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Renofluthrin Insecticidal Composition

Abstract: ABSTRACT RENOFLUTHRIN INSECTICIDAL COMPOSITION The present invention relates to a novel liquid insecticidal composition comprising 2,3,5,6-tetrafluoro-4-(methoxymethyl)benzyl3-(2,2-dichlorovinyl)-2,2- dimethylcyclopropane carboxylate, wherein total trans isomers (1R,3S and 1S,3R are present in almost equal amounts) ranging from 90% to 99.90% and total cis isomers (1R,3R and 1S,3S are present in almost equal amounts) ranging from 0.1 to 10% or 'Renofluthrin' as an active ingredient and one or more chemically acceptable excipients. The present invention further relates to the process of preparation of such liquid insecticidal composition.

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Patent Information

Application #
Filing Date
03 August 2022
Publication Number
06/2024
Publication Type
INA
Invention Field
CHEMICAL
Status
Email
Parent Application

Applicants

Agcare Technologies Private Limited
Block A, NDM-1, 4th & 5th Floor, Netaji Subhash Place, New Delhi- 110034, India

Inventors

1. Neeraj Kumar Jindal
F 3/21, Ground floor, Vasant Vihar-1, New Delhi-110057, India

Specification

DESC:


The following specification describes the invention and the manner in which it is to be
performed.

2

RENOFLUTHRIN INSECTICIDAL COMPOSITION

FIELD OF THE INVENTION
The present invention relates to a novel insecticidal composition comprising
pyrethroid insecticide as an active ingredient. Particularly, the present invention relates
5 to a novel and effective liquid insecticidal composition comprising Renofluthrin as an
active ingredient, wherein the said composition exhibits significant mosquito repellent
and insect control activity. The present invention further relates to the process of
preparation of such insecticidal composition.
BACKGROUND OF THE INVENTION
10 Mosquito menace is a global problem. Diseases like malaria, filariasis, Dengue fever,
yellow fever, Japanese encephalitis, Ross river virus, Burma forest virus, Murray
Valley encephalitis etc, are known to spread through mosquitoes. Even developed
countries such as USA have seen a resurgence of mosquito menace and diseases like
west Nile virus in the 21st century. Developing and least developed countries from
15 Africa, Asia, and Latin America and rest of the world have been unsuccessfully
attempting to control the mosquito menace and to eradicate the scourge of malaria and
other diseases.
Insecticides of various classes of chemical compounds such as pyrethroids,
organophosphates, carbamates, etc. can be applied to control the pest species. These
20 chemicals are included in the composition of the insecticidal products as active
ingredients. Such insectoacaricidal formulations are available in the form of
containerized aerosols, ready to-use liquids in propellant free package, dustable
powders, wettable powders, soluble powders, tablets and granules, emulsions and their
concentrates (macro-, micro-, suspoemulsions, flowable and microencapsulated
25 formulations), baits of all the kinds, bait stations, sticky traps, electric heaters with
mosquito mats and liquid vaporizers, coils, spirals, incense, crayons, gels, creams,
lotions, shampoos etc.
Pyrethrum is an insecticide of a natural origin, and is endowed with very positive
characteristics, such as high insecticide activity and a very low toxicity for mammals.
30 However, natural pyrethrum is readily oxidized by air in the presence of light

