AR029215A1 - Derivados de benzazol y tautomeros de los mismos utiles en el tratamiento de desordenes en los sistemas de autoinmunidad y neuronales, uso de dichos derivados en la preparacion de composiciones farmaceuticas aplicables en el tratamiento de dichos desordenes, metodo prar inhibir la expresion y/o acti - Google Patents

Derivados de benzazol y tautomeros de los mismos utiles en el tratamiento de desordenes en los sistemas de autoinmunidad y neuronales, uso de dichos derivados en la preparacion de composiciones farmaceuticas aplicables en el tratamiento de dichos desordenes, metodo prar inhibir la expresion y/o acti

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AR029215A1
AR029215A1 ARP000106912A ARP000106912A AR029215A1 AR 029215 A1 AR029215 A1 AR 029215A1 AR P000106912 A ARP000106912 A AR P000106912A AR P000106912 A ARP000106912 A AR P000106912A AR 029215 A1 AR029215 A1 AR 029215A1
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    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
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Abstract

Derivados de benzazol principalmente de uso como compuestos farmacéuticamente activos, así como formulaciones farmacéuticas formuladas con dichos derivados, los cuales son moduladores eficaces del pasaje de JNK y particularmente inhibidores eficientes y selectivos de JNK 2 y/o 3. Dichos derivados de benzazol, responden a al formula 1así como también sus tautomeros, sus isomeros geométricos, sus formas opticamente activas como enantiomeros, diastereomeros, y racematos, así como las sales farmacéuticamente aceptables de los mismos, donde: X es O, S o NRs, donde Rs es H o un alquilo C1-6 no sustituido o sustituido, siendo mayormente preferido X = S; G es un grupo pirimidinilo no sustituido o sustituido, o fusionado; R1 es seleccionado entre el grupo formado por hidrogeno, alcoxi (C1-6) no sustituido o sustituido, tioalcoxi C1-6 no sustituido o sustituido, alquilo C1-6 no sustituido o sustituido, alquenilo C2-6 no sustituido o sustituido, alquinilo C2-6 no sustituido o sustituido, grupos amino primario, secundario o terciario, aminoacilo, aminocarbonilo, alcoxicarbonilo C1-6 no sustituido o sustituido, arilo no sustituido o sustituido, heteroarilo no sustituido o sustituido, carboxilo, ciano, halogeno, hidroxi, nitro, sulfoxi, sulfonilo, sulfonamida, hidrazidas no sustituidas o sustituidas; y R2 es seleccionado del grupo que comprende hidrogeno, alquilo C1-6 no sustituido o sustituido, alquenilo C2-6 no sustituido o sustituido, alquinilo C2-6 no sustituido o sustituido; arilalquilo-C1-6 no sustituido o sustituido, arilo o heteroarilo no sustituido o sustituido, heteroarilalquilo-C1-6 no sustituido o sustituido, -C (O) û O R3, -C (O) û R3, -C (O) û NR3R3, con lo cual R3 y R3' son como se describen en la memoria, con la condicion que si X es S, R1 y R2 son H, G puede ser cualquiera de los siguientes grupos pirimidino: 2, 3 o 4 con la condicion adicional que si X es NH, R1 y R2 son H, G puede ser cualquiera de los siguientes grupos pirimidino: 5, 6 o 7 con la condicion final de si X es N-CH3, R1 y R2 son H, G puede ser cualquiera de los siguientes grupos pirimidino: 8, 9, 10, 11, 12, 0 13. Uso de dichos derivados en la preparacion de dichos derivados en la preparacion de composiciones farmacéuticas aplicables en el tratamiento de desordenes en los sistemas de autoinmunidad y neuronales. Método para inhibir la expresion y/o actividad JNK y métodos para el tratamiento de enfermedades mediadas por JNK. Composiciones farmacéuticas que incluyen dichos derivados y proceso para preparar los derivados mencionados.
ARP000106912A 1999-12-24 2000-12-22 Derivados de benzazol y tautomeros de los mismos utiles en el tratamiento de desordenes en los sistemas de autoinmunidad y neuronales, uso de dichos derivados en la preparacion de composiciones farmaceuticas aplicables en el tratamiento de dichos desordenes, metodo prar inhibir la expresion y/o acti AR029215A1 (es)

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EP99811207A EP1110957A1 (en) 1999-12-24 1999-12-24 Benzazole derivatives and their use as JNK modulators

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US (2) US7259162B2 (es)
EP (2) EP1110957A1 (es)
JP (1) JP4782344B2 (es)
KR (2) KR20070047853A (es)
CN (1) CN1252067C (es)
AR (1) AR029215A1 (es)
AT (1) ATE254123T1 (es)
AU (1) AU780241B2 (es)
BG (1) BG65986B1 (es)
BR (1) BR0016911A (es)
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UA (1) UA73151C2 (es)
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IL150346A (en) 2010-12-30
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