AR089014A1 - Antihelminticos de sulfonamida - Google Patents

Antihelminticos de sulfonamida

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Publication number
AR089014A1
AR089014A1 ARP120104468A ARP120104468A AR089014A1 AR 089014 A1 AR089014 A1 AR 089014A1 AR P120104468 A ARP120104468 A AR P120104468A AR P120104468 A ARP120104468 A AR P120104468A AR 089014 A1 AR089014 A1 AR 089014A1
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Argentina
Prior art keywords
cyano
nitro
halogen
optionally substituted
alkyl
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ARP120104468A
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English (en)
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Philip Lahm George
Kar Moumita
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Du Pont
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Publication of AR089014A1 publication Critical patent/AR089014A1/es

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    • 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
    • C07D215/12Heterocyclic 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 substituted hydrocarbon radicals attached to ring carbon 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
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • 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
    • A61K31/4709Non-condensed quinolines 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
    • A61K31/695Silicon compounds
    • 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
    • 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
    • C07D401/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/0803Compounds with Si-C or Si-Si linkages
    • C07F7/081Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
    • C07F7/0812Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring

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

Abstract

Se describen composiciones que los contienen y su uso para tratar infecciones de helmintos. Reivindicación 1: Un compuesto de la fórmula (1), un N-óxido o sal de este caracterizado porque, Q es fenilo o naftalenilo cada uno opcionalmente sustituido con hasta 5 sustituyentes seleccionados independientemente de R⁴ᵃ; o Q es un anillo heteroaromático de 5 a 6 miembros o un sistema anular bicíclico heteroaromático de 8 a 11 miembros, cada anillo o sistema anular contiene miembros del anillo seleccionados de átomos de carbono y hasta 4 heteroátomos seleccionados independientemente de hasta 2 O, hasta 2 S y hasta 4 N y opcionalmente sustituidos con hasta 5 sustituyentes seleccionados independientemente de R⁴ᵃ en miembros de anillo de átomos de carbono y R⁴ᵇ en miembros de anillo de átomos de nitrógeno; A es N, CH o CR¹; cada R¹ es independientemente halógeno, ciano, nitro, OR⁶, NR⁷ᵃR⁷ᵇ, C(O)R⁸, C(O)OR⁹, C(O)NR¹⁰R¹¹, S(O)ₚR¹² o S(O)₂NR¹⁰R¹¹; o alquilo C₁₋₆, alquenilo C₂₋₆ o alquinilo C₂₋₆, cada uno opcionalmente sustituido con sustituyentes seleccionados del grupo que consiste en halógeno, ciano, nitro, OR⁶, NR⁷ᵃR⁷ᵇ, C(O)R⁸, C(O)OR⁹, C(O)NR¹⁰R¹¹, S(O)ₚR¹² y S(O)₂NR¹⁰R¹¹; o cicloalquilo C₃₋₇, cicloalquilalquilo C₄₋₈ o cicloalquenilo C₅₋₇, cada uno opcionalmente sustituido con sustituyentes seleccionados independientemente del grupo que consiste en halógeno, ciano, nitro, alquilo C₁₋₄, haloalquilo C₁₋₄, OR⁶ y S(O)ₚR¹²; R² es hidrógeno, ciano, OR⁶, NR⁷ᵃR⁷ᵇ, C(O)R⁸, C(O)OR⁹, C(O)NR¹⁰R¹¹, S(O)ₚR¹² o S(O)₂NR¹⁰R¹¹; o alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆ o bencilo, cada uno opcionalmente sustituido con sustituyentes seleccionados independientemente del grupo que consiste en halógeno, ciano, nitro, OR⁶, NR⁷ᵃR⁷ᵇ, C(O)R⁸, C(O)OR⁹, C(O)NR¹⁰R¹¹, S(O)ₚR¹² y S(O)₂NR¹⁰R¹¹; o cicloalquilo C₃₋₇, cicloalquilalquilo C₄₋₈ o cicloalquenilo C₅₋₇, cada uno opcionalmente sustituido con sustituyentes seleccionados independientemente del grupo que consiste en halógeno, ciano, nitro, alquilo C₁₋₄, haloalquilo C₁₋₄, OR⁶ y S(O)ₚR¹²; R³ es hidrógeno, C(O)R⁸, C(O)OR⁹, C(O)NR¹⁰R¹¹, S(O)ₚR¹², S(O)₂NR¹⁰R¹¹ o Si(R¹³)₃; o alquilo C₁₋₆, alquenilo C₂₋₆ o alquinilo C₂₋₆, cada uno opcionalmente sustituido con sustituyentes seleccionados del grupo que consiste en halógeno, ciano, nitro, OR⁶, NR⁷ᵃR⁷ᵇ, C(O)R⁸, C(O)OR⁹, C(O)NR¹⁰R¹¹, S(O)ₚR¹² y S(O)₂NR¹⁰R¹¹; o cicloalquilo C₃₋₇, cicloalquilalquilo C₄₋₈ o cicloalquenilo C₅₋₇, cada uno opcionalmente sustituido con sustituyentes