3

(photooxidation) and is easily degraded, and therefore it is not suited for insecticidal
applications.
Numerous compounds have been synthetized, which have a slightly modified structure
of natural pyrethrum in order to preserve the insecticidal action and the low toxicity to
5 mammals, while at the same time imparting to the molecule a sufficient fastness to
light, so as to allow its use in insecticidal applications.
Whilst some of these compounds (synthetic pyrethroids) possess the characteristics
mentioned above, conventionally used liquid vaporising compositions may have high
photo-oxidation and work at perpetually high active concentrations. The liquid
10 vaporisers are designed to work in closed spaces hence the risk of being exposed to
such high amount of insecticidal composition can be perceived as a risk to health of
the user. Thus, it is necessary to formulate a suitable composition that is efficacious
and safe.
Recently, the inventors of IN316787 have developed a novel active ingredient
15 'Renofluthrin' which is found to be effective as a household insecticide. Renofluthrin
is found to be effective and practical for use in existing known formulation types and
also has potential to adapt for developing new formulations and delivery systems.
Active ingredient, 'Renofluthrin' is isomeric composition of 2,3,5,6- tetrafluoro-4-
(methoxymethyl) benzyl3-(2,2-dichlorovinyl)-2,2- dimethyl cyclopropane
20 carboxylate, wherein total trans isomers (1R,3S and 1S,3R are present in almost equal
amounts) ranging from 90% to 99.90% and total cis isomers (1R,3R and 1S,3S are
present in almost equal amounts) ranging from 0.1 to 10%. Hitherto, there is a need in
the art to formulate a liquid insecticidal composition which is safer to use and
economically advantageous. These objectives can be achieved by providing an
25 insecticidal composition that can achieve improved knock down efficacy at lower
amount of active as compared to the conventionally used insecticides.
Therefore, the present invention aims to overcome the problems in the prior art and
provide a stable and effective liquid insecticidal composition comprising of
Renofluthrin as an active ingredient.
30 OBJECTS AND ADVANTAGES OF THE INVENTION:

4

It is the main object of the present invention to provide a novel and effective
insecticidal composition comprising Renofluthrin.
It is another object of the present invention to provide a novel and effective insecticidal
composition that can be used to kill, knockdown and/or repel mosquitoes & insects.
5 It is another object of the present invention to provide a novel and effective insecticidal
composition that is safe to use.
It is another object of the present invention to provide a novel and effective
composition that shows lower inhalational toxicity.
It is another object of the present invention to provide a novel and effective insecticidal
10 composition that can be formulated easily.
It is another object of the present invention to provide a novel and effective insecticidal
composition that is ‘Ready to Use’.
It is another object of the present invention to provide a novel and effective insecticidal
composition that is economically preferrable.
15 It is another object of the present invention to provide a novel and effective insecticidal
composition that uses lower concentration of actives as compared to the conventional
formulations.
It is another object of the present invention to provide a novel and effective insecticidal
composition that shows better knock down efficacy over conventionally known
20 insecticidal compositions.
It is another object of the present invention to provide a homogenous fade-out of the
insecticidal composition through a wick.
It is another object of the present invention to provide a novel and effective insecticidal
composition for use with an emanation device wherein the emanation device is
25 selected from the group comprising of an electric heating device, a piezo electric
diffuser, liquid vaporiser and an ambient emanation device, etc.
It is another object of the present invention to provide a novel and effective insecticidal
composition, which targets flying and crawling insects.

5

It is another object of the present invention to develop a liquid insecticidal
composition, which is effective against all the mosquito species including but not
limited to Aedes spp, Culex Spp, Anopheles spp, Culiseta spp. and many other species
of crawling insects and of fly such as punky (Phlebotomus spp), sand fly, housefly
5 (usca spp and others), stable fly and face fly, etc posing risk to human health.
It is yet another object of the present invention to provide a novel and effective
insecticidal composition that is stable upon storage at room temperature.
Some or all these and other objects of the invention can be achieved by way of the
invention described hereinafter.
10 SUMMARY OF THE INVENTION
Accordingly, the present invention relates to a novel and effective insecticidal
composition comprising:
a) Renofluthrin; and
b) One or more chemically acceptable excipients.
15 In one embodiment of the present invention, the insecticidal composition comprises:
a) Renofluthrin present in an amount ranging from 0.01% to 5% weight of the total
composition; and
b) One or more chemically acceptable excipients.
In yet another embodiment, the present invention provides a process of preparation of
20 the insecticidal composition comprising:
a) Renofluthrin present in an amount ranging from 0.01% to 5% weight of the total
composition; and
b) One or more chemically acceptable excipients.
In still another preferred embodiment the insecticidal composition comprises
25 Renofluthrin, present in an amount ranging from 0.2% to 2.0% by weight of the total
composition.
In still another embodiment, the present invention provides a process of preparation of
the insecticidal liquid composition from Renofluthrin Technical.

