AR095183A1 - Derivados de azetidina como agentes antiparasitarios - Google Patents

Derivados de azetidina como agentes antiparasitarios

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Publication number
AR095183A1
AR095183A1 ARP130101605A ARP130101605A AR095183A1 AR 095183 A1 AR095183 A1 AR 095183A1 AR P130101605 A ARP130101605 A AR P130101605A AR P130101605 A ARP130101605 A AR P130101605A AR 095183 A1 AR095183 A1 AR 095183A1
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Argentina
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alkyl
cyano
haloalkyl
hydroxyl
cycloalkyl
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ARP130101605A
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English (en)
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M K Sheehan Susan
Vaillancourt Valerie
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Zoetis Llc
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Publication of AR095183A1 publication Critical patent/AR095183A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION 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
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/02Biocides, 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
    • A01N43/04Biocides, 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
    • A01N43/20Biocides, 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 three- or four-membered rings
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION 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
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/34Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom
    • A01N43/36Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom five-membered rings
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION 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
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/34Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom
    • A01N43/44Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom three- or four-membered rings
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION 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
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/48Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with two nitrogen atoms as the only ring hetero atoms
    • A01N43/561,2-Diazoles; Hydrogenated 1,2-diazoles
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION 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
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/72Biocides, 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
    • A01N43/74Biocides, 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 1,3
    • A01N43/761,3-Oxazoles; Hydrogenated 1,3-oxazoles
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION 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
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/72Biocides, 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
    • A01N43/82Biocides, 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 three ring hetero atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/42Oxazoles
    • A61K31/422Oxazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings

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  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Plant Pathology (AREA)
  • Zoology (AREA)
  • Environmental Sciences (AREA)
  • Wood Science & Technology (AREA)
  • Dentistry (AREA)
  • Agronomy & Crop Science (AREA)
  • Pest Control & Pesticides (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Composiciones del mismo y su uso como parasiticidas en animales. Reivindicación1: Un compuesto caracterizado porque tiene la fórmula (1), en la que A es fenilo, naftilo o heteroarilo, en el que dicho heteroarilo contiene de 1 a 4 heteroátomos, cada uno seleccionado de forma independiente de N, O y S; B es un compuesto del grupo de fórmulas (2); en donde ~~~ representa el punto de unión; R¹ᵃ, R¹ᵇ y R¹ᶜ son, cada uno de forma independiente, hidrógeno, halógeno, hidroxilo, ciano, nitro, alquilo C₁₋₆, haloalquilo C₁₋₆, alcoxi C₁₋₆, alquilo C₀₋₃-cicloalquilo C₃₋₆, haloalcoxi C₁₋₆, -C(O)NH₂, -SF₅ o -S(O)ₚR; R² es halógeno, ciano, alquilo C₁₋₆, haloalquilo C₁₋₆, nitro, hidroxilo, -C(O)NRᵃRᵇ, alquenilo C₂₋₆, alquinilo C₂₋₆, -S(O)ₚR o -OR; R³ es hidrógeno, halógeno, hidroxilo, ciano, alquilo C₁₋₆, haloalquilo C₁₋₆, alquilo C₀₋₃-cicloalquilo C₃₋₆, -C(O)NH₂, nitro, -SC(O)R, -C(O)NRᵃRᵇ, alquilo C₀₋₃NRᵃR⁴, NRᵃNRᵇR⁴, NRᵃORᵇ, ONRᵃRᵇ, N₃, -NHR⁴, -OR o -S(O)ₚR; R⁴ es hidrógeno, alquilo C₁₋₆, alquilo C₀₋₆-cicloalquilo C₃₋₆, -C(O)R⁵, -C(S)R⁵, -C(O)NRᵃR⁵, -C(O)C(O)NRᵃR⁵, -S(O)ₚRᶜ, -S(O)₂NRᵃR⁵, -C(NR⁷)R⁵, -C(NR⁷)NRᵃR⁵, alquilfenilo C₀₋₆, alquilheteroarilo C₀₋₆ o alquilheterociclo C₀₋₆; R⁵ es hidrógeno, alquilo C₁₋₆, alquenilo C₂₋₆, alquilo C₀₋₆-cicloalquilo C₃₋₆, alquilfenilo C₀₋₆, alquilheteroarilo C₀₋₆ o alquilheterociclo C₀₋₆; R⁶ es ciano, alquilo C₁₋₆, haloalquilo C₁₋₆, -C(O)NRᵃRᵇ, alquenilo C₂₋₆, alquinilo C₂₋₆, haloalquenilo C₂₋₆ o haloalquinilo C₂₋₆; R⁷ es hidrógeno, alquilo C₁₋₆, hidroxilo, ciano, nitro, -S(O)ₚRᶜ o alcoxi C₁₋₆; R⁸ es hidrógeno, alquilo C₁₋₆, hidroxilo, ciano, -S(O)ₚRᶜ o alcoxi C₁₋₆; R es alquilo C₁₋₆ o cicloalquilo C₃₋₆ cada uno sustituido opcionalmente con al menos un halógeno; Rᵃ es hidrógeno, alquilo C₁₋₆ o alquilo C₀₋₃-cicloalquilo C₃₋₆; en donde el alquilo y el alquilcicloalquilo están sustituidos opcionalmente con ciano o al menos un sustituyente halo; Rᵇ es hidrógeno, alquilo C₁₋₆, cicloalquilo C₃₋₆, alquilfenilo C₀₋₃, alquilheteroarilo C₀₋₃ o alquilheterociclo C₀₋₃, cada uno opcionalmente sustituido, cuando es químicamente posible, con al menos un sustituyente seleccionado de hidroxilo, ciano, halo o -S(O)ₙR; Rᶜ es alquilo C₁₋₆, haloalquilo C₁₋₆, haloalquilo C₁₋₆-cicloalquilo C₃₋₆, alquilo C₀₋₃-cicloalquilo C₃₋₆, alquilfenilo C₀₋₃, alquilheteroarilo C₀₋₃ o alquilheterociclo C₀₋₃ cada uno sustituido opcionalmente con al menos un sustituyente seleccionado de ciano, halo, hidroxilo, oxo, alquilo C₁₋₆, alcoxi C₁₋₆ haloalcoxi C₁₋₆, haloalquilo C₁₋₆, -S(O)ₚR, -SH, -S(O)ₚNRᵃRᵇ, -NRᵃRᵇ, -NRᵃC(O)Rᵇ, -SC(O)Rᵇ, -SCN o -C(O)NRᵃRᵇ; cada uno de R⁴ y R⁵ alquilo C₁₋₆ o alquilo C₀₋₆-cicloalquilo C₃₋₆ se pueden sustituir opcional e independientemente con al menos un sustituyente seleccionado de alquilo C₁₋₆ ciano, halo, hidroxilo, hidroxialquilo C₁₋₆ oxo, alcoxi C₁₋₆, haloalcoxi C₁₋₆, alquilo C₁₋₆, haloalquilo C₁₋₆, -S(O)ₚRᶜ, -SH, -S(O)ₚNRᵃRᵇ, -NRᵃRᵇ, -NRᵃC(O)Rᵇ, -SC(O)Rᶜ, -SCN o -C(O)NRᵃRᵇ; y en donde los restos R⁴ y R⁵, alquilfenilo C₀₋₆, alquilheteroarilo C₀₋₆ o alquilheterociclo C₀₋₆ pueden estar además opcionalmente sustituidos con al menos un sustituyente seleccionado de alquilo C₁₋₆, ciano, halo, oxo, =S, =NR⁷, hidroxilo, hidroxialquilo C₁₋₆, alcoxi C₁₋₆, alquilo C₁₋₆, haloalquilo C₁₋₆, -SH, -S(O)ₚR y haloalcoxi C₁₋₆; n es el número entero 0, 1 ó 2 y cuando n es 2, cada R² pueden ser idénticos o diferentes entre sí; y p es el número entero 0, 1 ó 2, estereoisómeros del mismo y sales farmacéutica o veterinariamente aceptables del mismo.
ARP130101605A 2012-05-09 2013-05-08 Derivados de azetidina como agentes antiparasitarios AR095183A1 (es)

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EP (1) EP2855457A1 (es)
JP (1) JP6049866B2 (es)
CN (1) CN104271568B (es)
AR (1) AR095183A1 (es)
AU (1) AU2013259847B2 (es)
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CA (1) CA2872989A1 (es)
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JP2015516424A (ja) 2015-06-11
CN104271568A (zh) 2015-01-07
CN104271568B (zh) 2016-05-04
WO2013169622A1 (en) 2013-11-14
US20150119377A1 (en) 2015-04-30
ZA201407696B (en) 2016-05-25
US9073912B2 (en) 2015-07-07
EP2855457A1 (en) 2015-04-08
AU2013259847A1 (en) 2014-10-30
BR112014027805A2 (pt) 2017-06-27
MX336431B (es) 2016-01-18
CL2014002868A1 (es) 2014-12-19
AU2013259847B2 (en) 2015-09-03
CO7141427A2 (es) 2014-12-12
JP6049866B2 (ja) 2016-12-21
MX2014013594A (es) 2014-12-04

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