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DK2811998T3 - Parasiticide orale veterinære sammensætninger omfattende systemisk virkende aktivstoffer, fremgangsmåder og anvendelser deraf - Google Patents

Parasiticide orale veterinære sammensætninger omfattende systemisk virkende aktivstoffer, fremgangsmåder og anvendelser deraf Download PDF

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Publication number
DK2811998T3
DK2811998T3 DK13703705.7T DK13703705T DK2811998T3 DK 2811998 T3 DK2811998 T3 DK 2811998T3 DK 13703705 T DK13703705 T DK 13703705T DK 2811998 T3 DK2811998 T3 DK 2811998T3
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Prior art keywords
soft chewable
compositions
combination
veterinary composition
chewable veterinary
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DK13703705.7T
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English (en)
Inventor
Mark D Soll
Diane Larsen
Susan Mancini Cady
Peter Cheifetz
Izabela Galeska
Saijun Gong
Original Assignee
Merial Inc
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/275—Nitriles; Isonitriles
    • A61K31/277—Nitriles; Isonitriles having a ring, e.g. verapamil
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23K—FODDER
    • A23K20/00—Accessory food factors for animal feeding-stuffs
    • A—HUMAN NECESSITIES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • 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
    • A01N43/72—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms
    • A01N43/80—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms five-membered rings with one nitrogen atom and either one oxygen atom or one sulfur atom in positions 1,2
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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Zoology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Inorganic Chemistry (AREA)
  • Polymers & Plastics (AREA)
  • Emergency Medicine (AREA)
  • Molecular Biology (AREA)
  • Animal Husbandry (AREA)
  • Food Science & Technology (AREA)
  • Wood Science & Technology (AREA)
  • Dentistry (AREA)
  • Environmental Sciences (AREA)
  • Plant Pathology (AREA)
  • Agronomy & Crop Science (AREA)
  • Pest Control & Pesticides (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Claims (33)

1. Blød tygbar veterinær sammensætning til behandling og/eller forebyggelse af en parasitinfektion eller -infestation hos et dyr omfattende: a) mindst ét isoxazolin-aktivt middel med formel (I):
hvor: A1, A2, A3, A4, A5 og A6 er uafhængigt valgt fra gruppen bestående af CR3 og N, forudsat at højst 3 af A1, A2, A3, A4, A5 og A6 er N; B1, B2 og B3 er uafhængigt valgt fra gruppen bestående af CR2 og N; W er O eller S; R1 er C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C4-C7 alkylcycloalkyl eller C4-C7cycloalkylalkyl, hver eventuelt substitueret med én eller flere substituenter uafhængigt valgt fra R6; hver R2 er uafhængigt H, halogen, Ci-Ce alkyl, Ci-Ce haloalkyl, Ci-Ce alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, C1-C6 alkylamino, C2-C6 dialkylamino, C2-C4 alkoxycarbonyl, -CN eller -NO2; hver R3 er uafhængigt H, halogen, Ci-Ce alkyl, Ci-Ce haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, Ci-C6 haloalkylsulfonyl, C1-C6 alkylamino, C2-C6 dialkylamino, -CN eller -NO2; R4 er H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C4-C7 alkylcycloalkyl, C4-C7 cycloalkylalkyl, C2-C7 alkylcarbonyl eller C2-C7 alkoxy carbonyl;
