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AR047538A1 - Piridazinonas como antagonistas de las integrinas alfa4 - Google Patents

Piridazinonas como antagonistas de las integrinas alfa4

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Publication number
AR047538A1
AR047538A1 ARP050100451A ARP050100451A AR047538A1 AR 047538 A1 AR047538 A1 AR 047538A1 AR P050100451 A ARP050100451 A AR P050100451A AR P050100451 A ARP050100451 A AR P050100451A AR 047538 A1 AR047538 A1 AR 047538A1
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Argentina
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alkyl
alkoxy
aryl
independently selected
heteroaryl
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ARP050100451A
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Janssen Pharmaceutica Nv
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Abstract

Métodos para preparar estos compuestos, composiciones, intermediarios y sus derivados y para el tratamiento de trastornos mediados por la integrina. Reivindicacion 1: Un compuesto de formula (1), donde: R1 es un sustituyente seleccionado en forma independiente del grupo integrado por hidrogeno, alquilo C1-6, alcoxi C1-6, arilo, heteroarilo, heterociclilo, heterociclilo fusionado con un benzo, cicloalquilo fusionado con un benzo, heterociclilo fusionado con un heteroarilo, cicloalquilo fusionado con un heteroarilo, ariloxi, heteroariloxi, heterocicliloxi, cicloalquiloxi, -NR10R20, halogeno, hidroxi, y -Salquilo(C1-6); donde el alcoxi C1-6 está opcionalmente sustituido con uno a cuatro sustituyentes seleccionados en forma independiente de Ra; donde Ra se selecciona en forma independiente del grupo integrado por hidroxialcoxi(C1-6), arilo, heteroarilo, heterociclilo, cicloalquilo, alcoxi(C1-6)-carbonilo, carboxi, amino, alquilamino, dialquilamino, uno a tres átomos de halogeno e hidroxi; donde R10 y R20 se seleccionan en forma independiente del grupo integrado por hidrogeno, alquilo C1-6, allilo, alquilo(C1-6)halogenado, hidroxi, hidroxialquilo(C1-4), arilo, arilalquilo C1-4, y cicloalquilo; además, R10 y R20 se toman opcionalmente junto con los átomos a los cuales están unidos para formar un anillo monocíclico de cinco a siete miembros; donde los sustituyentes arilo y ariloxi de R1 están opcionalmente sustituidos con un sustituyente seleccionado en forma independiente del grupo integrado por alquilo C1-6, hidroxialquilo C1-6, arilalquilo C1-6, alcoxi C1-6, arilo, heteroarilo, alcoxi(C1-6)-carbonilo, arilalcoxi(C1-6)-carbonilo, alquil(C1-6)-carbonilo, aminocarbonilo, alquilaminocarbonilo, dialquilaminocarbonilo, hidroxi, ciano, nitro, -SO2alquilo(C1-3), -SO2arilo, -SO2heteroarilo, trifluorometilo, trifluorometoxi y halogeno; y donde los sustituyentes heteroarilo y heterociclilo de R1 están opcionalmente sustituidos con un sustituyente seleccionado en forma independiente del grupo integrado por uno a tres sustituyente de alquilo C1-6, alcoxi C1-6, arilo, heteroarilo, uno a tres átomos de halogeno, e hidroxi; R2 es un sustituyente seleccionado en forma independiente del grupo integrado por hidrogeno, alquilo C1-6, alcoxi C1-6, alqueniloxi C2-6, hidroxi, amino, alquilamino, dialquilamino y halogeno; donde R1 y R2 se toman opcionalmente junto con los átomos a los cuales están unidos para formar un anillo heterocíclico o carbocíclico de cinco a siete miembros; R3 es un sustituyente seleccionado en forma independientemente del grupo integrado por hidrogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, heteroarilo, heterociclilo y cicloalquilo; donde alquilo, alquenilo, y alquinilo están opcionalmente sustituidos con un sustituyente seleccionado en forma independiente de aminocarbonilo, alquilaminocarbonilo, dialquilaminocarbonilo, arilo, heteroarilo, heterociclilo, cicloalquilo, carboxi, uno a tres átomos de halogeno, hidroxi, o -C(=O)alquiloC1-6; R4 es un sustituyente seleccionado en forma independientemente del grupo integrado por hidrogeno, fluoro, cloro y metilo; R5 es hidrogeno o alquilo C1-3, siempre que R5 sea alquilo C1-3 solo cuando tomado con Y y los átomos a los cuales R5 e Y están unidos para formar un heterociclo de cinco a siete miembros; Y se selecciona en forma independiente del grupo integrado por hidroximetilo, -C(=O)NH2, -C(=O)NH(OH), -C(=O)NH(alquilo C1- 6), -C(=O)NH(hidroxialquilo (C1-6)), -C(=O)N(alquilo C1-6)2, -C(=O)NHSO2alquilo(C1-4), carboxi, tetrazolilo y -C(=O)alcoxi C1-6; donde