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AR082153A1 - N-sulfonilbenzamidas utiles como inhibidor del canal de sodio - Google Patents

N-sulfonilbenzamidas utiles como inhibidor del canal de sodio

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Publication number
AR082153A1
AR082153A1 ARP110102490A ARP110102490A AR082153A1 AR 082153 A1 AR082153 A1 AR 082153A1 AR P110102490 A ARP110102490 A AR P110102490A AR P110102490 A ARP110102490 A AR P110102490A AR 082153 A1 AR082153 A1 AR 082153A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
independently
cycloalkyl
alkyl
het2
Prior art date
Application number
ARP110102490A
Other languages
English (en)
Inventor
Nunzio Sciammetta
Robert Ian Storer
Nigel Alan Swain
Andrew Simon Bell
Alan Daniel Brown
Groot Marcel John De
Steven Matthieu Gaulier
Russell Andrew Lewthwaite
Ian Roger Marsh
David Simon Millan
Pacheco Manuel Perez
David James Rawson
Original Assignee
Pfizer Ltd
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 Pfizer Ltd filed Critical Pfizer Ltd
Publication of AR082153A1 publication Critical patent/AR082153A1/es

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    • 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
    • C07D213/62Oxygen or sulfur atoms
    • C07D213/69Two or more oxygen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • 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
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    • 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
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    • 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
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    • C07D213/65One oxygen atom attached in position 3 or 5
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    • 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
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    • C07D213/70Sulfur atoms
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    • 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
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    • 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/84Nitriles
    • C07D213/85Nitriles in position 3
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    • 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
    • C07D215/20Oxygen atoms
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    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56Benzopyrazoles; Hydrogenated benzopyrazoles
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    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
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    • 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
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    • 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
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    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Quinoline Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Los inhibidores de Nav1.7 son potencialmente útiles para el tratamiento de un amplio rango de trastornos, en particular, del dolor.Reivindicación 1: Un compuesto caracterizado por la fórmula (1) o su sal farmacéuticamente aceptable, en donde X es O, S, NH, o CH2; Het1 es (i) un heteroarilo de 9 ó 10 miembros que comprende de 1 a 3 átomos de nitrógeno; o (ii) un heteroarilo de 6, 9 ó 10 miembros que comprende de 1 a 3 átomos de nitrógeno cuyo heteroarilo se sustituye, independientemente, con 1 a 3 sustituyentes seleccionados de Y1 e Y2; Y1 e Y2 se seleccionan, independientemente, de F; Cl; CN; NO2; alquilo C1-8, opcionalmente sustituido con cicloalquilo C3-8 y/o, si lo permite la valencia, con 1 a 8 F; cicloalquilo C3-8, opcionalmente sustituido, si lo permite la valencia, con 1 a 8 F; NR7R8; alquiloxi C1-8, opcionalmente sustituido, de forma independiente, con 1 a 3 R9, o, si lo permite la valencia, con 1 a 8 F; cicloalquiloxi C3-8, opcionalmente sustituido, silo permite la valencia, con 1 a 8 F; fenilo, opcionalmente sustituido, en forma independiente, con 1 a 3 R10; fenoxi, opcionalmente sustituido, en forma independiente, con 1 a 3 R10; Het2, Het2-oxi; y Het3; en donde cicloalquiloxi C3-8 puede fusionarse opcionalmente a un anillo de fenilo o puede sustituirse independientemente con 1 a 3 R10; R1 es alquilo C1-6 o cicloalquilo C3-8, cada uno de los cuales se sustituye opcionalmente, silo permite la valencia, con 1 a 8 F; R2, R3, R4 son, independientemente, H, F, Cl u -OCH3; R5 es H, CN, F, Cl o R6; R6 es un grupo seleccionado de alquilo C1-6 y alquiloxi C1-6, en donde cada grupo se sustituye, opcionalmente, si lo permite la valencia, con 1 a 8 F; R7 y R8 son, independientemente, H; alquilo C1-8, opcionalmente sustituido, en forma independiente, con 1 a 3 R11; cicloalquilo C3-8, opcionalmente sustituido, si lo permite la valencia, con 1 a 8 F; Het2 “unido a C” o Het3 “unido a C”; en donde cicloalquilo C3-8 puede fusionarse opcionalmente a un anillo de fenilo o puede sustituirse independientemente, si lo permite la valencia, con 1 a 8 F y/o con 1 a 3 R10; o R7 y R8, junto con el átomo de nitrógeno al que están unidos, forman un anillo de 7 a 9 miembros en puente, saturado; R9 es alquiloxi C1-6; cicloalquilo C3-8, opcionalmente sustituido con 1 a 3 F o alquilo C1-6; Het2 o fenilo, opcionalmente sustituido, en forma independiente, con 1 a 3 R6; R10 es Cl, CN o R6; R11 es F; alquiloxi C1-6; cicloalquilo C3-8, opcionalmente sustituido con 1 a 3 F; Het2 “unido a C”; o fenilo, opcionalmente sustituido, en forma independiente, con 1 a 3 R6; Het2 es un monoheterocicloalquilo saturado de 3 a 8 miembros que comprende 1 ó 2 miembros del anillo seleccionados de -NR12- y -O-, en donde dicho monoheterocicloalquilo se sustituye, opcionalmente, en un átomo de carbono del anillo con 1 a 3 sustituyentes seleccionados, independientemente, de F, alquilo C1-6, alquiloxi C1-4-alquileno C0-4 y cicloalquilo C3-8; Het3 es un heteroarilo de 5 ó 6 miembros que comprende de 1 a 3 átomos de nitrógeno, en donde dicho heteroarilo se sustituye, opcionalmente, con 1 a 3 sustituyentes seleccionados de F, Cl, CN y R6; y R12 es H, alquilo C1-6 o cicloalquilo C3-8, en donde alquilo C1-6 y cicloalquilo C3-8 se sustituye, opcionalmente, con 1 a 3 F; o, cuando Het2 está “unido a N”, está ausente.
ARP110102490A 2010-07-12 2011-07-11 N-sulfonilbenzamidas utiles como inhibidor del canal de sodio AR082153A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US36336510P 2010-07-12 2010-07-12
US201161477897P 2011-04-21 2011-04-21
US201161491659P 2011-05-31 2011-05-31

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AR082153A1 true AR082153A1 (es) 2012-11-14

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US (1) US8592629B2 (es)
EP (1) EP2593432B1 (es)
JP (1) JP2013532184A (es)
AR (1) AR082153A1 (es)
CA (1) CA2801032A1 (es)
ES (1) ES2525581T3 (es)
UY (1) UY33501A (es)
WO (1) WO2012007861A1 (es)

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