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  Use of macrolides in pest controlUSPTO Application #: 20050227931Title: Use of macrolides in pest control Abstract: There is now described a method of controlling pests with macrolide compounds; more specifically A) a method of controlling pests in and on transgenic crops of useful plants, such as, for example, in crops of maize, cereals, soya beans, tomatoes, cotton, potatoes, rice and mustard, with a macrolide compound, characterized in that a pesticidal composition comprising a macrolide compound in free form or in agrochemically useful salt form and at least one auxiliary is applied to the pests or their environment, in particular to the crop plant itself; B) A method of protecting plant propagation material and plant organs formed at a later point in time from attack by pests, characterized in that a pesticide comprising, as pesticidally active compound, at least one macrolide compound as active ingredient and at least one auxiliary in close spatial proximity to, or spatially together with, planting or applying the propagation material is employed to the site of planting or sowing; C) a method of controlling wood pests and molluscs with a macrolide compound, wherein a pesticidally active amount of a pesticide comprising, as pesticidally active compound, at least one macrolide, in free form or agrochemically utilizable salt form, as active ingredient and at least one auxiliary is applied to the pests or their environment; the corresponding use of these compounds, corresponding pesticides whose active ingredient is selected from amongst these compounds, a method for the preparation and the use of these compositions, and plant propagation material which is protected in this manner from attack by pests. (end of abstract) Agent: Syngenta Crop Protection , Inc. Patent And Trademark Department - Greensboro, NC, US Inventors: Dieter Hofer, Marius Sutter, Franz Brandl, Roger Graham Hall, Max Angst USPTO Applicaton #: 20050227931 - Class: 514028000 (USPTO) Related Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), O-glycoside, , Oxygen Of The Saccharide Radical Bonded Directly To A Nonsaccharide Hetero Ring Or A Polycyclo Ring System Which Contains A Nonsaccharide Hetero Ring, The Hetero Ring Has 8 Or More Ring Carbons The Patent Description & Claims data below is from USPTO Patent Application 20050227931. Brief Patent Description - Full Patent Description - Patent Application Claims
[0001] The present invention relates to a method of controlling pests with macrolide compounds; more specifically to [0002] (A) a novel method of controlling pests in and on transgenic crops of useful plants with a macrolide compound; [0003] (B) method of protecting plant propagation material and plant organs formed at a later point in time from attack by pests with such a macrolide compound; and [0004] (C) a method of controlling wood pests and molluscs with a macrolide compound. [0005] Certain pest control methods are proposed in the literature. However, these methods are not fully satisfactory in the field of pest control, which is why there is a demand for providing further methods for controlling and combating pests, in particular insects and representatives of the order Acarina, or for protecting plants, especially crop plants. This object is achieved according to the invention by providing the present method. [0006] (A) A first aspect of the present invention therefore relates to a method of controlling pests in crops of transgenic useful plants, such as, for example, in crops of maize, cereals, soya beans, tomatoes, cotton, potatoes, rice and mustard, characterized in that a pesticidal composition comprising a macrolide compound, in particular abamectin, in free form or in agrochemically useful salt form and at least one auxiliary is applied to the pests or their environment, in particular to the crop plant itself; to the use of the composition in question and to propagation material of transgenic plants which has been treated with it. [0007] Surprisingly, it has now emerged that the use of a macrolide compound for controlling pests on transgenic useful plants which contain--for instance--one or more genes expressing a pesticidally, particularly insecticidally, acaricidally, nematocidally or fugicidally active ingredient, or which are tolerant against herbicides, has a synergistic