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AR046791A1 - Tiadiazoles como ligandos del receptor cxc y cc-quimioquina; composiciones farmaceuticas que los contienen como principio activo y su empleo en la preparacion de medicamentos. - Google Patents

Tiadiazoles como ligandos del receptor cxc y cc-quimioquina; composiciones farmaceuticas que los contienen como principio activo y su empleo en la preparacion de medicamentos.

Info

Publication number
AR046791A1
AR046791A1 ARP040104753A ARP040104753A AR046791A1 AR 046791 A1 AR046791 A1 AR 046791A1 AR P040104753 A ARP040104753 A AR P040104753A AR P040104753 A ARP040104753 A AR P040104753A AR 046791 A1 AR046791 A1 AR 046791A1
Authority
AR
Argentina
Prior art keywords
substituted
group
unsubstituted
independently selected
alkyl
Prior art date
Application number
ARP040104753A
Other languages
English (en)
Original Assignee
Pharmacopeia Drug Discovery
Schering Corp
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Pharmacopeia Drug Discovery, Schering Corp filed Critical Pharmacopeia Drug Discovery
Publication of AR046791A1 publication Critical patent/AR046791A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/10—1,2,5-Thiadiazoles; Hydrogenated 1,2,5-thiadiazoles
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Abstract

La presente se refiere a tiadiazoles como ligandos del receptor CXC y CC-quimioquina, estos compuestos son útiles para el tratamiento de enfermedades intermediadas por quimioquina, tales como cáncer, angiogénesis, enfermedades oculares angiogénicas, enfermedades pulmonares, esclerosis múltiple, artritis reumatoidea, osteoartritis, apoplejía y lesiones isquémicas por reperfusión, dolor, (por ejemplo, dolor agudo, dolor agudo e inflamatorio crónico y dolor neuropático) usando un compuesto de fórmula (1A). Reivindicación 1:Un compuesto de la fórmula (1A) y las sales del mismo farmacéuticamente aceptables, donde: A está seleccionado del grupo de fórmulas (2) donde los anillos precedentes de dichos grupos A están sustituidos con 1 a 6 sustituyentes, cada uno de ellos independientemente seleccionados del grupo que consiste en grupos R9 (fórmulas 3) en las cuales o ambos anillos anteriores de dichos grupos A están sustituidos con 1 a 6 sustituyentes cada uno independientemente seleccionado del grupo que consiste en grupos R9 (fórmulas 4) donde los anillos fenilo anteriores de dichos grupos A están sustituidos con 1 a 3 sustituyentes cada uno independientemente seleccionado del grupo que consiste en grupos R9; (fórmulas 5) y B está seleccionado del grupo que consiste en (fórmulas 6), n es 0 a 6; p es 1 a 5; X es O, NR18 o S; Z s 1 a 3; R2 está seleccionado del grupo que consiste en: H, OH, -C(O)OH, -SH, -SO2NR13R14, -NHC(O)R13, -NHSO2NR13R14, -NHSO2R13, -NR13R14, - C(O)NR13R14, -C(O)NHOR13, -C(O)NR13OH, -S(O2)OH, -OC(O)R13, un grupo funcional ácido heterocíclico no sustituido y un grupo funcional ácido heterocíclico sustituido; donde hay de 1 a 6 sustituyentes en dicho grupo funcional ácido heterocíclico sustituido, donde cada sustituyente está independientemente seleccionado del grupo que consiste en: grupos R9; cada R3 y R4 está independientemente seleccionado del grupo que consiste en H, ciano, halógeno, alquilo, alcoxi, cicloalquilo sustituido con 1 a 4 grupos alquilo donde cada grupo alquilo está independientemente seleccionado, cicloalquilo no sustituido, cicloalquilo sustituido con 1 a 4 grupos alquilo, -OH, -CF3, -OCF3, -NO2, -C(O)R13, -C(O)OR13, -C(O)NHR17, -C(O)NR13R14, - SO(t)NR13R14, -SO(t)R13, -C(O)NR13OR14, arilo no sustituido o sustituido, heteroarilo no sustituido o sustituido, fórmulas (7), en las cuales hay de 1 a 6 sustituyentes en dicho grupo arilo sustituido y cada sustituyente está independientemente seleccionado del grupo que consiste en: grupos R9, y donde hay de 1 a 6 sustituyentes en dicho grupo heteroarilo sustituido y cada sustituyente está independientemente seleccionado del grupo que consiste