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AR069803A1 - 5- anilinoimiazopiridinas y metodos de uso - Google Patents

5- anilinoimiazopiridinas y metodos de uso

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Publication number
AR069803A1
AR069803A1 ARP080105524A ARP080105524A AR069803A1 AR 069803 A1 AR069803 A1 AR 069803A1 AR P080105524 A ARP080105524 A AR P080105524A AR P080105524 A ARP080105524 A AR P080105524A AR 069803 A1 AR069803 A1 AR 069803A1
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AR
Argentina
Prior art keywords
alkyl
cr14r15
cr19r20
nhc
carbocyclyl
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ARP080105524A
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English (en)
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Genentech Inc
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Publication of AR069803A1 publication Critical patent/AR069803A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Devices For Indicating Variable Information By Combining Individual Elements (AREA)

Abstract

Se refiere a imidazopiridinas de formula 1 con actividad anticancerígena y/o antiinflamatoria y, más específicamente, a imidazopiridinas las cuales inhiben la actividad de MEK quinasa. Proporciona composiciones y métodos utiles para inhibir el crecimiento celular anormal o para tratar un trastorno hiperproliferativo, o para tratar una enfermedad inflamatoria en un mamífero, también se refiere a métodos para utilizar los compuestos para el diagnostico in vitro, in situ, e in vivo o tratamiento de células de mamífero, o afecciones patologicas asociadas. Reivindicacion 1: Un compuesto de formula 1 y sus sales, donde: Z1 es CR1 o N; R1 es H, alquilo C1-3, halo, CF3, CHF2, CN, ORA o NRARA; R1' es H, alquilo C1-C3, halo, CF3, CHF2, CN, ORA, o NRARA; donde cada RA es independientemente H o alquilo C1-3; Z2 es CR2 o N; Z3 es CR3 o N; siempre que solamente uno de Z1, Z2 y Z3 pueda ser N al mismo tiempo; R2 y R3 se seleccionan, con independencia, entre H, halo, CN, CF3, -OCF3, -NO2, -(CR14R15)nC(=Y')R11, -(CR14R15)nC(=Y')OR11, -(CR14R15)nC(=Y')NR11R12, (CR14R15)nNR11R12, -(CR14R15)nOR11, -(CR14R15)nSR11, -(CR14R15)nNR12C(=Y')R11, -(CR14R15)nNR12C(=Y')OR11, -(CR14R15)nNR13C(=Y')NR11R12, -(CR14R15)nNR12SO2R11, -(CR14R15)nOC(=Y')R11, -(CR14R15)nOC(=Y')OR11, -(CR14R15)nOC(=Y')NR11R12, -(CR14R15)nOS(O)2(OR11), -(CR14R15)nOP(=Y')(OR11)(OR12), -(CR14R15)nOP(OR11)(OR12), -(CR14R15)nS(O)R11, -(CR14R15)nS(O)2R11, -(CR14R15)nS(O)2NR11R12, -(CR14R15)nS(O)(OR11), -(CR14R15)nS(O)2(OR11), -(CR14R15)nSC(Y')R11, -(CR14R15)nSC(=Y')OR11, -(CR14R15)nSC(=Y')NR11R12, alquilo C1-12, alquenilo C2-8, alquinilo C2-8, carbociclilo, heterociclilo, arilo, y heteroarilo; R4 es H, alquilo C1-6 o carbociclilo C3-4; Y es W-C(O)- o W'; W X1-N(R5)- o -R11'-O-; R5 