N-(cyanomethyl)-4-(trifluoromethyl)-3-pyridinecarboxamide a second
10 insecticide B, Spiromesifen and a third insecticide C which is selected from Bifenthrin,
Diafenthiuron, Deltamethrin, Lambda-cyhalothrin, Pymetrozine, Thiacloprid and
agriculturally acceptable excipient(s).
In one other aspect, the compositions of the present invention comprises first insecticide A, N-
(cyanomethyl)-4-(trifluoromethyl)-3-pyridinecarboxamide preferably in the range of 4-
15 15%w/w, and a second insecticide B, Abamectin in the range of 0.4-1.2%w/w and a third
insecticide C which is selected from Bifenthrin in the range of 16-24%w/w or Diafenthiuron
in the range of 25-30%w/w or Deltamethrin in the range of 2-3%w/w or Lambda-cyhalothrin
in the range of 3-5%w/w or Pymetrozine in the range of 13-25%w/w or Thiacloprid in the
range of 13-27%w/w and agriculturally acceptable excipient(s).
20 In one other aspect, the compositions of the present invention comprises first insecticide A, N-
(cyanomethyl)-4-(trifluoromethyl)-3-pyridinecarboxamide preferably in the range of 3.5-
15%w/w, and a second insecticide B, Chlorantraniliprole in the range of 3-12%w/w and a third
insecticide C which is selected from Bifenthrin in the range of 8-12%w/w or Diafenthiuron in
the range of 20-30%w/w or Deltamethrin in the range of 2-3%w/w or Lambda-cyhalothrin in
25 the range of 4-5%w/w or Pymetrozine in the range of 8-15%w/w or Thiacloprid in the range
of 12-18%w/w and agriculturally acceptable excipient(s).
In one other aspect, the compositions of the present invention comprises first insecticide A, N-
(cyanomethyl)-4-(trifluoromethyl)-3-pyridinecarboxamide preferably in the range of 3.3-
12.5%w/w, and a second insecticide B, Spirotetramat in the range of 3-10%w/w and a third
30 insecticide C, which is selected from Bifenthrin in the range of 8-12%w/w or Diafenthiuron in
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the range of 17-25%w/w or Deltamethrin in the range of 1-3%w/w or Lambda-cyhalothrin in
the range of 3-4%w/w or Pymetrozine in the range of 8-15%w/w or Thiacloprid in the range
of 8-18%w/w and agriculturally acceptable excipient(s).
In one other aspect, the compositions of the present invention comprises first insecticide A, N5 (cyanomethyl)-4-(trifluoromethyl)-3-pyridinecarboxamide preferably in the range of 3.3-
12.5%w/w, and a second insecticide B, Spiromesifen in the range of 3.6-28%w/w and a third
insecticide C which is selected from Bifenthrin in the range of 8-12%w/w or Diafenthiuron in
the range of 17-25%w/w or Deltamethrin in the range of 1-3%w/w or Lambda-cyhalothrin in
the range of 3-4%w/w or Pymetrozine in the range of 8-15%w/w or Thiacloprid in the range
10 of 8-18%w/w and agriculturally acceptable excipient(s).
In another aspect, the present invention provides a process of preparation of the compositions
comprising first insecticide A, N-(cyanomethyl)-4-(trifluoromethyl)-3-pyridinecarboxamide
and a second insecticide B which is selected from Abamectin, Chlorantraniliprole,
Spirotetramat, Spiromesifen and a third insecticide C different from insecticide A and B which
15 is selected from Bifenthrin, Diafenthiuron, Deltamethrin, Lambda-cyhalothrin, Pymetrozine
and Thiacloprid and agriculturally acceptable excipient(s).
In one another aspect, the compositions of the present invention is formulated as Capsule
suspension (CS), Dispersible concentrate (DC), Dustable powder (DP), Emulsifiable
concentrate (EC), Emulsifiable granule (EG), Emulsion water-in-oil (EO), Emulsifiable
20 powder (EP), Emulsion oil-in-water (EW), Granules (GR), Micro-emulsion (ME), Oildispersion (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
25 (ULV) suspension, Tablet (TB), Ultra-low volume (ULV) liquid, Water dispersible granules
(WDG/WG), Wettable powder (WP), Water dispersible tablet (WT), a mixed formulation of
CS and SC (ZC) or a mixed formulation of CS and SE (ZE), a mixed formulation of CS and
EW (ZW), preferably SC, SE, WP and WDG.
In one another aspect, the compositions of the present invention comprise one or more
30 excipient(s) selected from the group comprising of dispersing agent(s), wetting agent(s),
dispersing cum wetting agent(s), disintegrating agent(s), defoaming agent(s) / defoamer(s) /
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antifoaming agent(s) / antifoamer(s), biocide(s)/preservative(s), viscosity modifier(s)/
rheology modifier(s)/ thickener(s), anti-freeze agent(s), pH stabilizer(s), anti-caking agent(s),
solvent(s), filler(s), diluent(s) or a combination thereof and other additives as will be required
in a particular type of formulation.
