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AR051669A1 - Derivados de bencimidazol como antagonistas de integrina utiles como agentes anti cancer - Google Patents

Derivados de bencimidazol como antagonistas de integrina utiles como agentes anti cancer

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Publication number
AR051669A1
AR051669A1 ARP050104745A ARP050104745A AR051669A1 AR 051669 A1 AR051669 A1 AR 051669A1 AR P050104745 A ARP050104745 A AR P050104745A AR P050104745 A ARP050104745 A AR P050104745A AR 051669 A1 AR051669 A1 AR 051669A1
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AR
Argentina
Prior art keywords
cr4r5
aryl
alkyl
integer
atom
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ARP050104745A
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English (en)
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Osi Pharm Inc
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Publication of AR051669A1 publication Critical patent/AR051669A1/es

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/12—Heterocyclic 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 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
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Se relaciona con métodos para tratar crecimiento celular anormal en mamíferos mediante la administracion de los compuestos de formula (1), y con composiciones farmacéuticas para el tratamiento de dichos desordenes las cuales contienen los compuestos de formula (1). Reivindicacion 1: Un compuesto de la formula (1), o una sal o solvato farmacéuticamente aceptable de los mismos, en donde: la línea de puntos designa que un enlace doble o un enlace doble o un enlace unico conecta al nitrogeno en la posicion tres con el carbono en la posicion 2; cada A y A' es independientemente un enlace directo, -C(O)N(R4)-, -N(R4)C(O)-, -N(R4)SO2-, -SO2N(R4)-, -N(R4)C(O)(CR4R5)pNHC(O)-, -N(R4)C(O)(CR4R5)pN(R4)-, -N(R4)C(S)(CR4R5)pN(R4)-, - N(R4)C(O)(CR4R5)pC(O)-, -N(R4)C(O)O-, -N(R4)C(O)S-, -C(O)-, -N(R3)-, -S- o -O-, en donde p es un entero desde 0 hasta 5 y la línea de puntos de la izquierda de los grupos precedentes está unida al anillo de bencimidazol del compuesto de formula (1); X1 es -(CR4R5)m-C(A'-R1a)(A-R1)-(CR4R5)n-CO2H o -(CR4R5)m-C(A-R1)=C(R4)-(CR4R5)n-CO2H, en donde m y n son cada uno independientemente un entero desde 0 hasta 4 y los residuos (CR4R5)m y (CR4R5)n de los grupos X1 precedentes incluyen opcionalmente uno o dos enlaces dobles o triples carbono-carbono; X2 es H, alquilo C1-20, alquenilo C2-20, alquinilo C2-20, -(CR4R5)t(cicloalquilo C3-20), -(CR4R5)t(arilo C6-10), o -(CR4R5)t(heterociclo de 4 a 12 miembros), en donde: cada grupo X2, excepto H, está sustituido por X3; cada T es independientemente un entero desde 0 hasta 5; dichos grupos alquilo, alquenilo y alquinilo contienen opcionalmente 1 o 2 residuos hetero seleccionados a partir de O, -S(O)j- en donde j es un entero desde 0 hasta 2, y -N(R4)- con la salvedad de que dos átomos de O, dos átomos de S, o un átomo de O y de S no están directamente unidos entre sí, y con la salvedad de que un átomo de O, un átomo de S o un átomo de N no están unidos directamente a un enlace triple o a un enlace doble no aromático; dichos grupos cicloalquilo, arilo y X2 heterocíclico están opcionalmente fusionados a uno o dos sistemas de anillos independientemente seleccionados a partir de un anillo de benceno, un grupo cicloalquilo C5-8, y un grupo heterocíclico de 4 hasta 10 miembros; -(CR4R5)t- incluye opcionalmente un enlace doble o triple carbono-carbono donde t es un entero desde 2 hasta 5; o donde t es 1 el residuo -(CR4R5)t- de -(CR4R5)t(heterocíclico de 4 a 12 miembros) y - (CR4R5)t(cicloalquilo C3-20) está opcionalmente unido por un enlace doble carbono-carbono a un carbono del grupo cicloalquilo o a un carbono no aromático del grupo heterocíclico de 4 a 12 miembros; dicho cicloalquilo incluye opcionalmente uno o dos enlaces dobles o triples carbono-carbono; y X2, excepto cuando es H, está opcionalmente sustituido por 1 a 5 grupos R2; X3 es H, 2-aminoimidazolilo, 2-aminobencimidazoilo, 2-aminopiridilo, 2-aminopirimidilo, o 2-aminopirazinilo, en donde X3, excepto cuando es H, está opcionalmente sustituido por 1 o 2 grupos R2; X4 es H, alquilo C1-10, -NR3R4, -SR3, o -OR3; cada X5 y R2 está independientemente seleccionado a partir de alquilo C1-10, alquenilo C2-10, alquinilo C2-10, oxo (=O), tioxo (=S), halo, ciano, nitro, trifluorometilo, difluormetoxi, trifluormetoxi, azido, -OR3, -C(O)R3, -C(O)OR3, -NR4C(O)OR6, -NR4C(O)R3, -OC(O)R3, -NR4SO2R6, -SO2NR3R4, -NR4C(O)R3, -C(O)NR3R4, -O-C=CR3R4, -NR4C(O)NR3R4, -NR4C(S)NR3R4, -NR3R4, -S(O)j(CR4R5)t(arilo