es H o alquilo C1-12; X1 se selecciona entre R11' y -OR11; cuando X1 es R11', X1 se toma opcionalmente junto con R5 y el átomo de nitrogeno al cual están unidos para formar un anillo saturado o insaturado de 4-7 miembros que tiene 0-2 heteroátomos adicionales seleccionados entre O, S y N, donde dicho anillo está opcionalmente sustituido con uno o más grupos seleccionados entre halo, CN, CF3, -OCF3, -NO2, oxo, -(CR19R20)nC(=Y')R16, -(CR19R20)nC(=Y')OR16, -(CR19R20)nC(=Y')NR16R17, -(CR19R20)nNR16R17, -(CR19R20)nOR16, -(CR19R20)n-SR16, -(CR19R20)nNR16C(=Y')R17, -(CR19R20)nNR16C(Y')OR17, -(CR19R20)nNR18C(=Y')NR16R17, -(CR19R20)nNR17SO2R16, -(CR19R20)nOC(=Y')R16, -(CR19R20)nOC(=Y')OR16, -(CR19R20)OC(=Y')NR16R17, -(CR19R20)nOS(O)2(OR16), -(CR19R20)nOP(=Y')(OR16)(OR17), -(CR19R20)nOP(OR16)(OR17), -(CR19R20)nS(O)R16, -(CR19R20)nS(O)2R16, -(CR19R20)nS(O)2NR16R17, -(CR19R20)nS(O)(OR16), -(CR19R20)nS(O)2(OR16), -(CR19R20)nSC(=Y')R16, -(CR19R20)nSC(=Y')OR16, -(CR19R20)nSC(=Y')NR16R17, y R21; cada R11' es independientemente H, alquilo C1-12, alquenilo C2-8, alquinilo C2-8, carbociclilo, heterociclilo, arilo, o heteroarilo; R11, R12 y R13 son con independencia H, alquilo C1-12, alquenilo C2-8, alquinilo C2-8, carbociclilo, heterociclilo, arilo, o heteroarilo, o R11 y R12 junto con el nitrogeno al cual están unidos forman un anillo saturado, insaturado o aromático de 3-8 miembros que tiene 0-2 heteroátomos seleccionados entre O, S y N, donde dicho anillo está opcionalmente sustituido con uno o más grupos seleccionados entre halo, CN, CF3, -OCF3, -NO2, alquilo C1-6, -OH, -SH, -O(alquilo C1-6), -S(alquilo C1-6), -NH2, -NH(alquilo C1-6), -N(alquilo C1-6)2, -SO2(alquilo C1-6), -CO2H, -CO2(alquilo C1-6), -C(O)NH2, -C(O)NH(alquilo C1-6), -C(O)N(alquilo C1-6)2, -N(alquilo C1-6)C(O)(alquilo C1-6), -NHC(O)(alquilo C1-6, -NHSO2(alquilo C1-6), -N(alquilo C1-6)SO2(alquilo C1-6), -SO2NH2, -SO2NH(alquilo C1-6), -SO2N(alquilo C1-6)2, -OC(O)NH2, -OC(O)NH(alquilo C1-6), -OC(O)N(alquilo C1-6)2, -OC(O)O(alquilo C1-6), -NHC(C)NH(alquilo C1-6), -NHC(O)N(alquilo C1-6)2, -N(alquilo C1-6)C(O)NH(alquilo C1-6), -N(alquilo C1-6)C(O)N(alquilo C1-6)2, -NHC(O)NH(alquilo C1-6), -NHC(O)N(alquilo C1-6)2, -NHC(O)O(alquilo C1-6), y -N(alquilo C1-6)C(O)O(alquilo C1-6); R14 y R15 se seleccionan, con independencia, entre H, alquilo C1-12, arilo, carbociclilo, heterociclilo, y heteroarilo; W' es como el grupo de formulas (2); donde het es como se muestra en los restos de formulas (3); X2 es O, S, o NR9; R7 se selecciona entre