R5 er H, OR10, NRnR12 eller Q1; eller Ci-Ce alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C4-C7 alkylcycloalkyl eller C4-C7 cycloalkylalkyl, hver eventuelt substitueret med én eller flere substituenter uafhængigt valgt fra R7; eller R4 og R5 er taget sammen med det nitrogen til hvilket de er bundet til at danne en ring indeholdende 2 til 6 carbonatomer og eventuelt ét yderligere atom valgt fra gruppen bestående af N, S og O, hvilken ring eventuelt er substitueret med 1 til 4 substituenter uafhængigt valgt fra gruppen bestående af C1-C2 alkyl, halogen, -CN, -NO2 og C1-C2 alkoxy; hver R6 er uafhængigt halogen, Ci-Ce alkyl, Ci-Ce alkoxy, Ci-Ce alkylthio, Ci-Ce alkylsulfinyl, C1-C6 alkylsulfonyl, -CN eller -NO2; hver R7 er uafhængigt halogen; C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, Ci-C6 alkylthio, C1-C6 alkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 alkylamino, C2-C8 dialkylamino, C3-C6 cycloalkylamino, C2-C7 alkylcarbonyl, C2-C7 alkoxycarbonyl, C2-C7 alkylaminocarbonyl, C3-C9 dialkylaminocarbonyl, C2-C7 haloalkylcarbonyl, C2-C7 haloalkoxycarbonyl, C2-C7 haloalkylaminocarbonyl, C3-C9 dihaloalkylaminocarbonyl, hydroxy, -NH2, -CN eller -NO2; eller Q2; hver R8 er uafhængigt halogen, Ci-Ce alkoxy, Ci-Ce haloalkoxy, Ci-Ce alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, C1-C6 alkylamino, C2-C6 dialkylamino, C2-C4 alkoxycarbonyl, -CN eller -NO2; hver R9 er uafhængigt halogen, Ci-Ce alkyl, Ci-Ce haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, Ci-C6 haloalkylsulfonyl, C1-C6 alkylamino, C2-C8 dialkylamino, -CN, -NO2, phenyl eller pyridinyl; R10 er H; eller C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C4-C7 alkylcycloalkyl eller C4-C7 cycloalkylalkyl, hver eventuelt substitueret med én eller flere halogen; R11 er H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C4-C7 alkylcycloalkyl, C4-C7 cycloalkylalkyl, C2-C7 alkylcarbonyl eller C2-C7 alkoxy carbonyl; R12 er H; Q3; eller C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C4-C7 alkylcycloalkyl eller C4-C7 cycloalkylalkyl, hver eventuelt substitueret med én eller flere substituenter uafhængigt valgt fra R7; eller R11 og R12 er taget sammen med det nitrogen til hvilket de er bundet til at danne en ring indeholdende 2 til 6 carbonatomer og eventuelt ét yderligere atom valgt fra gruppen bestående af N, S og O, hvilken ring eventuelt er substitueret med 1 til 4 substituenter uafhængigt valgt fra gruppen bestående af C1-C2 alkyl, halogen, -CN, -NO2 og C1-C2 alkoxy; Q1 er en phenylring, en 5- eller 6-leddet heterocyklisk ring, eller en 8-, 9- eller 10-leddet kondenseret bicyklisk ringsystem eventuelt indeholdende én til tre heteroatomer valgt fra op til 1 O, op til 1 S og op til 3 N, hver ring eller ringsystem eventuelt substitueret med én eller flere substituenter uafhængigt valgt fra R8; hver Q2 er uafhængigt en phenylring eller en 5- eller 6-leddet heterocyklisk ring, hver ring eventuelt substitueret med én eller flere substituenter uafhængigt valgt fra R9; Q3 er en phenylring eller en 5- eller 6-leddet heterocyklisk ring, hver ring eventuelt substitueret med én eller flere substituenter uafhængigt valgt fra R9; og n er 0, 1 eller 2; og b) en farmaceutisk acceptabel bærer, hvor den farmaceutisk acceptable bærer omfatter ét eller flere overfladebehandlingsmidler, hvor overfladebehandlingsmidlet er valgt fra et polyethylenglycolstearat og et polyethylenglycolhydroxylstearat.
2. Blød tygbar veterinær sammensætning ifølge krav 1, hvor: W er O; R4 er H eller Ci-Ce alkyl; R5 er -CH2C(O)NHCH2CF3; hver af A1, A2, A3, A4, A5 og A6 er CH; R1 er C1-C6 alkyl hver eventuelt substitueret med én eller flere substituenter uafhængigt valgt fra R6; R6 er halogen eller Ci-Ce alkyl; og B1, B2, og B3 er uafhængigt CH, C-halogen, C-Ci-Ce alkyl, C-Ci-Ce haloalkyl, eller C-C1-C6 alkoxy.