5 In another aspect, the composition of the present invention comprises the dispersing agent is
selected from the group comprising ethoxylated polyarylphenol phosphate amine salt,
ethoxylated isodecyl alcohol, polymethyl methacrylate-polyethylene glycol graft copolymer,
blend of acrylic graft copolymer and emulsifier, polymethyl methacrylate-polyethylene oxide
graft copolymer, sodium salt of naphthalene sulfonate condensate, tristyrylphenol ethoxylate,
10 anionic tristyrylphenol phosphate surfactant, non-ionic surfactant, polyalkoxylated butyl ether
dispersant, sodium alkylnaphthalene sulfonate condensate, sodium lignosulphonate, sodium
naphthalene sulphonate salt, sodium alkylnaphthalene sulfonate phenol condensate, sodium
alkylnaphthalene sulfonate formaldehyde condensate, sodium polycarboxylate, modified
styrene acrylic polymeric dispersant, modified styrene acrylic polymeric aqueous dispersant,
15 proprietary blend of phosphate ester and sodium naphthalene sulphate formaldehyde
condensate, lignosulfonic acid dispersant, kraft lignosulfonate with a low degree sulfonation,
modified sodium lignosulphonate, naphthalene sulfonate formaldehyde condensate, mixture of
salt of naphthalene sulphonic acid and phenol, alkyl naphthalene sulfonate sodium salt,
modified naphthalene sulfonate formaldehyde condensate, highly sulfonated kraft lignin,
20 naphthalene sulfonate phenol condensate, sodium isopropyl naphthalene sulfonate or a
combination thereof and present in an amount from 0.1-20% w/w; the wetting agent is selected
from the group comprising sodium alkyl naphthalene sulfonate blend, nonionic proprietary
surfactant blend, sulphonated anionic wetter, copolymer condensate of ethylene and propylene
oxide, ethoxylated isodecyl alcohol, sodium alkyl naphthalene sulfonate formaldehyde
25 condensate, comb-type polymeric surfactant, polyalkylene oxide block copolymer, ethoxylated
polyarylphenol phosphate amine salt, sodium isopropyl naphthalene sulfonate, dibutyl
naphthalene sulfonic acid sodium salt, dialkyl naphthalene sulphonate, sodium dioctyl
sulfosuccinate or a combination thereof and present in an amount from 0.1-10% w/w; the
dispersing cum wetting agent is selected from the group comprising proprietary blend of
30 phosphate ester and sodium naphthalene sulfonate formaldehyde condensate, highly
sulfonation and low molecular weight kraft lignin polymer, sodium salt of aromatic ring
surfactant, ammonium salt of aromatic ring surfactant, sodium salt of naphthalene sulphonic
acid condensation, proprietary blend of anionic surfactant, Jeemox 1269 (Jeevan chemicals
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private limited), proprietary blend of polymeric surfactant, sodium methyl oleoyl taurate,
tristyrylphenol ethoxylate phosphate ester or a combination thereof and present in an amount
from 2-10% w/w; the disintegrating agent is selected from ammonium sulphate, lactose or a
combination thereof and present in an amount from 5-25% w/w; the antifoamer/defoamer is
5 selected from the group comprising polydimethylsiloxane antifoam emulsion, silicon
emulsion, polysiloxane emulsion or a combination thereof and present in an amount from 0.01
to 2% w/w; the biocide/preservative is selected from the group comprising 20% aqueous
dipropyleneglycol solution of 1,2- benzisothiazolin-3-one, formaldehyde, isothiazolinone or a
combination thereof and present in an amount from 0.01 to 1% w/w; the thickener is selected
10 from the group comprising xanthan gum, welan gum, guar gum, polyvinyl alcohol,
carboxymethylcellulose, polyvinylpyrrolidone, carboxyvinyl polymer, acrylic polymer, starch
derivative, polysaccharide, high purity silica, white carbon or a combination thereof and
present in an amount from 0.1-5% w/w; the anti-freeze agent is selected from the group
comprising glycerol, propylene glycol, diethylene glycol, monoethylene glycol or a
15 combination thereof and present in an amount from 0.1 to 10% w/w; the pH stabilizer is citric
acid and present in an amount from 0.1 to 3% w/w; the anti-caking agent is silica and present
in an amount from 0.1 to 6% w/w; the solvent is selected from the group comprising naphtha,
butan-1-ol, xylene, decanamide, N-methyl-2-pyrrolidone, dimethyl sulfoxide, cyclohexanone,
solvent C9, water or a combination thereof and present in an amount from 1 to 10% w/w; the
20 filler is selected from the group comprising, silica, precipitated silica, sodium bicarbonate,
china clay, lactose, bentonite clay, kaolin, diatomaceous earth or a combination thereof and
present in an amount quantity sufficient; and the diluent is demineralised water and present in
an amount quantity sufficient.
DETAILED DESCRIPTION OF THE INVENTION
25 The definitions provided herein for the terminologies used in the present disclosure are for
illustrative purpose only and in no manner limit the scope of the present invention disclosed in
the present disclosure.
Unless defined otherwise, all technical and scientific terms used herein have the same meaning
as commonly understood by a person of ordinary skill in the art to which the invention pertains.
