Title of Invention | SYNERGISTIC MIXTURE |
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Abstract | Synergistic mixture, comprising the active compounds indoxacarb of the formula |
Full Text | FORM 2 THE PATENTS ACT 1970 [39 OF 1970] & THE PATENTS RULES, 2003 COMPLETE SPECIFICATION [See Section 10; rule 13] "MIXTURE, COMPRISING THE ACTIVE COMPOUNDS INDOXACARB" BAYER AKTIENGESELLSCHAFT, a German company of D-51368 Leverkusen, Germany, The following specification particularly describes the invention and the manner in which it is to be performed: From the order of the Hymenoptera, for example, Camponotus herculeanus, Lasius fuliginosus, Lasius niger, Lasius umbratus, Monomorium pharaonis, Paravespuia spp., Tetramorium caespitum. From the order of the Anoplura, for example, Pediculus humanus capitis, PedicuJus 5 humanus corporis, Phthirus pubis. From the order of the Heteroptera, for example, Cimex hemipterus, Cimex lectularius, Rhodnius prolixus, Triatoma infestans. In the field of household insecticides, they are used alone or in combination with 10 other suitable active compounds, suh as phosphonic acid esters, carbamates, pyrethroids, growth regulators or active compounds from other known classes of insecticides. They are used as aerosols, pressureless spray products, for example pump and 1:> atomizer sprays, automatic fogging systems, foggers, foams, gels, evaporator products with evaporator tablets made of cellulose or polymer, liquid evaporators, gel and membrane evaporators, propeller-driven evaporators, energy-free, or passive, evaporation systems, moth papers, moth bags and moth gels, as granules or dusts, in baits for spreading or in bait stations. 20 As already mentioned above, it is possible to treat all plants and their parts according to the invention. In a preferred embodiment, wild plant species and plant cultivars, or those obtained by conventional biological breeding methods, such as crossing or protoplast fusion, and parts thereof, are treated. In a further preferred embodiment, 2,5 transgenic plants and plant cultivars obtained by genetic engineering, if appropriate in combination with conventional methods (Genetically Modified Organisms), and parts thereof are treated. The terms "parts", "parts of plants" and "plant parts" have been explained above. 30 Particularly preferably, plants of the plant cultivars which are in each case commercially available or in use are treated according to the invention. Plant 43 - cultivars are to be understood as meaning plants having certain properties ("traits") which have been obtained by conentional breeding, by mutagenesis or by recombinant DNA techniques. This can be varieties, bio- and genotypes Depending on the plant species or plant cultivars, their location and growth conditions (soils, climate, vegetation period, diet), the treatment according to the invention may also result in superadditive ("synergistic") effects. Thus, for example, reduced application rates and/or a widening of the activity spectrum and/or an increase in the activity of the substances and compositions which can be used 1)0 according to the invention, better plant growth, increased tolerance to high or low temperatures, increased tolerance to drought or to water or soil salt content, increased flowering performance, easier harvesting, accelerated maturation, higher harvest yields, better quality and/or a higher nutritional value of the harvested products, better storage stability and/or processability of the harvested products are possible 1|5 which exceed the effects which were actually to be expected. The transgenic plants or plant cultivars (i.e. those obtained by genetic engineering) which are preferred and to be treated according to the invention include all plants which, in the genetic modification, received genetic material which imparts 2p particularly advantageous useful traits to these plants. Examples of such traits are better plant growth, increased tolerance to high or low temperatures, increased tolerance to drought or to water or soil salt content, increased flowering performance, easier harvesting, accelerated maturation, higher harvest yields, better quality and/or a higher nutritional value of the harvested products, better storage stability and/or 2j> processability of the harvested products. Further and particularly emphasized examples of such properties are a better defence of the plants against animal and microbial pests, such as against insects, mites, phytopathogenic fungi, bacteria and/or viruses, and also increased tolerance of the plants to certain herbicidally active compounds. Examples of transgenic plants which may be mentioned are the 3(j) important crop plants, such as cereals (wheat, rice), maize, soya beans, potatoes, cotton, oilseed rape and also fruit plants (with the fruits apples, pears, citrus fruits and grapes), and particular emphasis is given to maize, soya beans, potatoes, cotton