effect. It is highly surprising that the use of a macrolide compound in combination with a transgenic plant exceeds the additive effect, to be expected in principle, on the pests to be controlled and thus extends the range of action of the macrolide compound and of the active principle expressed by the transgenic plant in particular in two respects: [0008] In particular, it has been found, surprisingly, that within the scope of invention (A) the pesticidal activity of a macrolide compound in combination with the effect expressed by the transgenic useful plant, is not only additive in comparison with the pesticidal activities of the macrolide compound alone and of the transgenic crop plant alone, as can generally be expected, but that a synergistic effect is present. The term "synergistic", however, is in no way to be understood in this connection as being restricted to the pesticidal activity, but the term also refers to other advantageous properties of the method according to the invention compared with the macrolide compound alone and the transgenic useful plant alone. Examples of such advantageous properties which may be mentioned are: extension of the pesticidal spectrum of action to other pests, for example to resistant strains; reduction in the application rate of the macrolide compound, or sufficient control of the pests with the aid of the compositions according to the invention even at an application rate of the macrolide compound alone and the transgenic useful plant alone are entirely ineffective; enhanced crop safety; improved quality of produce such as higher content of nutrient or oil, better fiber quality, enhanced shelf life, reduced content of toxic products such as mycotoxins, reduced content of residues or unfavorable constituents of any kind or better digestability; improved tolerance to unfavorable temperatures, draughts or salt content of water; enhanced assimilation rates such as nutrient uptake, water uptake and photosynthesis; favorable crop properties such as altered leaf aerea, reduced vegetative growth, increased yields, favorable seed shape/seed thickness or germination properties, altered colonialisation by saprophytes or epiphytes, reduction of senescense, improved phytoalexin production, improved of accelerated ripening, flower set increase, reduced boll fall and shattering, better attraction to beneficials and predators, increased pollination, reduced attraction to birds; or other advantages known to those skilled in the art. [0009] The macrolide compounds used according to the inventions part (A), (B) and (C) are known to those skilled in the art. They are the classes of substances which are disclosed as milbemycins and avermectins, for example in U.S. Pat. No. 4,310,519, U.S. Pat. No. 5,077,298, German Offenlegungsschrift 2 717 040 or U.S. Pat. No. 4,427,663. These macrolides are also to be understood as meaning, in accordance with the invention, the derivatives of these substances, that is, for example, milbemycin oxime, moxidectin, ivermectin, abamectin, emamectin and doramectin, and also spinosyns of the formula 1 [0010] in which R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 independently of one another are hydrogen or a substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl or heterocyclyl group and the substructures A and B independently of one another denote that the two carbon atoms, to which each of these substructures is bonded, are linked by a single bond, by a double bond or by a single bond and an epoxy bridge, in free form or, if appropriate, in agrochemically utilizable salt form. [0011] Within the scope of invention (A) abamectin is preferred. Abamectin is a mixture of avermectin B.sub.1a and avermectin B.sub.1b and is described, for example, in The Pesticide Manual, 10.sup.th Ed. (1994), The British Crop Protection Council, London, page 3. [0012] Also preferred within the scope of invention (A) is emamectin, which is 4"-Deoxy-4"-epi-N-methylamino avermectin B.sub.1b/B.sub.1a, known from U.S. Pat. No. 4,874,749 and as MK-244 described in Journal of Organic Chemistry, Vol. 59 (1994), pages 7704-7708. Agrochemically especially useful salts of emamectin are described in U.S. Pat. No. 5,288,710. [0013] Also preferred within the scope of invention (A) is the group of compounds consisting of the spinosyns and their derivatives; the group of compounds consisting of