30 Although other methods and materials similar, or equivalent, to those described herein can be
used in the practice of the present invention, the preferred materials and methods are described
herein.
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It is to be noted that, as used in the specification and the appended claims, 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
5 sense including “and/or” unless the content clearly dictates otherwise.
As used herein, the terms "comprises", "comprising", "includes", "including", “has”, “having”,
“contains”, “containing”, “characterized by” or any other variation thereof, are intended to
cover a non-exclusive inclusion, subject to any limitation explicitly indicated. For example, a
composition, mixture, process or a method that comprises a list of elements is not necessarily
10 limited to only those elements but may include other elements not expressly listed or inherent
to such composition, mixture, process or method.
The transitional phrase “consisting of” excludes any element, step or ingredient not specified.
If in the claim, such would close the claim to the inclusion of materials other than those recited
except for impurities ordinarily associated therewith. When the phrase “consisting of” appears
15 in a clause of the body of a claim, rather than immediately following the preamble, it limits
only the element set forth in that clause; other elements are not excluded from the claim as a
whole.
As used herein, the terms “composition” or “compositions” or "formulation" or "formulations"
can be used interchangeably, unless stated otherwise, is meant to encompass, and are not
20 limited to, compositions or formulations containing the combination of N-(cyanomethyl)-4-
(trifluoromethyl)-3-pyridinecarboxamide and a second insecticide B which is selected from
Abamectin, Chlorantraniliprole, Spirotetramat, Spiromesifen and a third insecticide C different
from insecticide A and B which is selected from Bifenthrin, Diafenthiuron, Deltamethrin,
Lambda-cyhalothrin, Pymetrozine and Thiacloprid.
25 As used herein, the term “agriculturally acceptable excipient (s)” refers to inert substances and
are auxiliary substances added to the processing or use of pesticide preparations and used to
improve the physical and chemical properties of formulations. The auxiliaries themselves are
essentially free of biological activity, but can affect the control effect.
The expression of various quantities in terms of “% w/w” or “%” means the percentage by
30 weight, relative to the weight of the total solute on or composition unless otherwise specified.
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The term “active ingredient” (a.i.) or “active agent” used herein refers to that component of the
composition responsible for control of insects-pests in crops of useful plants.
As used herein, the term "effective amount" means the amount of the active substances in the
compositions to achieve an observable effect on death, retardation, prevention, and removal,
5 destruction, or otherwise diminishing the occurrence and activity of the target pests. An
effective amount of the compositions will also vary according to the prevailing conditions such
as desired insecticidal effect and duration, weather, target pests and species, target crops, locus,
mode of application, and the like.
As used herein, the term “insecticide”, refers to any chemical substance used to destroy/kill,
10 inhibit or otherwise adversely affect the insect pests.
As used herein, “N-(cyanomethyl)-4-(trifluoromethyl)-3-pyridinecarboxamide” is a pyridine
carboxamide derivative compound and commonly known as “Flonicamid”. The term
“Flonicamid” encompasses Flonicamid or its agrochemically acceptable salt(s), derivative(s)
15 or any other modified form of Flonicamid. Flonicamid acts by inhibiting feeding and has
systemic and translaminar activity. It is used to control aphids and some other sucking insects
in fruit, cereals, potatoes, cotton, tea and vegetables.
As used herein, the term “Abamectin” encompasses its agrochemically acceptable salt(s),
derivative(s) or any other modified form of Abamectin. Abamectin is a mixture of Avermectin
20 B1a and Avermectin B1b wherein Avermectin B1a is representing by CAS name 5-O-demethyl
avermectin A1a and Avermectin B1b is representing by CAS name 5-O-demethyl-25-de (1-
methylpropyl)-25-(1-methylethyl) avermectin A1a. Abamectin is known for its insecticide,
acaricide (miticide) and a nematicide activities. It acts by stimulating the release of gamma
aminobutyric acid, an inhibitory neurotransmitter, thus finally activating chloride channels. It
25 is used for control of motile stage of mites, leaf miners, suckers, beetles etc. on ornamentals,
cotton, citrus fruit, pome fruit, nut crops, vegetables, potatoes and other crops.
As used herein, the term “Chlorantraniliprole” encompasses its agrochemically acceptable
salt(s), derivative(s) or any other modified form of Chlorantraniliprole. Chlorantraniliprole
having CAS name 3-bromo-N-[4-chloro-2-methyl-6-[(methylamino) carbonyl] phenyl]-1-(3-
30 chloro-2-pyridinyl)-1H-pyrazole-5-carboxamide belongs to the class of diamide insecticide. It
acts by activation of ryanodine receptors, leading to loss of internal calcium stores. It is used
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for control of wide range of chewing pests primarily Lepidoptera, Coleoptera, Dipetra and
Isoptera in a broad range of crops including fruit, vegetables, vines, cotton, sugarcane, rice and
grass.
