AR063099A1 - Compuestos y composiciones como inhibidores de la proteina quinasa - Google Patents

Compuestos y composiciones como inhibidores de la proteina quinasa

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AR063099A1
AR063099A1 ARP070104361A ARP070104361A AR063099A1 AR 063099 A1 AR063099 A1 AR 063099A1 AR P070104361 A ARP070104361 A AR P070104361A AR P070104361 A ARP070104361 A AR P070104361A AR 063099 A1 AR063099 A1 AR 063099A1
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Argentina
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alkyl
halo
substituted
heterocycloalkyl
heteroaryl
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Irm Llc
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Publication of AR063099A1 publication Critical patent/AR063099A1/es

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Abstract

La invencion proporciona una nueva clase de compuestos inhibidores de proteína quinasa y composiciones farmacéuticas que comprenden dichos compuestos. Los compuestos son utiles en el tratamiento o prevencion de enfermedades o trastornos asociados con la actividad anormal o irregular de la quinasa, en especial enfermedades o trastornos en los que ocurre la activacion anormal de las quinasas AbI, ARG, BCR-Abl, BRK, EphB, Fms, Fyn, KDR, c-Kit, LCK, PDGF-R, b-Raf, c-Raf, SAPK, Src, Tie2 y TrkB, como en los estados proliferativos benignos o malignos y en enfermedades autoinmunes. 1. Un compuesto de Formula (1) donde: A es un anillo de 5 miembros, insaturado o parcialmente insaturado que contiene 1 a 3 heteroátomos seleccionados entre -N=, - NR3-, -O- y -S-; donde R3 se selecciona entre hidrogeno, halo, alquiloC1-6-halo-sustituido, alquiloC1-6, -XOR4a, -XCN, -XC(O)OR4a, -XC(O)R4b, -XNR4aR4a, -XNR4aXNR4aR4a, -XC(O)NR4aXNR4aR4a, -XC(O)NR4aXR4b, -XC(O)NR4aXNR4aR4b, - XC(O)NR4aXOR4a, - XNR4aXNR4aR4b, -XNR4aXOR4a, -XNR4aXCF3, - XC(O)NR4aR4a, y -XR4b; donde cada X se selecciona independientemente entre un enlace y alquilenoC1-4; R4a se selecciona entre hidrogeno y alquiloC1-6 y R4b se selecciona entre ariIoC6-10, heteroariloC1-10, cicloalquiloC3-10 y heterocicloalquiloC3-10; donde cualquier cicloalquilo, heterocicloalquilo, arilo o heteroarilo de R4b está opcionalmente sustituido con 1 a 3 radicales seleccionados independientemente entre alquiloC1-6 y -NR4R4d; donde cada 4c y 4d se selecciona independientemente entre hidrogeno y alquiloC1-6; con la condicion de que el anillo A no es imidazol; donde cualquier anillo A puede estar opcionalmente sustituido con un radical R3 con la condicion de que R3 no es halo cuando está unido directamente a un átomo de nitrogeno; B es un anillo de 5 o 6 miembros, insaturado o parcialmente insaturado que contiene de 0 a 3 heteroátomos seleccionados entre -N=, -NR21-, -O- y -S-; donde R21 se selecciona entre hidrogeno, alquiloC1-6, alquiloC1-6-halo-sustituido y halo; donde B puede estar opcionalmente sustituido con 1 a 3 radicales seleccionados independientemente entre alquiloC1-6, alquiloC1-6-halo-sustituido y halo; Z se selecciona entre C y N; R1 se selecciona entre -XNR5R6, -XNR5XNR5R6, -XNR5XR5, - XNR5XOR6, -XNR6XC(O)OR5, -XNR6XC(O)NR6R6, -XOR5, -XC(O)R5, -XR5 y -XS(O)0-2R5 donde X se selecciona entre un enlace y alquilenoC1-4 opcionalmente sustituido con 1 a 2 radicales alquiloC1-6; R5 se selecciona entre hidrogeno, alquiloC1-6, arilC6-10-alquiloC0-4, heteroarilC1-10-alquiloC0-4, cicloalquilC3-10-alquiloC0-4 y heterocicloalquilC3-10-alquiloC0-4; y cada R6 se selecciona independientemente entre hidrogeno y alquiloC1-6; o R5 y R6 juntos con el