AR053014A1 - Compuestos de pirazol inhibidores de raf quinasa - Google Patents

Compuestos de pirazol inhibidores de raf quinasa

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Publication number
AR053014A1
AR053014A1 ARP060100401A ARP060100401A AR053014A1 AR 053014 A1 AR053014 A1 AR 053014A1 AR P060100401 A ARP060100401 A AR P060100401A AR P060100401 A ARP060100401 A AR P060100401A AR 053014 A1 AR053014 A1 AR 053014A1
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AR
Argentina
Prior art keywords
nr20r21
alkyl
aryl
heterocyclyl
alkynyl
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ARP060100401A
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English (en)
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Genentech Inc
Array Biopharma Inc
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Application filed by Genentech Inc, Array Biopharma Inc filed Critical Genentech Inc
Publication of AR053014A1 publication Critical patent/AR053014A1/es

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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Abstract

Los compuestos de pirazolilo de formulas (1) y (2) son utiles para inhibir la Raf quinasa y para el tratamiento de trastornos mediados por la misma. Se revelan métodos para el uso de compuestos de pirazolilo para el diagnostico in vitro, in situ e in vivo, el tratamiento o prevencion de dichos trastornos en células mamíferas, o afecciones patologicas asociadas. Composiciones farmacéuticas. Métodos de obtencion. Reivindicacion 1. Un compuesto seleccionado de formula (1) y (2), y sus estereoisomeros, tautomeros, solvatos y sales aceptables para uso farmacéutico en las cuales: el anillo A es: i) un anillo heterocíclico de 5 o 6 miembros que tiene uno o dos heteroátomos independientemente seleccionados de O, N, y S, ii) un anillo carbocíclico de 5 o 6 miembros opcionalmente fusionado a un heterociclo de 5 o 6 miembros, o iii) un anillo fenilo, donde dichos anillos heterocíclicos, carbocíclicos y fenilo están opcionalmente sustituidos con uno o más grupos seleccionados independientemente de F, Cl, Br, I, -C(=Y)R20, -C(=Y)OR20, -C(=Y)NR20R21, NR20R21, -NR20C(=Y)R21, -NR20C(=Y)OR21, -NR23C(=Y)NR20R21, =NOR20, =NR20, =N+(O)OR20, =NNR20R21, =O, -OR20, -OC(=Y)R20, -OC(=Y)OR20, - OC(=Y)NR20R21, -OS(O)2(OR20), - OP(=Y)(OR20)(OR21), -OP(OR20)(OR21), - P(=Y)(OR20)(OR21), -P(=Y)(OR)NR20R21, =S, -SR20, -S(O)R20, -S(O)2R20, -S(O)2NR20R21, -S(O)(OR20), -S(O)2(OR20), -SC(=Y)R20, -SC(=Y)OR20, - SC(=Y)NR20R21, alquilo C1-8, alquenilo C2-8, alquinilo C2-8, arilo C6- 20, carbociclilo C3-12, heterociclilo C2-20, y un grupo protector, y donde dicho alquilo, alquenilo, alquinilo, arilo, carbociclilo y heterociclilo están opcional e independientemente sustituidos con uno o más grupos seleccionados independientemente de F, Cl, Br, I, -C(=Y)R20, -C(=Y)OR20, -C(=Y)NR20R21, NR20R21, -NR20C(=Y)R21, -NR20C(=Y)OR21, - NR23C(=Y)NR20R21, -OR20, -OC(=Y)R20, -OC(=Y)OR20, -OC(=Y)NR20R21, - OS(O)2(OR20), -OP(=Y)(OR20)(OR21), -OP(OR20)(OR21), -P(=Y)(OR20)(OR21), - P(=Y)(OR)NR20R21, -SR20, -S(O)R20, -S(O)2R20, -S(O)2NR20R21, -S(O)(OR20), - S(O)2(OR20), -SC(=Y)R20, -SC(=Y)OR20, -SC(=Y)NR20R21, alquilo