HRP20201745T1 - Paraziticidni pripravci koji sadrže djelatno sredstvo izoksazolina, postupak za njih i njihove uporabe - Google Patents

Paraziticidni pripravci koji sadrže djelatno sredstvo izoksazolina, postupak za njih i njihove uporabe Download PDF

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Publication number
HRP20201745T1
HRP20201745T1 HRP20201745TT HRP20201745T HRP20201745T1 HR P20201745 T1 HRP20201745 T1 HR P20201745T1 HR P20201745T T HRP20201745T T HR P20201745TT HR P20201745 T HRP20201745 T HR P20201745T HR P20201745 T1 HRP20201745 T1 HR P20201745T1
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Croatia
Prior art keywords
alkyl
topical veterinary
preparation according
veterinary preparation
alkoxy
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HRP20201745TT
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English (en)
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Mark D. Soll
Joseph K. Rosentel
James Pate
Natalya Shub
Monica Tejwani-Motwani
Carol Belansky
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Boehringer Ingelheim Animal Health USA Inc.
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=47018471&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20201745(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Boehringer Ingelheim Animal Health USA Inc. filed Critical Boehringer Ingelheim Animal Health USA Inc.
Publication of HRP20201745T1 publication Critical patent/HRP20201745T1/hr

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    • 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
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    • 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
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    • A01N37/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids
    • A01N37/36—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing at least one carboxylic group or a thio analogue, or a derivative thereof, and a singly bound oxygen or sulfur atom attached to the same carbon skeleton, this oxygen or sulfur atom not being a member of a carboxylic group or of a thio analogue, or of a derivative thereof, e.g. hydroxy-carboxylic acids
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    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
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    • 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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    • A01N49/00—Biocides, pest repellants or attractants, or plant growth regulators, containing compounds containing the group, wherein m+n>=1, both X together may also mean —Y— or a direct carbon-to-carbon bond, and the carbon atoms marked with an asterisk are not part of any ring system other than that which may be formed by the atoms X, the carbon atoms in square brackets being part of any acyclic or cyclic structure, or the group, wherein A means a carbon atom or Y, n>=0, and not more than one of these carbon atoms being a member of the same ring system, e.g. juvenile insect hormones or mimics thereof
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Claims (21)

