EP2782572A1 - Utilisation de fluopyram pour lutter contre des endoparasites - Google Patents

Utilisation de fluopyram pour lutter contre des endoparasites

Info

Publication number
EP2782572A1
EP2782572A1 EP12788574.7A EP12788574A EP2782572A1 EP 2782572 A1 EP2782572 A1 EP 2782572A1 EP 12788574 A EP12788574 A EP 12788574A EP 2782572 A1 EP2782572 A1 EP 2782572A1
Authority
EP
European Patent Office
Prior art keywords
spp
endoparasites
fluopyram
animals
humans
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP12788574.7A
Other languages
German (de)
English (en)
Inventor
Achim Harder
Ulrich Görgens
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bayer Intellectual Property GmbH
Original Assignee
Bayer Intellectual Property GmbH
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Bayer Intellectual Property GmbH filed Critical Bayer Intellectual Property GmbH
Priority to EP12788574.7A priority Critical patent/EP2782572A1/fr
Publication of EP2782572A1 publication Critical patent/EP2782572A1/fr
Withdrawn legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents

Definitions

  • the invention relates to the use of fluopyram for the control of endoparasites in humans and animals and to a method for the treatment of humans and in animals for the control of endoparasites.
  • Endoparasites or especially helminthic nematodes such as e.g. Haemonchus contortus, Cooperia spp., Trichostrongylus spp. et al cause significant economic damage in the livestock of livestock.
  • Other nematodes affect the health of pets, such as dogs and cats.
  • Fluopyram is defined as compound according to formula (I)
  • Respiratory chain by blocking the electron transport of the respiratory chain of the succinate dehydrogenase complex.
  • Fluopyram with the chemical name N - ⁇ [3-chloro-5- (trifluoromethyl) -2-pyridinyl] ethyl ⁇ -2- (trifluoromethyl) -benzamide, and suitable processes for its preparation, starting from commercially available starting materials, in EP -A- 1 531 675.
  • WO 2004/016088 describes pyridylethylbenzamides and their use as fungicides. The possibility of combining one or more of the disclosed pyridylethylbenzamide derivatives with other known fungicides, insecticides, nematicides or acaricides to broaden the spectrum of activity is also described.
  • WO 2005/077901 teaches fungicidal compositions comprising at least one pyridylethylbenzamide and an inhibitor of electron transport in the respiratory chain of fungi.
  • the patent application does not mention mixtures of pyridylethylbenzamides with insecticides.
  • WO 2008/003738 teaches fungicidal compositions comprising at least one pyridylethylbenzamide and an insecticide.
  • a possible nematicidal effect of the compositions is described in the application, but not explicitly for mixtures comprising N- ⁇ 2- [3-chloro-5- (trifluoromethyl) -2-pyridinyl] ethyl ⁇ -2-trifluoromethylbenzamide.
  • the general nematicidal effect of fluopyram is described in WO-A 2008/126922.
  • fluopyram is outstandingly suitable for controlling endoparasites, in particular of helminthic nematodes in humans and in animals. Accordingly, the subject of the present invention is the use of fluopyram for the control of endoparasites in humans and in animals
  • control of endoparasites means a significant reduction of infestation by endoparasites compared to the untreated human or animal, preferably a substantial reduction (by 40-79%) compared to the untreated human or animal (100%). Particularly preferably, the infection is completely suppressed by endoparasites (by 70-100%) .
  • the control can be curative, ie for the treatment of already infected humans or animals or protective, ie for the protection of hitherto uninfected humans or animals.
  • Combinations of fluopyram with other drugs, including other endoparasiticides, may also be used in the control of endoparasites in the present invention.
  • active compounds can be present in stereoisomeric forms or as stereoisomer mixtures, e.g. as enantiomers or racemates. Both the stereoisomer mixtures and the pure stereoisomers can be used according to the invention. It is also possible to use, where appropriate, salts of the active compounds with pharmaceutically acceptable acids or bases and also solvates, in particular hydrates, of the active substances or their salts.
  • the active substances used in the products according to the invention may, depending on their structure, exist in stereoisomeric forms (enantiomers, diastereomers). According to the invention, the enantiomers or diastereomers and their respective mixtures can be used.
  • the present invention also encompasses the use of the tautomeric forms.
