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AR049511A1 - Compuestos y composiciones como inhibidores de quinasa de proteina - Google Patents

Compuestos y composiciones como inhibidores de quinasa de proteina

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Publication number
AR049511A1
AR049511A1 ARP050102354A ARP050102354A AR049511A1 AR 049511 A1 AR049511 A1 AR 049511A1 AR P050102354 A ARP050102354 A AR P050102354A AR P050102354 A ARP050102354 A AR P050102354A AR 049511 A1 AR049511 A1 AR 049511A1
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AR
Argentina
Prior art keywords
alkyl
halogen
heterocycloalkyl
substituted
heteroaryl
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ARP050102354A
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English (en)
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Irm Llc
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Publication of AR049511A1 publication Critical patent/AR049511A1/es

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Abstract

Métodos para utilizar tales compuestos con el fin de tratar o prevenir enfermedades o desordenes asociados con una actividad de quinasa anormal o desregulada, en particular enfermedades o desordenes que involucren la activacion anormal de las quinasas Abl, BCR-Abl, PDGF-R, trkB, c-SRC, BMX, FGFR3, b-RAF, SGK, Tie2, Lck, JNK2a2, MKK4, c-RAF, MKK6, SAPK2a y SAPK2b. Reivindicacion 1: Un compuesto de la formula (1), en donde: m y n se seleccionan independientemente a partir de 0, 1, y 2; R1 se selecciona a partir de -XNR5R6, -XOR5, -XC(O)R5, -XR5 y -XS(O)0-2R5; en donde X es un enlace o alquileno C1-4 opcionalmente sustituido por uno o dos radicales de alquilo C1-6; R5 se selecciona a partir de hidrogeno, alquilo C1-6, arilo C6-10- alquilo C0-4, heteroarilo C5-10-alquilo C0-4, cicloalquilo C3-10-alquilo C0-4, y heterocicloalquilo C3-10-alquilo C0-4; y R6 se selecciona a partir de hidrogeno y alquilo C1-6; o R5 y R6, junto con el átomo de nitrogeno con el que están unidos R5 y R6 entre sí, forman heteroarilo o heterocicloalquilo; en donde cualquier arilo, heteroarilo, cicloalquilo, y heterocicloalquilo de R5, o la combinacion de R5 y R6, pueden estar opcionalmente sustituidos con uno a tres radicales independientemente seleccionados a partir de halogeno, nitro, ciano, hidroxilo, alquilo C1-6, alcoxilo C1-6, alquilo sustituido por halogeno, alcoxilo sustituido por halogeno, -XNR7R8, -XOR7, -XNR7S(O)2R8, -XNR7S(O)R8, -XNR7SR8, -XC(O)NR7R8, -XC(O)NR7XNR7R8, - XNR7(O)NR7R8, -XNR7XNR7R8, -XNR7XOR7, -XNR7C(=NR7)NR7R8, -XS(O)2R9, -XNR7C(O)R8, -XNR7C(O)R9, -XR9, -XC(O)OR8, -XS(O)2NR7R8, -XS(O)NR7R8, y -XSNR7R8; en donde X es un enlace o alquileno C1-4; R7 y R8 se seleccionan independientemente a partir del grupo que consiste en hidrogeno y alquilo C1-4; y R9 se selecciona a partir de heterocicloalquilo C3-10 y heteroarilo C5-10; en donde el heterocicloalquilo o heteroarilo R9 está opcionalmente sustituido con un radical seleccionado a partir del grupo que consiste en alquilo C1-4, -XNR7XNR7R7, XNR7XOR7, y XOR7; R2 y R4 se seleccionan independientemente a partir de halogeno, hidroxilo, alquilo C1-4, alcoxilo C1-4, alquilo C1-4 sustituido por halogeno, y alcoxilo C1-4 sustituido por halogeno; R3 se selecciona a partir de -NR10R11, -NR10C(O)R11, -NR10S(O)0-2R11, y -NR10C(O)NR10R11; en donde R10 se selecciona a partir de hidrogeno y alquilo C1-6; R11 se selecciona a partir de arilo de C6-10, heteroarilo C5-10, cicloalquilo C3-10, y heterocicloalquilo C3-10; en donde cualquier arilo, heteroarilo, cicloalquilo, o heterocicloalquilo de R11 está opcionalmente sustituido por 1 a 3 radicales seleccionados a partir de halogeno, nitro, ciano, hidroxilo, alquilo C1-6, alcoxilo C1-6, alquilo sustituido por halogeno, alcoxilo sustituido por halogeno, -NR12C(O)R13, -NR12C(O)NR12R13, -C(O)NR12R13, -NR12S(O)0-2R13 y -S(O)0-2NR12R13; en donde R12 se selecciona a partir de hidrogeno y alquilo C1-6; R13 se selecciona a partir de arilo de C6-10, heteroarilo C5-10, cicloalquilo C3-10, y heterocicloalquilo C3-10; en donde cualquier arilo, heteroarilo, cicloalquilo, o heterocicloalquilo de R13 está opcionalmente sustituido con 1 a 3 radicales independientemente seleccionados a partir de halogeno, alquilo C1-6, alquilo sustituido por halogeno, alcoxilo C1-6, alcoxilo sustituido por halogeno, -XNR7R8, arilo C6-10-alquilo C0-4, heteroarilo C5-10-alquilo C0-4, cicloalquilo C3-10-alquilo C0-4, heterocicloalquilo C3-10-alcoxilo C0-4, y heterocicloalquilo C3-10-alquilo C0-4; en donde X, R7, y R8 son como se describen anteriormente, y en donde cualquier sustituyente de arilo, heteroarilo, cicloalquilo, o heterocicloalquilo de R13 está además opcionalmente sustituido por 1 a 3 radicales independientemente seleccionados a partir de halogeno, alquilo C1-6, alquilo C1-6 sustituido por halogeno, alquilo C1-6 sustituido por hidroxilo, alcoxilo C1-6, heterocicloalquilo C3-10, y alcoxilo C1-6 sustituido por halogeno; y las sales farmacéuticamente aceptables, hidratos, solvatos, e isomeros del mismo.
ARP050102354A 2004-06-10 2005-06-09 Compuestos y composiciones como inhibidores de quinasa de proteina AR049511A1 (es)

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