Title of Invention

ACTIVE COMPOUND COMBINATIONS

Abstract

Composition, characterized by a content of an active compound combination comprising: A) spinosad (I) B) 0.1 to 1.5 parts per weight compared to the weight of spinosad, of a fungicidally active compound form the series benomyl (IIa), thiophanate-methyl (IIb), acibenozolar (IIe), flutolanil (IId), furametpyr (IIe), fumoxadone (IIf), metalaxyl (IIg), mefluoxam (IIh), azoxystrobin (IIi) and metominostrobin (IIj), capropamide (IIk) and diclocymet (III), tricylazole (Urn) oryzemate (IIn) and C) 0.1 to 1.5 parts per weight compared to the weight of spinosad, of an insecticidally active compound from the series l-[(6-chloro-3-pyridinyl)-methyl]-N-rutro-2-imidazolidinimine of the formula .

Full Text

FORM 2 THE PATENTS ACT 1970 [39 OF 1970] COMPLETE SPECIFICATION [See Section 10] "ACTIVE COMPOUND COMBINATIONS" BAYER AKTIENGESELLSCHAFT, a body corporate organised under the laws of Germany, of D-51368 Leverkusen, Germany, The following specification particularly describes the nature of the invention and the manner in which it is to be performed:- The present invention relates to novel active compound combinations comprising the known spinosad and a further known, insecticidally active compound and a further known, fungicidally active compound which are particularly well suited to controlling animal pests and fungi. It is already known that spinosyns or spinosad can be used for controlling insects (WO 97/00 265, WO 93/09 126, WO 94/20 518, US-5 362 634, US-5 202 242, US-5 670 364, US-5 227 295, DowElanco trade magazine Down to Earth, Vol. 52, No. 1,1997; Pesticide Manual, 11 th Ed., 1997, page 1272). It has now been found that the novel active compound combinations comprising A) spinosad (I) B) a fungicidally active compound from the series benomyl (IIa), thiophanate-methyl (IIb), acibenzolar (IIe), flutolanil (IId), furametpyr (IIe), fumoxadone (IIf), metalaxyl (IIg), mefluoxam (IIh), azoxystrobin (IIi) and metomino-strobin (IIj) capropamide (IIk) and diclocymet (III), tricyclazole (IIrn), oryzemate (IIn) and C) an insecticidally active compound from the series l-[(6-chloro-3-pyridinyl)-methyl]-N-nitro-2-imidazolidinimine of the formula have very good insecticidal and fungicidal properties. Surprisingly, the insecticidal and fungicidal activity of the combinations according to the invention of three active compounds are significantly higher than the activities of the individual components. Accordingly, this is an unforeseeable true synergistic effect and not just an aggregation of activities. Spinosad is essentially a mixture of spinosyn A and spinosyn D (cf. Pesticide Manual, British Crop Protection Council, 11th Ed., 1997, page 1272 and Dow Elanco trade magazine Down to Earth, Vol. 52, No. 1, 1997 and the literature cited therein). benomyl (Ha) thiophanate-methyl (IIb) The fungicidally active compounds of the formulae (IIa) to (IId) and (IIf) to (IIj) are known from the Pesticide Manual, 11th Ed., 1997: metominostrobin (IIj) Furametpyr (IIe) has the following structure and is known from EP 315 502. Capropamide (Ilk) has the following structure N-(R)-[ 1 -(4-chloro-phenyl)-ethyl]-( 1 S)-2,2-dichloro-1 -ethyl-3t-methyl-1 r-cyclopro-panecarboxamide of the formula (IIka) and N-(R)- [ 1 -(4-chloro-phenyl)-ethyl]-( 1 R)-2,2-dichloro-1 -ethyl-3t-methyl-1 r-cyclopro-panecarboxamide of the formula (IIkb) The compound of the formula (IIk) and its individual isomers are known (cf. EP-A 0 341 475). Diclocymet (III) has the following structure and is known from JP 07206608. Tricyclazole (Urn) has the following structure and is known from Pesticide Manual, British Crop Protection Council, 11th Ed, 1997, page 999. Oryzemate (IIn) has the following structure and is known from Pesticide Manual, British Crop Protection Council, 11th Ed, 1997, page 1239. The active compound of the formula (IIIa) is l-[(6-chloro-3-pyridinyl)-methyl]-N-nitro-2-imidazolidinimine, which is an insecticide known under the name imidaclo-prid (cf. Pesticide Manual, 11th Ed. (1997, page 706). The active compound of the formula (IIIb) is known from