Classifications

• • A—HUMAN NECESSITIES
  • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
  • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
  • A01N25/00—Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests
  • A01N25/002—Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests containing a foodstuff as carrier or diluent, i.e. baits
  • A01N25/004—Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests containing a foodstuff as carrier or diluent, i.e. baits rodenticidal
• • A—HUMAN NECESSITIES
  • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
  • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
  • A01N31/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic oxygen or sulfur compounds
  • A01N31/06—Oxygen or sulfur directly attached to a cycloaliphatic ring system
• • A—HUMAN NECESSITIES
  • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
  • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
  • A01N35/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having two bonds to hetero atoms with at the most one bond to halogen, e.g. aldehyde radical
  • A01N35/06—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having two bonds to hetero atoms with at the most one bond to halogen, e.g. aldehyde radical containing keto or thioketo groups as part of a ring, e.g. cyclohexanone, quinone; Derivatives thereof, e.g. ketals
• • A—HUMAN NECESSITIES
  • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
  • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
  • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
  • A01N43/02—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms
  • A01N43/04—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with one hetero atom
  • A01N43/14—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with one hetero atom six-membered rings
  • A01N43/16—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with one hetero atom six-membered rings with oxygen as the ring hetero atom

Definitions

• the present invention relates to the use of vitamin D analogues in combination with low concentration anticoagulants in rodent control agents.
• Anticoagulants especially hydroxycoumarins
• Anticoagulants have been used since the 1950's as rodenticidal agents in baits and other rodent control agents. These agents inhibit the activity of the enzyme vitamin K-epoxide reductase, which converts oxidized vitamin K to its active form, the vitamin K-hydroquinone.
• This form of vitamin K is needed for ⁇ -carboxylations. Lack of the active form of vitamin K therefore causes insufficient carboxylation of numerous proteins, i.a. factor X of blood clotting.
• the conversion of prothrombin to thrombin, a step in the blood clotting cascade, is thereby disturbed, which can lead to a weakening and eventual death of an animal after ingestion of a corresponding dose of coumarin.
• First generation hydroxycumarines are commonly used in concentrations (always expressed as wt%, unless otherwise specified) of 0.02% to 0.06% in baits, those of the second generation of 0.0025% or 0.005%.
• vitamin D 2 and D 3 Another group of drugs used as rodenticide are two forms of vitamin D, ergocalciferol and cholecalciferol (vitamin D 2 and D 3 ).
• An overdose of the vitamin leads to hypercalcaemia.
• Calcium is increasingly absorbed intestinally from the diet and absorbed from bone minerals. The resulting high calcium concentration in the bloodstream causes sclerotization of soft tissues, and has a detrimental effect on the cardiovascular system.
• Calciferols are commonly used in the concentration range of 0.1% to 0.6% in feed baits.
• the present invention relates to the combination of at least one anticoagulant rodenticidal active ingredient with an analog of vitamin D, wherein at least one of the two components is used in a very low concentration (less than 0.0049%).
• Anticoagulants in the context of the invention are substances from the group of the indanedione derivatives or Hydroxycumarine, 1st and 2nd generation. These substances are used worldwide for the Control of rodents (cf., for example, DE 2506769, JP 48023942, CH 481580, Paposci (1974): Supplements Z. Angew. Zool, p. 155 and DE 2506769).
• anti-coagulating substances of the 1st generation are the 4-hydroxycoumarin derivatives (1-phenyl-2-acetyl) -3-ethyl-4-hydroxycoumarin ("warfarin”), 3 - ( ⁇ -acetonyl-4-chlorobenzyl) -4-hydroxycoumarin ( "Coumachlore”), 3- (l ', 2', 3 t, 4'-tetrahydro-l-naphthyl) -4-hydroxycoumarin ( "coumatetralyl”), and the indanedione derivatives, such as l, l -Diphenyl-2-acetyl-indan-1,3-dione (“diphacinone”) and (l'-p-chloro-phenyl-1-phenyl) -2-acetyl-indan-1,3-dione (“chlorodiphacinone”) called.
• indanedione derivatives such as l, l -Diphenyl-2-
• 2-azacycloalkylmethyl-substituted benzhydryl ketones and -carbinols may be mentioned: 1-phenyl-3- (2-piperidyl) -1- (p-tolyl) -2-propanone, 3,3-diphenyl-1- (2-pyrrolidinyl) -2-pentanone, 1,1-diphenyl-3 - [2- (hexahydro-1H-azepinyl)] - 2-propanone, 1- (4- Fluorophenyl) -1-phenyl-3 - (2-piperidyl) -2-propanone, 1- (4-methylthiophenyl) -l-phenyl-3- (5,5-dimethyl-2-pyrrolidinyl) -2-propanone, m.p.
• the following rare earth metal salts can also be used as anticoagulant: dineodymihydroxybenzene disulfonate (Acta physiol Acad., Hungar., 24, 373), dineodymium-3-sulfonato-pyridine-carboxylate (4) and cerium (i ⁇ ) -tris- (4 -aminobenzolsulfonat).
• Anticoagulants preferred according to the invention are the 1st generation anticoagulants, warfarin, coumatetralyl, chlorophacinones and diphacinones, and those of the second generation, such as bromadiolone, difenacoum, brodifacoum, flocoumafen and difethialone.
• Vitamin D analogs according to the invention are ergocalciferol and cholecalciferol. They are derivatives of a 3/3-hydroxy- ⁇ 5,7-17 / 3-substituted steroid. Calciferols are formed by irradiation from ergosterol. Further, other analogs and metabolites of vitamin D are suitable, such as e.g. Hydroxy cholecalciferol, dihydroxy cholecalciferol, hydroxy ergocalciferol, dihydroxy ergocalciferol. Ergocalciferol and cholecalciferol are preferred.
• anticoagulants or vitamin D analogues may also be present in the agents according to the invention (in such a case, the concentration data for the total content of anticoagulants or vitamin D analogs apply).
• compositions according to the invention at least either the anticoagulant or the vitamin D analogue is present in a concentration below 0.0049%, preferably between 0.001 and 0.0045%, more preferably between 0.002 and 0.004%, most preferably between 0.0025 and 0.0035%, included.
• the anticoagulant in the preparations according to the invention contains not more than 0.0049%, preferably between 0.001 and 0.0045%, more preferably between 0.002 and 0.004%, very particularly preferably between 0.0025 and 0.003%, then the vitamin D analog can as usual with 0.005% to 1.0%.
• the vitamin D analogue contains up to a maximum of 0.0049%, preferably between 0.001 and 0.0045%, more preferably between 0.002 and 0.004%, very particularly preferably between 0.0025 and 0.0035%, then the anticoagulant as usual with 0.005% to 1, 0%.
• anticoagulant as well as vitamin D analogues are present in the compositions according to the invention with a maximum of 0.0049%, preferably between 0.001 and 0.0049%, more preferably between 0.001 and 0.0045%, very particularly preferably between 0.002 and 0.004%, more preferably between 0.025 and 0.0035%.
• Rodenticides Control agents in the sense of the invention are all types of rodenticidal baits. These are well known from the prior art. To be recommended are those based on cereals, such as oatmeal, wheat, corn, etc. These may be free-flowing baits of one or more grain constituents, extruded baits such as granules or pellets, wax blocks, soft or pasty mixtures based on vegetable fats and flours, or gels based on oily or aqueous formulations. Especially recommended Pasty baits consisting of cereals or flours and vegetable fat. For example, pasty baits are well suited in sachets of 10 g to 200 g.
• dosage forms are liquid or gelled potions and so-called contact agents such as powders and foams. These agents are not baits, but are applied so that they adhere to the coat of rodents and only be taken orally when brushing.
• the agents according to the invention are suitable for controlling all types of rodents, including representatives of the genera Microtus, Arvicola, Rattus and Mus.
• the house mouse, Mus musculusldomesticus, the brown rat, Rattus norvegicus, as well as the house or roach rat, R. rattus are to be mentioned in the settlement area of humans.
• the application is possible in the field, as well as in buildings, also animal stables, storage and production rooms as well as in the sewer system.

