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AR083200A1 - Compuestos de n-heteroarilo - Google Patents

Compuestos de n-heteroarilo

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Publication number
AR083200A1
AR083200A1 ARP110103573A ARP110103573A AR083200A1 AR 083200 A1 AR083200 A1 AR 083200A1 AR P110103573 A ARP110103573 A AR P110103573A AR P110103573 A ARP110103573 A AR P110103573A AR 083200 A1 AR083200 A1 AR 083200A1
Authority
AR
Argentina
Prior art keywords
alkyl
aminocarbonyl
hydrogen
cycloalkyl
amino
Prior art date
Application number
ARP110103573A
Other languages
English (en)
Original Assignee
Intervet Int Bv
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 Intervet Int Bv filed Critical Intervet Int Bv
Publication of AR083200A1 publication Critical patent/AR083200A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/89Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to the ring nitrogen atom
    • 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
    • A61K31/47Quinolines; Isoquinolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/10Anthelmintics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/74Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/38Nitrogen atoms
    • C07D215/42Nitrogen atoms attached in position 4
    • C07D215/46Nitrogen atoms attached in position 4 with hydrocarbon radicals, substituted by nitrogen atoms, attached to said nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/42One nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/04Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D413/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

El medicamento puede usarse preferiblemente para tratar infecciones helmínticas y el tratamiento de parasitosis, tales como las provocadas por infecciones helmínticas. También se refiere a usos de los compuestos para elaborar medicamentos y tratamientos que comprenden la administración de los compuestos a animales que necesitan dichos tratamientos. También se refiere a compuestos de N-heteroarilo y a la preparación de dichos compuestos y a composiciones farmacéuticas y kits que comprenden los compuestos.Reivindicación 1: Un compuesto de la fórmula (1) y sus sales, solvatos, N-óxidos o profármacos farmacéuticamente aceptables, donde R1 es halógeno, alquilo C1-6, alquiloxi C1-6, alquiltio C1-6, alquenilo C2-6, alquinilo C2-6, alquiloxi C1-6-alquilo C1-6, alquiltio C1-6-alquilo C1-6, alquilo C1-6-carbonilo, alquenilo C2-6-carbonilo, SF5, alquilo C1-6-sulfonilo donde cada uno de los radicales que contienen carbonos opcionalmente está sustituido con uno o varios átomos de halógeno, preferiblemente átomos de flúor; R2 es hidrógeno, halógeno, alquilo C1-6, alquiloxi C1-6, alquiltio C1-6, alquenilo C2-6, alquinilo C2-6, alquiloxi C1-6- alquilo C1-6, alquiltio C1-6-alquilo C1-6, alquilo C1-6-carbonilo, alquenilo C2-6-carbonilo, alquenilo C2-6-carbonilo, donde cada uno de los radicales que contienen carbonos opcionalmente está sustituido con uno o varios átomos de halógeno, preferiblemente átomos de flúor; R3 es hidrógeno, alquilo C1-6 o cicloalquilo, preferiblemente hidrógeno; R4 es hidrógeno, alquilo C1-6 o cicloalquilo, preferiblemente hidrógeno; R5 es hidrógeno, alquilo C1-6, cicloalquilo, acilo, cicloalquiloxicarbonilo, alquiloxi C1-6-carbonilo; R6 es hidrógeno, alquilo C1-6, cicloalquilo, hidroxi, alquiloxi C1-6, fenil-alquiloxi C1-6, hidroxi-alquilo C1-6, alquiloxi C1-6-alquilo C1-6, fenil-alquiloxi C1-6-alquilo C1-6, tiol-alquilo C1-6, alquiltio C1-6-alquilo C1-6, fenil-alquiltio C1-6-alquilo C1-6, hidroxicarbonilo, hidroxicarbonil-alquilo C1-6, alquiloxi C1-6-carbonilo, alquiloxi C1-6-carbonil-alquilo C1-6, aminocarbonilo, aminocarbonil-alquilo C1-6, alquilo C1-6-aminocarbonilo, alquilo C1-6-aminocarbonilo-alquilo C1-6, di(alquilo C1-6)aminocarbonilo, di(alquilo C1-6)aminocarbonilo-alquilo C1-6, alquilo C1-6-amino-alquilo C1-6, di(alquilo C1-6)amino-alquilo C1-6, fenilo, fenil-alquilo C1-6, donde cada grupo fenilo está opcionalmente sustituido con hidroxi, cicloalquiloxi o alquiloxi C1-6; R7 es hidrógeno, alquilo C1-6 o