and oilseed rape. Traits that are particularly emphasized are the increased defence of the plants against insects by toxins formed in the plants, in particular those formed by the genetic material from Bacillus thuringiensis (for example by the genes CrylA(a), :i CryIA(b), CryIA(c), CryllA, CrylUA, CrymB2, Cry9c Cry2Ab, Cry3Bb and CrylF and also combinations thereof) (hereinbelow referred to as "Bt plants"). Traits that are also particularly emphasized are the increased defence of the plants to fungi, bacteria and viruses by systemic acquired resistance (SAR), systemin, phytoalexins, elicitors, and resistance genes and correspondingly expressed proteins and toxins. Traits that are furthermore particularly emphasized are the increased tolerance of the plants to certain herbicidally active compounds, for example imidazolinones, sulphonylureas, glyphosate or phosphinotricin (for example the "PAT" gene). The genes in question which impart the desired traits can also be present in combination with one another in the transgenic plants. Examples of "Bt plants" which may be lj> mentioned are maize varieties, cotton varieties, soya bean varieties and potato varieties which are sold under the trade names YIELD GARD® (for example maize, cotton, soya beans), KnockOut® (for example maize), StarLink® (for example maize), Bollgard® (cotton), Nucotn® (cotton) and NewLeaf® (potato). Examples of herbicide-tolerant plants which may be mentioned are maize varieties, cotton 2)0 varieties and soya bean varieties which are sold under the trade names Roundup Ready® (tolerance to glyphosate, for example maize, cotton, soya bean), Liberty Link® (tolerance to phosphinotricin, for example oilseed rape), IMI® (tolerance to imidazolinones) and STS® (tolerance to sulphonylureas, for example maize). Herbicide-resistant plants (plants bred in a conventional manner for herbicide 2)5 tolerance) which may be mentioned include the varieties sold under the name Clearfield® (for example maize). Of course, these statements also apply to plant cultivars having these or still-to-be-developed genetic traits, which plants will be developed and/or marketed in the future. The plants listed can be treated according to the invention in a particularly advantageous manner with the active compound mixtures according to the invention. 13 Le-A 31 981 Foreign-Countries . Use examples Formula for calculating the kill rate for a combination of two active compounds The expected action for a given combination of two active compounds can be calculated as follows (cf. Colby, S.R., "Calculating Synergistic and Antagonistic Responses of Herbicide Combinations", Weeds 15, pages 20-22, 1967): If X is the kill rate, expressed as a percentage of the untreated control, when employing active compound A at an application rate of m ppm, Y is the kill rate, expressed as a percentage of the untreated control, when 1J5 employing active compound B at an application rate of n ppm and E is the kill rate, expressed as a percentage of the untreated control, when employing active compounds A and B at application rates of m and n ppm, 23 then If the actual insecticidal kill rate exceeds the calculated value, the action of the combination is superadditive, i.e. a synergistic effect is present. In this case, the 2|5 actually observed kill rate must exceed the value calculated using the above formula for the expected kill rate (E). Example A Phaedon larvae test Solvent: 7 parts by weight of dimethylformamide $ Emulsifier: 2 parts by weight of alkylaryl polyglycol ether To produce a suitable preparation of active compound, 1 part by weight of active compound is mixed with the stated amounts of solvent and emulsifier, and the concentrate is diluted with emulsifier-containing water to the desired concentration. 1|3 Cabbage leaves (Brassica oleracea) are treated by being dipped into the preparation of active compound of the desired concentration and are populated with larvae of the mustard beetle (Phaedon cochleariae) while the leaves are still moist. l|5 After the desired period of time, the kill in % is determined. 100% means that all beetle larvae have been killed; 0% means that none of the beetle larvae have been killed. The kill rates determined are calculated using Colby's formula (see sheet 1). In this test, the following active compound combination according to the present 2]0 application showed a synergistically enhanced activity compared to the active compounds applied individually: Table A sheet 1 Plant-damaging insects Phaedon larvae test Active compounds Concentration of active compounds in ppm Kill rate in % after 3 days indoxacarb 0.5 20 imidacloprid indoxacarb + imidacloprid according to the invention found* = activity found calc.** = activity calculated using Colby's formula -49^ Table A sheet 2 Plant-damaging insects Phaedon larvae test Active compounds Concentration of active Kill rate compounds in ppm in % after 6 days indoxacarb 0.5 45 thiaclopnd 3 0 indoxacarb + thiaclopnd 0.5 + 3 found* calc.