en: grupos R9; o R3 y R4 tomados conjuntamente con los átomos de C a los cuales están unidos en el sustituyente B fenilo (un compuesto de (fórmulas 6)), forman un anillo fusionado de la fórmula (8) en la cual Z1 o Z2 es un anillo heterocíclico saturado no sustituido o sustituido (preferiblemente un anillo heterocíclico de 4 a 7 miembros), donde dicho anillo Z1 o Z2 contiene opcionalmente un heteroátomo adicional seleccionado del grupo que consiste en: O, S y NR18; donde hay de 1 a 3 sustituyentes de dicho anillo Z1 o Z2, y cada sustituyente está, independientemente seleccionado del grupo que consiste en: alquilo, arilo, hidroxi, hidroxialquilo, alcoxi, alcoxialquilo, arilalquilo, fluoralquilo, cicloalquilo, cicloalquilalquilo, heteroarilo, heteroarilalquilo, amino, - C(O)OR15, -C(O)NR15R16, -SOtNR15R16, -C(O)R15, -SO2R15 con la condición de que R15 no sea H, -NHC(O)NR15R16, -NHC(O)OR15, halógeno y un grupo heterocicloalquenilo; cada R5 y R6 son iguales o diferentes y están independientemente seleccionados del grupo que consiste en: H, halógeno, alquilo, alcoxi, CF3, -OCF3, -NO2, -C(O)R13, -C(O)OR13, -C(O)NR13R14, -SO(t)NR13R14, -C(O)NR13OR14, ciano, arilo no sustituido o sustituido y un grupo heteroarilo no sustituido o sustituido; donde hay de 1 a 6 sustituyentes en dicho grupo arilo sustituido y cada sustituyente está independientemente seleccionado del grupo que consiste en: grupos R9; y donde hay de 1 a 6 sustituyentes de dicho grupo heteroarilo sustituido y cada sustituyente está independientemente seleccionado del grupo que consiste en grupos R9; cada R7 y R8 está independientemente seleccionado del grupo que consiste en H, alquilo no sustituido o sustituido, arilo no sustituido o sustituido, heteroarilo no sustituido o sustituido, arilalquilo no sustituido o sustituido, heteroarilalquilo no sustituido o sustituido, cicloalquilo no sustituido o sustituido, cicloalquilalquilo no sustituido o sustituido, -CO2R13, -CONR13R14, alquinilo, alquenilo y cicloalquenilo; y donde hay uno o más sustituyentes en dichos grupos sustituidos R7 y R8, donde cada sustituyente está independientemente seleccionado del grupo que consiste en: a) halógeno, b) -CF3, c) -COR13, d) -OR13, e) -NR13R14, f) -NO2, g) -CN, h) -SO2OR13, i) - Si(alquilo)3, donde cada alquilo está independientemente seleccionado, j) -Si(arilo)3, donde cada alquilo está independientemente seleccionado, k) -(R13)2R14Si, donde cada R13 está independientemente seleccionado, l) -CO2R13, m) -C(O)NR13R14, n) - SO2NR13R14, o) -SO2R13, p) -OC(O)R13, q) -OC(O)NR13R14, r) -NR13C(O)R14, y s) -NR13CO2R14; (fluoralquilo es un ejemplo no limitativo de un grupo alquilo que está sustituido con halógeno); R8a está seleccionado del grupo que consiste en: H, alquilo, cicloalquilo y cicloalquilalquilo; cada R9 está independientemente seleccionado del grupo que consiste en: a) R13, b) halógeno, c) -CF3, d) -COR13, e) -OR13, f) -NR13R14, g) -NO2, h) -CN, i) -SO2R13, j) -SO2NR13R14, k) -NR13COR14, l) -CONR13R14, m) - NR13CO2R14, n) -CO2R13, o) un compuesto de fórmula 9, p) alquilo sustituido con uno o más grupos -OH, q) alquilo sustituido con uno o más grupos -NR13R14, y r) -N(R13)SO2R14; cada R10 y R11 está independientemente seleccionado del grupo que consiste en R13, halógeno, -CF3, -OCF3, -NR13R14, -NR13C(O)NR13R14, -OH, -C(O)OR13, -SH, -SO(t)NR13R14, -SO2R13, -NHC(O)R13, -NHSO2NR13R14, -NHSO2R13, -C(O)NR13R14, -C(O)NR13OR14, -OC(O)R13 y ciano; R12 está seleccionado del grupo que consiste en: H, - C(O)OR13, arilo no sustituido o sustituido, heteroarilo no sustituido o sustituido, arilalquilo no sustituido o sustituido, cicloalquilo no sustituido o sustituido, alquilo no sustituido o sustituido, cicloalquilalquilo no sustituido o sustituido y heteroarilalquilo no sustituido o sustituido, donde hay de 1 a 6 sustituyentes en los grupos R12 sustituidos y cada sustituyente está independientemente seleccionado del grupo que consiste en: grupos R9; cada R13 y