AR042531A1 - Derivados de pirimidina para el tratamiento de crecimiento celular anormal - Google Patents

Derivados de pirimidina para el tratamiento de crecimiento celular anormal

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Publication number
AR042531A1
AR042531A1 ARP030104710A ARP030104710A AR042531A1 AR 042531 A1 AR042531 A1 AR 042531A1 AR P030104710 A ARP030104710 A AR P030104710A AR P030104710 A ARP030104710 A AR P030104710A AR 042531 A1 AR042531 A1 AR 042531A1
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Argentina
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alkyl
cycloalkyl
heterocycloalkyl
group
independently selected
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ARP030104710A
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English (en)
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Pfizer Prod Inc
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Publication of AR042531A1 publication Critical patent/AR042531A1/es

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    • 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
    • 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
    • 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
    • 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
    • C07D403/14—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 three or more hetero rings
    • 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
    • C07D409/14—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
    • C07D413/14—Heterocyclic 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
    • 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
    • C07D513/00—Heterocyclic 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
    • C07D513/02—Heterocyclic 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 two hetero rings
    • C07D513/04—Ortho-condensed systems

Abstract

La presente se refiere a procedimientos de tratamiento de crecimiento celular anormal en mamíferos mediante la administración de los compuestos de fórmula (1) y a composiciones farmacéuticas para tratar dichos trastornos, que contienen los compuestos de fórmula (1). También se refiere a procedimientos d preparación de los compuestos de fórmula (1). Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1) o una sal, solvato, hidrato o profármaco farmacéuticamente aceptables del mismo, en la que R1 tiene la siguiente fórmula (2) en la que cada D se selecciona independientemente del grupo constituido por CR8 y N, con la condición de que R1 se una al grupo NH mediante un átomo de C del anillo; en la que E y G se seleccionan independientemente del grupo constituido por N y C; en la que X, W y Q se seleccionan independientemente del grupo constituido por N, O, S, SO2, CO, NR3, CR2 y CR2R3; en la que Y y Z están independientemente presentes o ausentes, si están presentes Y y Z se seleccionan del grupo constituido por N, O, S, SO2, CO, NR3, CR2 y CR2R3; en la que A está presente o ausente, si está presente A se selecciona del grupo constituido por O, S, y NH y en la que B está presente o ausente, si está presente B se selecciona del grupo constituido por CO, SO2, y NR6, con la condición de que cuando A sea O o S ese B está ausente; en la que n es un número entero entre 1 y 3; en la que cada R2 se selecciona independientemente entre el grupo constituido por H, alquilo (C1-6), cicloalquilo (C3-7), heterocicloalquilo (C4-7), O-alquilo(C1-6), O-cicloalquilo (C3-7), O-heterocicloalquilo (C4-7), NH2, NHR6, NR6R7, SR6, SOR6, SO2R6, CO2R6, CONH2, CONHR6,CONR6R7, SO2NH2, SO2NHR6, SO2NR6R7, NHCOR6, NR6CONR6, NHCONHR6, NR6CONHR6, NHCONR6R7, NR6CONR6R7, NHSO2R6, NR6SO2R6, con la condición de que el átomo de O, N o S de los sustituyentes anteriormente mencionados puede no estar unido a un átomo de C unido a otro heteroátomo, dichos restos alquilo, cicloalquilo, heterocicloalquilo de los grupos anteriormente mencionados se sustituyen opcionalmente con 1 a 3 sustituyentes seleccionados independientemente entre el