dicho alcoxi está opcionalmente sustituido con uno a dos sustituyentes seleccionados en forma independiente de hidroxi, -NR30R40, heterociclilo, heteroarilo, halogeno y -OCH2CH2OCH3; donde R30 y R40 se seleccionan en forma independiente del grupo integrado por hidrogeno, alquilo C1-6, hidroxi e hidroxialquilo C1-4, y dichos R30 y R40 se toman opcionalmente junto con los átomos a los que están unidos para formar un anillo monocíclico de cinco a siete miembros; W es O o S; Z se selecciona del grupo integrado por hidrogeno, alquilo C1-6, alquenilo C1-6, alquinilo C2-6, alcoxi C1-6, arilo, heteroarilo, cicloalquilo, heterociclilo, cicloalquiloxi, policicloalquiloxi, y policiclilo puenteado con aza donde policiclilo puenteado con aza está opcionalmente sustituido con Rd; donde alquilo y alcoxi están opcionalmente sustituidos con uno a tres sustituyentes seleccionados en forma independiente del grupo integrado por arilo, arilo(C1-4)alcoxi, heteroarilo opcionalmente sustituido con uno a tres sustituyentes de alquilo C1-2 o -C(=O)arilo, hidroxi, -(=O)alquilo C1-6, -NH2, -NHalquilo(C1-6), -N(alquilo C1-6)2, -NH(cicloalquilo) donde dicho cicloalquilo está opcionalmente espirofusionado a un heterociclilo, -NHC(=O)arilalcoxi(C1-4), -N(alquilo C1-6)C(=O)arilalcoxi(C1-4), -NHC(=O)heteroarilalquilo(C1-4), -N(alquilo C1- 6)C(=O)heteroarilalquilo(C1-4), -NHC(=O)arilalquilo(C1-4), -N(alquilo C1-6)C(=O)arilalquilo(C1-4), -NHC(=O)(alcoxi C1-4), -N(alquilo C1-6)C(=O)alcoxi(C1-4), -NHC(=O)NH2, -N(alquilo C1-4)C(=O)NH2, -NHC(=O)NHalquilo(C1-4), -NHC(=O)N(alquilo C1-4)2, - NHSO2arilo, -C(=O)NH2, -C(=O)NH(alquilo C1-6), -C(=O)N(alquilo C1-6)2, y halogeno; donde los sustituyentes arilo y heteroarilo de Z están opcionalmente sustituidos con uno a cuatro sustituyentes seleccionados en forma independiente del grupo integrado por alquilo C1-4, hidroxialquilo C1-4, alcoxi C1-4, hidroxi, halogeno, nitro, carboxi, amino, alquilamino, dialquilamino, -SO2alquilo(C1-4), y -C(=O)arilo; además, el heteroarilo está opcionalmente sustituido con oxo; donde los sustituyentes cicloalquilo y heterociclilo de Z están opcionalmente sustituidos con uno a cuatro sustituyentes seleccionados en forma independiente del grupo integrado por alquilo C1-5, alquilamino C1-5, di(alquilo C1-5)amino, -NH(cicloalquilo) donde dicho cicloalquilo está opcionalmente espirofusionado a un heterociclilo, aminocarbonilo, -NHC(=O)alcoxi(C1-4), -N(alquilo C1-6)C(=O)alcoxi(C1-4), -C(=O)alcoxi(C1-4), -NHC(=O)alquilo(C1-4), -N(alquilo C1-6)C(=O)alquilo(C1-4), - C(=O)arilalcoxi(C1-4), oxo, alcoxi, hidroxi, arilalcoxi C1-4, heteroarilalcoxi C1-4, heterociclilo, heteroarilo opcionalmente sustituido con uno a tres sustituyentes de alquilo C1-2, y arilo; donde el sustituyente arilo está opcionalmente sustituido con uno a cuatro sustituyentes seleccionados en forma independiente del grupo integrado por alquilo C1-4, halogeno, amino, alquilamino, dialquilamino, arilo, y heteroarilo; donde Rd es un sustituyente seleccionado en forma independiente del grupo integrado por alquilo C1-6, -C(=O)alquilo(C1-6), -C(=O)alcoxi(C1-6), -S(=O)alquilo(C1-4), -SO2alquilo(C1-4), -S(=O)arilo, y -SO2arilo; donde la porcion de alquilo y alcoxi de alquilo C1-6, -C(=O)alquilo(C1-6), -C(=O)alcoxi(C1-6), -S(=O)alquilo(C1- 4), y -SO2alquilo(C1-4), están opcionalmente sustituidos con uno a tres sustituyentes seleccionados en forma independiente del grupo integrado por alcoxi C1-3, hidroxi, arilo, heteroarilo, y heterociclilo; y donde dicho arilo y heteroarilo están opcionalmente sustituidos con uno a cinco sustituyentes seleccionados en forma independiente del grupo integrado por alquilo C1-6, hidroxialquilo C1-6, alcoxi C1-6 carboxi, hidroxi, ciano, nitro, amino, alquilamino, dialquilamino, -SO2alquilo(C1-3), -SO2arilo, -SO2heteroarilo, trifluorometilo, trifluorometoxi, y halogeno; y un isomero optico, enantiomero, diastereomero, racemato o su sal aceptable para uso farmacéutico de los mismos.
ARP050100451A 2004-02-10 2005-02-09 Piridazinonas como antagonistas de las integrinas alfa4 AR047538A1 (es)

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AU2005212424A1 (en) 2005-08-25
EP1720839A1 (en) 2006-11-15
BRPI0507574A (pt) 2007-07-03
KR20070004676A (ko) 2007-01-09
JP2007522225A (ja) 2007-08-09
CA2555594A1 (en) 2005-08-25
US20050192279A1 (en) 2005-09-01
CN1938283A (zh) 2007-03-28
MXPA06009100A (es) 2007-02-02

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