As used herein, the term “Spirotetramat” encompasses its agrochemically acceptable salt(s),
5 polymorph(s), derivative(s) or any other modified form of Spirotetramat. Spirotetramat having
CAS name cis-3-(2,5-dimethylphenyl)-8-methoxy-2-oxo-1-azaspiro[4,5]dec-3-en-4-yl ethyl
carbonate, belongs to the class of tetramic acid. It affects lipid biosynthesis through inhibition
of acetyl CoA carboxylase, acting mainly after ingestion but also on contact, affecting eggs
and larvae, with additional effects on adult fecundity. After penetrating the leaves, it is de10 esterified, and transported within both the xylem and phloem. It also has translaminar activity.
It is used for control of a range of sucking insects including whitefly, aphids, scales, mealybugs,
psyllids and thrips species in vegetables, cotton, soybeans, pome and stone fruits, grapes,
hopes, citrus, nut trees and bananas.
As used herein, the term “Spiromesifen” encompasses its agrochemically acceptable salt(s),
15 polymorph(s), derivative(s) or any other modified form of Spiromesifen. Spiromesifen having
CAS name 2-oxo-3-(2, 4, 6-trimethylphenyl)-1-oxasipro [4,4]non-3-en-4-yl 3, 3-dimethyl
butanoate, belongs to the class of tetronic acid. It is a lipid biosynthesis inhibitor and
nonsystemic. It is effective against whiteflies and against tetranychus spp.,
polyphagotarsonemus spp., and Paratrioza spp., in cotton, maize, potatoes, vegetables and
20 ornamentals.
As used herein, the term “Bifenthrin” encompasses its agrochemically acceptable salt(s),
derivative(s) or any other modified form of Bifenthrin. Bifenthrin having CAS name (2-methyl
[1,1’-biphenyl]-3-yl)methyl(1R.3R)-rel-3-[(1Z)-2-chloro-3,3,3-trifluoro-1-propen-1-yl]-2,2-
dimethylcyclopropanecarboxylate, belongs to the class of pyrethroid. It acts on the nervous
25 system of insects, disturbs the function of neurons by interaction with the sodium channel. It is
effective against a broad range of foliar pests in cereals, citrus, cotton, fruit, grapes,
ornamentals and vegetables.
As used herein, the term “Diafenthiuron” encompasses its agrochemically acceptable salt(s),
polymorph(s), derivative(s) or any other modified form of Diafenthiuron. Diafenthiuron having
30 CAS name N-[2,6-bis(1-methylethyl)-4-phenoxyphenyl]-N’-(1,1-dimethylethyl)thiourea,
belongs to the class of thiourea insecticide/acaricide. Diafenthiuron is a potent in vivo inhibitor
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of mitochondrial respiration. It is an insecticide/acaricide which kills larvae, nymphs and adults
by contact and/or stomach action and also shows some ovicidal action. It is effective against
phytophagous mites and other sucking pests in cotton, various field and fruit crops, ornamental
plants and vegetables.
5 As used herein, the term “Deltamethrin” encompasses its agrochemically acceptable salt(s),
derivative(s) or any other modified form of Deltamethrin. Deltamethrin having CAS name (S)-
cyano (3-phenoxyphenyl) methyl (1R, 3R)-3-(2,2-dibromoethenyl)-2,2-
dimethylcyclopropanecarboxylate, belongs to pyrethroid group of insecticides. It is a nonsystemic insecticide with contact and stomach action. It prevents the sodium channels from
10 functioning, so that no transmission of nerve impulses can take place. It is potent insecticide
effective by contact and ingestion against a wide range of pests in cereals, citrus, cotton, grapes,
maize, oilseed rape, soybeans, top fruits and vegetables.
As used herein, the term “Lambda-cyhalothrin” encompasses its agrochemically acceptable
salt(s), derivative(s) or any other modified form of Lambda-cyhalothrin. Lambda-cyhalothrin
15 having CAS name cyano (3-phenoxyphenyl) methyl 3-(2-chloro-3,3,3-trifluoro-1-propen-1-
yl)-2,2-dimethylcyclopropanecarboxylate, belongs to the class of pyrethroid insecticide. It is a
non-systemic insecticide with contact and stomach action, and repellent properties. It acts on
the nervous system of insects and disturbs the function of neurons by interaction with sodium
channel. It controls aphids, beetles, thrips, Lepidoptera larvae, Coleoptera larvae and adults
20 etc. in cereals, hops, ornamentals, potatoes, vegetables and other crops.
As used herein, the term “Pymetrozine” encompasses its agrochemically acceptable salt(s),
derivative(s) or any other modified form of Pymetrozine. Pymetrozine having CAS name 4, 5-
dihydro-6-methyl-4-[(E)-(3-pyridinylmethylene) amino]-1, 2, 4-triazin-(2H)-one, belongs to
the class of pyridine azomethine insecticide. Pymetrozine is selective against Homoptera,
25 causing them to stop feeding. It provides control of juvenile and adult stages of aphids and
whiteflies in vegetables, potatoes, ornamental, cotton, deciduous fruit, citrus, tobacco and hops
and plant hoppers in rice.
As used herein, the term “Thiacloprid” encompasses its agrochemically acceptable salt(s),
derivative(s) or any other modified form of Thiacloprid. Thiacloprid having CAS name [N
30 (Z)]-[3-[(6-chloro-3-pyridinyl) methyl]-2-thiazolidinylidene] cyanamide, belongs to the class
of neonicotinoid insecticide. It acts as an agonist of the nicotinic acetylcholine receptor in the
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central nervous system, thus disturbing synaptic signal transmissions. It is used against sucking
and biting insects in pome fruit, stone fruit, small berries, cotton, vegetables, sugar beet,
potatoes, rice and ornamentals.