  • the active compounds can also be used in the form of their salts, solvates and solvates of the salts.
  • Salts which are preferred in the context of the present invention are physiologically acceptable salts of the active compounds.
  • Physiologically acceptable salts of the active compounds comprise acid addition salts of mineral acids, carboxylic acids and sulfonic acids, for example salts of hydrochloric acid, hydrobromic acid, sulfuric acid, phosphoric acid, methanesulfonic acid, ethanesulfonic acid, toluenesulfonic acid, benzenesulfonic acid, naphthalenedisulfonic acid, acetic acid, trifluoroacetic acid, propionic acid, depending on the structure of the active substance. Lactic acid, tartaric acid, malic acid, citric acid, fumaric acid, maleic acid and benzoic acid.
  • Physiologically acceptable salts of the active compounds optionally also include salts of customary bases, such as, by way of example and by way of preference, alkali metal salts (for example sodium and potassium salts), alkaline earth salts (for example calcium and magnesium salts) and ammonium salts derived from ammonia or organic amines having 1 to 16 carbon atoms, such as, by way of example and by way of preference, ethylamine, diethylamine, triethylamine, ethyldiisopropylamine, monoethanolamine, diethanolamine, triethanolamine, dicyclohexylamine, dimethylaminoethanol, procaine, dibenzylamine, N-methylmorpholine, arginine, lysine, ethylenediamine, N-methylpiperidine and choline.
  • customary bases such as, by way of example and by way of preference, alkali metal salts (for example sodium and potassium salts), alkaline earth salts (for example calcium and
  • Solvates in the context of the invention are those forms of the active ingredients which form a complex in the solid or liquid state by coordination with solvent molecules. Hydrates are a special form of solvates that coordinate with water.
  • the present invention also includes prodrugs of the active ingredients.
  • prodrugs includes compounds which may themselves be biologically active or inactive, but are converted to the actual active ingredient during their residence time in the body (for example metabolically or hydrolytically).
  • the agents according to the invention are suitable in the case of favorable warm-blooded toxicity for controlling pathogenic endoparasites which occur in humans and in animal husbandry and animal breeding in productive, breeding, zoo, laboratory, experimental and hobby animals. They are effective against all or individual stages of development of the pests and against resistant and normally sensitive endoparasite isolates.
  • pathogenic Endoparasiten disease deaths and reductions in performance (eg in the production of meat, milk, wool, hides, eggs, honey, etc.) to be reduced, so that through the use of active ingredients more economical and easier animal husbandry is possible.
  • Pathogenic endoparasites include platyhelmintha (eg monogenea, cestodes and trematodes), nematodes, pentastoma and acanthocephala: Monogenea: eg: Gyrodactylus spp., Dactylogyrus spp., Polystoma spp.
  • platyhelmintha eg monogenea, cestodes and trematodes
  • nematodes eg. monogenea, cestodes and trematodes
  • pentastoma and acanthocephala Monogenea: eg: Gyrodactylus spp., Dactylogyrus spp., Polystoma spp.
  • Cestodes From the order of Pseudophyllidea, for example: Diphyllobothrium spp., Spirometra spp., Schistocephalus spp., Ligula spp., Bothridium spp., Diphlogonoporus spp.
  • Cyclophyllida eg: Mesocestoides spp., Anoplocephala spp., Paranoplocephala spp., Moniezia spp., Thysanosoma spp., Thysaniezia spp., Avitellina spp., Stilesia spp., Cittotaenia spp., Andyra spp., Bertiella spp.
  • Taenia spp. Echinococcus spp., Hydatigera spp., Davainea spp., Raillietina spp., Hymenolepis spp., Echinolepis spp., Echinocotyle spp., Diorchis spp., Dipylidium spp., Joyeuxiella spp., Diplopylidium spp.
  • Trematodes From the genus Digenea e.g. : Diplostomum spp. , Posthodiplostomum spp., Schistosoma spp., Trichobilharzia spp., Ornithobilharzia spp., Austrobilharzia spp., Gigantobilharzia spp., Leucochloridium spp., Brachylaima spp., Echinostoma spp., Echinoparyphium spp., Echinochasmus spp., Hypoderaeum spp., Fasciola Spp., Fasciolides spp., Fasciolopsis spp., Cyclocoelum spp., Typhlocoelum spp., Paramphistomum spp., Calicophoron spp, Cotylophoron spp., Giganto
  • Plagiorchis spp. Prosthogonimus spp., Dicrocoelium spp., Eurytrema spp., Troglotrema spp., Paragonimus spp., Collyriclum spp., Nanophyetus spp., Opisthorchis spp., Clonorchis spp. Metorchis spp., Heterophyes spp., Metagonimus spp.