3. Blød tygbar veterinær sammensætning ifølge krav 1, hvor: W er O; R1 er CF3; B2 er CH; B1 er C-CI; B3 er C-CF3; hver af A1, A2, A3, A4, A5 og A6 er CH; R4 er H; og R5 er -CH2C(O)NHCH2CF3.
4. Blød tygbar veterinær sammensætning ifølge krav 1, hvor den farmaceutisk acceptable bærer omfatter ét eller flere fyldstoffer.
5. Blød tygbar veterinær sammensætning ifølge krav 1, hvor den farmaceutisk acceptable bærer omfatter ét eller flere bindemidler.
6. Blød tygbar veterinær sammensætning ifølge krav 1, hvor den farmaceutisk acceptable bærer omfatter ét eller flere opløsningsmidler.
7. Blød tygbar veterinær sammensætning ifølge krav 1, hvor den farmaceutisk acceptable bærer omfatter ét eller flere befugtningsmidler.
8. Blød tygbar veterinær sammensætning ifølge krav 1, hvor den farmaceutisk acceptable bærer omfatter ét eller flere smøremidler.
9. Blød tygbar veterinær sammensætning ifølge krav 1, hvor den farmaceutisk acceptable bærer yderligere omfatter: (i) ét eller flere fyldstoffer; (ii) ét eller flere bindemidler; og (iii) ét eller flere opløsningsmidler.
10. Blød tygbar veterinær sammensætning ifølge krav 1, hvor den farmaceutisk acceptable bærer yderligere omfatter: (i) ét eller flere fyldstoffer; (ii) ét eller flere bindemidler; og (iii) ét eller flere smøremidler.
11. Blød tygbar veterinær sammensætning ifølge krav 1, hvor den farmaceutisk acceptable bærer yderligere omfatter: (i) ét eller flere fyldstoffer; (ii) ét eller flere bindemidler; og (iii) ét eller flere befugtningsmidler.
12. Blød tygbar veterinær sammensætning ifølge krav 1, hvor bæreren omfatter ét eller flere fyldstoffer, mindst ét aromastof, mindst ét bindemiddel, ét eller flere opløsningsmidler, ét eller flere overfladebehandlingsmidler, mindst ét befugtningsmiddel, eventuelt en antioxidant, og eventuelt et konserveringsmiddel.
13. Blød tygbar veterinær sammensætning ifølge et hvilket som helst af de foregående krav, hvor overfladebehandlingsmidlet er valgt fra polyoxyl-8-stearat (PEG-400-monostearat), polyoxyl-40-stearat (PEG-1750-monostearat), polyethylenglycol 12-hydroxystearat og polyethylenglycol-15-12-hydroxystearat.
14. Blød tygbar veterinær sammensætning ifølge et hvilket som helst af kravene 1 til 13, hvor overfladebehandlingsmidlet er polyethylenglycolhydroxylstearat.
15. Blød tygbar veterinær sammensætning ifølge krav 14, hvor overfladebehandlingsmidlet er polyethylenglycol-12-hydroxystearat.
16. Blød tygbar veterinær sammensætning ifølge krav 14, hvor overfladebehandlingsmidlet er polyethylenglycol-15-12-hydroxystearat.
17. Blød tygbar veterinær sammensætning ifølge krav 4, hvor det ene eller flere fyldstoffer er soyaproteinfinstoffer, majsstivelse, eller en blanding deraf.
18. Blød tygbar veterinær sammensætning ifølge krav 5, hvor bindemidlet er polyvinylpyrrolidon, en co-polymer af vinylacetat og vinylpyrrolidon, eller polyethylenglycol, eller en kombination deraf.
19. Blød tygbar veterinær sammensætning ifølge krav 5, hvor bindemidlet er polyvinylpyrrolidon eller polyethylenglycol, eller en kombination deraf.
20. Blød tygbar veterinær sammensætning ifølge krav 6, hvor opløsningsmidlet er flydende polyethylenglycol eller capryl/caprintriglycerid, eller en kombination deraf.
21. Blød tygbar veterinær sammensætning ifølge krav 7, hvor befugtningsmidlet er glycerin, propylenglycol, cetylalkohol eller glycerolmonostearat.