seleccionados independientemente del grupo que consiste en halógeno, ciano, nitro, alquilo C₁₋₄, haloalquilo C₁₋₄, OR⁶, NR⁷ᵃR⁷ᵇ, C(O)R⁸, C(O)OR⁹, C(O)NR¹⁰R¹¹, S(O)ₚR¹² y S(O)₂NR¹⁰R¹¹; o G; G es un anillo heterocíclico aromático de 5 a 6 miembros, un anillo heterocíclico no aromático de 3 a 7 miembros o un sistema anular bicíclico heterocíclico no aromático de 8 a 11 miembros, cada anillo o sistema anular contiene miembros anulares seleccionados de átomos de carbono y hasta 4 heteroátomos seleccionados independientemente de átomos de hasta 2 O, hasta 2 S y hasta 4 N, y opcionalmente sustituidos con hasta 5 sustituyentes seleccionados independientemente de R⁵ᵃ en miembros de anillo de átomos de carbono y R⁵ᵇ en miembros de anillo de átomos de nitrógeno; cada R⁴ᵃ es independientemente halógeno, ciano, nitro, OR⁶, NR⁷ᵃR⁷ᵇ, C(O)R⁸, C(O)OR⁹, C(O)NR¹⁰R¹¹, S(O)ₚR¹² o S(O)₂NR¹⁰R¹¹; o alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cada uno opcionalmente sustituido del grupo que consiste en halógeno, ciano, nitro, OR⁶, NR⁷ᵃR⁷ᵇ, C(O)R⁸, C(O)OR⁹, C(O)NR¹⁰R¹¹, S(O)ₚR¹² y S(O)₂NR¹⁰R¹¹; o cicloalquilo C₃₋₇, cicloalquilalquilo C₄₋₈ o cicloalquenilo C₅₋₇, cada uno opcionalmente sustituido con sustituyentes seleccionados independientemente del grupo que consiste en halógeno, ciano, nitro, alquilo C₁₋₄, haloalquilo C₁₋₄, OR⁶ y S(O)ₚR¹²; R⁴ᵇ es ciano, OR⁶, NR⁷ᵃR⁷ᵇ, C(O)R⁸, C(O)OR⁹, C(O)NR¹⁰R¹¹, S(O)ₚR¹² o S(O)₂NR¹⁰R¹¹; o alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆ o bencilo, cada uno opcionalmente sustituido con sustituyentes seleccionados independientemente del grupo que consiste en halógeno, ciano, nitro, OR⁶, NR⁷ᵃR⁷ᵇ, C(O)R⁸, C(O)OR⁹, C(O)NR¹⁰R¹¹, S(O)ₚR¹² y S(O)₂NR¹⁰R¹¹; o cicloalquilo C₃₋₇, cicloalquilalquilo C₄₋₈ o cicloalquenilo C₅₋₇, cada uno opcionalmente sustituido con sustituyentes seleccionados independientemente del grupo que consiste en halógeno, ciano, nitro, alquilo C₁₋₄, haloalquilo C₁₋₄, OR⁶ y S(O)ₚR¹²; cada R⁵ᵃ es independientemente halógeno, ciano, nitro, OR⁶, NR⁷ᵃR⁷ᵇ, C(O)R⁸, C(O)OR⁹, C(O)NR¹⁰R¹¹, S(O)ₚR¹² o S(O)₂NR¹⁰R¹¹; o alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cada uno opcionalmente sustituido del grupo que consiste en halógeno, ciano, nitro, OR⁶, NR⁷ᵃR⁷ᵇ, C(O)R⁸, C(O)OR⁹, C(O)NR¹⁰R¹¹, S(O)ₚR¹² y S(O)₂NR¹⁰R¹¹; o cicloalquilo C₃₋₇, cicloalquilalquilo C₄₋₈ o cicloalquenilo C₅₋₇, cada uno opcionalmente sustituido con sustituyentes seleccionados independientemente del grupo que consiste en halógeno, ciano, nitro, alquilo C₁₋₄, haloalquilo C₁₋₄, OR⁶ y S(O)ₚR¹²; cada R⁵ᵇ es ciano, OR⁶, NR⁷ᵃR⁷ᵇ, C(O)R⁸, C(O)OR⁹, C(O)NR¹⁰R¹¹, S(O)ₚR¹² o S(O)₂NR¹⁰R¹¹; o alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆ o bencilo, cada uno opcionalmente sustituido con sustituyentes seleccionados independientemente del grupo que consiste en halógeno, ciano, nitro, OR⁶, NR⁷ᵃR⁷ᵇ, C(O)R⁸, C(O)OR⁹, C(O)NR¹⁰R¹¹, S(O)ₚR¹² y S(O)₂NR¹⁰R¹¹; o cicloalquilo C₃₋₇, cicloalquilalquilo C₄₋₈ o cicloalquenilo C₅₋₇, cada uno opcionalmente sustituido con sustituyentes seleccionados independientemente del grupo que consiste en halógeno, ciano, nitro, alquilo C₁₋₄, haloalquilo C₁₋₄, OR⁶ y S(O)ₚR¹²; cada R⁶ es independientemente hidrógeno, alquilcarbonilo C₂₋₆, alcoxicarbonilo C₂₋₆, alquilaminocarbonilo C₂₋₆, dialquilaminocarbonilo C₃₋₈, alquilsulfenilo C₁₋₆, alquilsulfinilo C₁₋₆, alquilsulfonilo C₁₋₆, alquilaminosulfonilo C₂₋₆ o dialquilaminosulfonilo C₃₋₆; o alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆ o bencilo, cada uno opcionalmente sustituido con sustituyentes seleccionados independientemente del grupo que consiste en halógeno, ciano, nitro, alcoxi C₁₋₆, alquilamino C₁₋₆, dialquilamino C₂₋₈, alquilcarbonilo C₂₋₆, alcoxicarbonilo C₂₋₆, alquilaminocarbonilo C₂₋₆, dialquilaminocarbonilo C₃₋₆, alquilsulfenilo C₁₋₆, alquilsulfinilo C₁₋₆, alquilsulfonilo C₁₋₆, alquilaminosulfonilo C₂₋₆ y dialquilaminosulfonilo C₃₋₆ o cicloalquilo C₃₋₇, cicloalquilalquilo C₄₋₈ o cicloalquenilo C₅₋₇, cada uno opcionalmente sustituido con sustituyentes seleccionados independientemente del grupo que consiste en halógeno, ciano, nitro, alquilo C₁₋₄, haloalquilo C₁₋₄, alcoxi C₁₋₄, alquilsulfenilo C₁₋₄, alquilsulfinilo C₁₋₄ y alquilsulfonilo C₁₋₄; cada R⁷ᵃ es independientemente hidrógeno, alquilcarbonilo C₂₋₆, alcoxicarbonilo C₂₋₆, alquilaminocar
ARP120104468A 2011-11-28 2012-11-28 Antihelminticos de sulfonamida AR089014A1 (es)

