WO2013076231A1 - Utilisation de fluopyram pour lutter contre des endoparasites - Google Patents

Utilisation de fluopyram pour lutter contre des endoparasites Download PDF

Info

Publication number
WO2013076231A1
WO2013076231A1 PCT/EP2012/073432 EP2012073432W WO2013076231A1 WO 2013076231 A1 WO2013076231 A1 WO 2013076231A1 EP 2012073432 W EP2012073432 W EP 2012073432W WO 2013076231 A1 WO2013076231 A1 WO 2013076231A1
Authority
WO
WIPO (PCT)
Prior art keywords
spp
endoparasites
fluopyram
animals
humans
Prior art date
Application number
PCT/EP2012/073432
Other languages
German (de)
English (en)
Inventor
Achim Harder
Ulrich Görgens
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 WO2013076231A1 publication Critical patent/WO2013076231A1/fr

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.

Landscapes

  • 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.
PCT/EP2012/073432 2011-11-25 2012-11-23 Utilisation de fluopyram pour lutter contre des endoparasites WO2013076231A1 (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 (2)

Application Number Priority Date Filing Date Title
EP11190730.9 2011-11-25
EP11190730 2011-11-25

Publications (1)

Publication Number Publication Date
WO2013076231A1 true WO2013076231A1 (fr) 2013-05-30

Family

ID=47216314

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2012/073432 WO2013076231A1 (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)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2682115A4 (fr) * 2011-03-02 2014-11-26 Univ Tokyo Antiparasitaire interne
US20170014395A1 (en) * 2012-08-30 2017-01-19 The University Of Tokyo Endoparasite control agent and method for using the same
CN107312786A (zh) * 2017-07-14 2017-11-03 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

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004016088A2 (fr) 2002-08-12 2004-02-26 Bayer Cropscience S.A. Nouveau derive de 2-pyridylethylbenzamide
EP1531674A2 (fr) 2002-08-19 2005-05-25 Lorus Therapeutics Inc. Imidazoles 2,4,5-trisubstitues et utilisation de ceux-ci comme agents anti-microbiens
WO2005077901A1 (fr) 2004-02-12 2005-08-25 Bayer Cropscience Sa Composition fongique comprenant un derive de pyridylethylbenzamide et un compose capable d'inhiber le transport d'electrons de la chaine respiratoire dans des organismes fongiques phytopathogenes
WO2008003738A1 (fr) 2006-07-06 2008-01-10 Bayer Cropscience Ag Composition pesticide comprenant un dérivé de pyridyléhylbenzamide et composé insecticide
WO2008126922A1 (fr) 2007-04-12 2008-10-23 Nihon Nohyaku Co., Ltd. Composition d'agent nématicide et son procédé d'utilisation
WO2010108616A1 (fr) * 2009-03-25 2010-09-30 Bayer Cropscience Ag Combinaisons de matières actives nématicides, insecticides et acaricides comprenant des pyridyléthylbenzamides et des insecticides
WO2012084670A1 (fr) * 2010-12-20 2012-06-28 Basf Se Mélanges pesticides actifs contenant des composés pyrazole
WO2012118139A1 (fr) * 2011-03-02 2012-09-07 国立大学法人東京大学 Antiparasitaire interne

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004016088A2 (fr) 2002-08-12 2004-02-26 Bayer Cropscience S.A. Nouveau derive de 2-pyridylethylbenzamide
EP1531674A2 (fr) 2002-08-19 2005-05-25 Lorus Therapeutics Inc. Imidazoles 2,4,5-trisubstitues et utilisation de ceux-ci comme agents anti-microbiens
WO2005077901A1 (fr) 2004-02-12 2005-08-25 Bayer Cropscience Sa Composition fongique comprenant un derive de pyridylethylbenzamide et un compose capable d'inhiber le transport d'electrons de la chaine respiratoire dans des organismes fongiques phytopathogenes
WO2008003738A1 (fr) 2006-07-06 2008-01-10 Bayer Cropscience Ag Composition pesticide comprenant un dérivé de pyridyléhylbenzamide et composé insecticide
WO2008126922A1 (fr) 2007-04-12 2008-10-23 Nihon Nohyaku Co., Ltd. Composition d'agent nématicide et son procédé d'utilisation
EP2132987A1 (fr) * 2007-04-12 2009-12-16 Nihon Nohyaku CO., LTD. Composition d'agent nématicide et son procédé d'utilisation
WO2010108616A1 (fr) * 2009-03-25 2010-09-30 Bayer Cropscience Ag Combinaisons de matières actives nématicides, insecticides et acaricides comprenant des pyridyléthylbenzamides et des insecticides
WO2012084670A1 (fr) * 2010-12-20 2012-06-28 Basf Se Mélanges pesticides actifs contenant des composés pyrazole
WO2012118139A1 (fr) * 2011-03-02 2012-09-07 国立大学法人東京大学 Antiparasitaire interne

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2682115A4 (fr) * 2011-03-02 2014-11-26 Univ Tokyo Antiparasitaire interne
US9447042B2 (en) 2011-03-02 2016-09-20 The University Of Tokyo Endoparasite control agent
US20170014395A1 (en) * 2012-08-30 2017-01-19 The University Of Tokyo Endoparasite control agent and method for using the same
US10017490B2 (en) * 2012-08-30 2018-07-10 The University Of Tokyo Endoparasite control agent and method for using the same
CN107312786A (zh) * 2017-07-14 2017-11-03 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

Also Published As

Publication number Publication date
EP2782572A1 (fr) 2014-10-01

Similar Documents

Publication Publication Date Title
EP0828506B1 (fr) Agents endoparasiticides
WO2005055973A2 (fr) Agents endoparasiticides a application topique
EP0662326B1 (fr) Agents antiparasiticides contenant du praziquantel et de l'epsiprantel
EP0279343B1 (fr) Combinaisons de corps actifs anthelmintiques
EP1863535B1 (fr) Produit endoparasiticide
EP2793861B1 (fr) Préparations contenant un emopepside amorphe
KR100372348B1 (ko) 내부기생충구제를위한곤충의니코틴효능성아세틸콜린수용체에대한길항물질및효능물질
WO2009156071A1 (fr) Combinaison de dérivés d'amidine avec des depsipeptides cycliques
EP1259250B1 (fr) Agents endoparasiticides
MXPA96006179A (en) Agonists and antagonists of the receptors of the nicotinic acid acetilcoline of insects for the control of endoparasi
EP0912167B1 (fr) Granulats de derives d'hexahydropyrazine, administrables par voie orale
WO2013076231A1 (fr) Utilisation de fluopyram pour lutter contre des endoparasites
EP1357932B1 (fr) Modification cristalline d'un depsipeptide cyclique presentant une efficacite amelioree
EP1189615B1 (fr) Combinaison endoparasiticide synergique contenant des depsipeptides cycliques etdes piperazines
DE19828047A1 (de) Substituierte Cyclooctadepsipeptide
WO2009077162A1 (fr) Nouvelle utilisation de dérivés d'amidine
EP3115048A1 (fr) Agent de lutte contre les endoparasites
DE19515297A1 (de) Endoparasitizide Mittel

Legal Events

Date Code Title Description
121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 12788574

Country of ref document: EP

Kind code of ref document: A1

REEP Request for entry into the european phase

Ref document number: 2012788574

Country of ref document: EP

WWE Wipo information: entry into national phase

Ref document number: 2012788574

Country of ref document: EP

NENP Non-entry into the national phase

Ref country code: DE