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AR090230A1 - Derivados macrociclicos para el tratamiento de enfermedades - Google Patents

Derivados macrociclicos para el tratamiento de enfermedades

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Publication number
AR090230A1
AR090230A1 ARP130100694A AR090230A1 AR 090230 A1 AR090230 A1 AR 090230A1 AR P130100694 A ARP130100694 A AR P130100694A AR 090230 A1 AR090230 A1 AR 090230A1
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AR
Argentina
Prior art keywords
cr5r6
nr9r10
nr9c
cycloalkyl
alkyl
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English (en)
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Pfizer
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Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=48142828&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR090230(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Pfizer filed Critical Pfizer
Publication of AR090230A1 publication Critical patent/AR090230A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08Bridged systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • 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
    • C07D491/08Bridged 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
    • C07D491/12Heterocyclic 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 three hetero rings
    • C07D491/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D273/00Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
    • C07D273/02Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00 having two nitrogen atoms and only one oxygen atom
    • 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
    • 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

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

Abstract

Composiciones farmacéuticas que comprenden dichos compuestos y sales, y a sus usos. Los compuestos y las sales de la presente inhiben la quinasa del linfoma anaplásico (ALK) y/o EML4-ALK y son útiles para tratar o mejorar los trastornos proliferativos celulares anormales, tales como cáncer. Reivindicación 1: Un compuesto de la fórmula (1) en donde: X está seleccionado del grupo que consiste en (CR⁵R⁶)qO(CR⁵R⁶)ʳ-, -(CR⁵R⁶)qN(R¹)(CR⁵R⁶)ʳ-, -(CR⁵R⁶)qC(O)N(R¹)(CR⁵R⁶)ʳ y -(CR⁵R⁶)qN(R¹)C(O)(CR⁵R⁶)ʳ; Y y Z son cada uno, de modo independiente, N o CH, siempre que, cuando Y es N, Z sea CH y cuando Z es N, Y sea CH; A es un anillo seleccionado de arilo C₆₋₁₂ y heteroarilo de 5 - 6 miembros; R¹ está seleccionado del grupo que consiste en hidrógeno, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₆, arilo C₆₋₁₂, heteroalicíclico de 3 - 12 miembros y heteroarilo de 5 - 6 miembros, en donde cada hidrógeno en dicho alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₆, arilo C₆₋₁₂, heteroalicíclico de 3 - 12 miembros y heteroarilo de 5 - 6 miembros puede estar opcionalmente sustituido, de modo independiente, con halógeno, -OH, -NH₂, -S(O)ₜR⁹, -S(O)₂NR⁹R¹⁰, -S(O)₂OR⁹, -NO₂, -CN, -OR⁹, -C(O)R⁹, -OC(O)R⁹, -NR⁹C(O)R¹⁰, -C(O)OR⁹, -C(=NR⁹)NR⁹R¹⁰, -NR⁹C(O)NR⁹R¹⁰, -NR⁹S(O)₂R¹⁰ o -C(O)NR⁹R¹⁰; cada R² está seleccionado, de modo independiente, del grupo que consiste en halógeno, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₆, arilo C₆₋₁₂, heteroalicíclico de 3 - 12 miembros, heteroarilo de 5 - 6 miembros, -S(O)ₜR⁷, S(O)₂NR⁷R⁸, S(O)₂OR⁷, NO₂, -(CR⁵R⁶)qNR⁷R⁸, -N(CR⁵R⁶)(CR⁵R⁶)qNR⁷R⁸, -OR⁷, --O(CR⁵R⁶)(CR⁵R⁶)qOR⁷, -O(CR⁵R⁶)(CR⁵R⁶)qR⁷, -CN, -C(O)R⁷, -OC(O)R⁷, -O(CR⁵R⁶)qR⁷, -NR⁷C(O)R⁸, -(CR⁵R⁶)qC(O)OR⁷, -(CR⁵R⁶)qNR⁷R⁸, -C(=NR⁷)NR⁷R⁸, -NR⁷C(O)NR⁷R⁸, -NR⁷S(O)₂R⁸ y -(CR⁵R⁶)qC(O)NR⁷R⁸; en donde cada hidrógeno en dicho alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₆, arilo C₆₋₁₂, heteroalicíclico de 3 - 12 miembros, y heteroarilo de 5 - 6 miembros puede estar opcionalmente sustituido, de modo independiente, con halógeno, -OH, -NH₂, -S(O)ₜR⁹, -S(O)₂NR⁹R¹⁰, -S(O)₂OR⁹, -NO₂, -OR⁹, -CN, -C(O)R⁹, -OC(O)R⁹, -NR⁹C(O)R¹⁰, -C(O)OR⁹, -C(=NR⁹)NR⁹R¹⁰, -NR⁹C(O)NR⁹R¹⁰, -NR⁹S(O)₂R¹⁰ o -C(O)NR⁹R¹⁰; R³ y R⁴ están seleccionados cada uno, de modo independiente, de hidrógeno, alquilo C₁₋₆ y cicloalquilo C₃₋₆, en donde cada hidrógeno en alquilo C₁₋₆ y cicloalquilo C₃₋₆ puede estar opcionalmente sustituido, de modo independiente, con halógeno, -OH, -NH₂, -S(O)ₜR⁹, -S(O)₂NR⁹R¹⁰, -S(O)₂OR⁹, -NO₂, -CN, -OR⁹, -C(O)R⁹, -OC(O)R⁹, -NR⁹C(O)R¹⁰, -C(O)OR⁹, -C(=NR⁹)NR⁹R¹⁰, -NR⁹C(O)NR⁹R¹⁰, -NR⁹S(O)₂R¹⁰ o -C(O)NR⁹R¹⁰; cada R⁵ y R⁶ está seleccionado, de modo independiente, del grupo que consiste en hidrógeno, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₆, arilo C₆₋₁₂, heteroalicíclico de 3 - 12 miembros, heteroarilo de 5 - 6 miembros, -OH, -NH₂, -S(O)ₜR⁹, -S(O)₂NR⁹R¹⁰, -S(O)₂OR⁹, -NO₂, -CN, -OR⁹, -C(O)R⁹, -OC(O)R⁹, -NR⁹C(O)R¹⁰, -C(O)OR⁹, -C(=NR⁹)NR⁹R¹⁰, -NR⁹C(O)NR⁹R¹⁰, -NR⁹S(O)₂R¹⁰ y -C(O)NR⁹R¹⁰; en donde cada hidrógeno en dicho alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₆, arilo C₆₋₁₂, heteroalicíclico de 3 - 12 miembros, y heteroarilo de 5 - 6 miembros puede estar opcionalmente sustituido, de modo independiente, con halógeno, -OH, -NH₂, -S(O)ₜR⁹, -S(O)₂NR⁹R¹⁰, -S(O)₂OR⁹, -NO₂, -CN, -OR⁹, -C(O)R⁹, -OC(O)R⁹, -NR⁹C(O)R¹⁰, -C(O)OR⁹, -C(=NR⁹)NR⁹R¹⁰, -NR⁹C(O)NR⁹R¹⁰, -NR⁹S(O)₂R¹⁰ o -C(O)NR⁹R¹⁰; cada R⁷ y R⁸ está seleccionado, de modo independiente, del grupo que consiste en hidrógeno, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₆, arilo C₆₋₁₂, heteroalicíclico de 3 - 12 miembros, y heteroarilo de 5 - 6 miembros, en donde cada hidrógeno en dicho alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₆, arilo C₆₋₁₂, heteroalicíclico de 3 - 12 miembros y heteroarilo de 5 - 6 miembros puede estar opcionalmente sustituido, de modo independiente, con halógeno, -OH, -NH₂, -S(O)ₜR⁹, -S(O)₂NR⁹R¹⁰, -S(O)₂OR⁹, -NO₂, -OR⁹, -CN, -C(O)R⁹, -OC(O)R⁹, -NR⁹C(O)R¹⁰, -C(O)OR⁹, -C(=NR⁹)NR⁹R¹⁰, -NR⁹C(O)NR⁹R¹⁰, -NR⁹S(O)₂R¹⁰ o -C(O)NR⁹R¹⁰; cada R⁹ y R¹⁰ está seleccionado, de modo independiente, de hidrógeno, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₆, arilo C₆₋₁₂, heteroalicíclico de 3 - 12 miembros, y heteroarilo de 5 - 6 miembros; m es 0,1, 2 ó 3; n es 0,1, 2 ó 3; p es 0,1, 2, 3 ó 4; cada q es, de modo independiente, 0, 1, 2 ó 3; cada r es, de modo independiente, 0, 1, 2 ó 3; y cada t es, de modo independiente, 0, 1 ó 2; o una de sus sales farmacéuticamente aceptables.
ARP130100694 2012-03-06 2013-03-04 Derivados macrociclicos para el tratamiento de enfermedades AR090230A1 (es)