** according to the invention found* = activity found calc.** = activity calculated using Colby's formula Example B Plutella test (normally sensitive) Solvent: 7 parts by weight of dimethylformamide Emulsifier: 2 parts by weight of alkylaryl polyglycol ether To produce a suitable preparation of active compound, 1 part by weight of active compound is mixed with the stated amounts of solvent and emulsifier, and the concentrate is diluted with emulsifier-containing water to the desired concentration. Cabbage leaves (Brassica oleracea) are treated by being dipped into the preparation of active compound of the desired concentration and are populated with normally sensitive caterpillars of the diamondback moth (Plutella xylostella) while the leaves are still moist. After the desired period of time, the kill in % is determined. 100% means that all caterpillars have been killed; 0% means that none of the caterpillars have been killed. The kill rates determined are calculated using Colby's formula (see sheet 1). In this test, the following active compound combination according to the present application showed a synergistically enhanced activity compared to the active compounds applied individually: LfcA-34-984 Foreign Countries -yr- Table B Plant-damaging insects Pluteila test (normally sensitive) Active compounds Concentration of active Kill rate compounds in ppm in % after 6 days indoxacarb 0.1 65 thiacloprid 3 0 indoxacarb + thiacloprid according to the invention 0.1+3 found* calc.** J00 65 found* = activity found calc.** = activity calculated using Colby's formula 13 15 Example C Plutella test (resistant) Solvent: 7 parts by weight of dimethylformamide Emulsifier: 2 parts by weight of alkylaryl polyglycol ether To produce a suitable preparation of active compound, 1 part by weight of active compound is mixed with the stated amounts of solvent and emulsifier, and the concentrate is diluted with emulsifier-containing water to the desired concentration. Cabbage leaves (Brassica oleracea) are treated by being dipped into the preparation of active compound of the desired concentration and are populated with resistant caterpillars of the diamondback moth (Plutella xylostella) while the leaves are still moist. After the desired period of time, the kill in % is determined. 100% means that all caterpillars have been killed; 0% means that none of the caterpillars have been killed. The kill rates determined are calculated using Colby's formula (see sheet 1). 2f) In this test, the following active compound combination according to the present application showed a synergistcally enhanced activity compared to the active compounds applied individually: -5/- Table C Plant-damaging insects Plutella test (resistant) Active compounds Concentration of active compounds in ppm Kill rate in % after 6 days indoxacarb 0.1 55 thiacloprid indoxacarb + thiacloprid according to the invention 0.1+3 0 found* calc.** 55 85 found* = activity found calc.** = activity calculated using Colby's formula LeA34 984- ForeignCountries Example D Spodoptera frugiperda test Solvent: 7 parts by weight of dimethylformamide Emulsifier: 2 parts by weight of alkylaryl polyglycol ether To produce a suitable preparation of active compound, 1 part by weight of active compound is mixed with the stated amounts of solvent and emulsifier, and the concentrate is diluted with emulsifier-containing water to the desired concentration. Cabbage leaves (Brassica oleracea) are treated by being dipped into the preparation of active compound of the desired concentration and are populated with caterpillars of the armyworm (Spodoptera frugiperda) while the leaves are still moist. After the desired period of time, the kill in % is determined. 100% means that all caterpillars have been killed; 0% means that none of the caterpillars have been killed. The kill rates determined are calculated using Colby's formula (see sheet 1). In this test, the following active compound combination according to the present application showed a synergistically enhanced activity compared to the active compounds applied individually: Table D Plant-damaging insects Spodoptera frugiperda test Active compounds Concentration of active Kill rate compounds in ppm in % after 6 days indoxacarb 0.02 0 imidacloprid 0.6 0 indoxacarb + 0.02 + 0.6 found* calc.** ...... 100 0 imidacloprid according to the invention found* = activity found calc.** = activity calculated using Colby's formula Le A 34-9S4^ForeIgn Countries Example E Heliothis virescens test 5 Solvent: 7 parts by weight of dimethylformamide Emulsifier: 2 parts by weight of alkylaryl polyglycol ether To produce a suitable preparation of active compound, 1 part by weight of active compound is mixed with the stated amounts of solvent and emulsifier, and the 13 concentrate is diluted with emulsifier-containing water to the desired concentration. Soya bean shoots (Glycine max) are treated by being dipped into the preparation of active compound of the desired concentration and are populated with Heliothis virescens caterpillars while the leaves are still moist. 