R14 está independientemente seleccionado del grupo que consiste en: H, alquilo no sustituido o sustituido, cianoalquilo no sustituido o sustituido, arilo no sustituido o sustituido, heteroarilo no sustituido o sustituido, arilalquilo no sustituido o sustituido, heteroarilalquilo no sustituido o sustituido, cicloalquilo no sustituido o sustituido, cianocicloalquilo no sustituido o sustituido, cicloalquilalquilo no sustituido o sustituido, heterocíclico no sustituido o sustituido, fluoralquilo no sustituido o sustituido y heterocicloalquilalquilo no sustituido o sustituido (donde "heterocicloalquilo" significa heterocíclico); donde hay de 1 a 5 sustituyentes en dichos grupos R13 y R14 sustituidos y cada sustituyente está independientemente seleccionado del grupo que consiste en; alquilo, -CF3, -OH, alcoxi, arilo, arilalquilo, fluoralquilo, cicloalquilo, cicloalquilalquilo, heteroarilo, heteroarilalquilo, -N(R40)2, -C(O)OR15, -C(O)NR15R16, -S(O)tNR15R16, -C(O)R15, halógeno, - NHC(O)NR15R16 y -SO2R15 con la condición de que R15 no sea H; y con la condición de que para las porciones cianoalquilo sustituido y cianocicloalquilo sustituido, el átomo de C al cual está unido el grupo ciano no tiene unido también a dicho átomo de C un sustituyente seleccionado del grupo que consiste en: -OH, alcoxi, -N(R40)2, halógeno y -NHC(O)NR15R16; o R13 y R14 tomados conjuntamente con el N al cual están unidos en los grupos -C(O)NR13R14 y -SO2NR13R14 forman un anillo heterocíclico saturado no sustituido o sustituido, donde dicho anillo contiene opcionalmente un heteroátomo adicional seleccionado del grupo que consiste en: O. S y NR18; donde hay de 1 a 3 sustituyentes en los grupos R13 y R14 ciclados sustituidos y cada sustituyente está independientemente seleccionado del grupo que consiste en; CN, alquilo, cianoalquilo, arilo, hidroxi, hidroxialquilo, alcoxi, alcoxialquilo, arilalquilo, fluoralquilo, cicloalquilo, cianocicloalquilo, cicloalquilalquilo, heteroarilo, heteroarilalquilo, amino, -C(O)OR15, -C(O)NR15R16, -SOtNR15R16, -C(O)R15, -SO2R15 (con la condición de que R15 no sea H), -NHC(O)NR15R16, -NHC(O)OR15, halógeno y un grupo heterocicloalquenilo; y con la condición de que el átomo de C al cual está unido el grupo ciano no tenga que estar también unido al dicho átomo de C un sustituyente seleccionado del grupo que consiste en: hidroxi, alcoxi, amino, halógeno, -NHC(O)NR15R16 y -NHC(O)OR15; cada R15 y R16 está independientemente seleccionado del grupo que consiste en H, alquilo, arilo, arilalquilo, cicloalquilo y heteroarilo; R17 está seleccionado del grupo que consiste en: -SO2alquilo, -SO2arilo, -SO2cicloalquilo y -SO2heteroarilo; R18 está seleccionado del grupo que consiste en: H, alquilo, arilo, heteroarilo, -C(O)R19, -SO2R19 y -C(O)NR19R20; cada R19 y R20 está independientemente seleccionado del grupo que consiste en: alquilo, arilo y heteroarilo; R30 está seleccionado del grupo que consiste en: cicloalquilo, -CN, - NO2, o -SO2R15 con la condición de que R15 no sea H; cada R31 está independientemente seleccionado del grupo que consiste en: alquilo no sustituido, arilo no sustituido o sustituido, heteroarilo no sustituido o sustituido y cicloalquilo no sustituido o sustituido ; donde hay de 1 a 6 sustituyentes en dichos grupos R31 sustituidos y cada sustituyente está independientemente seleccionado del grupo que consiste en: alq
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JP4939229B2 (ja) 2012-05-23
MY139808A (en) 2009-10-30
CN1918138B (zh) 2011-05-04
ES2308299T3 (es) 2008-12-01
CA2550189A1 (en) 2005-07-21
US20060223864A1 (en) 2006-10-05
JP2007514746A (ja) 2007-06-07
CN1918138A (zh) 2007-02-21
EP1694659B1 (en) 2008-08-27
US20080090823A1 (en) 2008-04-17
US7786149B2 (en) 2010-08-31
HK1087711A1 (en) 2006-10-20
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US7338968B2 (en) 2008-03-04
MXPA06007076A (es) 2006-08-31
ATE406356T1 (de) 2008-09-15

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