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AR050279A1 - Indazoles como moduladores de lxr utiles en la preparacion de medicamentos pata el tratamiento de enfermedades cardiovasculares y mediadas por th1 y composiciones farmaceuticas que los contienen como principio activo. - Google Patents

Indazoles como moduladores de lxr utiles en la preparacion de medicamentos pata el tratamiento de enfermedades cardiovasculares y mediadas por th1 y composiciones farmaceuticas que los contienen como principio activo.

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Publication number
AR050279A1
AR050279A1 ARP050103205A ARP050103205A AR050279A1 AR 050279 A1 AR050279 A1 AR 050279A1 AR P050103205 A ARP050103205 A AR P050103205A AR P050103205 A ARP050103205 A AR P050103205A AR 050279 A1 AR050279 A1 AR 050279A1
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Argentina
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alkyl
optionally substituted
alkoxy
phenyl
halogen
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ARP050103205A
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Wyeth Corp
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Abstract

Estos compuestos son utiles para el tratamiento o inhibicion de las enfermedades mediadas por el LXR y por Th1. Reivindicacion 1: Un compuesto que tiene la formula (1) o (2) xaraxterizado porque: R1 es alquilo C1-6, CN, CO2R5, C(O)R5, alquenilo C2- 6, cicloalquenilo C3-8, alquinilo C2-6, NR5R6, C(O)NR5R6, fenilo, tiofeno, alcoxi C1-3, halogeno, o S(O)kR5; en donde: dicho alquilo C1-6 es opcionalmente substituido con desde 1 a 7 substituyentes seleccioandos independientemente del grupo que consiste en halogeno y OH; k es 0, 1 o 2; cada R5 y cada R6 es independientemente H, alquilo C1-6, cicloalquilo C3-8, S(O)2-alquilo o arilalquilo; o cada R5 y cada R6, forman independientemente, junto con el átomo de N al cual están unidos: un anillo saturado de 3 a 7 miembros que es opcionalmente substituido con alquilo C1-3, CH2OH, o C(=O)NH2; o un anillo de 3 a 7 miembros que contiene en su estructura central uno o dos heteroátomos adicionales que están opcionalmente substituidos con hasta tres substituyentes seleccionados del grupo que consiste de =O, alquilo C1-3, CO alquiloC1-6, y CO2alquilo C1-6; con la condicion de que cuando R1 es S(O)kR5, entonces dicho R5 de dicho S(O)kR5 no sea S(O)2-alquilo; R2 es alquilo C3-8, ciclaolquilo C3-8, alquenilo C2-8, cicloalquenilo C3-8, alquinilo C2-8, NR7R8, arilo, arilalquilo, heteroarilo, heteroarilalquilo o heterocicloalquilo, en donde dicho alquilo C3-8, dicho cicloalquilo C3-8 y dicho arilalquilo son cada uno opcionalmente ubstituidos con hasta cuatro substituyentes seleccionados independientemente del grupo que consiste de halogeno, CN y OR7, y en donde dicho heteoarilo es opcionalmente substituido con YD; o R2 es fenilo substituido con hasta cuatro substituyentes seleccionados independientemente a partir del grupo que consiste de alquilo C1-3, alquenilo C2-8, alquinilo C2-8, alcoxi C1-3, cicloalquilo C3-8, halogeno, OH, CH2OH, CN, NR7R8, N(R7)C(O)NR5R6, S(O)mR7, fenilo, NO2, C(O)R7, OC(O)R7, C(O)NR7R8, C(O)NR7D y YD, con la condicion de que cualquier grupo OH presente no esté en la posicion para, en donde: dicho alquilo C1-3 y dicho alcoxi C1-3 sean cada uno opcionalmente substituidos con desde 1 a 7 átomos de F; m es 0 a 2; y R5 y R6 son como se definion previamente; cada R7 y cada R8 es independientemente H o alquilo C1-3, o cada R7 y cada R8, junto con el átomo N al cual están unidos, formen independientemente: un anillo saturado de 3 a 7 miembros el cual está opcionalmente substituido con alquilo C1-3, CO2R14, CH2CO2R14, OCH2CO2R14, CH2OCH2CO2R14, C(O)NR14R15, CH2OH, o CH2CH2OH; o un anillo de 3 a 7 miembros que cotiene en su estructura central uno o más heteroátomos adicionales que están opcionalmente substituidos con CH2CO2R14; en donde R14 y R15 son cada uno independientemente H o alquilo C1-3; Y es un enlace, CH2, CH2CH2, alquiniloenilo