C6- 10), -S(O)j(CR4R5)t(heterociclo de 4 a 12 miembros), -S(O)j(alquilo C1-6), -(CR4R5)t(arilo C6-10), -(CR4R5)pC(O)(CR4R5)t(arilo C6-10), -(R4R5)pO(CR4R5)t(arilo C6-10), -NR4(CR4R5)t(arilo C6-10), -(CR4R5)t(heterocíclico de 4 a 12 miembros), y - (CR4R5)pC(O)(CR4R5)t(heterocíclico de 4 a 12 miembros), en donde cada t es independientemente un entero desde 0 hasta 5, cada p es independientemente un entero desde 0 hasta 5, y cada j es un entero desde 0 hasta 2; dichos grupos alquilo, alquenilo y alquinilo contienen opcionalmente 1 o 2 residuos hetero seleccionados a partir de O, -S(O)j- en donde j es un entero desde 0 hasta 2, y -N(R3)- con la salvedad de que dos átomos de O, dos átomos de S, o un átomo de O y de S no están unidos directamente entre sí, y con la salvedad de que un átomo de O, un átomo de S o un átomo de N no están unidos directamente a un enlace triple o a un enlace doble no aromático; dichos grupos cicloalquilo, arilo y R2 heterocíclico están opcionalmente fusionados a un grupo arilo C6-10, a un grupo cicloalquilo C5-8, o a un grupo heterocíclico de 4 a 12 miembros; y dichos residuos alquilo, alquenilo, alquinilo, arilo y heterocíclicos de los grupos R2 precedentes están opcionalmente sustituidos por 1 a 5 sustituyentes independientemente seleccionados a partir de oxo (=O); tioxo (=S), halo, ciano, nitro, trifluormetilo, difluormetoxi, azido, -NR4SO2R6, -SO2NR3R4, -C(O)R3, -C(O)OR3, -NR4C(O)OR6, -NR4C(O)R3, -C(O)NR3R4, -NR3R4, -OR3, alquilo C1- 10, -S(O)j(alquilo C1-6), -(CR4R5)t(arilo C6-10), y -(CR4R5)t(heterocíclico de 4 a 12 miembros), en donde cada t es independientemente un entero desde 0 hasta 5 y cada j es independientemente un entero desde 0 hasta 2; cada R1 y R1a está independientemente seleccionado a partir de H, alquilo C1-10, alquenilo C2-10, alquinilo C2-10, -(CR4R5)t(arilo C6-10) y -(CR4R5)t(heterocíclico de 4 a 12 miembros); en donde t es un entero desde 0 hasta 5; y R1, excepto cuando es H, está opcionalmente sustituido con 1 a 5 grupos R2; cada R3 está independientemente seleccionado a partir de H, alquilo C1-10, -(CR4R5)t(arilo C6-10), y (CR4R5)t(heterocíclico de 4 a 12 miembros), en donde cada t es independientemente un entero desde 0 hasta 5; dicho grupo alquilo incluye opcionalmente 1 o 2 residuos hetero seleccionados a partir de O, -S(O)j- en donde j es un entero con un rango desde 0 hasta 2, y -N(R4)- con la salvedad de que dos átomso de O, dos átomos de S, o un átomo de O y S no están unidos directamente entre sí; dichos grupos cicloalquilo, arilo y R3 heterocíclico están opcionalmente fusionados a un grupo arilo C6-10, a un grupo cicloalquilo C5-8, o a un grupo heterocíclico de 4 a 12 miembros; y R3, excepto cuando es H, está opcionalmente sustituido por 1 a 5 sustituyentes independientemente seleccionados a partir, de oxo, halo, ciano, nitro, trifluormetilo, difluormetoxi, trifluormetoxi, azido, -C(O)R4, -C(O)OR4, -OC(O)R4, -NR4C(O)R5, -C(O)NR4R5, -NR4R5, hidroxi, alquilo C1-6, trifluormetilo, trifluormetoxi, y alcoxi C1-6, y con la salvedad de que R3 debe estar unido a través de un átomo de carbono a menos que R3 sea H; cada R4 y R5 es independientemente H o alquilo C1-6; o donde R4 y R5 están unidos al mismo átomo de carbono, R4 y R5 pueden ser tomados conjuntamente para formar un grupo cicloalquilo C3-10; cada R5 está independientemente seleccionado a partir de alquilo C1-10, -(CR4R5)t(arilo C6-10), y -(CR4R5)t(heterocíclico de 4 a 12 miembros), en donde cada t es independientemente un entero desde 0 hasta 5; dicho grupo alquilo incluye opcionalmente 1 o 2 residuos hetero seleccionados a partir de O, -S(O)j- en donde j es un entero con un rango desde 0 hasta 2, y -N(R4)- con la salvedad de que dos átomos de O, dos átomos de S, o un átomo de O y de S no está unidos directamente entre sí; dichos grupos cicloalquilo, arilo y R6 heterocíclico están opcionalmente fusionados a un grupo arilo C6-10, a un grupo cicloalquilo C5-8, o a un grupo heterocíclico de 4 a 12 miembros; y R6 está opcionalmente sustituido por 1 a 5 sustituyentes independientemente seleccionados a partir de oxo, halo, ciano, nitro, trifluormetilo, difluormetoxi, trifluormetoxi, azido, -C(O)R4, -C(O)OR4, - OC(O)R4, -NR4C(O)R5, -C(O)NR4R5, -NR4R5, hidroxi, alquilo C1-6, trifluormetilo, trifluormetoxi, y alcoxi C1-6.
ARP050104745A 2004-11-12 2005-11-11 Derivados de bencimidazol como antagonistas de integrina utiles como agentes anti cancer AR051669A1 (es)

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EP (1) EP1828144A2 (es)
AR (1) AR051669A1 (es)
TW (1) TW200630361A (es)
WO (1) WO2006053342A2 (es)

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