1. Topikalni veterinarski pripravak za liječenje i prevenciju parazitne infekcije ili okuženosti kod životinje koja je odabrana od mačke i psa, naznačen time, da je spomenuti pripravak u obliku sastava za preciznu primjenu na potrebnom mjestu (engl. spot-on composition), naime spot-on pripravak koji služi za primjenu na lokalizirano područje na životinji, dok navedeni pripravak obuhvaća: a) od 1 do 25% (masa/volumen) najmanje jednog djelatnog sredstva izoksazolina formule (I): [image] u kojoj: A1, A2, A3, A4, A5 i A6 su neovisno odabrani iz skupine koja se sastoji od CR3 i N, uz uvjet da najviše tri od A1, A2, A3, A4, A5 i A6 budu N; B1, B2 i B3 su neovisno odabrani iz skupine koja se sastoji od CR2 i N; W je O ili S; R1 je C1-C6 alkil, C2-C6 alkenil, C2-C6 alkinil, C3-C6 cikloalkil, C4-C7 alkilcikloalkil ili C4-C7 cikloalkilalkil, od kojih je svaki opcijski supstituiran s jednim ili više supstituenata koji su neovisno odabrani od R6; svaki R2 je neovisno H, halogen, C1-C6 alkil, C1-C6 haloalkil, C1-C6 alkoksi, C1-C6 haloalkoksi, C1-C6 alkiltio, C1-C6 haloalkiltio, C1-C6 alkilsulfinil, C1-C6 haloalkilsulfinil, C1-C6 alkilsulfonil, C1-C6 haloalkilsulfonil, C1-C6 alkilamino, C2-C6 dialkilamino, C2-C4 alkoksikarbonil, -CN ili -NO2; svaki R3 je neovisno H, halogen, C1-C6 alkil, C1-C6 haloalkil, C3-C6 cikloalkil, C3-C6 halocikloalkil, C1-C6 alkoksi, C1-C6 haloalkoksi, C1-C6 alkiltio, C1-C6 haloalkiltio, C1-C6 alkilsulfinil, C1-C6 haloalkilsulfinil, C1-C6 alkilsulfonil, C1-C6 haloalkilsulfonil, C1-C6 alkilamino, C2-C6 dialkilamino, -CN ili -NO2; R4 je H, C1-C6 alkil, C2-C6 alkenil, C2-C6 alkinil, C3-C6 cikloalkil, C4-C7 alkilcikloalkil, C4-C7 cikloalkilalkil, C2-C7 alkilkarbonil ili C2-C7 alkoksikarbonil; R5 je H, OR10, NR11R12 ili Q1; ili C1-C6 alkil, C2-C6 alkenil, C2-C6 alkinil, C3-C6 cikloalkil, C4-C7 alkilcikloalkil ili C4-C7 cikloalkilalkil, od kojih je svaki opcijski supstituiran s jednim ili više supstituenata koji su neovisno odabrani od R7; ili R4 i R5 se uzimaju zajedno s dušikom na kojega su priključeni, kako bi tvorili prsten koji sadrži od 2 do 6 atoma ugljika i opcijski jedan dodatni atom koji je odabran iz skupine koja se sastoji od N, S i O, gdje je navedeni prsten opcijski supstituiran s jednim do četiri supstituenta neovisno odabrana iz skupine koju čine sljedeći: C1-C2 alkil, halogen, -CN, -NO2 i C1-C2 alkoksi; svaki R6 je neovisno halogen, C1-C6 alkil, C1-C6 alkoksi, C1-C6 alkiltio, C1-C6 alkilsulfinil, C1-C6 alkilsulfonil, -CN ili -NO2; svaki R7 je neovisno halogen; C1-C6 alkil, C3-C6 cikloalkil, C1-C6 alkoksi, C1-C6 alkiltio, C1-C6 alkilsulfinil, C1-C6 alkilsulfonil, C1-C6 alkilamino, C2-C8 dialkilamino, C3-C6 cikloalkilamino, C2-C7 alkilkarbonil, C2-C7 alkoksikarbonil, C2-C7 alkilaminokarbonil, C3-C9 dialkilaminokarbonil, C2-C7 haloalkilkarbonil, C2-C7 haloalkoksikarbonil, C2-C7 haloalkilaminokarbonil, C3-C9 dihaloalkilaminokarbonil, hidroksi, -NH2, -CN ili NO2; ili Q2; svaki R8 je neovisno halogen, C1-C6 alkoksi, C1-C6 haloalkoksi, C1-C6 alkiltio, C1-C6 haloalkiltio, C1-C6 alkilsulfinil, C1-C6 haloalkilsulfinil, C1-C6 alkilsulfonil, C1-C6 haloalkilsulfonil, C1-C6 alkilamino, C2-C6 dialkilamino, C2-C4 alkoksikarbonil, -CN ili -NO2; svaki R9 je neovisno halogen, C1-C6 alkil, C1-C6 haloalkil, C3-C6 cikloalkil, C3-C6 halocikloalkil, C1-C6 alkoksi, C1-C6 haloalkoksi, C1-C6 alkiltio, C1-C6 haloalkiltio, C1-C6 alkilsulfinil, C1-C6 haloalkilsulfinil, C1-C6 alkilsulfonil, C1-C6 haloalkilsulfonil, C1-C6 