C1-8, alquenilo C2-8, alquinilo C2-8, arilo C6-2O, carbociclilo C3-12, heterociclilo C2-20; X se selecciona de un heterociclilo C2-20, un carbociclilo C3-12, y un arilo C6-20, donde dicho heterociclo, carbociclilo y arilo están opcionalmente sustituidos con uno o más grupos seleccionados independientemente de F, Cl, Br, I, -C(=Y)R20, -C(=Y)OR20, - C(=Y)NR20R21, -NR20R21, -NR20C(=Y)R21, -NR20C(=Y)OR21, -NR23C(=Y)NR20R21, - OR20, -OC(=Y)R20, -OC(=Y)OR20, -OC(=Y)NR20R21, -OS(O)2(OR20), - OP(=Y)(OR20)(OR21), -OP(OR20)(OR21), -P(=Y)(OR20)(OR21), -P(=Y)(OR23)NR20R21, - SR20, -S(O)R20, -S(O)2R20, - S(O)2NR20R21, -S(O)(OR20), -S(O)2(OR20), -SC(=Y)R20, - SC(=Y)OR20, -SC(=Y)NR20R21, lactama de 5-7 miembros en el anillo, lactona de 5 a 7 miembros en el anillo, sultama de 5 a 7 miembros en el anillo, alquilo C1-8, alquenilo C2-8, alquinilo C2-8, carbociclilo C3-12, arilo C6-20, y heterociclilo C2-20, donde dicho alquilo, alquenilo, alquinilo, carbociclilo, arilo, y heterociclilo están opcionalmente sustituidos con uno o más grupos seleccionados independientemente de F, Cl, Br, I, OR20, NR20R21 -SR20, -S(O)R20, -S(O)2R20, alquilo, alquenilo, alquinilo, carbociclilo, arilo y heterociclilo; R1 se selecciona H, alquilo C1-8, alquenilo C2-8, alquinilo C2-8, alquiloC1-8NR20R21, un heterociclilo C2-20, un carbociclilo C3-12, y un arilo C6-20, donde dicho alquilo, alquenilo, alquinilo, heterociclo, carbociclilo y arilo están opcionalmente sustituidos con uno o más grupos seleccionados independientemente de F, Cl, Br, I, -C(=Y)R20, -C(=Y)OR20, -C(=Y)NR20R21, -NR20R21, OR20, CN, C(=O)NR20R21, C(=O)OR20, alquilo, alquiloC1-8 NR20R21, y heterociclilo; R2 se selecciona de H, F, Cl, Br, I, -C(=Y)R20, -C(=Y)OR20, -C(=Y)NR20R21, -OR20, -OC(=Y)R20, -OC(=Y)OR20, -OC(=Y)NR20R21, -OS(O)2(OR20), - OP(=Y)(OR20)(OR21), -OP(OR20)(OR21), - P(=Y)(OR20)(OR21), -P(=Y)(OR)NR20R21, - SR20, -S(O)R20, -S(O)2R20, -S(O)2NR20R21, -S(O)(OR20), -S(O)2(OR20), -SC(=Y)R20, - SC(=Y)OR20, -SC(=Y)NR20R21, lactama de 5-7 miembros en el anillo, lactona de 5 a 7 miembros en el anillo, sultama de 5 a 7 miembros en el anillo, alquilo C1-8, alquenilo C2-8, alquinilo C2-8, carbociclilo C3-12, arilo C6-20, y heterociclilo C2-20, donde dicho alquilo, alquenilo, alquinilo, carbociclilo, arilo, y heterociclilo están opcionalmente sustituidos con uno o más grupos seleccionados independientemente de F, Cl, Br, I, OR20, NR20R21 -SR20, -S(O)R20, -S(O)2R20, alquilo, alquenilo, alquinilo, carbociclilo, arilo y heterociclilo; o R1 y R2 de Formula (1) junto con los átomos a los cuales están unidos opcionalmente forman un anillo heterociclo fusionado de 5 o 6 miembros, saturado, parcialmente saturado o aromático que tienen al menos dos heteroátomos seleccionados independientemente de O, N y S, donde dicho anillo heterociclo está opcionalmente sustituido con uno o más grupos seleccionados independientemente de F, Cl, Br, I, -C(=Y)R20, -C(=Y)OR20, -C(=Y)NR20R21, -NR20R21, -NR20C(=Y)R21, -NR20C(=Y)OR21, -NR23C(=Y)NR20R21, -OR20, -OC(=Y)R20, -OC(=Y)OR20, -OC(=Y)NR20R21, -OS(O)2(OR20), - OP(=Y)(OR20)(OR21), - OP(OR20)(OR21), -P(=Y)(OR20)(OR21), -P(=Y)(OR23)NR20R21, -SR20, -S(O)R20, - S(O)2R20, -S(O)2NR20R21, -S(O)(OR20), -S(O)2(OR20), -SC(=Y)R20, -SC(=Y)OR20, - SC(=Y)NR20R21, lactama