AR047329A1 - Derivados de quinolinas para el tratamiento de enfermedades cardiovasculares. composiciones farmaceuticas - Google Patents

Derivados de quinolinas para el tratamiento de enfermedades cardiovasculares. composiciones farmaceuticas

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AR047329A1
AR047329A1 ARP040104624A ARP040104624A AR047329A1 AR 047329 A1 AR047329 A1 AR 047329A1 AR P040104624 A ARP040104624 A AR P040104624A AR P040104624 A ARP040104624 A AR P040104624A AR 047329 A1 AR047329 A1 AR 047329A1
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phenyl
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Abstract

Los compuestos pertenecen a la categoría de los derivados de quinolinas utilizados en el tratamiento de enfermedades mediadas por LXR, particularmente enfermedades cardiovasculares. Composiciones farmacéuticas. Reivindicacion 1: Un compuesto de la formula (1), el cual tiene la estructura, en donde: R1 es -H o C1-3 alquilo; X1 es un enlace C1-5 alquilo, -C(O)-, -C(=CR8R9)-, -O-, -S(O)t-, -NR8-, -CR8R9-, -CHR23, -CR8(OR9)-, -C(OR8)2-, -CR8(OC(O)R9)-, -C=NOR9-, -C(O)NR8-, -CH2O-, -CH2S-, -CH2NR8- , -OCH2-, -SCH2-, -NR8CH2-, o una formula (2); R2 es H, es alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6, -CH2OH, arilalquilo C7-11, fenilo, naftilo, perfluoroalquilo C1-3, CN, C(O)NH2, CO2R12 o fenilo sustituido independientemente por uno o más de los grupos independientemente seleccionados de C1-3 alquilo, C2-4 alquenilo, C2-4 alquinilo, C1-3 alcoxi, C1-3 perfluoroalquilo, halogeno, -NO2, -NR8R9, -CN, -OH, y C1-3 alquilo sustituidos con 1 a 5 átomos de fluor, o R2 es un heterociclo seleccionado del grupo que consiste de piridina, tiofeno, bencisoxazol, benzotiofeno, oxadiazol, pirrol, pirazol, imidazol y furano, cada uno de los cuales pueden estar opcionalmente sustituido con uno a tres grupos independientemente seleccionados de C1-3 alquilo, C1-3 alcoxi, C1-3 perfluoroalquilo, halogeno, -NO2, -NR8R9, -CN, y C1-3 alquilo sustituidos con 1 a 5 átomos de fluor; X2 es un enlace o -CH2-; R3 es fenilo, naftilo, o fenilo o naftilo sustituido independientemente por uno a cuatro grupos independientemente seleccionados de C1-3 alquilo, hidroxi, fenilo, acilo, halogeno, -NH2, -CN, -NO2, C1-3 alcoxi, C1-3 perfluoroalquilo, C1-3 alquilo sustituidos con 1 a 5 átomos de fluor, NR14R15, -C(O)R10, -C(O)NR10R11, - C(O)NR11A, -C=CR8, -CH=CHR8, -WA, -C:::CA, -CH=CHA, -WYA, -WYNR11-A, -WYR10, -WY(CH2)jA, -WCHR11(CH2)jA, -W(CH2)jA, -W(CH2)jR10, -CHR11W(CH2)jR10, -CHR11W(CH2)jA, -CHR11NR12YA, -CHR11NR12YR10, pirrol, -W(CH2)jA(CH2)kD(CH2)pZ, - W(CR18R19)A(CH2)kD(CH2)pZ, -(CH2)jWA(CH2)kD(CH2)pZ, -CH=CHA(CH2)kD(CH2)pZ, -C:::CA(CH2)kD(CH2)pZ, -W(CH2)jC:::CA(CH2)kD(CH2)pZ, y -W(CH2)jZ, o R3 es un heterociclo seleccionado de