15 After the desired period of time, the kill in % is determined. 100% means that all caterpillars have been killed; 0% means that none of the caterpillars have been killed. The kill rates determined are calculated using Colby's formula (see sheet 1). ^0 In this test, the following active compound combination according to the present application showed a synergistically enhanced activity compared to the active compounds applied individually: Le ^ 34-984=FoTererr€otffl^es Table E Plant-damaging insects !i Heliothis virescens test Active compounds Concentration of active Kill rate compounds in ppm in % after 3 days indoxacarb 0.1 0 indoxacarb + rmidactoprid. according to the invention imidacloprid 3 15 0.1 +3 found* calo**^ 100 15 found* = activity found calc.** = activity calculated using Colby's formula 13 Le A 3^84-f^ergjgnronntrips -? Formula for calculating the synergistic effect of a combination of two active compounds The expected action for a given combination of two active compounds can be calculated as follows (cf. Carpenter, C.S., "Mammalian Toxicity of 1-Naphthyl-7V-methylcarbamate [Sevin Insecticide]", Agricultural and Food Chemistry, Vol. 9, No. 1, pages 30-39, 1961): If Pa is the percentage of active compound A in the mixture, Pb is the percentage of active compound B in the mixture, 15 LC50 or 95)a is the concentration at which 50% (or 95%) of the animals treated with active compound A are killed and LC50 ( o r 95) b is the concentration at which 50% (or 95%) of the animals treated with active compound B are killed, 1 then the expected LC 50 (or 95) ( comb.) = Pa Pb If the calculated LC50 (or 95) is higher than the actual value and above the confidence interval, the action of the combination is superadditive, i.e. a synergistic effect is present. Le A 3d 984 Foreign Countries Example A Phaedon larvae test Solvent: 7 parts by weight of dimethylformamide Emulsifier:- 2 parts by weight of alkylaryl polyglycol ether To produce a suitable preparation of active compound, 1 part by weight of active compound is mixed with the stated amounts of solvent and emulsifier, and the concentrate is diluted with emulsifter-containing water to the desired concentration. Cabbage leaves (Brassica oleracea) are treated by being dipped into the preparation of active compound of the desired concentration and are populated with larvae of the mustard beetle (Phaedon cochleariae) while the leaves are still moist. Ip After the desired period of time, the kill in % is determined. 100% means that all beetle larvae have been killed; 0% means that none of the beetle larvae have been killed. The kill rates determined are calculated using Carpenter's formula (see sheet 1). 2f) In this test, the following active compound combination according to the present application showed a synergistically enhanced activity compared to the active compounds applied individually: Table A Plant-damaging insects Phaedon larvae test Active compounds LC50 after 6 days indoxacarb 0.1 ppm known clothianidin (X) 2.372 ppm known indoxacarb + clothianidin (X) (1:6) according to the invention calc.** 0.558 ppm found* 0.1 ppm found* = activity found calc.** = activity calculated using Carpenter's formula Le Ar3T984^Foreign Countries Example B Plutella test, sensitive strain Solvent: 7 parts by weight of dimethylformamide Emulsifier: 2 parts by weight of alkylaryl polyglycol ether To produce a suitable preparation of active compound, 1 part by weight of active compound is mixed with the stated amounts of solvent and emulsifier, and the concentrate is diluted with emulsifier-containing water to the desired concentration. Cabbage leaves (Brassica oleracea) are treated by being dipped into the preparation of active compound of the desired concentration and are populated with caterpillars of the diamondback moth (Plutella xylostella, sensitive strain) while the leaves are still moist. After the desired period of time, the kill in % is determined. 100% means that all caterpillars have been killed; 0% means that none of the caterpillars have been killed. The kill rates determined are calculated using Carpenter's formula (see sheet 1). In this test, the following active compound combination according to the present application showed a synergistically enhanced activity compared to the active compounds applied individually: Table B Plant-damaging insects Plutella test, sensitive strain Active compounds LC95 after 6 days indoxacarb 0.531 ppm known 10 clothianidin (X) 26.037 ppm known 15 indoxacarb + clothianidin (X) (1:6) according to the invention calc.** 3.311 ppm found* 0.322 ppm found* = activity found calc.