EP-A-0 428 941. The active compound of the formula (IIIc) is known from U.S. Patent No. 4,849,432. The active compound of the formula (IIId) is known from EP-A 0 580 553. The active compound of the formula (Hie) is known from WO 91/4965. The active compound of the formula (IIIf) is known from EP-A 0 649 845. The active compound of the formula (IIIg) is known from the abovementioned Pesticide Manual, page 880. The synergistic effect is particularly pronounced when the active compounds in the active compound combinations according to the invention are present in certain weight ratios. However, the weight ratios of the active compounds in the active compound combinations can be varied within a relatively wide range. In general, there are from 0.1 to 10 parts by weight, preferably from 0.2 to 5 parts by weight, of an active compound of the formulae (IIa) to (IIj) and from 0.1 to 1.5 parts by weight, preferably from 0.1 to 1.0 parts by weight of active compound of the formula (IIIa), (IIIb) or (IIIc) per part by weight of active compound of the formula (I). The active compound combinations are suitable for controlling animal pests, in particular insects, arachnids and nematodes which are encountered in agriculture, in forestry, in the preservation of stored products and of materials, and in the hygiene sector, while being well tolerated by crops and of favorable toxicity to warm-blooded animals. They can preferably be used as crop protection products. They are active against normally sensitive and resistant species and against all or some stages of development. The abovementioned pests include: From the order of the Isopoda, for example, Oniscus asellus, Armadillidium vulgare and Porcellio scaber. From the order of the Diplopoda, for example, Blaniulus guttulatus. From the order of the Chilopoda, for example, Geophilus carpophagus and Scutigera spp. From the order of the Symphyla, for example, Scutigerella immaculata. From the order of the Thysanura, for example, Lepisma saccharina. From the order of the Collembola, for example, Onychiurus armatus. From the order of the Orthoptera, for example, Acheta domesticus, Gryllotalpa spp., Locusta migratoria migratorioides, Melanoplus spp. and Schistocerca gregaria. From the order of the Blattaria, for example, Blarta orientalis, Periplaneta americana, Leucophaea maderae, Blattella germanica. From the order of the Dermaptera, for example, Forficula auricularia. From the order of the Isoptera, for example, Reticulitermes spp. From the order of the Phthiraptera, for example, Pediculus humanus corporis, Haematopinus spp., Linognathus spp., Trichodectes spp. and Damalinea spp. From the order of the Thysanoptera, for example, Hercinothrips femoralis, Thrips tabaci, Thrips palmi and Frankliniella accidentalis. From the order of the Heteroptera, for example, Eurygaster spp., Dysdercus intermedius, Piesma quadrata, Cimex lectularius, Rhodnius prolixus and Triatoma spp. From the order of the Homoptera, for example, Aleurodes brassicae, Bemisia tabaci, Trialeurodes vaporariorum, Aphis gossypii, Brevicoryne brassicae, Cryptomyzus ribis, Aphis fabae, Aphis pomi, Eriosoma lanigerum, Hyalopterus arundinis, Phylloxera vastatrix, Pemphigus spp., Macrosiphum avenae, Myzus spp., Phorodon humuli, Rhopalosiphum padi, Empoasca spp., Euscelis bilobatus, Nephotettix cincticeps, Lecanium corni, Saissetia oleae, Laodelphax striatellus, Nilaparvata lugens, Aonidiella aurantii, Aspidiotus hederae, Pseudococcus spp. and Psylla spp. From the order of the Lepidoptera, for example, Pectinophora gossypiella, Bupalus piniarius, Cheimatobia brumata, Lithocolletis blancardella, Hyponomeuta padella, Plutella xylostella, Malacosoma neustria, Euproctis chrysorrhoea, Lymantria spp., Bucculatrix thurberiella, Phyllocnistis citrella, Agrotis spp., Euxoa spp., Feltia spp., Earias insulana, Heliothis spp., Mamestra brassicae, Panolis flammea, Spodoptera spp., Trichoplusia ni, Carpocapsa pomonella, Pieris spp., Chilo spp., Pyrausta nubilalis, Ephestia kuehniella, Galleria mellonella, Tineola bisselliella, Tinea pellionella, Hofmannophila pseudospretella, Cacoecia