6

In still another embodiment, the present invention provides a process of preparation of
the insecticidal liquid composition from MUP comprising Renofluthrin.
In yet another preferred embodiment, the present invention provides a process of
preparation of the insecticidal liquid composition from 5% MUP comprising
5 Renofluthrin.
In another preferred embodiment of the present invention, the insecticidal composition
comprises Renoflutrhin or 2,3,5,6-tetrafluoro-4- (methoxymethyl)benzyl3-(2,2-
dichlorovinyl)-2,2-dimethylcyclopropane carboxylate, wherein total trans isomers
(1R,3S and 1S,3R are present in almost equal amounts) ranging from 90% to 99.90%
10 and total cis isomers (1R,3R and 1S,3S are present in almost equal amounts) ranging
from 0.1 to 10% as active ingredient.
In a further embodiment of the present invention, the present insecticidal composition
is used to kill, knockdown and/or repel mosquitoes & insects.
In a further embodiment of the present invention, the present insecticidal composition
15 can be formulated as composition for emanation by a heat source, liquid vaporiser
composition, electric liquid vaporiser composition, insect repellent liquid vaporiser
composition with a wick, etc.
In a further embodiment of the present invention, the insecticidal composition requires
a wick that vaporises the insecticidal composition upon heating and releases the
20 repellent composition in the air.
In still another embodiment of the present invention, the present insecticidal
composition is a Ready to Use formulation for repelling/ controlling mosquitoes &
insects in the indoor spaces.
DETAILED DESCRIPTION OF THE INVENTION
25 Discussed below are some representative embodiments of the present invention. The
invention in its broader aspects is not limited to the specific details and representative
methods. The illustrative examples are described in this section in connection with the
embodiments and methods provided. The invention according to its various aspects is
particularly pointed out read in view of this specification and appropriate equivalents.

7

All technical and scientific terms used herein have the same meanings as commonly
understood by someone ordinarily skilled in the art to which the present subject matter
belongs. 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,
5 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.
The expression of various quantities in terms of “% w/w” or “%” means the percentage
by weight, relative to the weight of the total formulation or composition unless
10 otherwise specified.
The term “insect” as used herein refers to flying and/or crawling insects and other
insects in the public hygiene area including but not limited to all the species of
mosquito, housefly, sand fly, stable and face fly etc.
The term “control” as used herein refers to kill, knockdown and/or repel mosquitoes,
15 other insects and flies.
The term “active ingredient” (a.i.) or “active agent” used herein refers to that
component of the composition responsible for control and killing of mosquitoes, other
insects and flies.
The term “Renofluthrin also abbreviated as RNF” used herein refers to 2,3,5,6-
20 tetrafluoro-4-(methoxymethyl)benzyl3-(2,2-dichlorovinyl)-2,2-
dimethylcyclopropane carboxylate, wherein total trans isomers (1R,3S and 1S,3R are
present in almost equal amounts) ranging from 90% to 99.90% and total cis isomers
(1R,3R and 1S,3S are present in almost equal amounts) ranging from 0.1 to 10%.
The term “Trans” as used herein refers to (1R,3S) and (1S,3R).
25 The term “Cis” as used herein refers to (1R,3R) and (1S,3S).
The term “formulation” and “composition” as used herein conveys the same meaning
and can be used interchangeably.
The term “knock-down” as used herein conveys knockdown in insects following
application of an insecticide which may be defined as the state of intoxication and
30 partial paralysis which usually precedes death.

8

The term “MUP” as used herein refers to any pesticide product other than an end use
product. The product may consist of the technical grade of active ingredient only or
may contain inert ingredients such as stabilizers or solvents.
The term “RTU” as used herein refers to Ready to Use Formulation.
5 The term “Peet-Grady Chamber test”, as used in the present invention means a
standardized procedure for the evaluation and testing of insect control compositions or
products. In the case of flying insects, the knock-down percentage is determined after
subjecting the insects to a composition provided by an emanation device for 60
minutes as recommended by the World Health Organisation’s guidelines for
10 evaluation of pesticides.
The term “Bio-efficacy”, as used in the present invention means efficacy of an insect
control composition or an insect control product to knockdown or kill a determined
type of insect.
In line with the above objective, the invention provides a novel and effective liquid
15 insecticidal composition comprising active ingredient 'Renofluthrin'. In another
embodiment, the invention provides cost effective, simple process for manufacturing
the composition comprising 'Renofluthrin'.
Renofluthrin is an isomeric composition of 2,3,5,6-tetrafluoro-4-
(methoxymethyl)benzyl3-(2,2-dichlorovinyl)-2,2-dimethylcyclopropane carboxylate
20 [CAS.RN-352271-52-4], wherein total trans isomers are present in an amount ranging
from 90% to 99.90% and total cis isomers are present in an amount ranging from 0.1%
to 10%. Chemical structure of Renofluthrin is represented below:

Renofluthrin
25 Renofluthrin is a pyrethroid ester insecticide for controlling mosquitoes and other
insects in household and public hygiene areas.

