AR045218A1 - Aminas ciclicas inhibidoras de bace-1 que poseen una benzamida sustituyente; composiciones farmaceuticas que las contienen y su uso en la fabricacion de medicamentos para tratar enfermedades cognitivas o neurodegenerativas. - Google Patents

Aminas ciclicas inhibidoras de bace-1 que poseen una benzamida sustituyente; composiciones farmaceuticas que las contienen y su uso en la fabricacion de medicamentos para tratar enfermedades cognitivas o neurodegenerativas.

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AR045218A1
AR045218A1 ARP040102780A ARP040102780A AR045218A1 AR 045218 A1 AR045218 A1 AR 045218A1 AR P040102780 A ARP040102780 A AR P040102780A AR P040102780 A ARP040102780 A AR P040102780A AR 045218 A1 AR045218 A1 AR 045218A1
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Argentina
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alkyl
heterocycloalkyl
cycloalkyl
heterocycloalkylalkyl
cycloalkylalkyl
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Schering Corp
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Abstract

La presente revela composiciones farmacéuticas que comprenden los compuestos de fórmula (1), las cuales pueden ser utilizadas para tratar enfermedades cognitivas o neurodegenerativas tales como la enfermedad de Alzheimer, enfermedades cognitivas o neurodegenerativas que comprenden compuestos de fórmula (1) en combinación con un inhibidor de beta-secretasa diferente de aquellos de fórmula (19, un inhibidor de HMG-CoA reductasa, un inhibidor de gamma-secretasa, un agente anti-inflamatorio no esteroideo, un antagonista de los receptores de N-metil-D-aspartato, un inhibidor de colinesterasa o un anticuerpo anti-amiloide. Reivindicación 1: Un compuesto que posee la fórmula estructural (1), o una de sus sales o solvatos aceptables para uso farmacéutico, en el cual R1 es como se muestra en el grupo de fórmulas (2), R es -C(O)-N(R27)(R28) o como se muestra en la fórmula (3); R2 es H, alquilo, cicloalquilo, heterocicloalquilo, cicloalquilalquilo, heterocicloalquilalquilo, arilo, heteroarilo, arilalquilo, heteroarilalquilo, alquenilo o alquinilo; R3 es H o alquilo; R4 es H o alquilo; R5 es H, alquilo, cicloalquilo, cicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, heterocicloalquilo o heterocicloalquilalquilo; R14 es 1 es 4 sustituyentes seleccionados independientemente del grupo conformado por H, alquilo, alquenilo, alquinilo, halo, -CN, haloalquilo, cicloalquilo, cicloalquilalquilo, arilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, heterocicloalquilalquilo, -OR35, -N(R24)(R25) y -SR35; R27 y R28 se seleccionan independientemente de alquilo, cicloalquilo, cicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, heterocicloalquilo, heterocicloalquilalquilo, hidroxialquilo y alcoxialquilo; o R27 y R28 junto con el N al cual se encuentran unidos, forman un anillo heterocicloalquilo no sustituido de 3-7 miembros, o un anillo heterocicloalquilo de 3 a 7 miembros sustituido con 1-3 sustituyentes seleccionados independientemente del grupo conformado por alquilo, alcoxialquilo, haloalcoxialquilo, cicloalquilo, cicloalquilalquilo y cicloalquilalcoxialquilo; cada R29 se selecciona independientemente de H, alquilo, cicloalquilo, cicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, heterocicloalquilo, heterocicloalquilalquilo, hidroxialquilo, y alcoxialquilo; y en el cual l, n, m, Y, y R6, R7, R8, R9, R10, R11, R12 y R13 son según lo definido en los siguientes grupos (A) a (C): (A) cuando l es 0-3; n es 0-3; m es 0 o m es 1 e Y es-C(R30)(R31)-,y la suma de l y n es 0-3; (i) R6, R7, R8, R9, R10 y R11 se seleccionan independientemente del grupo conformado por H, alquilo, cicloalquilo, cicloalquilalquilo, arilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, heterocicloalquilalquilo, alquenilo, alquinilo, halo, -NO2, -CN, -N(R15)(R16), -OR17, -SR17, -C(O)R18, -N(R15)-C(O)R17, -C(O)OR17, -C(O)N(R15)(R16), -O-C(O)R17 y -S(O)1-2R18; y R12 y R13 se seleccionan independientemente del grupo conformado por H, alquilo, cicloalquilo, cicloalquilalquilo, arilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, heterocicloalquilalquilo, alquenilo, alquinilo, -C(O)R18 y -C(O)OR17; o (ii) R7 y R9, junto con los carbonos anulares a los cuales se encuentran unidos, forman un cicloalquilo fusionado o grupo heterocicloalquilo fusionado y R6, R8, R10, R11, R12 y R13 son según lo definido en (A)(i); o R10 y R11, junto con el C anular al cual se encuentran unidos, forman -C(O)-; O R12 y R13, junto con el C anular al cual se encuentran unidos, forman -C(O)-; o (iii) R6 y R7, junto con el C