de 5-7 miembros en el anillo, lactona de 5 a 7 miembros en el anillo, sultama de 5 a 7 miembros en el anillo, alquilo C1-8, alquenilo C2-8, alquinilo C2-8, carbociclilo C3-12, arilo C6-20, y heterociclilo C2-20, donde dicho alquilo, alquenilo, alquinilo, carbociclilo, arilo, y heterociclilo están opcionalmente sustituidos con uno o más grupos seleccionados independientemente de F, Cl, Br, I, OR20, NR20R21 -SR20, -S(O)R20, -S(O)2R20, alquilo, alquenilo, alquinilo, carbociclilo, arilo y heterociclilo; R3, R4, y R5 se seleccionan independientemente de H, F, Cl, Br, I, -C(=Y)R20, - C(=Y)OR20, -C(=Y)NR20R21, -NR20R21, -NR20C(=Y)R21, -NR20C(=Y)OR21, -NR23C(=Y)NR20R21, -OR20, -OC(=Y)R20, -OC(=Y)OR20, -OC(=Y)NR20R21, - OS(O)2(OR20), -OP(=Y)(OR20)(OR21), -OP(OR20)(OR21), - P(=Y)(OR20)(OR21), - P(=Y)(OR23)NR20R21, -SR20, -S(O)R20, -S(O)2R20, -S(O)2NR20R21, -S(O)(OR20), -S(O)2(OR20), -SC(=Y)R20, -SC(=Y)OR20, -SC(=Y)NR20R21, lactama de 5-7 miembros en el anillo, lactona de 5 a 7 miembros en el anillo, sultama de 5 a 7 miembros en el anillo, alquilo C1-8, alquenilo C2-8, alquinilo C2-8, carbociclilo C3-12, arilo C6-20, y heterociclilo C2-20, donde dicho alquilo, alquenilo, alquinilo, carbociclilo, arilo, y heterociclilo están opcionalmente sustituidos con uno o más grupos seleccionados independientemente de F, Cl, Br, I, OR20, NR20R21 -SR20, -S(O)R20, -S(O)2R20, alquilo, alquenilo, alquinilo, carbociclilo, arilo y heterociclilo; R20 y R21 se seleccionan independientemente de H, alquilo C1-8, alquenilo C2- 8, alquinilo C2-8, arilo C6-20, heterociclilo C2-20, y un grupo protector, donde dicho alquilo, alquenilo, alquinilo, arilo y heterociclilo están opcional e independientemente sustituidos con uno o más grupos seleccionados independientemente de F, Cl, Br, I, -C(=Y)Ra, -C(=Y)ORa, -C(=Y)NRaRb, -ORa, -OC(=Y)Ra, -OC(=Y)ORa, -OC(=Y)NRaRb, -OS(O)2(ORa), -OP(=Y)(ORa)(ORb), -OP(ORa)(ORb), -P(=Y)(ORa)(ORb), - P(=Y)(OR)NRaRb, -SRa, -S(O)Ra, -S(O)2Ra, -S(O)2NRaRb, -S(O)(ORa), -S(O)2(ORa), -SC(=Y)Ra, - SC(=Y)ORa, y -SC(=Y)NRaRb, o R20 y R21 junto con los átomos a los cuales están unidos forman un anillo heterocíclico, donde dicho anillo heterocíclico está opcionalmente sustituido con uno o más grupos seleccionados independientemente de F, Cl, Br, I, alquilo, alquenilo y alquinilo; R23 es H, alquilo C1-8, alquenilo C2-8, alquinilo C2-8 o, arilo C6-20, heterociclilo C2-20, o un grupo protector; Ra y Rb son independientemente H, alquilo C1-8, alquenilo C2-8, alquinilo C2-8, arilo C6-20, o heterociclilo C2-20; Y es independientemente O, S, NR20, +N(O)R20, N(OR20), +N(O)(OR20), o N-NR20R21; y grupo protector se selecciona de trialquilsililo, dialquilfenilsililo, benzoato, bencilo, benciloximatilo, metilo, metoximetilo, triarilmetilo, ftalimido, t-butoxicarbonilo (BOC), benciloxicarbonilo (CBz), 9-fluorenilmetilenoxicarbonilo (Fmoc), y tetrahidropiranilo.
ARP060100401A 2005-02-04 2006-02-03 Compuestos de pirazol inhibidores de raf quinasa AR053014A1 (es)

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US (2) US7491829B2 (es)
EP (1) EP1846391A2 (es)
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