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AR040409A1 - Inhibidores de histona desacetilasa - Google Patents

Inhibidores de histona desacetilasa

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Publication number
AR040409A1
AR040409A1 AR20030101449A ARP030101449A AR040409A1 AR 040409 A1 AR040409 A1 AR 040409A1 AR 20030101449 A AR20030101449 A AR 20030101449A AR P030101449 A ARP030101449 A AR P030101449A AR 040409 A1 AR040409 A1 AR 040409A1
Authority
AR
Argentina
Prior art keywords
alkyl
carbamoyl
amino
sulfamoyl
group
Prior art date
Application number
AR20030101449A
Other languages
English (en)
Inventor
Elaine Stokes
Michael Waring
Keith Gibson
Original Assignee
Astrazeneca Ab
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 Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR040409A1 publication Critical patent/AR040409A1/es

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    • 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
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Abstract

Un compuesto de fórmula (1), sus sales aceptables para uso farmacéutico o ésteres o amidas hidrolizables in vivo del mismo; procesos para su preparación, composiciones farmacéuticas que los contienen y su uso en el tratamiento de enfermedades o trastornos clínicos mediados por la histona desacetilasa. Reivindicación 1: Un compuesto caracterizado porque responde a la fórmula (1) donde: el anillo A es un heterociclilo, donde si dicho heterociclilo contiene una porción -NH- dicho nitrógeno puede ser opcionalmente substituido por un grupo seleccionado entre G; R1 es un substituyente sobre carbono y se selecciona entre halo, nitro, ciano, hidroxi, oxo, trifluorometilo, trifluorometoxi, amino, carboxi, carbamoilo, mercapto, sulfamoilo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcoxi C1-6, alcanoilo C1-6, alcanoiloxi C1-6, N(alquil C1-6)amino, N,N-(alquil C1-6)2amino, alcanoilamino C1-6, N-(alquil C1-6)carbamoilo, N,N-(alquil C1-6)2carbamoilo, alquil C1-6 S(O)a donde a es entre 0 y 2, alcoxicarbonilo C1-6, N-(alquil C1-6)sulfamoilo o N,N-(alquil C1-6)2sulfamoilo, arilo, ariloxi, arilalquiloC1-6, grupo heterocíclico, (grupo heterocíclico)alquilo C1-6 o un grupo (D-E-); donde R1, incluido el grupo (D-E-), puede ser opcionalmente substituido sobre carbono por uno o más V; y donde si dicho grupo heterocíclico contiene una porción -NH- dicho nitrógeno puede ser opcionalmente substituido por un grupo seleccionado entre J; V es halo, nitro, ciano, hidroxi, oxo, trifluorometilo, trifluorometoxi, amino, carboxi, carbamoilo, mercapto, sulfamoilo, alquilo C1-6, C1-6 alquenilo C2-6, alquinilo C2-6, alcoxi C1-6, alcanoilo C1-6, alcanoiloxi C1-6, N(alquil C1-6)amino, N,N-(alquil C1-6)2amino, alcanoilamino C1-6, N-(alquil C1-6)carbamoilo, N,N-(alquil C1-6)2carbamoilo, alquil C1-6 S(O)a donde a es entre 0 y 2, alcoxicarbonilo C1-6, N-(alquil C1-6)sulfamoilo o N,N-(alquil C1-6)2sulfamoilo, o un grupo (D'-E'-); donde V, , incluido el grupo (D-E-), puede ser opcionalmente substituido sobre carbono por uno o más W; W y Z se seleccionan en forma independiente entre halo, nitro, ciano, hidroxi, oxo, trifluorometilo, trifluorometoxi, amino, carboxi, carbamoilo, mercapto, sulfamoilo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcoxi C1-6, alcanoilo C1-6, alcanoiloxi C1-6, N(alquil C1-6)amino, N,N-(alquil C1-6)2amino, alcanoilamino C1-6, N-(alquil C1-6)carbamoilo, N,N-(alquil C1-6)2carbamoilo, alquil C1-6 S(O)a donde a es entre 0 y 2, alcoxicarbonilo C1-6, N-(alquil C1-6)sulfamoilo o N, N-(alquil C1-6)2sulfamoilo; G, J y K se seleccionan en forma independiente alquilo