AR071778A1 - Imidazo[1,2-b]piridazinas inhibidores de proteinquinasas, composiciones farmaceuticas que las contienen y uso de las mismas en el tratamiento del cancer, enfermedades oseas y autoinmunes, entre otras. - Google Patents

Imidazo[1,2-b]piridazinas inhibidores de proteinquinasas, composiciones farmaceuticas que las contienen y uso de las mismas en el tratamiento del cancer, enfermedades oseas y autoinmunes, entre otras.

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AR071778A1
AR071778A1 ARP090101724A ARP090101724A AR071778A1 AR 071778 A1 AR071778 A1 AR 071778A1 AR P090101724 A ARP090101724 A AR P090101724A AR P090101724 A ARP090101724 A AR P090101724A AR 071778 A1 AR071778 A1 AR 071778A1
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alkyl
heterocycloalkyl
substituted
heteroaryl
cycloalkyl
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Irm Llc
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Abstract

Composiciones farmaceuticas que comprenden tales compuestos y metodos para usar dichos compuestos en el tratamiento o la prevencion de enfermedades o trastornos asociados a la actividad anormal o desregulada de quinasas, especialmente Ros, KDR, FMS, c-FMS, FLT3, c-Kit, JAK2, JAK3, Aurora, PDGFR, Lck, TrkA, TrkB, TrkC, IGF-1R, ALK4, ALK5 y ALK o combinaciones de estas. Reivindicacion 1: Un compuesto de formula (1), su sal aceptable para uso farmaceutico, su solvato aceptable para uso farmaceutico, en donde: R1 es un resto de formula (2) en donde, X1, X2, X3 y X4 son cada uno de manera independiente CR9, C o N, con la condicion de que al menos uno de X1, X2, X3 y X4 es N y como m ximo solo dos de X1, X2, X3 y X4 son N; X5 es C(R3)2, O, S, S(O)2, S(O), o NR3; m es 1, 2, 3 o 4; n es 0, 1, 2 o 3; k es 0, 1, 2, 3, 4, 5 o 6; cada R3 se selecciona de manera independiente entre halogeno, nitro, -N(R4)2, -OR9, -CN, =O, -C(O)N(R4)2, -N(R4)C(O)OR4, -N(R4)C(O)R4, -C(O)R9, -C(O)OR9, -R6, -OR6, -L1R5, -L1R6, -Y1R5, -Y1R6, -S(O)2R9, -S(O)2N(R4)2, -NR4S(O)2, -OC(O)R9, -(CH2)pOR9, -L1C(O)R8, -L1R8, -C(O)R9, -OC(O)R9, -C(O)OR9, -C(O)R9, -N(R9)2, -C(O)N(R4)2, -N(R4)C(O)R4, -N(R4)C(O)OR4, -S(O)2R9, -S(O)2N(R4)2, -NR4S(O)2, alquilo C1-8, arilo C6-14, cicloalquilo C3-8, alquilo C1-8 halo-sustituido, alcoxi C1-8, hidroxil-alquilo C1-8, alcoxi C1-8 halo-sustituido, heterocicloalquilo C2-14 y heteroarilo C2-13, en donde los alquilo C1-8, arilo C6-14, cicloalquilo C3-8, heterocicloalquilo C2-14 y heteroarilo C2-13 de R3 est n sustituidos opcionalmente con 1 a 3 sustituyentes seleccionados de manera independiente entre