In an embodiment, the present invention provides a synergistic insecticidal compositions
5 comprising first insecticide A, N-(cyanomethyl)-4-(trifluoromethyl)-3-pyridinecarboxamide
and a second insecticide B which is selected from Abamectin, Chlorantraniliprole,
Spirotetramat, Spiromesifen and a third insecticide C different from insecticide A and B which
is selected from Bifenthrin, Diaffenthiuron, Deltamethrin, Lambda-cyhalothrin, Pymetrozine
and Thiacloprid and agriculturally acceptable excipient(s).
10 In an embodiment, the compositions of the present invention comprises first insecticide A, N-
(cyanomethyl)-4-(trifluoromethyl) pyridine-3-carboxamide in the range of 1-20%w/w; a
second insecticide B which is selected from Abamectin in the range of 0.1-3%w/w or
Chlorantraniliprole in the range of 1-15%w/w or Spirotetramat in the range of 1-13%w/w or
Spiromesifen in the range of 3.6-28%w/w; a third insecticide C different from insecticide A
15 and B which is selected from Bifenthrin in the range of 5-27%w/w or Deltamethrin in the range
of 0.1-5%w/w or Diafenthiuron in the range of 14-33%w/w or Lambda cyhalothrin in the range
of 1-8%w/w or Pymetrozine in the range of 5-28%w/w or Thiacloprid in the range of 5-
30%w/w and agriculturally acceptable excipient(s).
In an embodiment, the compositions of the present invention is selected from a group
20 comprising first insecticide A, N-(cyanomethyl)-4-(trifluoromethyl)-3-pyridinecarboxamide a
second insecticide B, Abamectin and a third insecticide C which is selected from Bifenthrin,
Diafenthiuron, Deltamethrin, Lambda-cyhalothrin, Pymetrozine, Thiacloprid and
agriculturally acceptable excipient(s) or first insecticide A, N-(cyanomethyl)-4-
(trifluoromethyl)-3-pyridinecarboxamide a second insecticide B, Chlorantraniliprole and a
25 third insecticide C which is selected from Bifenthrin, Diafenthiuron, Deltamethrin, Lambdacyhalothrin, Pymetrozine, Thiacloprid and agriculturally acceptable excipient(s) or first
insecticide A, N-(cyanomethyl)-4-(trifluoromethyl)-3-pyridinecarboxamide a second
insecticide B, Spirotetramat and a third insecticide C which is selected from Bifenthrin,
Diafenthiuron, Deltamethrin, Lambda-cyhalothrin, Pymetrozine, Thiacloprid and
30 agriculturally acceptable excipient(s) or first insecticide A, N-(cyanomethyl)-4-
(trifluoromethyl)-3-pyridinecarboxamide a second insecticide B, Spiromesifen and a third
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insecticide C which is selected from Bifenthrin, Diafenthiuron, Deltamethrin, Lambdacyhalothrin, Pymetrozine, Thiacloprid and agriculturally acceptable excipient(s).
In an embodiment, the compositions of the present invention comprises first insecticide A, N-
(cyanomethyl)-4-(trifluoromethyl)-3-pyridinecarboxamide preferably in the range of 4-
5 15%w/w, and a second insecticide B, Abamectin in the range of 0.4-1.2%w/w and a third
insecticide C which is selected from Bifenthrin in the range of 16-24%w/w or Diafenthiuron
in the range of 25-30%w/w or Deltamethrin in the range of 2-3%w/w or Lambda-cyhalothrin
in the range of 3-5%w/w or Pymetrozine in the range of 13-25%w/w or Thiacloprid in the
range of 13-27%w/w and agriculturally acceptable excipient(s).
10 In an embodiment, the compositions of the present invention comprises first insecticide A, N-
(cyanomethyl)-4-(trifluoromethyl)-3-pyridinecarboxamide preferably in the range of 3.5-
15%w/w, and a second insecticide B, Chlorantraniliprole in the range of 3-12%w/w and a third
insecticide C which is selected from Bifenthrin in the range of 8-12%w/w or Diafenthiuron in
the range of 20-30%w/w or Deltamethrin in the range of 2-3%w/w or Lambda-cyhalothrin in
15 the range of 4-5%w/w or Pymetrozine in the range of 8-15%w/w or Thiacloprid in the range
of 12-18%w/w and agriculturally acceptable excipient(s).
In an embodiment, the compositions of the present invention comprises first insecticide A, N-
(cyanomethyl)-4-(trifluoromethyl)-3-pyridinecarboxamide preferably in the range of 3.3-
12.5%w/w, and a second insecticide B, Spirotetramat in the range of 3-10%w/w and a third
20 insecticide C, which is selected from Bifenthrin in the range of 8-12%w/w or Diafenthiuron in
the range of 17-25%w/w or Deltamethrin in the range of 1-3%w/w or Lambda-cyhalothrin in
the range of 3-4%w/w or Pymetrozine in the range of 8-15%w/w or Thiacloprid in the range
of 8-18%w/w and agriculturally acceptable excipient(s).
