ES2154253T1 - Inhibicion de la actividad de la quinasa p38 utilizando ureas heterociclicas sustituidas. - Google Patents

Inhibicion de la actividad de la quinasa p38 utilizando ureas heterociclicas sustituidas.

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Publication number
ES2154253T1
ES2154253T1 ES98964709T ES98964709T ES2154253T1 ES 2154253 T1 ES2154253 T1 ES 2154253T1 ES 98964709 T ES98964709 T ES 98964709T ES 98964709 T ES98964709 T ES 98964709T ES 2154253 T1 ES2154253 T1 ES 2154253T1
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ES
Spain
Prior art keywords
substituted
alkyl
per
heteroaryl
cycloalkyl
Prior art date
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Granted
Application number
ES98964709T
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English (en)
Other versions
ES2154253T3 (es
Inventor
Jacques Dumas
Uday Khire
Timothy B Lowinger
Holger Paulsen
Bernd Riedl
William J Scott
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Bayer AG
Bayer Corp
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Bayer AG
Bayer Corp
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Publication of ES2154253T1 publication Critical patent/ES2154253T1/es
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Publication of ES2154253T3 publication Critical patent/ES2154253T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
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Abstract

Un método para el tratamiento de una enfermedad mediada por p38 distinta del cáncer, que comprende administrar un compuesto de fórmula I **fórmula** en la cual B es un resto arilo o heteroarilo hasta tricíclico sustituido o no sustituido que puede tener hasta 30 átomos de carbono que tiene al menos una estructura aromática de 5 ó 6 miembros que contiene 0-4 miembros del grupo constituido por nitrógeno, oxígeno y azufre, en la cual si B es un grupo sustituido, está sustituido conunoo más sustituyentes seleccionados independientemente del grupo constituido por halógeno, hasta perhalosustitución, y Xn, en el cual n es 0-3 y cada X se selecciona independientemente del grupo constituido por -CN, -CO2R5,-C(O)NR5 R5'', -C(O)R5, -NO2, -OR5, -SR5, -NR5 R5'', -NR5 C-(O)-OR5'', -NR5 C(O)R5'', alquilo C1-C10, alquenilo C2-C10, alcoxi C1-C10, cicloalquilo C3-C10, arilo C6-C14, alcarilo C7-C24, heteroarilo C3-C13, alc-heteroarilo C4-C23, alquilo C1-C10 sustituido, alquenilo C2-C10 sustituido, alcoxi C1-C10 sustituido, cicloalquilo C3-C10 sustituido, alc-heteroarilo C4-C23 sustituido e -Y-Ar; en el cual si X es un grupo sustituido, está sustituido con uno o más sustituyentes seleccionados independientemente del grupo constituido por -CN, -CO2R5, -C(O)R5, -C(O)NR5 R5'', -OR5, -SR5, -NR5 R5'',-NO2, -NR5 C-(O)R5'',-NR5 C-(O)OR5'', y halógeno hasta per-halosustitución; donde R5 y R5'' se seleccionan independientemente de H, alquilo C1-C10, alquenilo C2-C10, cicloalquilo C3-C10, arilo C6-C14, heteroarilo C3-C13, alcarilo C7-C24, alc-heteroarilo C4-C23, alquilo C1-C10 hasta per-halosustituido, cicloalquilo C3-C10 hasta per-halosustituido, alquenilo C2-C10 hasta per-halosustituido,arilo C6-C14 hasta per-halosustituido y heteroarilo C3-C13 hasta per-halosustituido,donde Y es -O-, -S-, -N(R5 )-, -(CH2)-m, -C(O)-, -CH(OH)-, -(CH2)mO-, -(CH2)mS-, -(CH2)mN(R5 )-, -O(CH2)m-, -CHX a -, -NR5 C(O)NR5 R5''-, -NR5 C(O)-, -C(O)NR5 -, -CX a2 -, -S-(CH2)m- y -N(R5)(CH2)m-, m = 1-3, y X a es halógeno; y Ar es una estructura