alkilamino, C2-C6 dialkilamino, -CN, -NO2, fenil ili piridinil; R10 je H; ili C1-C6 alkil, C2-C6 alkenil, C2-C6 alkinil, C3-C6 cikloalkil, C4-C7 alkilcikloalkil ili C4-C7 cikloalkilalkil, od kojih je svaki opcijski supstituiran s jednim ili više halogena; R11 je H, C1-C6 alkil, C2-C6 alkenil, C2-C6 alkinil, C3-C6 cikloalkil, C4-C7 alkilcikloalkil, C4-C7 cikloalkilalkil, C2-C7 alkilkarbonil ili C2-C7 alkoksikarbonil; R12 je H; Q3; ili C1-C6 alkil, C2-C6 alkenil, C2-C6 alkinil, C3-C6 cikloalkil, C4-C7 alkilcikloalkil ili C4-C7 cikloalkilalkil, od kojih je svaki opcijski supstituiran s jednim ili više supstituenata neovisno odabranih od R7; ili R11 i R12 se uzimaju zajedno s dušikom na kojega su priključeni, kako bi tvorili prsten koji sadrži od 2 do 6 atoma ugljika i opcijski jedan dodatni atom koji je odabran iz skupine koja se sastoji od N, S i O, gdje je navedeni prsten opcijski supstituiran s jednim do četiri supstituenta neovisno odabrana iz skupine koju čine sljedeći: C1-C2 alkil, halogen, -CN, -NO2 i C1-C2 alkoksi; Q1 je fenilni prsten, 5-člani ili 6-člani heterociklički prsten, ili je 8-člani, 9-člani ili 10-člani kondenzirani biciklički sustav prstena, koji opcijski sadrži jedan do tri heteroatoma odabrana od najviše jednog O, najviše jednog S i najviše tri N, gdje je svaki sustav prstena opcijski supstituiran s jednim ili više supstituenata koji su neovisno odabrani od R8; svaki Q2 je neovisno fenilni prsten ili 5-člani ili 6-člani heterociklički prsten, pri čemu je svaki prsten opcijski supstituiran s jednim ili više supstituenata koji su neovisno odabrani od R9; Q3 je fenilni prsten ili 5-člani ili 6-člani heterociklički prsten, pri čemu je svaki prsten opcijski supstituiran s jednim ili više supstituenata koji su neovisno odabrani od R9; i n je 0, 1 ili 2; te b) farmaceutski prihvatljiv nosač koji je prikladan za primjenu na koži životinje; i pritom nosač sadrži dimetil-izosorbid.
2. Topikalni veterinarski pripravak prema patentnom zahtjevu 1, naznačen time, da: W je O; R4 je H ili C1-C6 alkil; R5 je -CH2C(O)NHCH2CF3; svaki od A1, A2, A3, A4, A5 i A6 je CH; R1 je C1-C6 alkil koji je svaki opcijski supstituiran s jednim ili više supstituenata koji su neovisno odabrani od R6; R6 je halogen ili C1-C6 alkil; i B1, B2 i B3 su neovisno CH, C-halogen, C-C1-C6 alkil, C-C1-C6 haloalkil, ili C-C1-C6 alkoksi.
3. Topikalni veterinarski pripravak prema patentnom zahtjevu 1, naznačen time, da: W je O; R1 je CF3; B2 je CH; B1 je C-Cl; B3 je C-CF3; svaki od A1, A2, A3, A4, A5 i A6 je CH; R4 je H; i R5 je -CH2C(O)NHCH2CF3.
4. Topikalni veterinarski pripravak prema patentnom zahtjevu 1, naznačen time, da farmaceutski prihvatljiv nosač nadalje obuhvaća otapalo koje je odabrano od sljedećih: glicerol formal, diizopropil adipat (DIPA), izopropil palmitat, silikonski fluid, propilenglikol (ili neki drugi alifatski dihidrički alkoholi), propilenglikol esteri, alkil esteri dikarboksilnih kiselina, te esteri ili diesteri masne kiseline, ili njihove kombinacije.
5. Topikalni veterinarski pripravak prema patentnom zahtjevu 1, naznačen time, da farmaceutski prihvatljiv nosač nadalje obuhvaća dialkilester dikarboksilne kiseline.
6. Topikalni veterinarski pripravak prema patentnom zahtjevu 5, naznačen time, da dialkilester dikarboksilne kiseline je dietil-sebakat.