H, halo, CN, CF3, -OCF3, -NO2, -(CR14R15)nC(=Y')R11, -(CR14R15)nC(=Y')OR11, -(CR14R15)nC(=Y')NR11R12, -(CR14R15)nNR11R12, -(CR14R15)nOR11, -(CR14R15)nSR11, -(CR14R15)nNR12C(=Y')R11, -(CR14R15)nNR12C(=Y')OR11, -(CR14R15)nNR13C(=Y')NR11R12, -(CR14R15)nNR12SO2R11, -(CR14R15)nOC(=Y')R11, -(CR14R15)nOC(=Y')OR11, -(CR14R15)nOC(=Y')NR11R12, -(CR14R15)nOS(O)2(OR11), -(CR14R15)nOP(=Y')(OR11)(OR12), -(CR14R15)nOP(OR11)(OR12), -(CR14R15)nS(O)R11, -(CR14R15)nS(O)2R11, -(CR14R15)nS(O)2NR11R12, -(CR14R15)nS(O)(OR11), -(CR14R15)nS(O)2(OR11), -(CR14R15)nSC(Y')R11, -(CR14R15)nSC(=Y')OR11, -(CR14R15)nSC(=Y')NR11R12, alquilo C1-12, alquenilo C2-8, alquinilo C2-8, carbociclilo, heterociclilo, arilo, y heteroarilo; R8 se selecciona entre alquilo C1-12, arilo, carbociclilo, heterociclilo, y heteroarilo; R9 se selecciona entre H, -(CR14R15)nC(=Y')R11, -(CR14R15)nC(=Y')OR11, -(CR14R15)nC(=Y')NR11R12, -(CR14R15)qNR11R12, -(CR14R15)qOR11, -(CR14R15)qSR11, -(CR14R15)qNR12C(=Y')R11, -(CR14R15)qNR12C(=Y')OR11, -(CR14R15)qNR13C(=Y')NR11R12, -(CR14R15)qNR12SO2R11, -(CR14R15)qOC(=Y')R11, -(CR14R15)qOC(=Y')OR11, -(CR14R15)qOC(=Y')NR11R12, -(CR14R15)qOS(O)2(OR11), -(CR14R15)qOP(=Y')(OR11)(OR12), -(CR14R15)qOP(OR11)(OR12), -(CR14R15)nS(O)R11, -(CR14R15)nS(O)2R11, -(CR14R15)nS(O)2NR11R12, alquilo C1-12, alquenilo C2-8, alquinilo C2-8, carbociclilo, heterociclilo, arilo, y heteroarilo; R10 es H, alquilo C1-6 o carbociclilo C3-4; X4 es como el resto de formula (4); R6 es H, halo, alquilo C1-6, alquenilo C2-8, alquinilo C2-8, carbociclilo, heteroarilo, heterociclilo, -OCF3, -NO2, -Si(alquilo C1-6), -(CR19R20)nNR16R17, -(CR19R20)nOR16, o -(CR19R20)n-SR16; R6' es H, halo, alquilo C1-6, carbociclilo, CF3, -OCF3, -NO2, -Si(alquilo C1-6), -(CR19R20)nNR16R17, -(CR19R20)nOR16, -(CR19R20)n-SR16, alquenilo C2-8, alquinilo C2-8, heterociclilo, arilo, o heteroarilo; p es 0, 1, 2 o 3; n es 0,1, 2 o 3; q es 2 o 3; donde cada uno de dicho alquilo, alquenilo, alquinilo, carbociclilo, heterociclilo, arilo y heteroarilo de R1, R2, R3, R4, R5, R6, R6', R7, R8, R9, R10, R11, R11', R12, R13, R14, R15 y RA es independientemente opcionalmente sustituido con uno o más grupos seleccionados, con independencia, entre halo, CN, CF3, -OCF3, -NO2, oxo, -Si(alquilo C1-6), -(CR19R20)nC(=Y')R16, -(CR19R20)nC(=Y')OR16, -(CR19R20)nC(=Y')NR16R17, -(CR19R20)nNR16R17, -(CR19R20)nOR16, -(CR19R20)nSR16, -(CR19R20)nNR16C(=Y')R17, -(CR19R20)nNR16C(=Y')OR17, -(CR19R20)nNR18C(=Y')NR16R17, -(CR19R20)nNR17SO2R16, -(CR19R20)nOC(=Y')R16, -(CR19R20)OC(=Y')OR16, -(CR19R20)OC(=Y')NR16R17, -(CR19R20)nOS(O)2(OR16), -(CR19R20)nOP(=Y')(OR16)(OR17), -(CR19R20)nOP(OR16)(OR17), -(CR19R20)nS(O)R16, -(CR19R20)nS(O)2R16, -(CR19R20)nS(O)2NR16R17, -(CR19R20)nS(O)(OR16), -(CR19R20)nS(O)2(OR16), -(CR19R20)nSC(=Y')R16, -(CR19R20)nSC(=Y')OR16, -(CR19R20)nSC(=Y')NR16R17, y R21; cada R16, R17 y R18 es independientemente H, alquilo C1-12, alquenilo C2-8, alquinilo C2-8, carbociclilo, heterociclilo, arilo, o heteroarilo, donde dicho alquilo, alquenilo, alquinilo, carbociclilo, heterociclilo, arilo, o heteroarilo es opcionalmente