piridina, pirimidina, tiofeno, furano, benzotiofeno, indol, benzofurano, bencimidazol, benzotiazol, benzoxazol, y quinolina, cada uno de los cuales pueden estar opcionalmente sustituido con uno a tres grupos independientemente seleccionados de C1-3 alquilo, C1-3 alcoxi, C1-3 hidroxi, fenilo, acilo, halogeno, -NH2, -CN, -NO2, C1-3 perfluoroalquilo, C1-3 alquilo sustituidos con 1 a 5 átomos de fluor, -C(O)R10, -C(O)NR10R11, -C(O)NR11A, -C=CR8, -CH=CHR8, -WA, -C:::CA, -CH=CHA, -WYA, -WYR10, -WY(CH2)jA, -W(CH2)jA, -W(CH2)jR10, -CHR11W(CH2)jR10, - CHR11W(CH2)jA, -CHR11NR12YA, -CHR11NR12YR10, -WCHR11(CH2)jA, -W(CH2)jA(CH2)kD(CH2)pZ, -W(CR18R19)A(CH2)kD(CH2)pZ, -(CH2)jWA(CH2)kD(CH2)pZ, -CH=CHA(CH2)kD(CH2)pZ, -C:::CA(CH2)kD(CH2)pZ, -W(CH2)jC:::CA(CH2)kD(CH2)pZ, y -W(CH2)jZ; W es un enlace, -O-, - S-, -S(O)-, -S(O)2-, -NR11-, o -N(COR12)-; Y es -CO-, -S(O)2-, -CONR13, -CONR13CO-, -CONR13SO2-, -C(NCN)-, -CSNR13, -C(NH)R13, o -C(O)O-; j es 0 a 3; k es 0 a 3; t es 0 a 2; D es un enlace, -CH=CH-, -C:::C-, -C=, -C(O)-, fenilo, -O-, -NH-, -S-, - CHR14-, -CR14R15-, -OCHR14-, -OCR14R15-, o -CH(OH)CH(OH)-; p es 0 a 3; Z es -CO2R11, -CONR10R11, -C(=NR10)NR11R12, -CONH2NH2, -CN, -CH2OH, -NR16R17, fenilo, CONHCH(R20)COR12, ftalimida, pirrolidin-2,5-diona, tiazolidin-2,4-diona, tetrazolil, pirrol, indol, oxazol, 2-tioxo-1,3-tiazolinin-4-ona, C1-7 aminas, C3-7 aminas cíclicas, o C1-3 alquilo sustituido con uno o dos grupos OH; en donde dicho pirrol está opcionalmente sustituido con uno o dos sustituyentes independientemente seleccionados del grupo que consiste de -CO2CH3, -CO2H, -COCH3, -CONH2 y -CN; en donde dichas C1-7 aminas están opcionalmente sustituidas con uno a dos sustituyentes independientemente seleccionados del grupo que consiste de -OH, halogeno, -OCH3, y -C:::CH; en donde dichos fenilo está opcionalmente sustituido con CO2R11, y en donde dicho C3-7 aminas cíclicas están opcionalmente sustituidas con uno o dos sustituyentes independientemente seleccionados del grupo que consiste de -OH, -CH2OH, C1-3 alquilo, -CH2OCH3, -CO2CH3, y -CONH2, y en donde dicho oxazol está opcionalmente sustituido con CH2CO2R11; A es fenilo, naftilo, tetrahidronaftilo, indano o bifenilo, cada uno de los cuales puede estar opcionalmente sustituido por uno a cuatro grupos independientemente seleccionados de halogeno, C1-3 alquilo, C2-4 alquenilo, C2-4 alquinilo, acilo, hidroxi, halogeno, -CN, -NO2, -CO2R11, -CH2CO2R11, fenilo, C1-3 perfluoroalcoxi, C1-3 perfluoroalquilo, -NR10R11, -CH2NR10R11, -SR11, C1-6 alquilo sustituidos con 1 a 5 átomos de fluor, C1-3 alquilo sustituido con 1 a 2 -OH grupos, C1-6 alcoxi opcionalmente sustituido con 1 a 5 átomos de fluor, o fenoxi opcionalmente sustituido con 1 a 2 CF3 grupos; o A es un heterociclo seleccionado de