the naturally occurring spinosyns; or the group of compounds consisting of the derivatives of the naturally occurring spinosyns. Preferably, the active ingredient may comprise, within the scope of the subject-matter of the invention (A), spinosyn A; spinosyn D; or a mixture composed of spinosyn A and spinosyn D; especially preferred is spinosad. Spinosad is known from the "The Pesticide Manual", 11.sup.th Ed. (1997), The British Crop Protection Council, London, United Kingdom, pages 1272-1273. [0014] The agrochemically compatible salts of the macrolide compounds are, for example, acid addition salts of inorganic and organic acids, in particular of hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, perchloric acid, phosphoric acid, formic acid, acetic acid, trifluoroacetic acid, oxalic acid, malonic acid, toluenesulfonic acid or benzoic acid. Preferred within the scope of the present invention is a composition known per se which comprises, as active ingredient, abamectin or spinosad in the free form, and emamectin as the benzoate salt. [0015] The transgenic plants used according to the invention (A) are plants, or propagation material thereof, which are transformed by means of recombinant DNA technology in such a way that they are--for instance--capable of synthesizing selectively acting toxins as are known, for example, from toxin-producinginvertebrates, especially of the phylum Arthropoda, as can be obtained from Bacillus thuringiensis strains; or as are known from plants, such as lectins; or in the alternative capable of expressing a herbicidal or fungicidal resistance. Examples of such toxins, or transgenic plants which are capable of synthesizing such toxins, have been disclosed, for example, in EP-A-0 374 753, WO 93/07278, WO 95/34656, EP-A-0 427 529 and EP-A-451 878 and are incorporated by reference in the present application. [0016] The methods for generating such transgenic plants are widely known to those skilled in the art and described, for example, in the publications mentioned above. [0017] The toxins which can be expressed by such transgenic plants include, for example, toxins, such as proteins which have insecticidal properties and which are expressed by transgenic plants, for example Bacillus cereus proteins or Bacillus popliae proteins; or Bacillus thuringiensis endotoxins (B.t.), such as CryIA(a), CryIA(b), CryIA(c), CryIIA, CryIIIA, CryIIIB2 or CytA; VIP1; VIP2; VIP3; or insecticidal proteins of bacteria colonising nematodes like Photorhabdus spp or Xenorhabdus spp such as Photorhabdus luminescens, Xenorhabdus nematophilus etc.; proteinase inhibitors, such as trypsin inhibitors, serine protease inhibitors, patatin, cystatin, papain inhibitors; ribosome-inactivating proteins (RIP), such as ricin, maize RIP, abrin, luffin, saporin or bryodin; plant lectins such as pea lectins, barley lectins or snowdrop lectins; or agglutinins; toxins produced by animals, such as scorpion toxins, spider venoms, wasp venoms and other insect-specific neurotoxins; steroid metabolism enzymes, such as 3-hydroxysteroid oxidase, ecdysteroid UDP-glycosyl transferase, cholesterol oxidases, ecdysone inhibitors, HMG-COAreductase, ion channel blockers such as sodium and calcium, juvenile hormone esterase, diuretic hormone receptors, stilbene synthase, bibenzyl synthase, chitinases and glucanases. [0018] Examples of known transgenic plants which comprise one or more genes which encode insecticidal resistance and express one or more toxins are the following: KnockOut.RTM. (maize), YieldGard.RTM. (maize); NuCOTN 33B.RTM. (cotton), Boligard.RTM. (cotton), NewLeaf.RTM. (potatoes), NatureGard.RTM. and Protecta.RTM.. [0019] The following table comprises further examples of targets and principles and crop phenotypes of transgenic crops which show tolerance against pests mainly insects, mites, nematodes, virus, bacteria and diseases or are tolerant to specific herbicides or classes of herbicides. 