9

In one embodiment of the present invention, the present insecticidal composition is a
ready-to-use liquid formulation product comprising lower concentration of
Renofluthrin, prepared from active ingredient, or technical grade, or from its MUP
formulation.
5 In another embodiment of the present invention, the present insecticidal composition
comprises 2,3,5,6-tetrafluoro-4-(methoxymethyl)benzyl3-(2,2-dichlorovinyl)-2,2-
dimethylcyclopropane carboxylate, wherein total trans isomers (1R,3S and 1S,3R are
present in almost equal amounts) ranging from 90% to 99.90% and total cis isomers
(1R,3R and 1S,3S are present in almost equal amounts) ranging from 0.1 to 10%.
10 In yet another embodiment of the present invention, the present insecticidal
composition is an insecticidal liquid vaporiser composition comprising 'Renofluthrin'
or its diluted forms, including MUP formulations.
In still another embodiment of the present invention, Renofluthrin is diluted in solvent
or mix of solvents.
15 In yet another embodiment of the present invention, the present insecticidal
composition comprises Renofluthrin in an amount ranging from 0.01 % to 5% w/w.
In another embodiment of the present invention, the present insecticidal composition
controls household mosquitoes, flies and other insects in the public hygiene area
including but not limited to Aedes spp, Culex Spp, Anopheles spp, Culiseta spp. and
20 many other species of fly such as punky (Phlebotomus spp), sand fly, housefly (usca
spp and others), stable fly and face fly, etc.
In still another embodiment of the present invention, the present insecticidal
composition controls insects in the indoor spaces.
In another embodiment of the present invention, the present insecticidal composition
25 comprises one or more chemically acceptable excipients selected from but not limited
to antioxidants, perfume, anti-foaming agent, emulsifiers, surfactants, wetting agent,
antimicrobial/anti-bacterial agent, adjuvants, fillers, colouring pigments or dyes,
preservatives, buffering agent and solvent thereof.

10

According to another embodiment of the present invention, the antioxidant is selected
from Butylated Hydroxy Toluene (BHT), Butylated hydroxyanisole (BHA) and Tert-
butylhydroquinone (tBHQ)
According to yet another embodiment of the present invention, the antioxidant is
5 present in an amount ranging from 0.5-2% weight of the total composition.
According to another embodiment of the present invention, the solvent is selected from
one or more of solvent such as Glycol ether solvents, Ketrul D-80, Deodorised
kerosene, Hydroseal G3H, Toluene, DMF, etc.
According to another embodiment of the present invention glycol ether solvents are
10 selected from the group comprising of, but not limited to Tripropylene glycol
monomethyl ether, Ethylene glycol dimethyl ether Ethylene Glycol Monobutyl Ether,
Diethylene Glycol Monomethyl Ether, Diethylene Glycol Monobutyl Ether, Ethylene
Glycol Monohexyl Ether, Diethylene Glycol Dimethyl Ether, Butyl Carbitol, etc.
According to yet another embodiment the solvent is present in an amount ranging from
15 90-99.5% weight of the total composition.
According to another embodiment of the present invention the perfume is optionally
present in an amount ranging from 0-2% weight of the total composition.
According to another embodiment of the present invention there is provided a
replaceable refill of liquid insecticidal composition as per the present invention for use
20 with an electrically powered heated emanation device; wherein the refill comprises:
a body forming a reservoir for the liquid composition;
a wick protruding out of the body at one end thereof and at its other end being in
contact with the liquid composition wherein, in use, the wick transports the liquid
insecticidal composition from the reservoir and out of the body; and wherein the liquid
25 composition comprises Renofluthrin present in an amount ranging from 0.01% to 5%
weight of the total composition; and one or more chemically acceptable excipients.
In another embodiment of the present invention, the process of manufacturing the
liquid vaporiser composition is disclosed which comprises:

11

General Procedure for the Preparation of Renofluthrin MUP
Renofluthrin ranging from 2% to 18% w/w concentration was diluted in one or more
Glycol Ethers and subsequently a limited quantity of Toluene solvent maybe added to
make final MUP composition 100% w/w. In this 100% w/w MUP formulation,
5 Toluene is nil or not more than 10% w/w, rest of the quantity being one or more Glycol
ethers. Preferably glycol ethers are selected from the group comprising of, but not
limited to, Tripropylene glycol monomethyl ether, Ethylene glycol dimethyl ether,
Ethylene Glycol Monobutyl Ether, Diethylene Glycol Monomethyl Ether, Diethylene
Glycol Monobutyl Ether, Ethylene Glycol Monohexyl Ether, Diethylene Glycol
10 Dimethyl Ether, Butyl Carbitol, etc.
Preparation of 100 grams quantity of Renofluthrin 5% MUP
40-90% w/w (i.e., 40-90g) of solvent(s), (one, or mixture of more than one Glycol
ethers) was taken in a vessel, followed by stirring the liquid. 5% w/w Renofluthrin
active ingredient (adjusted, for 100% purity) was added gradually to this mixture i.e.,
15 for example if the Renofluthrin active ingredient purity is 95%, then 5.26gw/w of
Renofluthrin is taken. The mixture was stirred till it forms clear liquid solution. Then
3g toluene solvent was added. To this solution additional quantity of Glycol ether
solvent was added to complete 100 grams w/w and the stirring was continued further
for upto 30 minutes. This gave Renofluthrin 5% MUP formulation liquid with 92%
20 Glycol Ethers and 3% Toluene.
General Procedure for Manufacture of Renofluthrin RTU Liquid vaporiser (LV)
Formulation

12

The invention is illustrated by the following example below and is not limited
5 thereto.
Examples
A Stable Liquid Vaporiser (LV) Formulation of Renofluthrin from 5% MUP
Weight for 100gms of Renofluthrin LV
Sr.No. Ingredients Weight in Grams
1 Renofluthrin MUP 5% 4-40
2 Perfume 0-2
3 Stabilizer/ anti-oxidant 0.5-2
4 Solvent Q.S

13

Example 1
A Stable Liquid Vaporiser (LV) Formulation of Renofluthrin 0.7% from 5% MUP
Weight for 100gms of 0.7% Renofluthrin
Sr.No. Ingredients Weight in Grams
1 Renofluthrin MUP 5% 14
2 Perfume 1.0
3 Butylated hydroxytoluene
(BHT)

1.0
4 Ketrul D-80 42.0
5 Hydroseal G3-H Q.S
Example 2

A stable Liquid Vaporiser (LV) Formulation of Renofluthrin 0.5% from 5% MUP
Sr.No. Ingredients Weight in Grams
1 Renofluthrin MUP 5% 10
2 Perfume 1.0
3 Butylated hydroxytoluene
(BHT)

1.0
4 Deodorized Kerosene Q.S
Example 3

A stable Liquid Vaporiser (LV) Formulation of Renofluthrin 0.9% from 5% MUP
Sr.No. Ingredients Weight in Grams
1 Renofluthrin MUP 5% 18
2 Butylated hydroxytoluene
(BHT)

1.0

3 Ethylene Glycol Dimethyl
Ether

Q.S

Example 4

A stable Liquid Vaporiser (LV) Formulation of Renofluthrin 1.5% from 5% MUP
Sr.No. Ingredients Weight in Grams
1 Renofluthrin MUP 5% 30
2 Perfume 1.0
3 Butylated hydroxytoluene
(BHT)

1.0
4 Deodorized Kerosene Q.S

14

Example 5

A stable Liquid Vaporiser (LV) Formulation of Renofluthrin 1.5% from Technical
Sr.No. Ingredients Weight in Grams
1 Renofluthrin Technical 93%
min.