C2-4, -O-, CH2OCH2, OCH2, CH2O, -N(R7)-, -N(COR7)-, S(O)j, -N(R7)CH2-, -N(R7)CONR8, -N(COR7)CH2-, S(O)jCH2, -CH2N(R7)CH2- , -CH2N(COR7)CH2-, -OCH2O-, -OC(R7)(CO2R8)- o -CH2S(O)jCH2-; en donde R7 y R8 están definidos previamente; y j es 0, 1 o 2; D es tetrahidronaftaleno, tetrahidronaftalol, tetralona, naftaleno, antraceno, bencilo o fenilo, cada uno de los cuales es opcionalmente substituido con hasta cinco grupos R seleccionados independientemente; cada R es independientemente seleccionado a partir del grupo que consiste de alquilo C1-6, alcoxi C1-3, halogeno, -C(=O)H, -C(O)-alquilo C1-3, CH2OH, CN, NH2, NO2, alquenilo C2-4, alquinilo C2-4, S(O)jR9, y WX; en donde dicho alquilo C1-6 y dicho alcoxi son cada uno opcionalmente substituidos con desde 1 a 7 átomos de F; y j es 0, 1 o 2; o D es un grupo heterocicloalquilo, heterocicloalquiloalquilo, heteroarilalquilo, heteroarilo o arilalquilo, cada uno de los cuales es opcionalmente substituido con hasta cuatro grupos Ra independientemente seleccionados; cada Ra es independientemente seleccionado a partir del grupo que consiste de alquilo C1- 8, fenilo, bencil, cicloalquilo C3-8, arilalquilo C7-11, alcoxi C1-3, halogeno, -C(=O)H, -C(O)-alquilo C1-3, CH2OH, CN, NO2, NH2, OH, =O, alquenilo C2-6, alquinilo C2-4, S(O)jR9 y WX; en donde dicho alquilo C1-8, dicho alquenilo C2-6, dicho alquinilo C2-4 y dicho alcoxi C1-3 son cada uno opcionalmente substituidos con desde 1 a 7 átomos de F; y j es 0, 1 o 2; W es un enlace, -CH2-, -CH2CH2-, -NR7-, -Q-N(R7)-, CHR8-, -(CHR8)2-, -CHR9-, -CR9R10-, -CO-, -O-, -CH2-, -OCHR9-, o -OCR9R10-; en donde R7 y R8 son como se definion previamente; y Q es alquiloenilo C1-6; cada r9 y cada R10 es independientemente alquilo C1-3 o OH; o cualquiera de R9 y R10, junto con el átomo al cual están unidos, pueden formar un anillo saturado de 3 a 7 miembros que contiene opcionalmente un átomo O, N o S; X es CO2R11, COR11, C(R11)2OH, CO2R5, C(O)NR5R6, NR5R&, QNR5CO2R6, OH, CH2OH, CN, SO2NR5R6, P(O)(OR5)(OR6), cicloalquiloalquilo, arilo, arilalquilo, heterocicloalquilo o heteroarilo, en donde. dicho arilo, dicho arilalquilo, dicho heterocicloalquilo y dicho heteroarilo son independientemente cada uno opcionalmente substituidos con hasta tres substituyentes seleccioandos a partir del grupo que consiste de alquilo C1-3, alcoxi C1-3, halogeno, H, OH, NO2 y bencilo que está opcionalmente substituido con hasta cinco átomos halogeno; en donde cada alquilo C1-3 y dicho alcoxi C1-3 están cada uno opcionalmente substituidos con desde 1 a 7 átomos de F; Q es alquilenilo C1-6; R11 es H o alquilo C1-6; y R5 y R6 son como se definio anteriormente; R3 es alquilo C1-8, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-8, cicloalquenilo C3-8, fenilo, o ZA, en donde: dicho fenilo es opcionalmente substituido con alquilo C1-3; Z es CH2, CH2CH2, o CH2O; A es bifenilo, bencilo, naftilo, piridilo, 8-quinolilo, cicloalquilo C3-8 o fenilo; en donde dicho fenilo es opcionalmente substituido con hasta cinco grupos R18 seleccionados independientemente; en donde cada uno de dichos R18 es independientemente seleccionado a partir del grupo que consiste de alquilo C1-6, alcoxi C1-3, halogeno, OH, NO2, CN, fenilo, pirrol-1-il, C(O)R12, CO2R12, NR12R13, C(O)NR12R13 y S(O)nR12; en donde cada alquilo C1-6 y dicho alcoxi C1-3 son cada uno opcionalmente substituidos con desde 1 a 7 átomos de F; n es 0, 1 o 2; y R12 y R13 son cada uno independientemente H o alquilo C1-3; R20 es h o alquilo C1-3; y R4 es H, halogeno, metilo o metoxi; con la condicion de que cuando el compuesto tiene la estructura (2), entonces R2 es fenilo o heteroarilo, cada uno de los cuales es substituido por YD, en donde YD es como se definio previamente; o una sal farmacéuticamente aceptable de los mismos.
ARP050103205A 2004-08-03 2005-08-01 Indazoles como moduladores de lxr utiles en la preparacion de medicamentos pata el tratamiento de enfermedades cardiovasculares y mediadas por th1 y composiciones farmaceuticas que los contienen como principio activo. AR050279A1 (es)

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