In an embodiment, the compositions of the present invention comprises first insecticide A, N25 (cyanomethyl)-4-(trifluoromethyl)-3-pyridinecarboxamide preferably in the range of 3.3-
12.5%w/w, and a second insecticide B, Spiromesifen in the range of 3.6-28%w/w and a third
insecticide C which is selected from Bifenthrin in the range of 8-12%w/w or Diafenthiuron in
the range of 17-25%w/w or Deltamethrin in the range of 1-3%w/w or Lambda-cyhalothrin in
the range of 3-4%w/w or Pymetrozine in the range of 8-15%w/w or Thiacloprid in the range
30 of 8-18%w/w and agriculturally acceptable excipient(s).
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In another embodiment, the compositions of the present invention is formulated as Capsule
suspension (CS), Dispersible concentrate (DC), Dustable powder (DP), Emulsifiable
concentrate (EC), Emulsifiable granule (EG), Emulsion water-in-oil (EO), Emulsifiable
powder (EP), Emulsion oil-in-water (EW), Granules (GR), Micro-emulsion (ME), Oil5 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
10 (WDG/WG), Wettable powder (WP), Water dispersible tablet (WT), a mixed formulation of
CS and SC (ZC) or a mixed formulation of CS and SE (ZE), a mixed formulation of CS and
EW (ZW), preferably SC, SE, WP and WDG.
In one other embodiment, the compositions of the present invention comprise one or more
excipient(s) selected from the group comprising of dispersing agent(s), wetting agent(s),
15 dispersing cum wetting agent(s), disintegrating agent(s), defoaming agent(s) / defoamer(s) /
antifoaming agent(s) / antifoamer(s), biocide(s)/preservative(s), viscosity modifier(s)/
rheology modifier(s)/ thickener(s), anti-freeze agent(s), pH stabilizer(s), anti-caking agent(s),
solvent(s), filler(s), diluent(s) or a combination thereof and other additives as will be required
in a particular type of formulation.
20 The compositions of present invention uses dispersing agents to prevent agglomeration of solid
particles and keep them suspended in fluid. Non-limiting examples of dispersing agent that can
be used in the present invention include, but not limited to ethoxylated polyarylphenol
phosphate amine salt, ethoxylated isodecyl alcohol, polymethyl methacrylate-polyethylene
glycol graft copolymer, blend of acrylic graft copolymer and emulsifier, polymethyl
25 methacrylate-polyethylene oxide graft copolymer, sodium salt of naphthalene sulfonate
condensate, tristyrylphenol ethoxylate, anionic tristyrylphenol phosphate surfactant, non-ionic
surfactant, polyalkoxylated butyl ether dispersant, sodium alkylnaphthalene sulfonate
condensate, sodium lignosulphonate, sodium naphthalene sulphonate salt, sodium
alkylnaphthalene sulfonate phenol condensate, sodium alkylnaphthalene sulfonate
30 formaldehyde condensate, sodium polycarboxylate, modified styrene acrylic polymeric
dispersant, modified styrene acrylic polymeric aqueous dispersant, proprietary blend of
phosphate ester and sodium naphthalene sulphate formaldehyde condensate, lignosulfonic acid
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dispersant, kraft lignosulfonate with a low degree sulfonation, modified sodium
lignosulphonate, naphthalene sulfonate formaldehyde condensate, mixture of salt of
naphthalene sulphonic acid and phenol, alkyl naphthalene sulfonate sodium salt, modified
naphthalene sulfonate formaldehyde condensate, highly sulfonated kraft lignin, naphthalene
5 sulfonate phenol condensate, sodium isopropyl naphthalene sulfonate. One or more dispersing
agents may be used in the compositions of the present invention. The dispersing agent is present
in the range from 0.1-20% w/w.
The compositions of present invention uses wetting agent to facilitate the process of dispersion
of the granules in the liquid. Non-limiting examples of wetting agents that can be used in the
10 present invention include, but not limited to sodium alkyl naphthalene sulfonate blend,
nonionic proprietary surfactant blend, sulphonated anionic wetter, copolymer condensate of
ethylene and propylene oxide, ethoxylated isodecyl alcohol, sodium alkyl naphthalene
sulfonate formaldehyde condensate, comb-type polymeric surfactant, polyalkylene oxide block
copolymer, ethoxylated polyarylphenol phosphate amine salt, sodium isopropyl naphthalene
15 sulfonate, dibutyl naphthalene sulfonic acid sodium salt, dialkyl naphthalene sulphonate,
sodium dioctyl sulfosuccinate. One or more wetting agents may be used in the compositions of
the present invention. The wetting agents is present in the range from 0.1-10% w/w.