grupo constituido por H, halo, alquilo (C1-6), CN, NH2, NHR10, N(R10)2, OR10, alquilo (C1-6), cicloalquilo (C3-7), heterocicloalquilo (C4-7), CO2R11, CONH2, CONR11 y CONR11R12; en la que cada R3 se selecciona independientemente entre el grupo constituido por H, alquilo(C1-6), cicloalquilo (C3-7), heterocicloalquilo (C4-7), CO2R6, CONH2, CONHR6 y CONR6R7 o R2 y R3 tomados juntos con el átomo de C se unen para poder formar un anillo cicloalquilo de 3-7 eslabones o anillo heterocicloalquilo de 4-7 eslabones, en los que cada grupo metileno presente en dicho anillo cicloalquilo de 3-7 eslabones y dicho anillo heterocicloalquilo de 4-7 eslabones se pueden reemplazar opcionalmente con un grupo C=O, dichos restos alquilo, cicloalquilo, heterocicloalquilo de los grupos anteriormente mencionados están opcionalmente sustituidos con 1 a 3 sustituyentes seleccionados independientemente entre el grupo constituido por H, halo, alquilo (C1-6), CN, NH2, NHR10, N(R10)2, OR10, alquilo (C1-6), cicloalquilo (C3-7), heterocicloalquilo (C4-7), CO2R11, CONH2, CONHR11 y CONR11R12; en la que R4 se selecciona del grupo constituido por H, alquilo (C1-6), cicloalquilo (C3-7), heterocicloalquilo (C4-7), arilo (C6-10) y heteroarilo de 5-10 eslabones, los restos alquilo, cicloalquilo, heterocicloalquilo, arilo y heteroarilo de los grupos anteriormente mencionados se sustituyen opcionalmente con 1 a 3 sustituyentes seleccionados independientemente del grupo constituido por H, halo, OH, NO2, alquilo(C1-6), C(R6)=CR6R7, C:::CR6, cicloalquilo (C3-7), heterocicloalquilo (C4-7), O-alquilo(C1-6), O-cicloalquilo (C3-7), O-heterocicloalquilo (C4-7), C=N-OH, C=N-O-alquilo (C1-6), NH2, NHR6, NR6R7, SR6, SOR6, SO2R6, CO2R6, CONH2, CONHR6, CONR6R7, SO2NH2, SO2NHR6, SO2NR6R7, NHCOR6, NR6CONR6, NHCONHR6, NR6CONHR6, NHCONR6R7, NR6CONR6R7, NHSO2R6, NR6SO2R6, con la condición de que el átomo de O, N o S de los sustituyentes anteriormente mencionados puede no estar unido a un átomo de C unido a otro heteroátomo; en la que R5 se selecciona del grupo constituido por H, Br, Cl, CN, CF3, CH2F, CHF2, SO2CH3, CONH2, ciclopropilo, ciclobutilo, C6H5, CONHR6, CONR6R7, CO2R6, C(R9)=C(R9)2 y C:::CR9; en la que R6 se selecciona independientemente del grupo constituido por H, alquilo (C1-6), cicloalquilo (C3-7), heterocicloalquilo (C4-7), arilo (C6-10) y heteroarilo de 5-10 eslabones, dichos restos alquilo, cicloalquilo, heterocicloalquilo, arilo y heteroarilo de los grupos anteriormente mencionados están opcionalmente sustituidos con 1 a 3 sustituyentes seleccionados independientemente entre el grupo constituido por H, halo, alquilo(C1-6), CN, NH2, NHR10, N(R10)2, OR10, alquilo (C1-6), cicloalquilo (C3-7), heterocicloalquilo (C4-7), CO2R11, CONH2, CONHR11 y CONR11R12; en la que cada R7 se selecciona independientemente del grupo constituido por H, alquilo (C1-6), cicloalquilo (C3-7), heterocicloalquilo (C4-7), arilo (C6-10) y heteroarilo de 5-10 eslabones, dichos restos alquilo, cicloalquilo, heterocicloalquilo, arilo y heteroarilo de los grupos anteriormente mencionados se sustituyen opcionalmente con 1 a 3 sustituyentes seleccionados independientemente del grupo constituido por H, halo, alquilo (C1-6), CN, NH2, NHR10, N(R10)2, OR10, alquilo (C1-6), cicloalquilo (C3-7), heterocicloalquilo (C4-7), CO2R11, CONH2, CONHR11 y CONR11R12; en la que cada R8 se selecciona independientemente del grupo constituido por H, halo, ciano, alquilo (C1-6) cicloalquilo (C3-7), heterocicloalquilo (C4-7), O-alquilo(C1-6), O-cicloalquilo (C3-7), O-heterocicloalquilo (C4-7), NH2, NHR6, NR6R7, SR6, SOR6, SO2R6, CO2R6, CONH2, CONHR6, CONR6R7, SO2NH2, SO2NHR6, SO2NR6R7, NHCOR6, NR6CONR6, NHCONHR6, NR6CONHR6, NHCONR6R7, NR6CONR6R7, NHSO2R6, NR6SO2R6, dichos restos alquilo, cicloalquilo, heterocicloalquilo de los grupos anteriormente mencionados se sustituyen opcionalmente con 1 a 3 sustituyentes seleccionados independientemente entre el grupo constituido por H, halo, alquilo (C1-6), CN, NH2, NHR3, N(R3)2, OR3, alquilo (C1-6), cicloalquilo (C3-7), heterocicloalquilo (C4-7), CO2R6, CONH2, CONHR6 y CONR6R7; en la que cada R9 se selecciona independientemente del grupo constituido por H, CF3 y alquilo (C1-6), dicho alquilo (C1-6) se sustituye opcionalmente con 1 a 6 átomos halo; en la que cada R10 se selecciona independientemente del grupo constituido por H, alquilo (C1-6), cicloalquilo(C3-7), heterocicloalquilo (C4-7), CO2R11, CONH2, CONHR11, CONR11R12, SOR11, SO2R11, SO2NH2, SO2NHR11, SO2NR11R12, dichos restos alquilo, cicloalquilo, heterocicloalquilo de los grupos anteriormente mencionados se sustituyen opcionalmente con 1 a 3 sustituyentes seleccionados independientemente entre el grupo constituido por H, halo, alquilo (C1-6), CN, NH2, NHR13, N(R13)2, OR13, alquilo (C1-6), cicloalquilo (C3-7), heterocicloalquilo (C4-7), CO2R14, CONH2, CONHR14 y CONR14R15; en la que cada R11 se selecciona independientemente del grupo constituido por H, alquilo (C1-6), cicloalquilo (C3-7), heterocicloalquilo (C4-7), arilo (C6-10), heteroarilo de(C5-10) eslabones, dichos restos alquilo, cicloalquilo, heterocicloalquilo, arilo y heteroarilo de los grupos anteriormente mencionados se sustituyen opcionalmente con 1 a 3 sustituyentes seleccionados independientemente entre el grupo constituido por H, halo, alquilo (C1-6), CN, NH2, NHR13, N(R13)2, OR13, alquilo (C1-6), cicloalquilo (C3-7), heterocicloalquilo (C4-7), CO2R14, CONH2, CONHR14 y CONR14R15; en la que cada R12 se selecciona independientemente del grupo constituido por H, alquilo (C1-6), cicloalquilo (C3-7), heterocicloalquilo (C4-7), arilo (C6-10), heteroarilo de(C5-10) eslabones, dichos restos alquilo, cicloalquilo, heterocicloalquilo, arilo y heteroarilo de los grupos anteriormente mencionados se sustituyen opcionalmente con 1 a 3 sustituyentes seleccionados independientemente del grupo constituido por H, halo, alquilo (C1-6), CN, NH2, NHR13, N(R13)2, OR13, alquilo (C1-6), cicloalquilo (C3-7), heterocicloalquilo (C4-7), CO2R14, CONH2, CONHR14 y CONR14R15; en la que cada R13 se selecciona independientemente del grupo constituido por H, alquilo (C1-6), cicloalquilo (C3-7), heterocicloalquilo (C4-7), CO2R14, CONH2, CONHR14, CONR14R15, SOR14, SO2R14, SO2NH2, SO2NHR14, SO2NR14R15; en la que cada R14 se selecciona independientemente del grupo constituido por H, alquilo (C1-6), cicloalquilo (C3-7), heterocicloalquilo (C4-7), arilo (C6-10), heteroarilo de (C5-10) eslabones, dichos restos alquilo, cicloalquilo, heterocicloalquilo, arilo y heteroarilo de los grupos anteriormente mencionados se sustituyen opcionalmente con 1 a 3 sustituyentes seleccionados independientemente entre el grupo constituido por H, halo, alquilo (C1-6), CN, NH2, NH-alquilo (C1-6), N-(alquilo (C1-6))2, O-alquilo (C1-6), y en la que cada R15 se selecciona independientemente del grupo constituido por H, alquilo (C1-6), cicloalquilo (C3-7), heterocicloalquilo (C4-7), arilo (C6-10), heteroarilo de(C5-10) eslabones, dichos restos alquilo, cicloalquilo, heterocicloalquilo, arilo y heteroarilo de los grupos anteriormente mencionados se sustituyen opcionalmente con 1 a 3 sustituyentes seleccionados independientemente del grupo constituido por H, halo, alquilo (C1-6), CN, NH2, NH-alquilo (C1-6), N-(alquilo(C1-6))2, O-alquilo(C1-6).
ARP030104710A 2002-12-20 2003-12-18 Derivados de pirimidina para el tratamiento de crecimiento celular anormal AR042531A1 (es)

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US43567002P 2002-12-20 2002-12-20

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Country Link
US (1) US20040220177A1 (es)
EP (1) EP1578732A2 (es)
JP (1) JP2006515298A (es)
AR (1) AR042531A1 (es)
AU (1) AU2003288603A1 (es)
BR (1) BR0317435A (es)
CA (1) CA2510848A1 (es)
GT (2) GT200300292A (es)
HN (1) HN2003000422A (es)
MX (1) MXPA05006420A (es)
NL (1) NL1025071C2 (es)
PA (1) PA8593101A1 (es)
PE (1) PE20040934A1 (es)
TW (1) TW200413330A (es)
UA (1) UA80767C2 (es)
UY (1) UY28135A1 (es)
WO (1) WO2004056786A2 (es)

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