podana, Capua reticuiana, Choristoneura fumiferana, Clysia ambiguella, Homona magnanima, Tortrix viridana and Cnaphalocerus spp., Oulema oryzae. From the order of the Coleoptera, for example, Anobium punctatum, Rhizopertha dominica, Bruchidius obtectus, Acanthoscelides obtectus, Hylotrupes bajulus, Agelastica aini, Leptinotarsa decemlineata, Phaedon cochleariae, Diabrotica spp., Psylliodes chrysocephala, Epilachna varivestis, Atomaria spp., Oryzaephilus surinamensis, Anthonomus spp., Sitophilus spp., Otiorrhynchus sulcatus, Cosmopolites sordidus, Ceuthorrhynchus assimilis, Hypera postica, Dermestes spp., Trogoderma spp., Anthrenus spp., Attagenus spp., Lyctus spp., Meligethes aeneus, Ptinus spp., Niptus hololeucus, Gibbium psylloides, Tribolium spp., Tenebrio molitor, Agriotes spp., Conoderus spp., Melolontha melolontha, Amphimallon solstitialis and Costelytra zealandica, Lissorhoptrus oryzophilus. From the order of the Hymenoptera, for example, Diprion spp., Hoplocampa spp., Lasius spp., Monomorium pharaonis and Vespa spp. From the order of the Diptera, for example, Aedes spp., Anopheles spp., Culex spp., Drosophila melanogaster, Musca spp., Fannia spp., Calliphora erythrocephala, Lucilia spp., Chrysomyia spp., Cuterebra spp., Gastrophilus spp., Hyppobosca spp., Stomoxys spp., Oestrus spp., Hypoderma spp., Tabanus spp., Tannia spp., Bibio hortulanus, Oscinella frit, Phorbia spp., Pegomyia hyoscyami, Ceratitis capitata, Dacus oleae, Tipula paludosa, Hylemyia spp. and Liriomyza spp. From the order of the Siphonaptera, for example, Xenopsylla cheopis and Ceratophyllus spp. From the order of the Arachnida, for example, Scorpio maurus, Latrodectus mactans, Acarus siro, Argas spp., Ornithodoros spp., Dermanyssus gallinae, Eriophyes ribis, Phyllocoptruta oleivora, Boophilus spp., Rhipicephalus spp., Amblyomma spp., Hyalomma spp., Ixodes spp., Psoroptes spp., Chorioptes spp., Sarcoptes spp., Tarsonemus spp., Bryobia praetiosa, Panonychus spp. and Tetranychus spp.. The phytoparasitic nematodes include, for example, Pratylenchus spp., Radopholus similis, Ditylenchus dipsaci, Tylenchulus semipenetrans, Heterodera spp., Globodera spp., Meloidogyne spp., Aphelenchoides spp., Longidorus spp., Xiphinema spp. and Trichodorus spp.. The active compound combinations according to the invention furthermore have very good fungicidal properties and can be employed for controlling phytopathogenic fungi, such as Plasmodiophoromycetes, Oomycetes, Chytridiomycetes, Zygomy¬cetes, Ascomycetes, Basidiomycetes, Deuteromycetes, etc. The active compound combinations according to the invention are particularly suitable for controlling Pyricularia, Pellicularia, Cochliobolus, Gibberella, Rhizoctonia and Fusarium spp. The active compound combinations according to the invention in particular have very good activity against pests and fungi in rice cultivation. The fact that the active compound combinations are well tolerated by plants in the concentrations required for controlling plant diseases permits a treatment of above-ground parts of plants, of seedlings and seed and of the soil. The active compound combinations according to the invention can be employed for foliar application or else as seed dressings. The active compounds can be converted to the customary formulations, such as solutions, emulsions, wettable powders, suspensions, powders, dusts, pastes, soluble powders, granules, suspension-emulsion concentrates, natural and synthetic materials impregnated with active compound, and very fine capsules in polymeric substances. These formulations are produced in a known manner, for example by mixing the active compounds with extenders, that is, liquid solvents and/or solid carriers, optionally with the use of surface-active agents, that is emulsifying agents and/or dispersing agents, and/or foam-forming agents. In the case of the use of water as an extender, organic solvents can, for example, also be used as auxiliary solvents. As liquid solvents, there are suitable in the main: aromatics, such as xylene, toluene or alkylnaphthalenes, chlorinated aromatics and chlorinated aliphatic