1.61 to 1.62
2 Perfume 1.0
3 Butylated hydroxytoluene
(BHT)

1.0
4 Deodorized Kerosene Q.S

Toxicity Profile of Renofluthrin
5 In an insecticide / pesticide compound, toxicity and efficacy play a vital role. New
insecticide compounds are based on their effect on target pests and their Toxicology
profile. For indoor use, inhalational toxicity is very important.
Acute Inhalation Toxicity:
In mosquito repellent and flying insect repellent products, Inhalation toxicity is very
10 important. Most flying insect repellent products are based on evaporation and vapours
of the active ingredient. Household insecticide product forms like coils, mats, aerosol
sprays, liquid evaporators, other forms of burning and vaporising formulations are
based on evaporation of the active ingredient. Concentration in air of the insecticide
and its evaporation are the most important aspects in flying insect repellent product.
15 Inhalation toxicity is measured in 'Lethal concentration' LC50 values. LC50 (lethal
concentration) is expressed as weight of test substance per standard volume of air (i.e.
mg/L). Higher the mg/L value of LC50, lower the inhalation toxicity and safer the
product.
Known insecticide compounds have the following reported LC50 values:
20 • Insecticide 'Prallethrin' LC50 is 0.658 mg/L (reported in literature in unit of
measurement 658 mg/m3 which in mg/L is 0.658)
• Insecticide 'Transfluthrin' LC50 is 0.513 mg/L (reported in literature in unit of
measurement 513 mg/m3 which in mg/L is 0.513)
• Insecticide 'Metofluthrin' LC50 is reported as > 1.08 and < 1.96 mg/L

15

These results are published and reported for the respective insecticides.
Acute Inhalation Toxicity Study of Renofluthrin was performed in Rats as per OECD
guideline No. 403. In Globally Harmonized System of Classifications and Labelling
of Chemicals (GHS), for Dust & mists (mg/1), the insecticide 'Renofluthrin' of the
5 present invention falls in category 4 which is > 1.0 and < 5 mg/L.
which shows that Renofluthrin has the lowest Inhalation toxicity amongst all the
compounds commonly used as active ingredient in household insecticide products.
Bio-efficacy and activity of Insecticidal Liquid Vaporiser composition
comprising Renofluthrin
10 The comparative, bio-ef?cacy of Reno?uthrin liquid insecticidal composition, on
target pests has been established vis-a-vis commonly marketed liquid vaporiser
compositions containing Transfluthrin 0.88% and 1.6% against free flying
mosquitoes’ species ‘Aedes aegypti’ in Peet Grandy Chamber. Mosquito species
‘Aedes aegypti’ is a major vector of dengue fever, chikungunya and yellow fever
15 viruses, and other viral diseases. The effectiveness and ef?cacy of insecticidal liquid
composition were tested for Renofluthrin samples @ 0.5%, 0.7% and 0.9% w/w. A
comparative study was also carried out to evaluate the bio-efficacy of Renofluthrin
against Transfluthrin. Transfluthrin is a fast-acting pyrethroid insecticide and most
widely used mosquito repellent. It is available as Transfluthrin 0.88 % & 1.60 %
20 Liquid Vaporizer composition in the market.
The effectiveness / ef?cacy of mosquito repellent formulation is normally measured
in “Knock-down time” (KT) in minutes of percentage of the test population of
mosquitoes i.e. KT50 and KT90 values, referring to knock down time of 50% and 90%
of the test insects quantity respectively. Lower the time in minutes required for KT
25 Value, higher the effectiveness of the insecticide. Results can vary based on study
conditions, mosquito species, and protocols.
Trial Details
The purpose of the study was to assess the bio-efficacy of Liquid Vaporizer (LV)
samples (Renofluthrin with different concentrations) against 0.88% and 1.6%
30 Transfluthrin against Aedes aegypti species of mosquito in Peet Grandy Chamber. The
LVs were pre-heated for about 24 hours for wick saturation. Before starting the

16

experiment, initial weight of LV was recorded, and test was started with cold start
(without preheating). The LV with heater was placed in the centre of the chamber and
was switched on. The number of insects knockdown were counted and recorded every
2 minutes upto 20 minutes and there after every 5 minutes upto 60 minutes.
5 The order of efficacy for KT90 was as follows Renofluthrin 0.9% LV > Renofluthrin
0.7% LV > Renofluthrin 0.5% LV > Transfluthrin 1.6% LV > Transfluthrin 0.88%
LV.
The summary of the results obtained is shown in Table 1 below:
Sr. No. Name of test
item

