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
ureas
heterociclical
quinasa
inhibition
activity
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
ES98964709T
Other languages
English (en)
Other versions
ES2154253T3 (es
Inventor
Jacques Dumas
Uday Khire
Timothy B Lowinger
Holger Paulsen
Bernd Riedl
William J Scott
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bayer AG
Bayer Corp
Original Assignee
Bayer AG
Bayer Corp
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Publication of ES2154253T1 publication Critical patent/ES2154253T1/es
Application granted granted Critical
Publication of ES2154253T3 publication Critical patent/ES2154253T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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    • A61K31/33—Heterocyclic compounds
    • 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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    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
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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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