hydrocarbons, such as chlorobenzenes, chloroethylenes or meth¬ylene chloride, aliphatic hydrocarbons, such as cyclohexane or paraffins, for example mineral oil fractions, mineral and vegetable oils, alcohols, such as butanol or glycol as well as their ethers and esters, ketones, such as acetone, methyl ethyl ketone, methyl isobutyl ketone or cyclohexanone, strongly polar solvents, such as dimethyl-formamide and dimethyl sulfoxide, as well as water. As solid carriers there are suitable: for example ammonium salts and ground natural minerals, such as kaolins, clays, talc, chalk, quartz, attapulgite, montmorillonite or diatomaceous earth, and ground synthetic minerals, such as highly disperse silica, alumina and silicates; as solid carriers for granules there are suitable: for example crushed and fractionated natural rocks such as calcite, marble, pumice, sepiolite and dolomite, as well as synthetic granules of inorganic and organic meals, and granules of organic material such as sawdust, coconut shells, maize cobs and tobacco stalks; as emulsifying and/or foam-forming agents there are suitable: for example nonionic and anionic emulsifiers, such as polyoxyethylene fatty acid esters, polyoxyethylene fatty alcohol ethers, for ex¬ample alkylaryl polyglycol ethers, alkylsulfonates, alkyl sulfates, arylsulfonates as well as albumen hydrolysis products; as dispersing agents there are suitable: for ex¬ample lignin-sulfite waste liquors and methylcellulose. Tackifiers such as carboxymethylcellulose and natural and synthetic polymers in the form of powders, granules or latices, such as gum arabic, polyvinyl alcohol and poly¬vinyl acetate, as well as natural phospholipids, such as cephalins and lecithins, and synthetic phospholipids, can be used in the formulations. Other additives can be mineral and vegetable oils. It is possible to use colorants such as inorganic pigments, for example iron oxide, titanium oxide and Prussian Blue, and organic dyestuffs, such as alizarin dyestuffs, azo dyestuffs and metal phthalocyanine dyestuffs, and trace nutrients such as salts of iron, manganese, boron, copper, cobalt, molybdenum and zinc. The formulations in general contain between 0.1 and 95 % by weight of active com¬pounds, preferably between 0.5 and 90%. The active compound combinations can be employed as such, in the form of their formulations or in the use forms prepared therefrom, such as ready-to-use solutions, emulsifiable concentrates, emulsions, suspensions, wettable powders, soluble pow¬ders and granules. Application is carried out in a customary manner, for example by watering, spraying, atomizing, broadcasting, spreading, dry dressing, wet dressing, liquid dressing, slurry treatment of seeds or incrustation. According to the invention all plants and plant parts can be treated. The term plants includes all plants and plant populations, such as desired or undesired wild plants and cultivated plants (including naturally occurring cultivated varieties). Cultivated plants can be plant varieties that were obtained by conventional breeding and op¬timizing processes or by biotechnological and genetic engineering methods or a com¬bination of such processes and methods, including transgenic plants and including plant varieties that cannot or can be protected by plant patents or plant variety rights. Plant parts are all parts and organs of plants occurring above or below the surface of the soil, e.g. shoots, leaves, needles, stalks and stems, trunks, flowers, fruits and seeds as well as roots, tubers, bulbs and rhizomes. The term plant parts also includes harvested crops and propagation material, e.g. cuttings, tubers, bulbs, rhizomes, shoots and seeds. According to the invention the plants and plant parts are treated using the usual methods by applying the active ingredients or compositions containing them directly to the plants or plant parts or to their surroundings (including the soil) or storeroom, e.g. by dipping, spraying, dusting, fogging, spreading and in the case of propagation material also by coating using one or multiple layers. In the treatment of parts of plants, the