cicloalquilo; o R6 está unido a R8 para formar un grupo alquileno C1-3 y R7 está unido a R9 para formar un grupo alquileno C1-3, donde uno o ambos de dichos grupos alquileno C1-3 están opcionalmente sustituidos con uno o varios radicales alquilo C1-6 o cicloalquilo; n es un número entero de 1 a 3; X es un grupo carbonilo, tiocarbonilo o sulfonilo, preferiblemente un grupo carbonilo; A es un enlace o NR8, donde R8 es hidrógeno o alquilo C1-6, preferiblemente hidrógeno; E es un enlace o NR9, donde R9 es hidrógeno o alquilo C1-6, preferiblemente hidrógeno; B es N o CR10, donde R10 es hidrógeno o alquilo C1-6, preferiblemente hidrógeno; D es N o CR11, donde R11 es hidrógeno o alquilo C1-6, preferiblemente hidrógeno; Y1 es C o N, donde C está sustituido con R12 que es hidrógeno, halógeno, alquilo C1-6, alquenilo C1-6, cicloalquilo, cicloalquiloxi, haloalquilo C1-6, alcoxi C1-6, haloalcoxi C1-6, nitrilo, nitro, amino, alquilo C1-6-amino, cicloalquilamino, di(alquilo C1-6)amino, (alquilo C1-6)-(cicloalquil)amino, N-pirrolidinilo, N-piperidinilo, N-morfolinilo, alquiltio C1-6, cicloalquiltio, haloalquiltio C1-6, alquilo C1-6-carbonilo, haloalquilo C1-6-carbonilo, alquilo C1-6-carbonilamino, aminocarbonilo, alquilo C1-6-aminocarbonilo, di(alquilo C1-6)-aminocarbonilo, alcoxi C1-6-carbonilo, fenilo, dioxolano tal como 1,3-dioxolano, dioxano tal como 1,3-dioxano, o dioxepano tal como 1,3-dioxepano, cada uno de dichos anillos no está sustituido o está sustituido con alquilo C1-6; Y2 es C o N, donde C está sustituido con R13 que es hidrógeno, halógeno, alquilo C1-6, alquenilo C1-6, cicloalquilo, cicloalquiloxi, haloalquilo C1-6, alcoxi C1-6, haloalcoxi C1-6, nitrilo, nitro, amino, alquilo C1-6-amino, cicloalquilamino, di(alquilo C1-6)amino, (alquilo C1-6)-(cicloalquil)amino, N-pirrolidinilo, N-piperidinilo, N-morfolinilo, tiol, hidroxi, alquiltio C1-6, cicloalquiltio, haloalquiltio C1-6, alquilo C1-6-carbonilo, haloalquilo C1-6-carbonilo, aminocarbonilo, alquilo C1-6-aminocarbonilo, di(alquilo C1-6)-aminocarbonilo, alquilo C1-6-carbonilamino, alcoxi C1-6-carbonilo, dioxolano tal como 1,3-dioxolano, dioxano tal como 1,3-dioxano, o dioxepano tal como 1,3-dioxepano, cada uno de dichos anillos no está sustituido o está sustituido con alquilo C1-6; Y3 es C o N, donde C está sustituido con R14 que es hidrógeno, halógeno, alquilo C1-6, alquenilo C1-6, cicloalquilo, cicloalquiloxi, haloalquilo C1-6, alcoxi C1-6, haloalcoxi C1-6, nitrilo, nitro, amino, alquilo C1-6-amino, cicloalquilamino, di(alquilo C1-6)amino, (alquilo C1-6)-(cicloalquil)amino, N-pirrolidinilo, N-piperidinilo, N-morfolinilo, tiol, hidroxi, alquiltio C1-6, cicloalquiltio, haloalquiltio C1-6, alquilo C1-6-carbonilo, haloalquilo C1-6-carbonilo, alquilo C1-6-carbonilamino, aminocarbonilo, alquilo C1-6-aminocarbonilo, di(alquilo C1-6)aminocarbonilo, alcoxi C1-6-carbonilo, dioxolano tal como 1,3-dioxolano, dioxano tal como 1,3-dioxano, o dioxepano tal como 1,3-dioxepano, cada uno de dichos anillos no está sustituido o está sustituido con alquilo C1-6; Y4 es C o N, donde C está sustituido con R15 que es hidrógeno, halógeno, alquilo C1-6, alquenilo C1-6, cicloalquilo, cicloalquiloxi, haloalquilo C1-6, alcoxi C1-6, haloalcoxi C1-6, nitrilo, nitro, amino, alquilo C1-6-amino, cicloalquilamino, di(alquilo C1-6)amino, (alquilo C1-6)-(cicloalquil)amino, N-pirrolidinilo, N-piperidinilo, N-morfolinilo, alquiltio C1-6, haloalquiltio C1-6, alquilo C1-6-carbonilo, haloalquilo C1-6-carbonilo, alquilo C1-6-carbonilamino, aminocarbonilo, alquilo C1-6-aminocarbonilo, di(alquilo C1-6)aminocarbonilo, alcoxi C1-6-carbonilo, fenilo, dioxolano tal como 1,3-dioxolano, dioxano tal como 1,3-dioxano, o dioxepano tal como 1,3-dioxepano, cada uno de dichos anillos no está sustituido o está sustituido con alquilo C1-6; o Y1 e Y2 y/o Y3 e Y4 se unen entre sí para formar un sistema de anillos, y donde por lo menos uno de B y D es un átomo de nitrógeno.
ARP110103573A 2010-09-29 2011-09-28 Compuestos de n-heteroarilo AR083200A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP10181553 2010-09-29
US38846610P 2010-09-30 2010-09-30