KT50
(Minutes)
(Average
value of 2
replicates)

KT90
(Minutes)
(Average
value of 2
replicates)

% 24
Hours
mortality

Weight
Loss
(g)/hr

Weight
Loss A.I
mg/hr

1. Renofluthrin
0.5% LV

18.67 25.44 100 0.0530 0.265

2. Renofluthrin
0.7% LV

15.88 22.77 100 0.04576 0.320

3. Renofluthrin
0.9% LV

13.65 18.87 100 0.0662 0.596

4. Transfluthrin
0.88% LV

23.42 32.40 100 0.1517 1.335

5. Transfluthrin
1.6% LV

17.68 28.53 100 0.0660 1.056

(Lower minutes shows better effect)
10 From the above table it is evident that Renofluthrin 0.9% LV showed the best results
by recording lowest KT50 and KT90 values as against other samples, followed by
Renofluthrin 0.7% LV. Further both Renofluthrin 0.9% & 0.7% LV have shown
better efficacy as compared to both Transfluthrin 0.88% LV and Transfluthrin 1.6%
LV.
15 Renofluthrin at a lower dose of 0.5% LV also demonstrated results that were at par
with both Transfluthrin 0.88% LV and Transfluthrin 1.6% LV.

17

Thus, the inventors of the present invention have successfully demonstrated
improved bio-efficacy of Renofluthrin over the existing LV formulation of
Transfluthrin that is widely used in the market. Further Renofluthrin shows enhanced
mosquito control at a much lower dose of active, thus reducing the risk of being
5 exposed to high amount of active present in such household insect repellent products.

From the foregoing it will be observed that numerous modifications and variations
can be effectuated without departing from the true spirit and scope of the novel
concepts of the present invention. It is to be understood that no limitations with
respect to the specific embodiments illustrated is intended or should be inferred. It
10 should be understood that all such modifications and improvements are properly
covered within the scope of this application.
Dated this 21st day of July, 2023

Anshu Agrawal
IN-PA-4170
Patent Agent for the Applicant

To
The Controller of Patents
The Patent Office
At New Delhi

18

,CLAIMS:WE CLAIM:

1. A novel liquid insecticidal composition comprising of 2,3,5,6-tetrafluoro-4-
(methoxymethyl)benzyl3-(2,2-dichlorovinyl)-2,2-dimethylcyclopropane
carboxylate, wherein total trans isomers (1R,3S and 1S,3R are present in almost
equal amounts) ranging from 90% to 99.90% and total cis isomers (1R,3R and
1S,3S are present in almost equal amounts) ranging from 0.1 to 10% or
Renofluthrin having the following structure:

as active ingredient and one or more chemically

acceptable excipients.

2. The composition as claimed in claim 1, wherein the active ingredient is present in an
amount ranging from 0.01% to 5% by weight of the total composition.

3. The composition as claimed in claim 1, wherein the novel liquid insecticidal
composition is manufactured from MUP comprising Renofluthrin.

4. The composition as claimed in claim 1, wherein the novel liquid insecticidal
composition is manufactured from Renofluthrin technical.

5. The insecticidal composition as claimed in claim 1, wherein the chemically acceptable
excipients are one or more selected from the group comprising of antioxidants,
perfume, anti-foaming agent, wetting agent, antimicrobial/anti-bacterial agent,
adjuvants, fillers, colouring pigments or dyes, preservatives, buffering agent and
solvent thereof.

6. The insecticidal composition as claimed in claim 1 or claim 5, wherein the antioxidant
stabilizer is selected from Butylated Hydroxy Toluene (BHT), Butylated
hydroxyanisole (BHA) and Tert-butylhydroquinone (tBHQ) and is present in an
amount ranging from 0.5-2% by weight of the total composition.

20

7. The insecticidal composition as claimed in claim 1 or claim 5, wherein the solvent is
selected from one or more of Glycol ether solvents, Toluene, Ketrul D-80, Deodorised
kerosene and Hydroseal G-3H and is present in an amount ranging from 90-99.5% by
weight of the total composition.

