AR042024A1 - Compuestos farmaceuticos derivados de piridona, pirimidona y pirazinona - Google Patents

Compuestos farmaceuticos derivados de piridona, pirimidona y pirazinona

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Publication number
AR042024A1
AR042024A1 ARP030104153A ARP030104153A AR042024A1 AR 042024 A1 AR042024 A1 AR 042024A1 AR P030104153 A ARP030104153 A AR P030104153A AR P030104153 A ARP030104153 A AR P030104153A AR 042024 A1 AR042024 A1 AR 042024A1
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AR
Argentina
Prior art keywords
alkyl
phenyl
optionally substituted
alkoxy
independently selected
Prior art date
Application number
ARP030104153A
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English (en)
Inventor
Bladh
Larrson
Lawitz
Lepisto
Lonn
Nikkidis
Klingstedt
Original Assignee
Astrazeneca Ab
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Filing date
Publication date
Priority claimed from SE0203348A external-priority patent/SE0203348D0/xx
Priority claimed from SE0300388A external-priority patent/SE0300388D0/xx
Priority claimed from SE0302120A external-priority patent/SE0302120D0/xx
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR042024A1 publication Critical patent/AR042024A1/es

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Abstract

Procesos para su preparación, composiciones que los contienen y su uso en terapia. Los compuestos son inhibidores de la elastasa de los neutrófilos. Reivindicación 1: Un compuesto caracterizado porque responde a la fórmula (1), donde: X representa O o S; Y1 representa N o CR2; y cuando R1 representa OH, Y1 también pude representar, en la forma tautomérica, NR6; Y2 representa CR3; y cuando Y1 representa CR2, entonces Y2 también puede representar N; R1 representa H o alquilo C1-6; donde dicho alquilo está sustituido opcionalmente con uno o más sustituyentes seleccionados en forma independiente entre halógeno, CN, CHO, OR7, NR8R9, S(O)mR10, y SO2NR11R12; y cuando Y1 representa N, R1 también puede representar OH; R7 representa H, alquilo C1-6 o fenilo; donde dicho fenilo está además sustituido opcionalmente con halógeno, alquilo C1-6 y alcoxi C1-6; R2 representa H, halógeno o alquilo C1-6; R3 representa H o F; G1 representa fenilo o un anillo heteroaromático de cinco o seis miembros que contiene entre 1 y 3 heteroátomos seleccionados en forma independiente entre O, S y N; o G1 representa un anillo cicloalquilo saturado o parcialmente insaturado de cinco o seis miembros; o G1 representa un anillo heterocíclico saturado o parcialmente insaturado de cinco o seis miembros que contiene un heteroátomo seleccionado entre O, S, y NR13 donde R13 representa H o alquilo C1-6; R5 representa H, halógeno, alquilo C1-6, CN, alcoxi C1-6, NO2, NR14R15, alquilo C1-3 sustituido con uno o más átomos de F o alcoxi C1-3 sustituido con uno o más átomos de F; R14 y R15 representan en forma independiente H o alquilo C1-3; donde dicho alquilo está además sustituido opcionalmente con uno o más átomos de F; n representa un entero seleccionado entre 1, 2 ó 3 y cuando n representa 2 o 3, cada grupo R5 se selecciona en forma independiente; R4 y R6 representan en forma independiente H o alquilo C1-6; donde dicho alquilo está además sustituido opcionalmente con OH o alcoxi C1-6; o R4 y L están unidos de manera que el grupo -NR4L representa un anillo azacíclico de 5 a 7 miembros que incorpora opcionalmente un heteroátomo adicional seleccionado entre O, S y NR16; L representa un enlace, O, NR29 o alquilo C1-6; donde dicho alquilo incorpora opcionalmente un heteroátomo seleccionado entre O, S y NR16, y donde dicho alquilo está además sustituido opcionalmente con OH o OMe; G2 representa un sistema de anillos monocíclico seleccionado entre: fenilo o fenoxi; un anillo heteroaromático de 5 ó 6 miembros que contiene entre uno y tres heteroátomos seleccionados en forma independiente entre O, S y N; un cicloalquilo C3-6 saturado o parcialmente insaturado; o un anillo heterocíclico saturado o parcialmente insaturado C4-7 que contiene uno o dos