aromática de 5-10 miembros que contiene 0-4 miembros del grupo constituido por nitrógeno, oxígeno y azufre que está insustituido o sustituido con halógeno hasta per-halosustitución y opcionalmente sustituido con Zn1, donde n1 es 0 a 3 y cada Z se selecciona independientemente del grupo constituido por -CN, -CO2R5, -C(O)NR5 R5'', -C(O)-NR5, -NO2, =O, -OR5, -SR5, -NR5 R5'', -C(O)R5, -SO2R5, -SO2NR5 R5'', -NR5 C(O)OR5'', -NR5 C(O)R5'', alquilo C1-C10, alcoxiC1-C10, cicloalquilo C3-C10, arilo C6-C14, heteroarilo C3-C13, alcarilo C7-C24, alc-heteroarilo C4-C23, alquilo C1-C10 sustituido, cicloalquilo C3-C10 sustituido, alcarilo C7-C24 sustituido y alc-heteroarilo C4-C23 sustituido; donde si Z es un grupo sustituido, está sustituido con uno o más sustituyentes seleccionados independientemente del grupo constituido por -CN, -CO2R5, -C(O)R5, -C(O)NR5 R5'', =O, -OR5, -SR5, -NO2,-NR5 R5'', -NR5 C-(O)R5'', -NR5 C-(O)OR5'', alquilo C1-C10, alcoxi C1-C10, cicloalquilo C3-C10, heteroariloC-C10, arilo C6-C14, alc-heteroarilo C4-C24 y alcarilo C7-C24. A es un resto heteroarilo seleccionado del grupo constituido por **fórmula** donde R1 se selecciona del grupo constituido por halógeno, alquilo C3-C10, cicloalquilo C3-C10, heteroarilo C1-C13, arilo C6-C14, alcarilo C7-24, alquilo C1-C10 hasta per-halosustituido, cicloalquilo C3-C10 hasta per-halosustituido, heteroarilo C1-C13 hasta Per-halosustituido, arilo C6-C14 hasta per-halosustituido, y alcarilo C7-24 hasta per-halosustituido; R2 se selecciona del grupo constituido por H, -C(O)R4, -CO2R4, -C(O)NR3 R3'', alquilo C1-C10, cicloalquilo C3-C10, alcarilo C7-C24, alc-heteroarilo C4-C23, alquilo C1-C10 sustituido, cicloalquilo C3-C10 sustituido, alcarilo C7-C24 sustituido y alc-heteroarilo C4-C23 sustituido, en el caso en que R2 es un grupo sustituido, el mismo está sustituido conuno o más sustituyentes seleccionados independientemente del grupo constituido por -CN, -CO2R4, -C(O)-NR3 R3'', -NO2, -OR4, -SR4, yhalógeno hasta per-halosustitución, donde R3y R3'' se seleccionan independientemente del grupo constituido por H, -OR4, -SR4, -NR4 R4'', -C(O)R4, -CO2R4, -C(O)NR4 R4'', alquilo C1-C10, cicloalquilo C3-C10, arilo C6-C14, heteroarilo C3-C13, alcarilo C7-C24, alc-heteroarilo C4-C23, alquilo C1-C10 hasta per-halosustituido, cicloalquilo C3-C10 hasta per-halosustituido, arilo C6-C14 hasta per-halosustituido y heteroarilo C3-C13 hasta per-halosustituido; y donde R4 y R4'' se seleccionan independientemente del grupo constituido por H, alquilo C1-C10, cicloalquilo C3-C10, arilo C6-C14, heteroarilo C3-C13; alcarilo C7-C24, alc-heteroarilo C4-C23, alquilo C1-C10 hasta per-halosustituido, cicloalquilo C3-C10 hasta per-halosustituido, arilo C6-C14 hasta per-halosustituido y heteroarilo C3-C13 hasta per-halosustituido, R a es alquilo C1-C10, cicloalquilo C3-C10, alquilo C1-C10 hasta per-halosustituido y cicloalquilo C3-C10 hasta per-halosustituido; y R b es hidrógeno o halógeno, R c es hidrógeno, halógeno, alquilo C1-C10, alquilo C1-C10 hasta per-halosustituido o se combina con R1 y los átomos de carbono del anillo a los cuales están unidos R1 y Rc para formar un anillo de cicloalquilo, arilo o hetarilo de 5 ó 6 miembros con 0-2 miembros seleccionados de O,N y S.
ES98964709T 1997-12-22 1998-12-22 Inhibición de la actividad de p38 cinasa usando ureas heterocíclicas sustituidas. Expired - Lifetime ES2154253T3 (es)

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