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US (1) US20140315857A1 (es)
EP (1) EP2785694A1 (es)
JP (1) JP2015502936A (es)
KR (1) KR20140094026A (es)
CN (1) CN103958476A (es)
AR (1) AR089014A1 (es)
AU (1) AU2012346433A1 (es)
BR (1) BR112014012759A8 (es)
CA (1) CA2855001A1 (es)
CL (1) CL2014001377A1 (es)
CO (1) CO6980661A2 (es)
IL (1) IL232404A0 (es)
MA (1) MA35742B1 (es)
MX (1) MX2014006317A (es)
PH (1) PH12014501181A1 (es)
RU (1) RU2014126367A (es)
SG (1) SG11201402664VA (es)
TN (1) TN2014000166A1 (es)
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US20140315857A1 (en) 2014-10-23
PH12014501181A1 (en) 2014-09-08
TW201326128A (zh) 2013-07-01
EP2785694A1 (en) 2014-10-08
KR20140094026A (ko) 2014-07-29
AU2012346433A1 (en) 2014-05-08
CA2855001A1 (en) 2013-06-06
CL2014001377A1 (es) 2014-10-17
MX2014006317A (es) 2014-06-23
BR112014012759A8 (pt) 2017-06-20
RU2014126367A (ru) 2016-01-27
CO6980661A2 (es) 2014-06-27
IL232404A0 (en) 2014-06-30
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TN2014000166A1 (en) 2015-09-30
MA35742B1 (fr) 2014-12-01

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