heteroátomos seleccionados en forma independiente entre O, S(O)p y NR17 y que opcionalmente incorpora además un grupo carbonilo; o G2 representa un sistema de anillos bicíclico en el cual cada uno de los dos anillos se selecciona en forma independiente entre: fenilo; un anillo heteroaromático de 5 ó 6 miembros que contiene entre uno y tres heteroátomos seleccionados en forma independiente entre O, S y N; un cicloalquilo C3-6 saturado o parcialmente insaturado; o un anillo heterocíclico saturado o parcialmente insaturado C4-7 que contiene uno o dos heteroátomos seleccionados en forma independiente entre O; S(O)p y NR17 y que opcionalmente incorpora además un grupo carbonilo; y los dos anillo están fusionados entre sí, o están unidos directamente entre sí o están separados por un grupo de enlace seleccionado entre O, S(O)q o CH2, donde dicho sistema de anillos monocíclico o bicíclico está además sustituido opcionalmente con entre uno y tres sustituyentes seleccionados en forma independiente entre CN, OH, alquilo C1-6, alcoxi C1-6, halógeno, NR18R19, NO2, OSO2R38, CO2R20, C(=NH)NH2, C(O)NR21R22, C(S)NR23R24, SC(=NH)NH2, NR31C(=NH)NH2, S(O)sR25, SO2NR26R21, alcoxi C1-3 sustituido con uno o más átomos de F y alquilo C1-3 sustituido con SO2R39 o con uno o más átomos de F; o cuando L no representa un enlace, G2 también puede representar H; m, p, q, s y t representan en forma independiente un entero seleccionado entre 0, 1 ó 2; R8 y R9 representan en forma independiente H, alquilo C1-6, formilo o alcanoilo C2-6; donde dicho alquilo está además sustituido opcionalmente con fenilo sustituido opcionalmente con halógeno, alquilo C1-6, alcoxi C1-6 o SO2R30; o el grupo NR8R9 en conjunto representa un anillo azacíclico de 5 a 7 miembros que incorpora opcionalmente un heteroátomo adicional seleccionado entre O, S y NR28; R18 y R19 representan en forma independiente H, alquilo C1-6, formilo, alcanoilo C2-6, S(O)tR32 o SO2NR33R34; donde dicho grupo alquilo está además sustituido opcionalmente con halógeno, CN, alcoxi C1-4 o CONR41R42; R25 representa H, alquilo C1-6 o cicloalquilo C3-6; donde dicho grupo alquilo está además sustituido opcionalmente con uno o más sustituyentes seleccionados en forma independiente entre OH, CN, CONR35R36, CO2R37, OCOR40; cicloalquilo C3-6, un anillo heterocíclico saturado C4-7 que contiene uno o dos heteroátomos seleccionados en forma independiente entre O, S(O)p y NR43 y fenilo o un anillo heteroaromático de 5 ó 6 miembros que contiene entre uno y tres heteroátomos seleccionados en forma independiente entre O, S y N; donde dicho anillo aromático está además sustituido opcionalmente con uno o más sustituyentes seleccionados en forma independiente entre halógeno, CN, alquilo C1-4, alcoxi C1-4, OH, CONR44R45, CO2R46, S(O)sR47 y NHCOCH3; R26 y R27 representan en forma independiente H, alquilo C1-6, formilo o alcanoilo C2-6; R32 representa H, alquilo C1-6 o cicloalquilo C3-6; R38 representa H, alquilo C1-6 o fenilo; donde dicho fenilo está además sustituido opcionalmente con halógeno, alquilo C1-6 o alcoxi C1-6; R10, R11, R12, R16, 17, R20, R21, R22, R23, R24, R28, R29, R30, R31, R33, R34, R35, R36, R37, R39, R40, R41, R42, R43, R44, R45, R46 y R47 representan en forma independiente H o alquilo C1-6; y sales aceptables para uso farmacéutico del mismo, con la condición de que se excluyen los siguientes compuestos: N-bencil-5,6-dimetil-2-oxo-1-fenil-1,2-dihidropiridin-3-carboxamida; N-(2-fenetil)-5,6-dimetil-2-oxo-1-fenil-1,2-dihidropiridin-3-carboxamida; N-(2-hidroxietil)-2,4-dioxo-3-fenil-1,2,3,4-tetrahidropirimidin-5-carboxamida; N-[2-(dimetilamino)etil]-2,4-dioxo-3-fenil-1,2,3,4-tetrahidropirimidin-5-carboxamida; ácido 4-[2-[[[1,2-dihidro-1-(4-metilciclohexil)-2-oxo-3-piridinil]carbonil]amino]etil]-benzoico; y ácido 4-[2-[[(1-ciclohexil-1,2-dihidro-2-oxo-3-piridinil)carbonil]amino]etil]-benzoico.
ARP030104153A 2002-11-12 2003-11-12 Compuestos farmaceuticos derivados de piridona, pirimidona y pirazinona AR042024A1 (es)

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