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• Life Sciences & Earth Sciences (AREA)
• Health & Medical Sciences (AREA)
• General Health & Medical Sciences (AREA)
• Zoology (AREA)
• Engineering & Computer Science (AREA)
• Dentistry (AREA)
• Plant Pathology (AREA)
• Wood Science & Technology (AREA)
• Agronomy & Crop Science (AREA)
• Environmental Sciences (AREA)
• Pest Control & Pesticides (AREA)
• Food Science & Technology (AREA)
• Toxicology (AREA)
• Agricultural Chemicals And Associated Chemicals (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Fodder In General (AREA)

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• 2009
  • 2009-10-07 JP JP2011531379A patent/JP2012505259A/ja not_active Withdrawn
  • 2009-10-07 KR KR1020117010761A patent/KR20110069168A/ko not_active Application Discontinuation
  • 2009-10-07 BR BRPI0920208-0A patent/BRPI0920208A2/pt not_active IP Right Cessation
  • 2009-10-07 CN CN2009801405854A patent/CN102176819A/zh active Pending
  • 2009-10-07 RU RU2011119138/13A patent/RU2011119138A/ru not_active Application Discontinuation
  • 2009-10-07 AU AU2009304313A patent/AU2009304313A1/en not_active Abandoned
  • 2009-10-07 WO PCT/EP2009/007177 patent/WO2010043322A1/de active Application Filing
  • 2009-10-07 US US13/124,308 patent/US20110268692A1/en not_active Abandoned
  • 2009-10-07 EP EP09736829A patent/EP2343972A1/de not_active Withdrawn
• 2011
  • 2011-03-29 IL IL211992A patent/IL211992A0/en unknown
  • 2011-04-11 CO CO11044647A patent/CO6382078A2/es not_active Application Discontinuation
  • 2011-04-12 CR CR20110190A patent/CR20110190A/es unknown

Non-Patent Citations (1)

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