The compositions of present invention also uses dispersing cum wetting agent. Non-limiting
examples of dispersing cum wetting agent that can be used in the present invention include,
20 but not limited to, proprietary blend of phosphate ester and sodium naphthalene sulfonate
formaldehyde condensate, highly sulfonation and low molecular weight kraft lignin polymer,
sodium salt of aromatic ring surfactant, ammonium salt of aromatic ring surfactant, sodium salt
of naphthalene sulphonic acid condensation, proprietary blend of anionic surfactant, Jeemox
1269, proprietary blend of polymeric surfactant, sodium methyl oleoyl taurate, tristyrylphenol
25 ethoxylate phosphate ester. One or more dispersing cum wetting agent may be used in the
compositions of the present invention. Dispersing cum wetting agent is present in the range
from 2-10% w/w.
The compositions of present invention also uses disintegrating agent that can swell or
disintegrate the composition. Non-limiting examples of disintegrating agent that can be used
30 in the present invention include, but not limited to, ammonium sulphate, lactose. One or more
disintegrating agent may be used in the compositions of the present invention. Disintegrating
agent is present in the range from 5-25% w/w.
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The composition of present invention also uses defoaming agent. The term “defoaming
agent(s)” or “defoamer(s)” or “antifoaming agent(s)” “antifoamer(s)” refers to a chemical
additive that reduces and hinders the formation of foam in liquid, semi-solid, or solid
formulations. The terms defoaming agent and anti-foaming agent can be used interchangeably.
5 Suitable defoamer used herein, but not limited to, polydimethylsiloxane antifoam emulsion,
silicon emulsion, polysiloxane emulsion, organic fluorine compounds. One or more defoaming
agent may be used in the compositions of the present invention. Defoaming agent is present in
the range from 0.01 to 2% w/w.
The compositions of present invention uses biocide/preservatives to prevent the composition
10 from spoilage due to bacteria, yeasts and fungi or deterioration due to undesirable chemical
changes. Suitable biocide/preservative used herein, but not limited to 20% aqueous dipropylene
glycol solution of 1,2- benzisothiazolin-3-one, formaldehyde, potassium sorbate, 4-
hydroxybenzoic acid esters, 2-methyl-4-isothiazolin-3-one, 5-chloro-2-methyl-4-isothiazolin3-one or a combination thereof and present in the range from 0.01-1% w/w.
15 The compositions of present invention uses thickener which are usually polymeric material,
and at a low concentration increases the viscosity of an aqueous solution and helps to stabilize
the composition. Suitable thickener used herein, but not limited to xanthan gum, welan gum,
guar gum, polyvinyl alcohol, carboxymethylcellulose, polyvinylpyrrolidone, carboxyvinyl
polymer, acrylic polymer, starch derivative, polysaccharide, high purity silica, white carbon or
20 a combination thereof and present in the range from 0.1-5% w/w.
The compositions of present invention uses anti-freeze agent which are used to prevent
deleterious effects due to freezing and lyophilization (lyophilisation). Suitable anti-freeze agent
used herein, but not limited to glycerol, propylene glycol, diethylene glycol, monoethylene
glycol or a combination thereof and present in the range from 0.1 to 10% w/w.
25 The compositions of present invention uses pH stabilizer also known as pH modifier and is
used in any agrochemically acceptable composition for increasing or decreasing pH to have a
storage stable formulation. The pH stabilizer is citric acid and present in the range from 0.1 to
3% w/w.
The compositions of present invention uses anti-caking agent. The anti-caking agent is silica
30 and present in the range from 0.1 to 6% w/w.
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The compositions of present invention uses solvent. Suitable solvent is selected from the group
comprising naphtha, butan-1-ol, xylene, decanamide, N-methyl-2-pyrrolidone, dimethyl
sulfoxide, cyclohexanone, solvent C9, water or a combination thereof and present in range from
1 to 10% w/w.
5 The compositions of present invention uses filler. Suitable fillers that may be used in the
compositions of the present invention include, but not limited to, silica, precipitated silica,
sodium bicarbonate, china clay, lactose, bentonite clay, kaolin, diatomaceous earth. The filler
may be used in an amount of quantity sufficient to make 100%w/w formulation.
The compositions of present invention uses diluents. Suitable diluents that may be used in the
10 composition of the present invention is demineralised water and present in an amount quantity
sufficient to make 100%w/w formulation.
The compositions of the present invention is found to be effective to control wide spectrum of
insect pests from the orders of Lepidoptera, Isoptera, Acarina, Thysanoptera, particularly the
compositions of present invention gave excellent control on aphid, jassids, whitefly, mites,
15 thrips, shoots and fruits borer, stem borer, leaf folder and BPH. Further the composition of the
present invention may be used to control variety of insect pests in cereals, paddy/rice, pulses,
oilseeds, horticulture crops, fibre crops, vegetables and spice crops, particularly the
compositions of present invention tested on Tea, Cotton, Rice, Brinjal and Chilli crops and
gave better results compared to solo and binary compositions.
20 The present invention also provides a process of preparing a compositions comprising first
insecticide A, N-(cyanomethyl)-4-(trifluoromethyl)-3-pyridinecarboxamide and a second
insecticide B which is selected from Abamectin, Chlorantraniliprole, Spirotetramat,
Spiromesifen and a third insecticide C different from insecticide A and B which is selected
from Bifenthrin, Diafenthiuron, Deltamethrin, Lambda-cyhalothrin, Pymetrozine and
25 Thiacloprid and agriculturally acceptable excipient(s).
In an embodiment, the present invention provides a process for the preparation of a WP
formulations which comprises: a) weighing and mixing of required active ingredients and other
ingredients; b) milling in a suitable air jet mill; c) grinding the material to obtain desired particle
size (D90- <10 micron) and d) mixing homogeneously in a blender to obtain the wettable
30 powder formulation.