** = activity calculated using Carpenter's formula Example C Plutella test, resistant strain 5 Solvent: 7 parts by weight of dimethylformamide Emulsifier: 2 parts by weight of alkylaryl polyglycol ether To produce a suitable preparation of active compound, 1 part by weight of active compound is mixed with the stated amounts of solvent and emulsifier, and the 10 concentrate is diluted with emulsifier-containing water to the desired concentration. Cabbage leaves (Brassica oleracea) are treated by being dipped into the preparation of active compound of the desired concentration and are populated with caterpillars of the diamondback moth (Plutella xylostella, resistant strain) while the leaves are 15 still moist. After the desired period of time, the kill in % is determined. 100% means that all caterpillars have been killed; 0% means that none of the caterpillars have been killed. The kill rates determined are calculated using Carpenter's formula (see sheet 1). :o In this test, the following active compound combination according to the present application showed a synergistically enhanced activity compared to the active compounds applied individually: Table C Plant-damaging insects Plutella test, resistant strain Active compounds LC95 after 6 days indoxacarb 0.234 ppm known clothianidin (X) 50.722 ppm known indoxacarb + clothianidin (X) (1:6) according to the invention calc.** 1.592 ppm found* 0.214 ppm found* = activity found calc.** = activity calculated using Carpenter's formula Le A 3ASS4^eretgn-ecuntries Example D Spodoptera frugiperda test Solvent: 7 parts by weight of dimethylformamide Emulsifier: 2 parts by weight of alkylaryl polyglycol ether To produce a suitable preparation of active compound, 1 part by weight of active compound is mixed with the stated amounts of solvent and emulsifier, and the concentrate is diluted with emulsifier-containing water to the desired concentration. Cabbage leaves (Brassica oleracea) are treated by being dipped into the preparation of active compound of the desired concentration and are populated with caterpillars of the armyworm (Spodoptera frugiperda) while the leaves are still moist. After the desired period of time, the kill in % is determined. 100% means that all caterpillars have been killed; 0% means that none of the caterpillars have been killed. The kill rates determined are calculated using Carpenter's formula (see sheet 1). In this test, the following active compound combination according to the present application showed a synergistically enhanced activity compared to the active compounds applied individually: -66- Le A*M-934Tofelgn Countries Table D Plant-damaging insects Spodoptera frugiperda test Active compounds LC50 after 6 days p indoxacarb 0.136 ppm known 10 clothianidin 0.662 ppm known 15 indoxacarb + clothianidin (X) (1:30) according to the invention calc.** 0.589 ppm found* 0.027 ppm 10 found* = activity found calc.** = activity calculated using Carpenter's formula We Claim: 1. Synergistic mixture, comprising the active compounds indoxacarb of the formula 2. Synergistic mixture, comprising the active compounds indoxacarb of the formula and thiacloprid of the formula (IX) -68- 3. Synergistic mixtures as claimed in any of Claims 1 and 2 in which the ratio of indoxacarb to the compound (Z)-3-(6-chIoro-3-pyridylmethyl)-l,3-thiazo\idm-2-y\idencyanamide or the compound (E)-l-(2-cmoro-l,3-thiazol-5-ylmethyl)-3-methyl-2-nitroguanidine is from 1:0.1 to 1:100. Dated this the 26th day of December, 2001 v |
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1216-mum-2001-correspondence(22-02-2007).pdf
1216-mum-2001-correspondence(ipo)-(15-02-2007).pdf
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1216-mum-2001-description(granted).doc
1216-mum-2001-description[cancelled].pdf
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1216-mum-2001-form 1(26-12-2001).pdf
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1216-mum-2001-form 2[title page].pdf
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1216-mum-2001-form 5(26-12-2001).pdf
1216-mum-2001-petition under rule 137(01-09-2006).pdf
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Patent Number | 208354 | ||||||||||||||||||
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Indian Patent Application Number | 1216/MUM/2001 | ||||||||||||||||||
PG Journal Number | 30/2008 | ||||||||||||||||||
Publication Date | 25-Jul-2008 | ||||||||||||||||||
Grant Date | 24-Jul-2007 | ||||||||||||||||||
Date of Filing | 26-Dec-2001 | ||||||||||||||||||
Name of Patentee | BAYER AKTIENGESELLSCHAFT | ||||||||||||||||||
Applicant Address | D-51368 LEVERKUSEN, | ||||||||||||||||||
Inventors:
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PCT International Classification Number | A01N 47/44 | ||||||||||||||||||
PCT International Application Number | N/A | ||||||||||||||||||
PCT International Filing date | |||||||||||||||||||
PCT Conventions:
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