AR080982A1 - Derivados de quinoxalina - Google Patents

Derivados de quinoxalina

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Publication number
AR080982A1
AR080982A1 ARP110101476A AR080982A1 AR 080982 A1 AR080982 A1 AR 080982A1 AR P110101476 A ARP110101476 A AR P110101476A AR 080982 A1 AR080982 A1 AR 080982A1
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Argentina
Prior art keywords
alkyl
substituted
nr14r15
alkoxy
haloalkyl
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English (en)
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Astex Therapeutics Ltd
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Publication of AR080982A1 publication Critical patent/AR080982A1/es

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Abstract

Composiciones farmacéuticas que comprenden dichos compuestos, a procesos para la preparacion de dichos compuestos y al uso de dichos compuestos en el tratamiento de enfermedades, por ejemplo, cáncer. Reivindicacion 1: Un compuesto de la formula (1) incluyendo cualquier forma tautomérica o estereoquímicamente isomérica de ellos, en donde n representa un numero entero igual a 0, 1, 2, 3 o 4; R1 representa hidrogeno, alquilo C1-6, alquenilo C2-4, hidroxialquilo C1-6, haloalquilo C1-6, hidroxihaloalquilo C1-6, cianoalquilo C1-4, alcoxi C1-6-alquilo C1-6, en donde cada alquilo C1-6 puede estar opcionalmente sustituido con uno o dos grupos hidroxilo, alquilo C1-6 sustituido con -NR4R5, alquilo C1-6 sustituido con -C(=O)-NR4R5, -S(=O)2-alquilo C1-6, -S(=O)2-haloalquilo C1-6, -S(=O)2-NR14R15, alquilo C1-6 sustituido con -S(=O)2-alquilo C1-6, alquilo C1-6 sustituido con -S(=O)2-haloalquilo C1-6, alquilo C1-6 sustituido con -S(=O)2-NR14R15, alquilo C1-6 sustituido con -NH-S(=O)2-alquilo C1-6, alquilo C1-6 sustituido con -NH-S(=O)2-haloalquilo C1-6, alquilo C1-6 sustituido con -NR12-S(=O)2-NR14R15, R6, alquilo C1-6 sustituido con R6, alquilo C1-6 sustituido con -C(=O)-R6, hidroxialquilo C1-6 sustituido con R6, alquilo C1-6 sustituido con -Si(CH3)3, alquilo C1-6 sustituido con -P(=O)(OH)2 o alquilo C1-6 sustituido con -P(=O)(Oalquilo C1-6)2; cada R1a está seleccionado, de modo independiente, de hidrogeno, alquilo C1-4, hidroxialquilo C1-4, alquilo C1-4 sustituido con amino o mono- o di(alquil C1-4)amino o -NH(cicloalquilo C3-8), cianoalquilo C1-4, alcoxi C1-4-alquilo C1-4 y alquilo C1-4 sustituido con uno o varios átomos de fluor; cada R2 está seleccionado, de modo independiente, de hidroxilo, halogeno, ciano, alquilo C1-4, alquenilo C2-4, alquinilo C2-4, alcoxi C1-4, hidroxialquilo C1-4, hidroxialcoxi C1-4, haloalquilo C1-4, haloalcoxi C1-4, hidroxihaloalquilo C1-4, hidroxihaloalcoxi C1-4, alcoxi C1-4-alquilo C1-4, haloalcoxi C1-4-alquilo C1-4, alcoxi C1-4-alquilo C1-4, en donde cada alquilo C1-4 puede estar opcionalmente sustituido con uno o dos grupos hidroxilo, hidroxihaloalcoxi C1-4-alquilo C1-4, R13, alquilo C1-4 sustituido con R13, alquilo C1-4 sustituido con -C(=O)-R13, alcoxi C1-4 sustituido con R13, alcoxi C1-4 sustituido con -C(=O)-R13, -C(=O)-R13, alquilo C1-4 sustituido con -NR7R8, alquilo C1-4 sustituido con -C(=O)-NR7R8, alcoxi C1-4 sustituido con -NR7R8, alcoxi C1-4 sustituido con -C(=O)-NR7R8, -NR7R8 y -C(=O)-NR7R8, o cuando dos grupos R2 están unidos a átomos de carbono adyacentes, se pueden tomar juntos para formar un radical de la formula -O-(C(R17)2)p-O-; -X-CH=CH-; o -X-CH=N-; en donde R17 representa hidrogeno o fluor, p representa 1 o 2 y X representa O o S; R3 representa hidroxilo, alcoxi C1-6, hidroxialcoxi C1-6, alcoxi C1-6 sustituido con -NR10R11, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6 opcionalmente sustituido con -O-C(=O)-alquilo C1-6, hidroxialquilo C1-6 opcionalmente sustituido con -O-C(=O)-alquilo C1-6, hidroxialquenilo C2-6, hidroxialquinilo C2-6, hidroxihaloalquilo C1-6, cianoalquilo C1-6, alquilo C1-6 sustituido con carboxilo, alquilo C1-6 sustituido con -C(=O)-alquilo C1-6, alquilo C1-6 sustituido con -C(=O)-O-alquilo C1-6, alquilo C1-6 sustituido con alcoxi C1-6-alquil C1-6-O-C(=O)-, alquilo C1-6 sustituido con alcoxi C1-6-alquil C1-6-C(=O)-, alquilo C1-6 sustituido con -O-C(=O)-alquilo C1-6, alcoxi C1-6-alquilo C1-6, en donde cada alquilo C1-6 puede estar opcionalmente sustituido con uno o dos grupos hidroxilo o con -O-C(=O)-alquilo C1-6, alquenilo C2-6 sustituido con alcoxi C1-6, alquinilo C2-6 sustituido con alcoxi C1-6, alquilo C1-6 sustituido con R9 y opcionalmente sustituido con -O-C(=O)-alquilo C1-6, alquilo C1-6 sustituido con -C(=O)-R9, alquilo C1-6 sustituido con hidroxilo y R9, alquenilo C2-6 sustituido con R9, alquinilo C2-6 sustituido con R9, alquilo C1-6 sustituido con -NR10R11, alquenilo C2-6 sustituido con -NR10R11, alquinilo C2-6 sustituido con -NR10R11, alquilo C1-6 sustituido con hidroxilo y -NR10R11, alquilo C1-6 sustituido con uno o dos halogenos y -NR10R11, -alquil C1-6-C(R12)=N-O-R12, alquilo C1-6 sustituido con -C(=O)-NR10R11, alquilo C1-6 sustituido con -O-C(=O)-NR10R11, -S(=O)2-alquilo C1-6, -S(=O)2-haloalquilo C1-6, -S(=O)2-NR14R15, alquilo C1-6 sustituido con -S(=O)2-alquilo C1-6, alquilo C1-6 sustituido con -S(=O)2-haloalquilo C1-6, alquilo C1-6 sustituido con -S(=O)2-NR14R15, alquilo C1-6 sustituido con -NR12-S(=O)2-alquilo C1-6, alquilo C1-6 sustituido con -NH-S(=O)2-haloalquilo C1-6, alquilo C1-6 sustituido con -NR12-S(=O)2-NR14R15, R13, alquilo C1-6 sustituido con -P(=O)(OH)2 o alquilo C1-6 sustituido con -P(=O)(Oalquilo C1-6)2; R4 y R5 representan cada uno, de modo independiente, hidrogeno, alquilo C1-6, hidroxialquilo C1-6, haloalquilo C1-6, hidroxihaloalquilo C1-6, alcoxi C1-6-alquilo en donde cada alquilo C1-6 puede estar opcionalmente sustituido con uno o dos grupos hidroxilo, -S(=O)2-alquilo C1-6, -S(=O)2-haloalquilo C1-6, -S(=O)2-NR14R15, alquilo C1-6 sustituido con -S(=O)2-alquilo C1-6, alquilo C1-6 sustituido con -S(=O)2-haloalquilo C1-6, alquilo C1-6 sustituido con -S(=O)2-NR14R15, alquilo C1-6 sustituido con -NH-S(=O)2-alquilo C1-6, alquilo C1-6 sustituido con -NH-S(=O)2-haloalquilo C1-6, alquilo C1-6 sustituido con -NH-S(=O)2-NR14R15, R13 o alquilo C1-6 sustituido con R13; R6 representa cicloalquilo C3-8, cicloalquenilo C3-8, fenilo, heterociclilo monocíclico de 4 a 7 miembros que contiene al menos un heteroátomo seleccionado de N, O o S; dicho cicloalquilo C3-8, cicloalquenilo C3-8, fenilo, heterociclilo monocíclico de 4 a 7 miembros, opcionalmente y, de modo independiente, cada uno sustituido con 1, 2, 3, 4 o 5 sustituyentes, estando seleccionado cada sustituyente de modo independiente de ciano, alquilo C1-6, cianoalquilo C1-6, hidroxilo, carboxilo, hidroxialquilo C1-6, halogeno, haloalquilo C1-6, hidroxihaloalquilo C1-6, alcoxi C1-6, alcoxi C1-6-alquilo C1-6, alquil C16-O-C(=O)-, -NR14R15, -C(=O)-NR14R15, alquilo C1-6 sustituido con -NR14R15, alquilo C1-6 sustituido con -C(=O)-NR14R15, -S(=O)2-alquilo C1-6, -S(=O)2- haloalquilo C1-6, -S(=O)2-NR14R15, alquilo C1-6 sustituido con -S(=O)2-alquilo C1-6, alquilo C1-6 sustituido con -S(=O)2-haloalquilo C1-6, alquilo C 1-6 sustituido con -S(=O)2-NR4R15, alquilo C1-6 sustituido con -NH-S(=O)2- alquilo C1-6, alquilo C1-6 sustituido con -NH-S(=O)2-haloalquilo C1-6 o alquilo C1-6 sustituido