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AR082201A1 - Bencenosulfonamidas utiles como inhibidores del canal de sodio - Google Patents

Bencenosulfonamidas utiles como inhibidores del canal de sodio

Info

Publication number
AR082201A1
AR082201A1 ARP110102479A ARP110102479A AR082201A1 AR 082201 A1 AR082201 A1 AR 082201A1 AR P110102479 A ARP110102479 A AR P110102479A AR P110102479 A ARP110102479 A AR P110102479A AR 082201 A1 AR082201 A1 AR 082201A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
cycloalkyl
alkyl
ring
heteroaryl
Prior art date
Application number
ARP110102479A
Other languages
English (en)
Inventor
Thomas Ryckmans
David James Rawson
Robert Ian Storer
Groot Marcel John De
Paul Anthony Stupple
Brian Edward Marron
Nigel Alan Swain
Alan Daniel Brown
Christopher William West
Original Assignee
Icagen Inc
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 Icagen Inc, Pfizer Ltd filed Critical Icagen Inc
Publication of AR082201A1 publication Critical patent/AR082201A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D237/20—Nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (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 una sal de este farmacéuticamente aceptable, en donde: R1 es un heteroarilo de 5 ó 6 miembros “unido a C”, que comprende (a) 1 ó 2 átomos de nitrógeno o, cuando tiene 5 miembros, (b) 1 ó 2 átomos de nitrógeno y un átomo de azufre; dicho heteroarilo se sustituye, opcionalmente, en un átomo de carbono del anillo con F o Cl; R2, R3 y R4 son, independientemente, H, F, Cl u -OCH3; R5 es CN, F, Cl o R6; Ra es (a) fenilo opcionalmente sustituido con 1 a 3 sustituyentes seleccionados, independientemente, de F, Cl, CN, H2N-alquileno C1-4-, alquil C1-4-NH-alquilen C1-4-cicloalquilo C3-8 o R6; o (b) un heteroarilo de 5 ó 6 miembros “unido a C” que comprende 1 ó 2 átomos de nitrógeno; dicho heteroarilo se sustituye, opcionalmente, con R7 o R8, o con R7 y R8; Rb es H, F, Cl, CN o R6; R6 es alquilo C1-4 o alquiloxi C1-4, cada uno opcionalmente sustituido, si lo permite la valencia, con 1 a 8 F; Z1 es (a) fenilo, opcionalmente sustituido con 1 a 3 sustituyentes seleccionados, independientemente, de F, Cl o R6; o (b) un heteroarilo de 5 ó 6 miembros “unido a C” que comprende 1 ó 2 átomos de nitrógeno; dicho heteroarilo se sustituye, opcionalmente, con R7 o R8, o con R7 y R8; R7 se une a un carbono del anillo de Z1 y se selecciona de F, Cl, NR9R10, R6, cicloalquilo C3-8 o Het1; R8 se une a un nitrógeno del anillo de Z1 y se selecciona de (a) alquilo C1-4 o cicloalquilo C3-8, cada uno opcionalmente sustituido, si lo permite la valencia, con 1 a 3 F; o (b) Het1 “unido a C”; Het1 es un monoheterocicloalquilo saturado de 3 a 8 miembros que comprende 1 ó 2 miembros del anillo seleccionados de -NR11- 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; y R9, R10 y R11 se seleccionan, independientemente, de H, alquilo C1-6 o cicloalquilo C3-8; o, cuando Het1 está “unido a N”, R11 está ausente de ese átomo de nitrógeno.
ARP110102479A 2010-07-09 2011-07-08 Bencenosulfonamidas utiles como inhibidores del canal de sodio AR082201A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US36292710P 2010-07-09 2010-07-09
US201161492525P 2011-06-02 2011-06-02

Publications (1)

Publication Number Publication Date
AR082201A1 true AR082201A1 (es) 2012-11-21

Family

ID=45439019

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110102479A AR082201A1 (es) 2010-07-09 2011-07-08 Bencenosulfonamidas utiles como inhibidores del canal de sodio

Country Status (8)

Country Link
US (1) US8772293B2 (es)
EP (1) EP2590951B1 (es)
JP (1) JP5830534B2 (es)
AR (1) AR082201A1 (es)
CA (1) CA2804593C (es)
ES (1) ES2533065T3 (es)
UY (1) UY33491A (es)
WO (1) WO2012004743A1 (es)

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