8. The insecticidal composition as claimed in claim 7, wherein one or more of Glycol
ether solvent is selected from the group comprising of Tripropylene glycol monomethyl
ether, Ethylene glycol dimethyl ether, Ethylene Glycol Monobutyl Ether, Diethylene
Glycol Monomethyl Ether, Diethylene Glycol Monobutyl Ether, Ethylene Glycol
Monohexyl Ether, Diethylene Glycol Dimethyl Ether, Butyl Carbitol, etc.

9. The insecticidal composition as claimed in claim 1 or claim 5, wherein the perfume is
optionally present in an amount ranging from 0-2% by weight of the total composition.

10. A process for preparation of liquid insecticidal composition comprising the steps of:
a. Mixing Renofluthrin 5% MUP or Renofluthrin Technical in an amount of 0.01-
5% along with Antioxidants in an amount of 0.5-2% and one or more solvents
in an amount of 90-99.5% by weight, optionally with perfume in an amount of
0-2% by weight;
b. Stirring the mixture from step a) to obtain a clear homogeneous liquid;
c. Filtration of the homogeneous liquid obtained in step b) to get Renofluthrin
Liquid Vaporiser composition.

11. The insecticidal composition as claimed in claim 1, wherein the composition can be
used to kill, knockdown and/or repel mosquitoes & insects.

12. The novel liquid insecticidal composition as claimed in claim 1 is a composition for
emanation by a heat source, liquid vaporiser composition, electric liquid vaporiser
composition or insect repellent liquid vaporiser composition with a wick.

13. A replaceable refill of liquid insecticidal composition as claimed in claim 1 for use with
an electrically powered heated emanation device; wherein the refill comprises:

a) a body forming a reservoir for the liquid composition;

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b) a wick protruding out of the body at one end thereof and at its other end being
in contact with the liquid composition wherein, in use, the wick transports the
liquid insecticidal composition from the reservoir and out of the body.

Documents

Application Documents

# Name Date
1 202211044483-PROVISIONAL SPECIFICATION [03-08-2022(online)].pdf 2022-08-03
2 202211044483-POWER OF AUTHORITY [03-08-2022(online)].pdf 2022-08-03
3 202211044483-FORM FOR SMALL ENTITY(FORM-28) [03-08-2022(online)].pdf 2022-08-03
4 202211044483-FORM 1 [03-08-2022(online)].pdf 2022-08-03
5 202211044483-EVIDENCE FOR REGISTRATION UNDER SSI(FORM-28) [03-08-2022(online)].pdf 2022-08-03
6 202211044483-DECLARATION OF INVENTORSHIP (FORM 5) [03-08-2022(online)].pdf 2022-08-03
7 202211044483-CORRESPONDENCE-OTHERS [21-07-2023(online)].pdf 2023-07-21
8 202211044483-COMPLETE SPECIFICATION [21-07-2023(online)].pdf 2023-07-21
9 202211044483-FORM28 [20-11-2023(online)].pdf 2023-11-20
10 202211044483-Covering Letter [20-11-2023(online)].pdf 2023-11-20
11 202211044483-FORM 18 [08-05-2024(online)].pdf 2024-05-08
12 202211044483-MARKED COPIES OF AMENDEMENTS [18-09-2024(online)].pdf 2024-09-18
13 202211044483-FORM 13 [18-09-2024(online)].pdf 2024-09-18
14 202211044483-AMENDED DOCUMENTS [18-09-2024(online)].pdf 2024-09-18
15 202211044483-MSME CERTIFICATE [20-12-2024(online)].pdf 2024-12-20
16 202211044483-FORM28 [20-12-2024(online)].pdf 2024-12-20
17 202211044483-FORM 18A [20-12-2024(online)].pdf 2024-12-20
18 202211044483-FER.pdf 2025-01-22
19 202211044483-OTHERS [17-07-2025(online)].pdf 2025-07-17
20 202211044483-MARKED COPY [17-07-2025(online)].pdf 2025-07-17
21 202211044483-FORM 3 [17-07-2025(online)].pdf 2025-07-17
22 202211044483-FER_SER_REPLY [17-07-2025(online)].pdf 2025-07-17
23 202211044483-CORRECTED PAGES [17-07-2025(online)].pdf 2025-07-17
24 202211044483-CLAIMS [17-07-2025(online)].pdf 2025-07-17

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