halogeno, amino, nitro, hidroxilo, ciano, -OR9, -C(O)N(R4)2, -N(R4)C(O)OR4, -N(R4)C(O)R4, -C(O)R9, -C(O)OR9, -R6, -OR6, -L1R5, -L1R6, -Y1R5, -Y1R6, -S(O)2R9, -S(O)2N(R4)2, -NR4S(O)2, -OC(O)R9, -(CH2)pOR9, -L1C(O)R8, -L1R8, -C(O)R9, -OC(O)R9, -C(O)OR9, -C(O)R9, -N(R9)2, -C(O)N(R4)2, -N(R4)C(O)R4, -N(R4)C(O)OR4, -S(O)2R9, -S(O)2N(R4)2, -NR4S(O)2, alquilo C1-8, aminoalquilo C1-8, alcoxi C1-8, alquiltio C1-8, hidroxil-alquilo C1-8, alquilo C1-8 halo-sustituido, alcoxi C1-8 halo-sustituido, cicloalquilo C3-8, heterocicloalquilo C2-14, arilo C6-14 y heteroarilo C2-13; alternativamente cada R3 es independientemente un alquilo C1-8, en donde por lo menos dos R3 juntos forman un cicloalquilo C3-8 fusionado con un heterociclo y en donde cada alquilo C1-8 de R3 est  sustituido en forma opcional con 1 a 3 sustituyentes seleccionados de manera independiente entre halogeno, amino, nitro, hidroxilo, ciano, -OR9, alquilo C1-8, aminoalquilo C1-8, alcoxi C1-8, alquiltio C1-8, hidroxil-alquilo C1-8, alquilo C1-8 halo-sustituido, alcoxi C1-8 halo-sustituido, cicloalquilo C3-8, heterocicloalquilo C2-14, arilo C6-14 y heteroarilo C2-13; R2 es arilo C6-14, heteroarilo C2-13 o heterocicloalquilo C2-14, en donde los arilo C6-14, heteroarilo C2-13 o heterocicloalquilo C2-14 de R2 est n sustituidos opcionalmente con 1 a 3 sustituyentes seleccionados de manera independiente entre halogeno, heterocicloalquilo C2-14, heteroarilo C2-13, alquilo C1-8, cicloalquilo C3-8, -CN, -C(O)N(R4)2, -N(R4)C(O)OR4, -N(R4)C(O)R4, -C(O)R9, -OR9, -C(O)OR9, -N(R4)2, -R6, -OR6, -L1R5, -L1R6, -Y1R5, -Y1R6, -S(O)2R9, -S(O)2N(R4)2, -NR4S(O)2R4, -OC(O)R9, alcoxi C1-8, hidroxil-alquilo C1-8, alquilo C1-8 halo-sustituido y alcoxi C1-8 halo-sustituido; cada R4 se selecciona de manera independiente entre H, alquilo C1-8, -L1R5, L1R6, -L1R8, heteroarilo C2-13, arilo C6-14, heterocicloalquilo C2-14 y cicloalquilo C3-8, en donde los alquilo C1-8, heteroarilo C2-13 y cicloalquilo C3-8est n sustituidos opcionalmente con 1 a 3 sustituyentes seleccionados de manera independiente entre halogeno, deuterio, -CD3, -S(O)2R9, -CN, alquilo C1-8, -OR9, -N(R9)2 y -(CH2)pOR9; L1 es un enlace, alquileno C1-8, alquenileno C2-8, -O(CH2)p-, -C(O)-, -N(R9)-, (CH2)pC(O)-, -C(O)(CH2)pO(CH2)p- o -C(O)O-; Y1 es arileno C6-14, heteroarileno C2-13, cicloalquileno C3-8, heterocicloalquileno C2-14 o alcoxileno C1-8, cada uno de los cuales est  sustituido en forma opcional con 1 a 3 sustituyentes seleccionados de manera independiente entre halogeno, heterocicloalquilo C2-14, heteroarilo C2-13, alquilo C1-8, cicloalquilo