1TABLE A1 Crop: Maize Effected target or expressed principle(s) Crop phenotype/Tolerance to Acetolactate synthase (ALS) Sulfonylureas, Imidazolinones, Triazolopyrimidines, Pyrimidyloxybenzoates, Phtalides AcetylCoA Carboxylase (ACCase) Aryloxyphenoxyalkanecarboxylic acids, cyclohexanediones Hydroxyphenylpyruvate dioxygenase (HPPD) Isoxazoles such as Isoxaflutol or Isoxachlortol, Triones such as mesotrione or sulcotrione Phosphinothricin acetyl transferase Phosphinothricin O-Methyl transferase altered lignin levels Glutamine synthetase Glufosinate, Bialaphos Adenylosuccinate Lyase (ADSL) Inhibitors of IMP and AMP synthesis Adenylosuccinate Synthase Inhibitors of adenylosuccinate synthesis Anthranilate Synthase Inhibitors of tryptophan synthesis and catabolism Nitrilase 3,5-dihalo-4-hydroxy-benzonitriles such as Bromoxynil and loxinyl 5-Enolpyruvyl-3phosphoshikimate Glyphosate or sulfosate Synthase (EPSPS) Glyphosate oxidoreductase Glyphosate or sulfosate Protoporphyrinogen oxidase (PROTOX) Diphenylethers, cyclic imides, phenylpyrazoles, pyridin derivatives, phenopylate, oxadiazoles etc. Cytochrome P450 eg. P450 SU1 Xenobiotics and herbicides such as Sulfonylureas Dimboa biosynthesis (Bx1 gene) Helminthosporium turcicum, Rhopalosiphum maydis, Diplodia maydis, Ostrinia nubilalis, lepidoptera sp. CMIII (small basic maize seed peptide plant pathogenes eg. fusarium, alternaria, sclerotina Corn-SAFP (zeamatin) plant pathogenes eg. fusarium, alternaria, sclerotina, rhizoctonia, chaetomium, phycomyces Hm1 gene Cochliobulus Chitinases plant pathogenes Glucanases plant pathogenes Coat proteins viruses such as maize dwarf mosaic virus, maize chlorotic dwarf virus Bacillus thuringiensis toxins, VIP 3, lepidoptera, coleoptera, diptera, Bacillus cereus toxins, Photorabdus and nematodes, eg. ostrinia nubilalis, Xenorhabdus toxins heliothis zea, armyworms eg. spodoptera frugiperda, corn rootworms, sesamia sp., black cutworm, asian corn borer, weevils 3-Hydroxysteroid oxidase lepidoptera, coleoptera, diptera, nematodes, eg. ostrinia nubilalis, heliothis zea, armyworms eg. spodoptera frugiperda, corn rootworms, sesamia sp., black cutworm, asian corn borer, weevils Peroxidase lepidoptera, coleoptera, diptera, nematodes, eg. ostrinia nubilalis, heliothis zea, armyworms eg. spodoptera frugiperda, corn rootworms, sesamia sp., black cutworm, asian corn borer, weevils Aminopeptidase inhibitors eg. Leucine lepidoptera, coleoptera, diptera, aminopeptidase inhibitor (LAPI) nematodes, eg. ostrinia nubilalis, heliothis zea, armyworms eg. spodoptera frugiperda, corn rootworms, sesamia sp., black cutworm, asian corn borer, weevils Limonene synthase corn rootworms Lectines lepidoptera, coleoptera, diptera, nematodes, eg. ostrinia nubilalis, heliothis zea, armyworms eg. spodoptera frugiperda, corn rootworms, sesamia sp., black cutworm, asian corn borer, weevils Protease Inhibitors eg. cystatin, patatin, weevils, corn rootworm virgiferin, CPTI ribosome inactivating protein lepidoptera, coleoptera, diptera, nematodes, eg. ostrinia nubilalis, heliothis zea, armyworms eg. spodoptera frugiperda, corn rootworms, sesamia sp., black cutworm, asian corn borer, weevils maize 5C9 polypeptide lepidoptera, coleoptera, diptera, nematodes, eg. ostrinia nubilalis, heliothis zea, armyworms eg. spodoptera frugiperda, corn rootworms, sesamia sp., black cutworm, asian corn borer, weevils HMG-CoA reductase lepidoptera, coleoptera, diptera, nematodes, eg. ostrinia nubilalis, heliothis zea, armyworms eg. spodoptera frugiperda, corn rootworms, sesamia sp., black cutworm, asian corn borer, weevils [0020] 2TABLE A2 Crop Wheat Effected target or expressed principle(s) Crop phenotype/Tolerance to Acetolactate synthase (ALS) Sulfonylureas, Imidazolinones, Triazolopyrimidines, Pyrimidyloxybenzoates, Phtalides AcetylCoA Carboxylase (ACCase) Aryloxyphenoxyalkanecarboxylic acids, cyclohexanediones Hydroxyphenylpyruvate dioxygenase (HPPD) Isoxazoles such as Isoxaflutol or Isoxachlortol, Triones such as mesotrione or sulcotrione Phosphinothricin acetyl transferase Phosphinothricin O-Methyl transferase altered lignin levels Glutamine synthetase Glufosinate, Bialaphos Adenylosuccinate Lyase (ADSL) Inhibitors of IMP and AMP synthesis Adenylosuccinate Synthase Inhibitors of adenylosuccinate synthesis Anthranilate Synthase Inhibitors of tryptophan synthesis and catabolism Nitrilase 3,5-dihalo-4-hydroxy-benzonitriles such as Bromoxynil and loxinyl 5-Enolpyruvyl-3phosphoshikimate Glyphosate or sulfosate Synthase (EPSPS) Glyphosate oxidoreductase Glyphosate or sulfosate Protoporphyrinogen oxidase (PROTOX) Diphenylethers, cyclic imides, phenylpyrazoles, pyridin derivatives, phenopylate, oxadiazoles etc. Cytochrome P450 eg. P450 SU1 Xenobiotics and herbicides such as Sulfonylureas Antifungal polypeptide AlyAFP plant pathogenes eg septoria