  • Nematodes From the order of Trichinellida, for example: Trichuris spp., Capillaria spp., Trichomosoides spp., Trichinella spp. From the order of Tylenchida, for example: Micronema spp., Strongyloides spp.
  • Rhabditina From the order of Rhabditina, for example: Strongylus spp., Triodontophorus spp., Oesophagodontus spp., Trichonema spp., Gyalocephalus spp., Cylindropharynx spp., Poteriostomum spp., Cyclococercus spp., Cylicostephanus spp., Oesophagostomum spp., Chabertia spp. , Stephanurus spp., Ancylostoma spp., Uncinaria spp., Bunostomum spp.
  • Globocephalus spp. Syngamus spp., Cyathostoma spp., Metastrongylus spp., Dictyocaulus spp., Muellerius spp., Protostrongylus spp., Neostrongylus spp., Cystocaulus spp., Pneumostrongylus spp., Spicocaulus spp., Elapho strongylus spp.
  • Parelaphostrongylus spp. Crenosoma spp., Paracrenosoma spp., Angiostrongylus spp., Aelurostrongylus spp., Filaroides spp., Parafilaroides spp., Trichostrongylus spp., Haemonchus spp., Ostertagia spp., Marshallagia spp., Cooperia spp., Nematodirus spp , Hyostrongylus spp., Obeliscoides spp., Amidostomum spp., Ollulanus spp.
  • Acantocephala From the order of Oligacanthorhynchida, for example: Macracanthorhynchus spp., Prosthenorchis spp .; from the order of Polymorphida, for example: Filicollis spp .; from the order of Moniliformida, for example: Moniliformis spp.,
  • Echinorhynchida e.g. Acanthocephalus spp., Echinorhynchus spp., Leptorhynchoides spp.
  • Pentastoma From the order of porocephalis e.g. Linguatula spp.
  • fluopyram is used to control cestodes (tapeworms) as listed above (e.g., Taenia spp.).
  • fluopyram is used for controlling the nematodes listed above, in particular Oxyuris spp., Enterobius spp., Passalurus spp., Syphacia spp., Aspiculuris spp., Heterakis spp., Toxascaris spp., Toxocara spp.
  • Baylisascaris spp. Parascaris spp., Ascaridia spp .; Gnathostoma spp., Physaloptera spp., Thelazia spp., Gongylonema spp., Habronema spp., Parabronema spp., Draschia spp., Dracunculus spp .; Stephano colaria spp., Para hypo tartaria spp., Setaria spp., Loa spp., Dirofilaria spp., Litomosoides spp., Brugia spp., Wuchereria spp (except Wuchereria bancrofti)., Onchocerca spp.
  • the following nematodes are particularly preferably controlled: Trichinellida, Tylenchida, Rhabditina or the following Spirurida: Physaloptera spp., Thelazia spp., Gongylonema spp., Habronema spp., Parabronema spp., Draschia spp., Dracunculus spp.
  • the subject of a further particularly preferred embodiment is the use of fluopyram for the control of strongylida, in particular Haemonchus spp. (eg Haemonchus contortus), Trichostrongylus spp. (eg Trichostrongylus colubriformis), Cooperia spp., Ostertagia spp or Teladorsagia spp ..
  • Haemonchus spp. eg Haemonchus contortus
  • Trichostrongylus spp. eg Trichostrongylus colubriformis
  • Cooperia spp. eg., Ostertagia spp or Teladorsagia spp ..
  • the subject of a further particularly preferred embodiment is the use of fluopyram for controlling Parascaris spp.
  • Animals can be fish, reptiles, birds or especially mammals.
  • the livestock include in particular mammals such as cattle, horses, sheep, pigs, goats, camels, water buffalo, donkeys, rabbits, fallow deer, reindeer, fur animals such as mink, chinchilla, raccoon.
  • mammals such as cattle, horses, sheep, pigs, goats, camels, water buffalo, donkeys, rabbits, fallow deer, reindeer, fur animals such as mink, chinchilla, raccoon.
  • cattle sheep and pigs Also included in the use according to the invention are the following species other than mammals but which are also farm animals: birds such as chickens, geese, turkeys, ducks, ostriches; Fresh and saltwater fish such as salmon, trout, carp, perch, pike, eels; reptiles; Insects such as honeybee and silkworm.
  • Laboratory and experimental animals include, among others, mice, rats, guinea pigs, golden hamsters.
  • Hobby animals include horses, preferably dogs or cats. In dogs or cats, Toxoscaris spp., Toxocara spp., Trichuris spp., Trichinella spp. and the hookworms Ancylostoma spp. and Uncinaria spp. fought.
  • the products can also be used in humans.
  • herbivores are preferred for the application of the above-mentioned combinations, ie animals which mainly feed on plants.
  • ruminants such as sheep, goats, cattle.
  • sheep are particularly preferably treated.
  • cattle are treated.
  • the application can be both prophylactic and therapeutic.
  • the application of the active ingredient is carried out in a conventional manner directly or in the form of suitable preparations.
  • Usual doses of fluopyram per day are 1 to 100 mg / kg body weight, preferably 2 to 60 mg / kg body weight.