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US201261607485P 2012-03-06 2012-03-06
US201361759307P 2013-01-31 2013-01-31

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EP (1) EP2822953B9 (es)
JP (2) JP5823066B2 (es)
KR (1) KR101692600B1 (es)
CN (1) CN104169286B (es)
AP (1) AP2014007881A0 (es)
AR (1) AR090230A1 (es)
AU (1) AU2013229173B2 (es)
BR (1) BR112014022106B1 (es)
CA (1) CA2863892C (es)
CL (1) CL2014002084A1 (es)
CO (1) CO7061081A2 (es)
CR (1) CR20140370A (es)
CY (2) CY1118771T1 (es)
DK (1) DK2822953T5 (es)
DO (1) DOP2014000188A (es)
EA (1) EA026155B9 (es)
ES (1) ES2621220T3 (es)
FR (1) FR19C1062I2 (es)
GE (1) GEP201606560B (es)
GT (1) GT201400187A (es)
HR (1) HRP20170287T2 (es)
HU (2) HUE034118T2 (es)
IL (1) IL234062A (es)
LT (2) LT2822953T (es)
LU (1) LUC00131I2 (es)
MD (1) MD4590C1 (es)
ME (1) ME02630B (es)
MX (1) MX350844B (es)
MY (1) MY169142A (es)
NI (1) NI201400102A (es)
NL (1) NL301006I2 (es)
NO (1) NO2019034I1 (es)
NZ (1) NZ627900A (es)
PE (1) PE20142339A1 (es)
PH (1) PH12014501992A1 (es)
PL (1) PL2822953T3 (es)
PT (1) PT2822953T (es)
RS (1) RS55814B1 (es)
SG (1) SG11201404451TA (es)
SI (1) SI2822953T1 (es)
TW (1) TWI476199B (es)
UY (1) UY34657A (es)
WO (1) WO2013132376A1 (es)
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