C3-8, -CN, -C(O)N(R4)2, -N(R4)C(O)OR4, -N(R4)C(O)R4, -C(O)R9, -OR9, -C(O)OR9, -N(R4)2, -R6, -OR6, -L1R5, -L1R6, -Y1R5, -Y1R6, -S(O)2R9, -S(O)2N(R4)2, -NR4S(O)2R4, -OC(O)R9, alcoxi C1-8, hidroxil-alquilo C1-8, alquilo C1-8 halo-sustituido y alcoxi C1-8 halo-sustituido; R5 es arilo C6-14, heteroarilo C2-13, heterocicloalquilo C2-14, -N(R9)2, -N(R9)C(O)R9, -C(O)N(R9)2, -(CH2)pOR9 o -OR9; R6 es arilo C6-14, heteroarilo C2-13, heterocicloalquilo C2-14, -OCH(R7)2, -C(O)R7, alquilo C1-8, o cicloalquilo C3-8, en donde los alquilo C1-8, cicloalquilo C3-8, arilo C6-14, heteroarilo C2-13, y heterocicloalquilo C2-14 de R6 est n sustituidos opcionalmente con 1 a 3 sustituyentes seleccionados de manera independiente entre halogeno, -CN, -OR9, -(CH2)pOR9, -L1C(O)R8, -L1R8, -L1R5, -C(O)R9, -OC(O)R9, -C(O)OR9, -C(O)R8, -OC(O)N(R4)2, -N(R9)2, -C(O)C(O)OR9, -(CH2)pN(R9)2, -N(R4)2, -C(O)N(R4)2, -N(R4)C(O)R4, -N(R4)C(O)OR4, -(CH2)pS(O)2R9, -S(O)2R9, -S(O)2N(R4)2, -NR4S(O)2R4, -NR4S(O)2R9, heterocicloalquilo C2-14, heteroarilo C2-13, alquilo C1-8, alqueno C2-8, alcoxi C1-8, alquilo C1-8 hidroxilo-sustituido, alquilo C1-8 halo-sustituido y alcoxi C1-8 halo-sustituido; o R6 es arilo C6-14, heteroarilo C2-13, heterocicloalquilo C2-14 o cicloalquilo C3-8 que tiene un puente alquilo C1-4; o R6 es un heterocicloalquilo C2-14 sustituido en forma opcional con 1 a 3 sustituyentes seleccionados de manera independiente entre halogeno, =O, -CN, -OR9, -(CH2)pOR9, -L1C(O)R8, -L1R8, -L1R5, -C(O)R9, -OC(O)R9, -C(O)OR9, -C(O)R8, OC(O)N(R4)2, -N(R9)2, -C(O)C(O)OR9, -(CH2)pN(R9)2, -N(R4)2, -C(O)N(R4)2, -N(R4)C(O)R4, -N(R4)C(O)OR4, -(CH2)pS(O)2R9, -S(O)2R9, -S(O)2N(R4)2, -NR4S(O)2R4, -NR4S(O)2R9, heterocicloalquilo C2-14, heteroarilo C2-13, alquilo C1-8, alqueno C2-8, alcoxi C1-8, alquilo C1-8 hidroxilo-sustituido, alquilo C1-8 halo-sustituido y alcoxi C1-8 halo-sustituido; cada R7 se selecciona de manera independiente entre H, alquilo C1-8 y -L1R8; R8 es H, -N(R9)2, -N(R4)2, -SR9, -CN, alquilo C1-8, cicloalquilo C3-8 y heterocicloalquilo C2-14, en donde los alquilo C1-8, cicloalquilo C3-8 y heterocicloalquilo C2-14 de R8 est n sustituidos opcionalmente con 1 a 3 sustituyentes seleccionados de manera independiente entre halogeno, alquilo C1-6, -CN, -OR9, -(CH2)pOR9, -L1C(O)R8, -C(O)R9, -OC(O)R9, -C(O)OR9, -N(R9)2, -N(R4)2, -C(O)N(R4)2, -N(R4)C(O)R4, -N(R4)C(O)OR4, -S(O)2R9, -S(O)2N(R4)2, y -NR4S(O)2; cada R9 se selecciona de manera independiente entre H, cicloalquilo C3-8 y alquilo C1-8; y cada p es independientemente 1, 2, 3, 4, 5 o 6.
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