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  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Epidemiology (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)

Abstract

L'invention concerne l'utilisation de fluopyram pour lutter contre des endoparasites chez l'homme et l'animal, des médicaments à base de fluopyram ainsi que des procédés pour produire des médicaments et un procédé pour traiter l'homme et l'animal pour lutter contre des endoparasites, en particulier des nématodes.
EP12788574.7A 2011-11-25 2012-11-23 Utilisation de fluopyram pour lutter contre des endoparasites Withdrawn EP2782572A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP12788574.7A EP2782572A1 (fr) 2011-11-25 2012-11-23 Utilisation de fluopyram pour lutter contre des endoparasites

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP11190730 2011-11-25
EP12788574.7A EP2782572A1 (fr) 2011-11-25 2012-11-23 Utilisation de fluopyram pour lutter contre des endoparasites
PCT/EP2012/073432 WO2013076231A1 (fr) 2011-11-25 2012-11-23 Utilisation de fluopyram pour lutter contre des endoparasites

Publications (1)

Publication Number Publication Date
EP2782572A1 true EP2782572A1 (fr) 2014-10-01

Family

ID=47216314

Family Applications (1)

Application Number Title Priority Date Filing Date
EP12788574.7A Withdrawn EP2782572A1 (fr) 2011-11-25 2012-11-23 Utilisation de fluopyram pour lutter contre des endoparasites

Country Status (2)

Country Link
EP (1) EP2782572A1 (fr)
WO (1) WO2013076231A1 (fr)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5973989B2 (ja) 2011-03-02 2016-08-23 国立大学法人 東京大学 内部寄生虫防除剤
ES2661375T3 (es) * 2012-08-30 2018-03-28 The University Of Tokyo Agente endoparasiticida y método para usarlo
CN107312786B (zh) * 2017-07-14 2019-10-29 内蒙古农业大学 一种重组斯氏副柔线虫半胱氨酸蛋白酶的制备方法及应用

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
OA19202A (en) 2002-08-12 2006-10-13 Trinity Bay Equipment Holdings, LLC Protector assembly for flexible pipe coils and method of using same.
EP1531674B1 (fr) 2002-08-19 2014-06-18 Lorus Therapeutics Inc. Imidazoles 2,4,5-trisubstitues et utilisation de ceux-ci comme agents anti-microbiens
JP4711973B2 (ja) 2004-02-12 2011-06-29 バイエル・クロツプサイエンス・アクチエンゲゼルシヤフト ピリジルエチルベンズアミド誘導体及び植物病原性菌類微生物における呼吸鎖の電子伝達を阻害することが可能な化合物を含んでいる殺菌剤組成物
WO2008003738A1 (fr) 2006-07-06 2008-01-10 Bayer Cropscience Ag Composition pesticide comprenant un dérivé de pyridyléhylbenzamide et composé insecticide
US8648101B2 (en) 2007-04-12 2014-02-11 Nihon Nohyaku Co., Ltd. Nematicidal agent composition and method of using the same
ES2527833T3 (es) * 2009-03-25 2015-01-30 Bayer Cropscience Ag Combinaciones de principios activos nematicidas que comprenden fluopiram y otro principio activo
WO2012084670A1 (fr) * 2010-12-20 2012-06-28 Basf Se Mélanges pesticides actifs contenant des composés pyrazole
JP5973989B2 (ja) * 2011-03-02 2016-08-23 国立大学法人 東京大学 内部寄生虫防除剤

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
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Also Published As

Publication number Publication date
WO2013076231A1 (fr) 2013-05-30

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