and fusarioum glucose oxidase plant pathogenes eg. fusarium, septoria pyrrolnitrin synthesis genes plant pathogenes eg. fusarium, septoria serine/threonine kinases plant pathogenes eg. fusarium, septoria and other diseases Hypersensitive response eliciting plant pathogenes eg. fusarium, septoria polypeptide and other diseases Systemic acquires resistance (SAR) viral, bacterial, fungal, nematodal genes pathogens Chitinases plant pathogenes Glucanases plant pathogenes double stranded ribonuclease viruses such as BYDV and MSMV Coat proteins viruses such as BYDV and MSMV Bacillus thuringiensis toxins, VIP 3, lepidoptera, coleoptera, diptera, Bacillus cereus toxins, Photorabdus and nematodes, Xenorhabdus toxins 3-Hydroxysteroid oxidase lepidoptera, coleoptera, diptera, nematodes, Peroxidase lepidoptera, coleoptera, diptera, nematodes, Aminopeptidase inhibitors eg. Leucine lepidoptera, coleoptera, diptera, aminopeptidase inhibitor nematodes, Lectines lepidoptera, coleoptera, diptera, nematodes, aphids Protease Inhibitors eg. cystatin, patatin, lepidoptera, coleoptera, diptera, virgiferin, CPTI nematodes, aphids ribosome inactivating protein lepidoptera, coleoptera, diptera, nematodes, aphids HMG-CoA reductase lepidoptera, coleoptera, diptera, nematodes, eg. ostrinia nubilalis, heliothis zea, armyworms eg. spodoptera frugiperda, corn rootworms, sesamia sp., black cutworm, asian corn borer, weevils [0021] 3TABLE A3 Crop Barley Effected target or expressed principle(s) Crop phenotype/Tolerance to Acetolactate synthase (ALS) Sulfonylureas, Imidazolinones, Triazolopyrimidines, Pyrimidyloxybenzoates, Phtalides AcetylCoA Carboxylase (ACCase) Aryloxyphenoxyalkanecarboxylic acids, cyclohexanediones Hydroxyphenylpyruvate dioxygenase (HPPD) Isoxazoles such as Isoxaflutol or Isoxachlortol, Triones such as mesotrione or sulcotrione Phosphinothricin acetyl transferase Phosphinothricin O-Methyl transferase altered lignin levels Glutamine synthetase Glufosinate, Bialaphos Adenylosuccinate Lyase (ADSL) Inhibitors of IMP and AMP synthesis Adenylosuccinate Synthase Inhibitors of adenylosuccinate synthesis Anthranilate Synthase Inhibitors of tryptophan synthesis and catabolism Nitrilase 3,5-dihalo-4-hydroxy-benzonitriles such as Bromoxynil and loxinyl 5-Enolpyruvyl-3phosphoshikimate Glyphosate or sulfosate Synthase (EPSPS) Glyphosate oxidoreductase Glyphosate or sulfosate Protoporphyrinogen oxidase (PROTOX) Diphenylethers, cyclic imides, phenylpyrazoles, pyridin derivatives, phenopylate, oxadiazoles etc. Cytochrome P450 eg. P450 SU1 Xenobiotics and herbicides such as Sulfonylureas Antifungal polypeptide AlyAFP plant pathogenes eg septoria and fusarioum glucose oxidase plant pathogenes eg. fusarium, septoria pyrrolnitrin synthesis genes plant pathogenes eg. fusarium, septoria serine/threonine kinases plant pathogenes eg. fusarium, septoria and other diseases Hypersensitive response eliciting plant pathogenes eg. fusarium, septoria polypeptide and other diseases Systemic acquires resistance (SAR) viral, bacterial, fungal, nematodal genes pathogens Chitinases plant pathogenes Glucanases plant pathogenes double stranded ribonuclease viruses such as BYDV and MSMV Coat proteins viruses such as BYDV and MSMV Bacillus thuringiensis toxins, VIP 3, lepidoptera, coleoptera, diptera, Bacillus cereus toxins, Photorabdus and nematodes, Xenorhabdus toxins 3-Hydroxysteroid oxidase lepidoptera, coleoptera, diptera, nematodes, Peroxidase lepidoptera, coleoptera, diptera, nematodes, Aminopeptidase inhibitors eg. Leucine lepidoptera, coleoptera, diptera, aminopeptidase inhibitor nematodes, Lectines lepidoptera, coleoptera, diptera, nematodes, aphids Protease Inhibitors eg. cystatin, patatin, lepidoptera, coleoptera, diptera, virgiferin, CPTI nematodes, aphids ribosome inactivating protein lepidoptera, coleoptera, diptera, nematodes, aphids HMG-CoA reductase lepidoptera, coleoptera, diptera, nematodes, aphids Continue reading... Full patent description for Use of macrolides in pest control Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this Use of macrolides in pest control patent application. ###  How KEYWORD MONITOR works... a FREE service from FreshPatents1. Sign up (takes 30 seconds). 2. Fill in the keywords to be monitored. 3. Each week you receive an email with patent applications related to your keywords. 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