C1-8, alquenilo C2-8, alquinilo C2-8, alcanoilo C1-8, alquilsulfonilo C1-8, alcoxicarbonilo C1-8, carbamoilo, N-(alquil C1-8)carbamoilo, N,N-(alquil C1-8)2carbamoilo, benciloxicarbonilo, benzoilo y fenilsulfonilo, arilo, arilalquilo C1-6 o (grupo heterocíclico) alquilo C1-6; donde G, J y K pueden ser opcionalmente substituidos sobre carbono por uno o más Q; y donde si dicho grupo heterocíclico contiene una porción -NH- dicho nitrógeno puede ser opcionalmente substituido por un grupo seleccionado entre hidrógeno o alquilo C1-6; Q es halo, nitro, ciano, hidroxi, oxo, trifluorometilo, trifluorometoxi, amino, carboxi, carbamoilo, mercapto, sulfamoilo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcoxi C1-6, alcanoilo C1-6, alcanoiloxi C1-6, N-(alquil C1-6)amino, N,N-(alquil C1-6)2amino, alcanoilamino C1-6, N-(alquil C1-6)carbamoilo, N,N-(alquil C1-6)2carbamoilo, alquil C1-6 S(O)a donde a es entre 0 y 2, alcoxicarbonilo C1-6, alcoxi C1-6 carbonilamino, N-(alquil C1-6)sulfamoilo, N,N-(alquil C1-6)2sulfamoilo, arilo, ariloxi, arilalquilo C1-6, arilalcoxi C1-6, grupo heterocíclico, (grupo heterocíclico)alquilo C1-6, (grupo heterocíclico)alcoxi C1-6, o un grupo (D"-E"-); donde Q, incluido el grupo (D"-E"-), puede ser opcionalmente substituido sobre carbono por uno o más Z; D, D' y D" se seleccionan en forma independiente entre alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquil C3-8alquilo C1-6, arilo, arilalquilo C1-6, grupo heterocíclico, (grupo heterocíclico)alquilo C1-6; donde D, D' y D" pueden ser opcionalmente substituidos sobre carbono por uno o más F'; y donde si dicho grupo heterocíclico contiene una porción -NH- dicho nitrógeno puede ser opcionalmente substituido por un grupo seleccionado entre K; E, E' y E" se seleccionan en forma independiente entre -N(R1)-, -O-, -C(O)O-, -OC(O)-, -C(O)-,-N(Ra)C(O)-, -N(Ra)C(O)N(Rb)-, -N(Ra)C(O)O-, -OC(O)N(Ra)-,-C(O)N(Ra)-, -S(O)r-,- SO2N(Ra)-, -N(Ra)SO2-; donde Ra y Rb se seleccionan en forma independiente hidrógeno o alquilo C1-6 opcionalmente substituido por uno más F y r es 0-2; F y F' se seleccionan en forma independiente entre halo, nitro, ciano, hidroxi, trifluorometil, trifluorometoxi, amino, carboxi, carbamoilo, mercapto, sulfamoilo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcoxi C1-6, alcanoilo C1-6, alcanoiloxi C1-6, N-(alquil C1-6)amino, N,N-(alquil C1-6)2amino, alcanoilamino C1-6, N-(alquil C1-6)carbamoilo, N,N-(alquil C1-6)2carbamoilo, alquil C1-6 S(O)a donde a es entre 0 y 2, alcoxi C1-6 carbonilo, N-(alquil C1-6)sulfamoilo y N,N-(alquil C1-6)2sulfamoilo ; m es 0, 1, 2, 3 o 4; donde los valores de R1 pueden ser iguales o diferentes; el anillo B es un anillo seleccionado entre (2) y (3) donde, X1 y X2 se seleccionan entre CH o N, y Y1, Y2, Y3, y Y4 se seleccionan entre CH o N con la condición de que al menos uno de Y1, Y2, Y3 y Y4 sea N; R es halo; n es 0, 1 o 2; donde los valores de R2 pueden ser iguales o diferentes; R3 es amino o hidroxi; R4 es halo, nitro, ciano, hidroxi, trifluorometilo, trifluorometoxi, amino, carboxi, carbamoilo, mercapto, sulfamoilo, alquilo C1-3, alquenilo C2-3, alquinilo C2-3, alcoxi C1-3, alcanoilo C1-3, alcanoiloxi C1-3, N-(alquil C1-3)amino, N,N-(alquil C1-3)2amino, alcanoil C1-3amino, N-(alquil C1-3)carbamoilo, N, N-(alquil C1-3)2carbamoilo, alquil C1-3 S(O)a donde a es entre 0 y 2, alcoxicarbonilo C1-6, N-(alquil C1-6)sulfamoilo, N,N-(alquil C1-3)2sulfamoilo; y p es 0, 1 o 2; donde los valores de R4 pueden ser iguales o diferentes; o una sal aceptable para uso farmacéutico o éster hidrolizable in vivo o amida del mismo.
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