7. Topikalni veterinarski pripravak prema bilo kojem od patentnih zahtjeva 1 do 6, naznačen time, da on nadalje obuhvaća najmanje jedno neko drugo djelatno sredstvo.
8. Topikalni veterinarski pripravak prema patentnom zahtjevu 7, naznačen time, da najmanje jedno neko drugo djelatno sredstvo je avermektin ili milbemicin.
9. Topikalni veterinarski pripravak prema patentnom zahtjevu 8, naznačen time, da avermektin ili milbemicin je eprinomektin, ivermektin, selamektin, milbemektin, milbemicin D, milbemicin oksim ili moksidektin.
10. Topikalni veterinarski pripravak prema patentnom zahtjevu 7, naznačen time, da najmanje jedno neko drugo djelatno sredstvo je regulator rasta kukca.
11. Topikalni veterinarski pripravak prema patentnom zahtjevu 10, naznačen time, da regulator rasta kukca je (S)-metopren, piriproksifen, hidropren, ciromazin, fluazuron, lufenuron ili novaluron.
12. Topikalni veterinarski pripravak prema patentnom zahtjevu 7, naznačen time, da najmanje jedno neko drugo djelatno sredstvo je anthelmintsko djelatno sredstvo koje je odabrano od tiabendazola, oksibendazola, mebendazola, fenbendazola, oksfendazola, albendazola, triklabendazola, febantela, levamisola, pirantela, morantela, prazikvantela, klozantela, klorsulona, djelatnog sredstva amino-acetonitrila ili ariloazol-2-il-cijanoetilamino-djelatnog sredstva.
13. Topikalni veterinarski pripravak prema patentnom zahtjevu 1, naznačen time, da pripravak obuhvaća od 5 do 15% (masa/volumen) spoja formule (I).
14. Topikalni veterinarski pripravak prema patentnom zahtjevu 1, naznačen time, da djelatno sredstvo izoksazolina je enantiomer od 4-[5-[3-kloro-5-(trifluorometil)fenil]-4,5-dihidro-5-(trifluorometil)-3-izoksazolil]-N-[2-okso-2-[(2,2,2-trifluoroetil)amino]etil]-1-naftalenkarboksamida.
15. Topikalni veterinarski pripravak prema bilo kojem od patentnih zahtjeva 1 do 14, naznačen time, da se upotrebljava u liječenju ili prevenciji parazitne okuženosti ili parazitne infekcije kod mačke ili psa.
16. Topikalni veterinarski pripravak prema bilo kojem od patentnih zahtjeva 1 do 14, za uporabu prema patentnom zahtjevu 15, naznačen time, da se kod pripravka radi o spot-on pripravku, te pritom volumen pripravka iznosi od 0,1 do 10 ml.
17. Topikalni veterinarski pripravak prema bilo kojem od patentnih zahtjeva 1 do 14, za uporabu prema patentnom zahtjevu 16, naznačen time, da volumen pripravka iznosi od 0,1 do 5 ml.
18. Topikalni veterinarski pripravak prema bilo kojem od patentnih zahtjeva 1 do 14, za uporabu prema patentnom zahtjevu 16, naznačen time, da volumen pripravka iznosi od 0,1 do 1 ml.
19. Topikalni veterinarski pripravak prema bilo kojem od patentnih zahtjeva 1 do 14, za uporabu prema bilo kojem od patentnih zahtjeva 15 do 18, naznačen time, da životinja je mačka.
20. Topikalni veterinarski pripravak prema bilo kojem od patentnih zahtjeva 1 do 14, za uporabu prema patentnom zahtjevu 19, naznačen time, da volumen pripravka iznosi od 0,5 ml do 1 ml.
21. Topikalni veterinarski pripravak prema bilo kojem od patentnih zahtjeva 1 do 14, za uporabu prema patentnom zahtjevu 19, naznačen time, da volumen pripravka iznosi od 0,5 ml do 2 ml.
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