Publications (1)

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AR083200A1 true AR083200A1 (es) 2013-02-06

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ARP110103573A AR083200A1 (es) 2010-09-29 2011-09-28 Compuestos de n-heteroarilo

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US (1) US8877934B2 (es)
EP (1) EP2621903B1 (es)
JP (1) JP5791725B2 (es)
KR (1) KR101916481B1 (es)
CN (2) CN103189356B (es)
AR (1) AR083200A1 (es)
AU (1) AU2011310592B2 (es)
BR (1) BR112013006030B1 (es)
CA (1) CA2811369C (es)
CO (1) CO6710926A2 (es)
ES (1) ES2622881T3 (es)
HU (1) HUE034042T2 (es)
MX (1) MX340985B (es)
NZ (1) NZ607580A (es)
PL (1) PL2621903T3 (es)
RU (1) RU2596185C2 (es)
WO (1) WO2012041873A1 (es)

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EP2621903B1 (en) 2017-03-01
WO2012041873A1 (en) 2012-04-05
JP2014500235A (ja) 2014-01-09
US20130196993A1 (en) 2013-08-01
US8877934B2 (en) 2014-11-04
JP5791725B2 (ja) 2015-10-07
RU2596185C2 (ru) 2016-08-27
CA2811369A1 (en) 2012-04-05
BR112013006030A2 (pt) 2016-06-07
CN103189356A (zh) 2013-07-03
PL2621903T3 (pl) 2017-08-31
BR112013006030B1 (pt) 2020-03-17
CN105294549A (zh) 2016-02-03
AU2011310592B2 (en) 2015-01-22
MX340985B (es) 2016-08-01
KR101916481B1 (ko) 2018-11-07
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EP2621903A1 (en) 2013-08-07
KR20130139889A (ko) 2013-12-23
CA2811369C (en) 2019-09-03
NZ607580A (en) 2015-01-30
CO6710926A2 (es) 2013-07-15
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RU2013119681A (ru) 2014-11-10
ES2622881T3 (es) 2017-07-07

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