con -NH-S(=O)2-NR14R15; R7 y R8 representan cada uno, de modo independiente, hidrogeno, alquilo C1-6, hidroxialquilo C1-6, haloalquilo C1-6, hidroxihaloalquilo C1-6 o alcoxi C1-6-alquilo C1-6; R9 representa cicloalquilo C3-8, cicloalquenilo C3-8, fenilo, naftilo o heterociclilo monocíclico o bicíclico de 3 a 12 miembros que contiene al menos un heteroátomo seleccionado de N, O o S, estando dicho cicloalquilo C3-8, cicloalquenilo C3-8, fenilo, naftilo o heterociclilo monocíclico o bicíclico de 3 a 12 miembros opcional e independientemente sustituido con 1, 2, 3, 4 o 5 sustituyentes, estando seleccionado cada sustituyente de modo independiente de =O, alquilo C1-4, hidroxilo, carboxilo, hidroxialquilo C1-4, ciano, cianoalquilo C1-4, alquil C1-4-O-C(=O)-, alquilo C1-4 sustituido con alquil C1-4-O-C(=O)-, alquil C1-4-C(=O)-, alcoxi C1-4-alquilo C1-4, en donde cada alquilo C1-4 puede estar opcionalmente sustituido con uno o dos grupos hidroxilo, halogeno, haloalquilo C1-4, hidroxihaloalquilo C1-4, -NR14R15, -C(=O)-NR14R15, alquilo C1-4 sustituido con -NR14R15, alquilo C1-4 sustituido con -C(=O)-NR14R15, alcoxi C1-4, -S(=O)2-alquilo C1-4, -S(=O)2-haloalquilo C1-4, -S(=O)2-NR14R15, alquilo C1-4 sustituido con -S(=O)2-NR14R15, alquilo C1-4 sustituido con -NH-S(=O)2-alquilo C1-4, alquilo C1-4 sustituido con - NH-S(=O)2-haloalquilo C1-4, alquilo C1-4 sustituido con -NH-S(=O)2-NR14R15, R13, -C(=O)-R13, alquilo C1-4 sustituido con R13, fenilo opcionalmente sustituido con R16, fenilalquilo C1-6, en donde el fenilo está opcionalmente sustituido con R16, un heterociclilo monocíclico aromático de 5 o 6 miembros que contiene al menos un heteroátomo seleccionado de N, O o S en donde dicho heterociclilo está opcionalmente sustituido con R16; o cuando dos de los sustituyentes de R9 están unidos al mismo átomo, se pueden tomar juntos para formar un heterociclilo monocíclico saturado de 4 a 7 miembros que contiene al menos un heteroátomo seleccionado de N, O o S; R10 y R11 representan cada uno, de modo independiente, hidrogeno, carboxilo, alquilo C1-6, cianoalquilo C1-6, alquilo C1-6 sustituido con -NR14R15, alquilo C1-6 sustituido con -C(=O)-NR14R15, haloalquilo C1-6, hidroxialquilo C1-6, hidroxihaloalquilo C1-6, alcoxi C1-6, alcoxi C1-6-alquilo C1-6, en donde cada alquilo C1-6 puede estar opcionalmente sustituido con uno o dos grupos hidroxilo, R6, alquilo C1-6 sustituido con R6, -C(=O)-R6, -C(=O)-alquilo C1-6, -C(=O)-hidroxialquilo C1-6, -C(=O)-haloalquilo C1-6,-C(=O)- hidroxihaloalquilo C1-6, alquilo C1-6 sustituido con -Si(CH3)3, -S(=O)2-alquilo C1-6, -S(=O)2-haloalquilo C1-6, -S(=O)2-NR14R15, alquilo C1-6 sustituido con -S(=O)2-alquilo C1-6, alquilo C1-6 sustituido con -S(=O)2-haloalquilo C1-6, alquilo C1-6 sustituido con -S(=O)2-NR14R15, alquilo C1-6 sustituido con -NH-S(=O)2-alquilo C1-6, alquilo C1-6 sustituido con -NH-S(=O)2-haloalquilo C1-6 o alquilo C1-6 sustituido con -NH-S(=O)2-NR14R15; R12 representa hidrogeno o alquilo C1-4 opcionalmente sustituido con alcoxi C1-4; R13 representa cicloalquilo C3-8 o un heterociclilo monocíclico saturado de 4 a 6 miembros que contiene al menos un heteroátomo seleccionado de N, O o S, en donde dicho cicloalquilo C3-8 o heterociclilo monocíclico está opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados cada uno, de modo independiente, de halogeno, hidroxilo, alquilo C1-6, -C(=O)-alquilo C1-6, alcoxi C1-6 o -NR14R15; R14 y R15 representan cada uno, de modo independiente, hidrogeno o haloalquilo C1-4 o alquilo C1-4 opcionalmente sustituido con un sustituy
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