anular al cual se encuentran unidos, forman -C(=O)-, y R8, R9, R10, R11, R12 y R13 son según lo definido en (A)(i); o (iv) R8 y R9, junto con el C anular al cual se encuentran unidos, forman -C(=O)-, y R6, R7, R10, R11, R12 y R13 son según lo definido en (A)(i); (B) cuando l es 1; n es 0-2; y m es 0: R6 y R8, junto con los C anulares a los cuales se encuentran unidos, forman un grupo arilo fusionado o un grupo heteroarilo fusionado, R7 y R9 forman un enlace, y R10, R11, R12 y R13 son según lo definido en (A)(i); (C) cuando l es 0-3; n es 0-3; m es 1 y Y es -O-, -NR19-, -S-, -SO- o -SO2-; y la suma de l y n es 0-3; R6, R7, R8, R9; R12 y R13 se seleccionan independientemente del grupo conformado por H, alquilo, cicloalquilo, cicloalquilalquilo, arilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, heterocicloalquilalquilo, alquenilo, alquinilo, -C(O)N(R15)(R16), -C(O)R18, -C(O)OR17 y -O-C(O)R17; y R10 y R11 son según lo definido en (A)(i), o R10 y R!11, junto con el C anular al cual se encuentran unidos, forman -C(O)-; o R12 y R13, junto con el C anular al cual se encuentran unidos, forman -C(O)-; o cuando Y es -O- o -NR19-, R6 y R7, junto con el C anular al cual se encuentran unidos, forman -C(O)-; o cuando Y es -O- o -NR19-, R8 y R9, junto con el C anular al cual se encuentran unidos, forman -C(O)-; donde R15 es H o alquilo; R16 es H, alquilo, cicloalquilo, cicloalquilalquilo, arilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, heterocicloalquilalquilo, alquenilo o alquinilo; o R15 y R16, junto con el N al cual se encuentran unidos, forman un anillo heterocicloalquilo; R17 es H, alquilo, cicloalquilo, arilo, heteroarilo, cicloalquilalquilo, arilalquilo, heteroarilalquilo, heterocicloalquilo, heterocicloalquilalquilo, alquenilo o alquinilo o -N(R24)(R25); R19 es H, alquilo, cicloalquilo, cicloalquilalquilo, arilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, heterocicloalquilalquilo, -COR18, -C(O)OR40, -SOR18, -SO2R18 o -CN; R24 y R25 se seleccionan independientemente del grupo conformado por H, alquilo, cicloalquilo, cicloalquilalquilo, arilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, heterocicloalquilalquilo, alquenilo y alquinilo; o R24 y R25 junto con el N al cual se encuentran unidos, forman un anillo heterocicloalquilo de 3 a 7 miembros; R30 es H, alquilo, cicloalquilo, cicloalquilalquilo, arilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, heterocicloalquilalquilo, alquenilo, alquinilo, halo, -NO2, -CN, -N(R15)(R16), -OR17, -SR17, -C(O)R18, -N(R15)-C(O)R17, -C(O)OR17, -C(O)N(R15)(R16), -O-C(O)R17 y -S(O)1-2R18; R31 es H o alquilo; y donde cada uno de los grupos alquilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, heterocicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, alquenilo y alquinilo en los grupos R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R24, R25 y R30 son independientemente no sustituidos o sustituidos con 1 a 5 grupos R32 seleccionados independientemente del grupo conformado por halo, alquilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, heterocicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, -NO2, -CN, haloalquilo, haloalcoxi, -N(R33)(R34), -NH(cicloalquilo), aciloxi, -OR35, -SR35, -C(O)R36, -C(O)OR35, -PO(OR35)2, -NR35C(O)R36, -NR35C(O)OR39, -NR35S(O)0-2R39, y -S(O)0-2R39; o dos grupos R32 en el mismo átomo de C anular en cicloalquilo, cicloalquilalquilo, heterocicloalquilo o heterocicloalquilalquilo juntos forman =O; R33 y R34 se seleccionan independientemente del grupo conformado por H y alquilo; R35 es H, alquilo, cicloalquilo, arilo, heteroarilo, cicloalquilalquilo, arilalquilo, heteroarilalquilo, heterocicloalquilo, heterocicloalquilalquilo, alquenilo o alquinilo; R36 es H, alquilo, cicloalquilo, arilo, heteroarilo, cicloalquilalquilo, arilalquilo, heteroarilalquilo, heterocicloalquilo, heterocicloalquilalquilo, alquenilo, alquinilo o -N(R37)(R38); R37 y R38 se seleccionan independientemente del grupo conformado por H, alquilo, cicloalquilo, cicloalquilalquilo, arilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, heterocicloalquilalquilo, alquenilo y alquinilo; o R37 y R38 junto con el N al cual se encuentran unidos, forman un anillo heterocicloalquilo de 3 a 7 miembros; R39 es alquilo, arilo, heteroarilo, arilalquilo, heteroarilalquilo, heterocicloalquilo, heterocicloalquilalquilo, alquenilo o alquinilo; y R40 es alquilo, cicloalquilo, arilo, heteroarilo, cicloalquilalquilo, arilalquilo, heteroarilalquilo, heterocicloalquilo, heterocicloalquilalquilo, alquenilo o alquinilo.
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