22. Blød tygbar veterinær sammensætning ifølge krav 7, hvor befugtningsmidlet er glycerin.
23. Blød tygbar veterinær sammensætning ifølge krav 12, hvor aromastofferne er en kunstig kød- eller bøfaroma.
24. Blød tygbar veterinær sammensætning ifølge krav 1, hvor sammensætningen omfatter: a) et fyldstof valgt fra majsstivelse, præ-gelatineret majsstivelse, majsglutenmel og soja protein-fin stoffer, og en kombination deraf; b) et opløsningsmiddel valgt fra flydende polyethylenglycoler, propylenglycol, propylencarbonat, capryl/caprintriglycerider, capryl/caprin/linolentriglycerider, capryl/caprin/succin-triglycerider, propylenglycoldicaprylat/dicaprat, glycerol caprylat/caprat og polyglycoliserede glycerider, og en kombination deraf; c) bindemiddel valgt fra polyvinylpyrrolidon, polyethylenglycoler, co-polymerer af vinylacetat og vinylpyrrolidon, kartoffelstivelse og majsstivelse, og en kombination deraf; d) befugtningsmiddel valgt fra glycerol, propylen glycol, cetylalcohol, glycerinmonostearat og polyethylenglycoler, og en kombination deraf; og e) naturlig eller kunstig kød- eller bøfaroma.
25. Blød tygbar veterinær sammensætning ifølge et hvilket som helst af de foregående krav, hvor sammensætningen omfatter en forbindelse med formel (I) ved en koncentration på ca. 1 til ca. 20 vægtprocent.
26. Blød tygbar veterinær sammensætning ifølge krav 24, hvor: a) fyldstoffet er en kombination af majsstivelse og sojaprotein-finstoffer og er til stede ved en koncentration på ca. 30% til ca. 50% (vægt/vægt); b) opløsningsmidlet er en blanding af flydende polyethylenglycol og capryl/caprintriglycerider og er til stede ved en koncentration på ca. 5% til ca. 20% (vægt/vægt); c) bindemidlet er polyethylenglycol eller polyvinylpyrrolidon, eller en kombination deraf, og er til stede ved en koncentration på ca. 5% til ca. 15% (vægt/vægt); d) befugtningsmidlet er glycerin og er til stede ved en koncentration på ca. 5% til ca. 20% (vægt/vægt); e) overfladebehandlingsmidlet er polyethylenglycol 12-hydroxystearat og er til stede ved en koncentration på ca. 1% til ca. 5% (vægt/vægt).
27. Blød tygbar veterinær sammensætning ifølge et hvilket som helst af de foregående krav, hvor forbindelsen med formel (I) er til stede ved en koncentration på ca. 1 til ca. 5 vægtprocent.
28. Blød tygbar veterinær sammensætning ifølge et hvilket som helst af kravene 1-26, hvor the forbindelse med formel (I) er til stede ved en koncentration på ca. 10 til ca. 20 vægtprocent.
29. Sammensætning ifølge krav 1 der er valgt fra gruppen bestående af:
30. Blød tygbar veterinær sammensætning ifølge et hvilket som helst af kravene 1 til 28, hvor isoxazolinaktivstoffet er 4-[5-[3-chlor-5-(trifluormethyl)phenyl]-4,5-dihydro- i 5-(trifluormethyl)-3-isoxazolyl]-N-[2-oxo-2-[(2,2,2-trifluorethyl)amino]ethyl]-l-naphthalencarboxamid.
31. Blød tygbar veterinær sammensætning ifølge et hvilket som helst af kravene 1 til 30 til anvendelse i behandling eller forebyggelse afen parasitinfestation og/eller ) -infektion hos et dyr.
32. Blød tygbar veterinær sammensætning til anvendelse ifølge krav 31, hvor parasitterne er lopper eller tæger.
33. Blød tygbar veterinær sammensætning til anvendelse ifølge krav 31, hvor parasitten er en nematode, en cestode, en trematode eller en filarie-parasit.
DK13703705.7T 2012-02-06 2013-01-31 Parasiticide orale veterinære sammensætninger omfattende systemisk virkende aktivstoffer, fremgangsmåder og anvendelser deraf DK2811998T3 (da)

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