active compound concentrations in the use forms can be varied within a relatively wide range. In general, they are between 1 and 0.0001% by weight, preferably between 0.5 and 0.001%. In the treatment of seed, amounts of active compound of from 0.001 to 50 g per kilo¬gram of seed, preferably 0.01 to 10 g, are generally required. In the treatment of the soil, active compound concentrations of from 0.00001 to 0.1% by weight, preferably from 0.0001 to 0.02% by weight, are required at the site of action. The good insectidical activity of the active compound combinations according to the invention is demonstrated by the examples below. Whereas the individual active compounds and even the combination of in each case two active compounds have weaknesses in the insectidical activity, the combination of three active compounds has an activity which exceeds, with a synergistic effect, a simple summation of activity. In insecticides, a synergistic effect is always present when the insecticidal activity of the active compound combinations is greater than the sum of the activities of the active compounds applied individually. In fungicides, a synergistic effect is always present when the fungicidal activity of the active compound combinations is greater than the sum of the activities of the active compounds applied individually. Use example Critical concentration test/soil insects Test insect: Diabrotica balteata - larvae in the soil Solvent: 4 parts by weight of acetone Emulsifier: 1 part 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 amount of solvent, the stated amount of emulsi¬fier is added and the concentrate is diluted with water to the desired concentration. Here, the concentration of the active compound in the preparation virtually does not matter at all; only the amount by weight of active compound per volume unit of soil, which is stated in ppm (mg/1), is critical. The soil is filled into 0.5 1 pots and these are allowed to stand at 20°C. Immediately after the preparation, 5 maize corns are placed into each pot. After 3 days, the test insects are placed into the treated soil. After a further 7 days, the efficacy is determined. The efficacy is calculated from the number of emerging maize plants. Active compounds, application rates and results are shown in the table below: Table Soil insecticides Diabrotica baltcata - larvae in the soil Table Soil insecticides Diabrotica balteata - larvae in the soil WE CLAIM: 1. Composition, characterized by a content of an active compound combination comprising: A) spinosad (I) B) 0.1 to 1.5 parts per weight compared to the weight of spinosad, of a fungicidally active compound form the series benomyl (IIa), thiophanate-methyl (IIb), acibenozolar (IIe), flutolanil (IId), furametpyr (IIe), fumoxadone (IIf), metalaxyl (IIg), mefluoxam (IIh), azoxystrobin (IIi) and metominostrobin (IIj), capropamide (IIk) and diclocymet (III), tricylazole (Urn) oryzemate (IIn) and C) 0.1 to 1.5 parts per weight compared to the weight of spinosad, of an insecticidally active compound from the series l-[(6-chloro-3-pyridinyl)-methyl]-N-rutro-2-imidazolidinimine of the formula . 2. Process for preparing pesticides, wherein active compound combinations as claimed in claim 1 are mixed with extenders and/ or surfactants, wherein the active compound combination amounts to 0.1 to 95% of the total weight of the pesticide mixture. 3. Composition substantially as hereinbefore described with reference to the foregoing examples. 4. Process for preparing pesticides substantially as hereinbefore described with reference to the foregoing examples. Dated this 25th day of November, 1999. (RANJNA MEHTA-DUTT) OF REMFRY & SAGAR ATTORNEY FOR THE APPLICANTS

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854-bom-1999-form 1(25-11-1999).pdf

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854-bom-1999-form 2(granted)-(19-01-2007).doc

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854-bom-1999-form 3(25-11-1999).pdf

854-bom-1999-form 3(27-01-2000).pdf

854-bom-1999-form 5(25-11-1999).pdf

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