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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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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alkyl
halogen
heterocycloalkyl
substituted
heteroaryl
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Irm Llc
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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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EP (1) EP1758892B1 (es)
JP (1) JP4688876B2 (es)
CN (1) CN1960988B (es)
AR (1) AR049511A1 (es)
AU (1) AU2005254982B2 (es)
BR (1) BRPI0511978A (es)
CA (1) CA2567662C (es)
EC (1) ECSP067070A (es)
ES (1) ES2396135T3 (es)
IL (1) IL179613A0 (es)
MA (1) MA28679B1 (es)
MX (1) MXPA06014247A (es)
MY (1) MY144044A (es)
NO (1) NO20070160L (es)
PE (1) PE20060398A1 (es)
RU (1) RU2401265C2 (es)
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TW (1) TW200610762A (es)
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