sustituido con uno o más grupos seleccionados entre halo, CN, -OCF3, CF3, -NO2, alquilo C1-6, -OH, -SH, -O(alquilo C1-6), -S(alquilo C1-6), -NH2, -NH(alquilo C1-6), -N(alquilo C1-6)2, -SO2(alquilo C1-6), -CO2H, -CO2(alquilo C1-6), -C(O)NH2, -C(O)NH(alquilo C1-6), -C(O)N(alquilo C1-6)2, -N(alquilo C1-6)C(O)(alquilo C1-6), -NHC(O)(alquilo C1-6), -NHSO2(alquilo C1-6), -N(alquilo C1-6)SO2(alquilo C1-6), -SO2NH2, -SO2NH(alquilo C1-6), -SO2N(alquilo C1-6)2, -OC(O)NH2, -OC(O)NH(alquilo C1-6), -OC(O)N(alquilo C1-6)2, -OC(O)O(alquilo C1-6), -NHC(O)NH(alquilo C1-6), -NHC(O)N(alquilo C1-6)2, -N(alquilo C1-6)C(O)NH(alquilo C1-6), -N(alquilo C1-6)C(O)N(alquilo C1-6)2, -NHC(O)NH(alquilo C1-6), -NHC(O)N(alquilo C1-6)2, -NHC(O)O(alquilo C1-6), y -N(alquilo C1-6)C(O)O(alquilo C1-6); o R16 y R17 junto con el nitrogeno al cual están unidos forman un anillo saturado, insaturado o aromático de 3-8 miembros que tiene 0-2 heteroátomos seleccionados entre O, S y N, donde dicho anillo está opcionalmente sustituido con uno o más grupos seleccionados entre halo, CN, -OCF3, CF3, -NO2, alquilo C1-6, -OH, -SH, -O(alquilo C1-6), -S(alquilo C1-6), -NH2, -NH(alquilo C1-6), -N(alquilo C1-6)2, -SO2(alquilo C1-6), -CO2H, -CO2(alquilo C1-6), -C(O)NH2, -C(O)NH(alquilo C1-6), -C(O)N(alquilo C1-6)2, -N(alquilo C1-6)C(O)(alquilo C1-6), -NHC(O)(alquilo C1-6), -NHSO2(alquilo C1-6), -N(alquilo C1-6)SO2(alquilo C1-6), -SO2NH2, -SO2NH(alquilo C1-6), -SO2N(alquilo C1-6)2, -OC(O)NH2, -OC(O)NH(alquilo C1-6), -OC(O)N(alquilo C1-6)2, -OC(O)O(alquilo C1-6), -NHC(O)NH(alquilo C1-6), -NHC(O)N(alquilo C1-6)2, -N(alquilo C1-6)C(O)NH(alquilo C1-6), -N(alquilo C1-6)C(O)N(alquilo C1-6)2, -NHC(O)NH(alquilo C1-6), -NHC(O)N(alquilo C1-6)2, -NHC(O)O(alquilo C1-6), y -N(alquilo C1-6)C(O)O(alquilo C1-6); R19 y R20 se seleccionan, con independencia, entre H, alquilo C1-12, -(CH2)n-arilo, -(CH2)n-carbociclilo, -(CH2)n-heterociclilo, y -(CH2)n-heteroarilo; R21 es alquilo C1-12, alquenilo C2-8, alquinilo C2-8, carbociclilo, heterociclilo, arilo, o heteroarilo, donde cada miembro de R21 es opcionalmente sustituido con uno o más grupos seleccionados entre halo, oxo, CN, -OCF3, CF3, -NO2, alquilo C1-6, -OH, -SH, -O(alquilo C1-6), -S(alquilo C1-6), -NH2, -NH(alquilo C1-6), -N(alquilo C1-6)2, -SO2(alquilo C1-6), -CO2H, -CO2(alquilo C1-6), -C(O)NH2, -C(O)NH(alquilo C1-6), -C(O)N(alquilo C1-6)2, -N(alquilo C1-6)C(O)(alquilo C1-6), -NHC(O)(alquilo C1-6), -NHSO2(alquilo C1-6), -N(alquilo C1-6)SO2(alquilo C1-6), -SO2NH2, -SO2NH(alquilo C1-6), -SO2N(alquilo C1-6)2, -OC(O)NH2, -OC(O)NH(alquilo C1-6), -OC(O)N(alquilo C1-6)2, -OC(O)O(alquilo C1-6), -NHC(O)NH(alquilo C1-6), -NHC(O)N(alquilo
ARP080105524A 2007-12-19 2008-12-18 5- anilinoimiazopiridinas y metodos de uso AR069803A1 (es)

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