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In an embodiment, the present invention provides a process for the preparation of a WDG
formulations which comprises: a) preparing homogenous mixture of all ingredients; b) milling
and grinding till desired particle size; c) preparing dough; d) extruding the granules and drying
to obtain the water dispersible granules formulation.
5
In another embodiment, the present invention provides a process for the preparation of a SC
formulations which comprises: a) diluting and solubilizing a biocide, defoamer, antifreeze
agent and anti-settling agent in demineralised water in a mixing vessel and adding dispersing
and wetting agent under stirring to get homogeneous mixture; b) adding active ingredients one
10 by one under stirring and mixing till homogeneous slurry obtained; c)wet grinding at suitable
temperature till desired particle size obtained, and d) adding previously prepared viscosity
modifier solution and stirring to obtain SC formulation.
In another embodiment, the present invention provides a process for the preparation of a SE
formulations. The process comprises: a) mixing of excipients and active ingredients to prepare
15 to prepare a first composition in the form of SC, b) mixing at least one active ingredient with
a solvent, an emulsifier (second dispersing agent) to obtain a second composition in the form
of EC; e) mixing of first composition, second composition results in a composition of the
present invention in SE form.
The compositions of the present invention can be applied by any one of the methods selected
20 from atomization, spreading, dusting, spraying, diffusion, immersion, irrigation (chemigation),
injection, mixing, sprinkling (water immersion), foaming, dressing, coating, blasting,
fumigation, smoking, smog and painting.
The rate of application amount of the prepared compositions varies depending on, for example,
25 the blending ratio of active ingredients, meteorological condition, dosage form, application
time, application method, application place, weed to be controlled, and a target crop, in
ordinary cases.
The inventors of the present invention have surprisingly found that the compositions of the
present invention showed enhances control over existing compositions. Moreover the
30 composition of the present invention is more effective than their individual counterparts. This
allows a substantial reduction in the application rates of each of these active ingredients, while
maintaining good efficacy. The decrease in application rates reduces treatment cost to the
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farmer and also eases the burden on the environment both from manufacturing waste and crop
protection chemical residues.
The insecticidal compositions of present invention provides a wide spectrum control of insectpests, delays the emergence of the resistant strains, minimizes the risk of development of
5 resistance and achieves effective and economical control of undesired insect-pest.
The insecticidal compositions of the present invention provides a number of other advantages:
 Increased efficacy in comparison to the other formulations tested during the trial.
 Is synergistic hence denies the need of sequential application of solo insecticides to
control different pest spectra thereby reducing the environmental load of insecticides.
10  Uses lesser amounts of active ingredients hence considerable reduction in cost, which
would benefit farmers.
 The compositions provided one shot solution to farmers to control broad spectrum of
pests.
 Is storage stable.
15  Is non-phytotoxic.
 Reduction in environmental load of insecticidal residues.
 Reduction in quantity of water required for spray of the product in agriculture fields.
 Reduction in generation of empty containers of product, thereby, reducing concerns of
their disposal.
20  Provides a broad range of product choice for effective pest management.
Thus, from the foregoing description, it will be apparent to one of the person skilled in the art
that many changes and modifications can be made thereto without departing from the scope of
the invention as set forth in the description. Accordingly, it is not intended that the scope of the
25 foregoing description be limited to the description set forth above, but rather that such
description be construed as encompassing such features that reside in the present invention,
including all the features and embodiments that would be treated as equivalents thereof by
those skilled in the relevant art.
The embodiments of the present invention are more particularly described in the following
30 examples that are intended as illustrations only, since numerous modifications and variations
within the scope of the present invention will be apparent to those of skill in the art. Unless
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otherwise noted, all parts, percentages and ratios reported in the following examples are on a
weight basis and all reagents used in the examples were obtained or are available from the
chemical suppliers.
EXAMPLES
5 The insecticidal compositions of the present invention comprising first insecticide A, N-
(cyanomethyl)-4-(trifluoromethyl)-3-pyridinecarboxamide, and a second insecticide B which
is selected from Abamectin, Chlorantraniliprole, Spirotetramat, Spiromesifen and a third
insecticide C different from insecticide A and B which is selected from Bifenthrin,
Diafenthiuron, Deltamethrin, Lambda-cyhalothrin, Pymetrozine and Thiacloprid, in the form
10 of suspension concentrate (SC), suspoemulsion (SE), wettable powder (WP) and water
dispersible granule (WDG) is provided in table 1-135. The unit of each component of the
compositions are expressed in “% w/w” i.e. the percentage by weight, relative to the weight of
the total solution or composition. All the compositions are prepared by following the processes
as disclosed in description. All the prepared composition of the present invention has been
15 tested for stability/shelf life at accelerated temperature.