nitrogeno al cual R5 y R6 están ambos unidos forman heteroarilo o heterocicloalquilo; o R1 junto con el N1 del anillo pirimidina al cual R1 está unido forman 2,3-dihidroimidazo[1,2-f]pirimidina; donde cualquier arilo, heteroarilo, cicloalquilo y heterocicloalquilo de R5 o la combinacion de R5 y R6 puede estar opcionalmente sustituido con 1 a 3 radicales seleccionados independientemente entre halo, nitro, ciano, hidroxi, alquiloC1-6, alcoxiC1-6, alquilo-halo-sustituido, alcoxi-halo-sustituido, -XNR7R8, -XOR7, - XNR7S(O)2R8, -XNR7S(O)R8, -XNR7SR8, -XC(O)NR7R8, -XC(O)NR7XNR7R8, XNR7C(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; donde X es un enlace o alquilenoC1-4; R7 y R8 se seleccionan independientemente del grupo formado por hidrogeno y alquiloC1-4; y R9 se selecciona entre heterocicloalquiloC3-10 y heteroariloC1-10; donde dicho heterocicloalquilo o heteroarilo de R9 está opcionalmente sustituido con un radical seleccionado del formado por alquiloC1-4, -XNR7XNR7R7, XNR7XOR7 y -XOR7; R2 se selecciona entre -R11, -CONR10R11, SO2NR10R11, -NR10R11, -NR10C(O)R11, -NR10S(O)0-2R11 y -NR10C(O)NR10R11; donde R10 se selecciona entre hidrogeno y alquiloC1-6; R11 se selecciona entre ariloC6-10, heteroariloC1-10, cicloaIquiloC3-10 y heterocicloalquiloC3-10; donde cualquier arilo, heteroarilo, cicloalquilo o heterocicloalquilo de R11 está opcionalmente sustituido con 1 a 3 radicales seleccionados entre halo, nitro, ciano, hidroxi, alquiloC1-6, alcoxiC1-6, alquiloC1-6-halo-sustituido, alquiloC1-6-ciano-sustituido, alquiloC1-6-hidroxi- sustituido, alcoxiC1-6-halo-sustituido, -X2R13, -X2NR12C(O)R13, -X2NR12C(O)NR12R13, - X2NR12R12, -X2NR12R13, -X2NR12X2R13, -X2NR12NR12R12, -X2NR12X2OR12, -X2C(O)NR12R13, -X2NR12S(O)0-2R13 y -X2S(O)0-2NR12R13 donde X2 se selecciona entre un enlace, alquilenoC1-4 y alquenilenoC2-4; R12 se selecciona entre hidrogeno, alquiloC1-6 y aIquiloC1-6-hidroxi-sustituido; R13 se selecciona entre ariloC6-10, heteroariloC1-10, cicloalquiloC3-10 y heterocicloalquiloC3-10; donde cualquier arilo, heteroarilo, cicloalquilo o heterocicloalquilo de R13 está opcionalmente sustituido con 1 a 3 radicales seleccionados independientemente entre halo, ciano, hidroxi, nitro, amino, alquiloC1-6, alquiloC1-6-halo-sustituido, alquiloC1-6-hidroxi-sustituido, alquiloC1-6-ciano-sustituido, alquiloC1-6-hidroxi-sustituido, alcoxiC1-6, alcoxiC1-6-halo- sustituido, -X3NR7R8, -X3NR7X3OR7, arilC6-10-alquiloC0-4, heteroarilC1-10-alquiloC0-4, cicloalquilC3-10-alquiloC0-4, heterocicloalquilC3-10-alcoxiC0-4; y heterocicloalquilC3-10-alquiloC0-4; donde X3 se selecciona entre un enlace y alquilenoC1-4; R7 y R8 son como se describieron anteriormente y donde cualquiera de los sustituyentes arilo, heteroarilo, cicloalquilo o heterocicloalquilo de R13 está además opcionalmente sustituido con 1 a 3 radicales seleccionados independientemente entre halo, hidroxi, alquiloC1-6, alquiloC1-6-halo-sustituido, alquiloC1-6-hidroxi-sustituido, aIcoxiC1-6, heterocicloalquiloC3-10 y alcoxiC1-6-halo-sustituido; R20 se selecciona entre hidrogeno y alquiloC1-6 y sus sales farmacéuticamente aceptables.
ARP070104361A 2006-10-02 2007-10-02 Compuestos y composiciones como inhibidores de la proteina quinasa AR063099A1 (es)

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JP (1) JP5153777B2 (es)
KR (1) KR101101675B1 (es)
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AR (1) AR063099A1 (es)
AU (1) AU2007305016B2 (es)
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CA (1) CA2663366C (es)
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