pirrol, piridina, pirridin-N-oxido, pirimidina, pirazol, tiofeno, furano, quinolina, oxazol, tiazol, imidazol, isoxazol, indol, benzo[1,3]-dioxol, benzo[1,2,5]-oxadiazol, isocromen-1-ona, benzotiofeno, benzofurano, 2,3-dihidrobenzo[1,4]-dioxina, bitienilo, quinazolin-2,4-91,3H]diona, y 3-H-isobenzofuran-1-ona, cada uno de los cuales puede estar opcionalmente sustituido por uno a tres grupos independientemente seleccionados de halogeno, C1-3 alquilo, acilo, hidroxi, -CN, -NO2, C1-3 perfluoroalquilo, -NR10R11, -CH2NR10R11, -SR11, C1-3 alquilo sustituidos con 1 a 5 átomos de fluor, C1-3 alcoxi opcionalmente sustituido con 1 a 5 átomos de fluor, R4, R5, y R6 son cada uno, independientemente, -H o -F; R7 es hidrogeno, C1-4 alquilo, C1-4 perfluoroalquilo, halogeno, -NO2, -CN, fenilo o fenilo sustituido con uno o dos grupos independientemente seleccionados de halogeno, C1-2 alquilo y OH; con la condicion de que si R7 es hidrogeno, entonces R3 es seleccionado de: a) fenilo sustituido por -W(CH2)jA(CH2)kD(CH2)pZ, -W(CR18R19)A(CH2)kD(CH2)pZ, -(CH2)jWA(CH2)kD(CH2)pZ, -CH=CHA(CH2)kD(CH2)pZ, -C:::CA(CH2)kD(CH2)pZ, o -W(CH2)jC:::CA(CH2)kD(CH2)pZ, en donde el residuo de fenilo está además opcionalmente sustituido con uno o más grupos independientemente seleccionados de C1-2 alquilo, C1-2 perfluoroalquilo, halogeno, y CN; y b) un heterociclo seleccionado de piridina, pirimidina, tiofeno, y furano, cada uno de los cuales está sustituido por uno de - W(CH2)jA(CH2)kD(CH2)pZ, -W(CR18R19)A(CH2)kD(CH2)pZ, -(CH2)jWA(CH2)kD(CH2)pZ, -CH=CHA(CH2)kD(CH2)pZ, -C:::CA(CH2)kD(CH2)pZ, o -W(CH2)jC:::CA(CH2)kD(CH2)pZ; además con la condicion que si X1R2 forma hidrogeno, entonces R3 es seleccionado de: a) fenilo sustituido por -W(CH2)jA(CH2)kD(CH2)pZ, -W(CR18R19)A(CH2)kD(CH2)pZ, -(CH2)jWA(CH2)kD(CH2)pZ, -CH=CHA(CH2)kD(CH2)pZ, -C:::CA(CH2)kD(CH2)pZ, o -W(CH2)jC:::CA(CH2)kD(CH2)pZ, en donde el residuo de fenilo está además opcionalmente sustituido con uno o más grupos independientemente seleccionados de C1-2 alquilo, C1-2 perfluoroalquilo, halogeno, y CN; y b) un heterociclo seleccionado de piridina, pirimidina, tiofeno, y furano, cada uno de los cuales está sustituido por uno de - W(CH2)jA(CH2)kD(CH2)pZ, -W(CR18R19)A(CH2)kD(CH2)pZ, -(CH2)jWA(CH2)kD(CH2)pZ, -CH=CHA(CH2)kD(CH2)pZ, -C:::CA(CH2)kD(CH2)pZ, o -W(CH2)jC:::CA(CH2)kD(CH2)pZ; además con la condicion que R3 y R7 no pueden ser ambos hidrogeno; cada R8 es independientemente -H, o C1-3 alquilo; cada R9 es independientemente -H, o C1-3 alquilo; cada R10 es independientemente -H, -OH, alcoxi C1-3, C1-7 alquilo, C3-7 alquenilo, C3-7 alquinilo, C3-7 cicloalquilo, -CH2CH2OCH3, 2-metil-tetrahidro-furano, 2- metil-tetrahidro-pirano, 4-metil-piperidina, morfolina, pirrolidina, o fenilo opcionalmente sustituido con uno o dos grupos alcoxi C1-3, en donde dicho C1-7 alquilo está opcionalmente sustituido con 1, 2 o 3 grupos independientemente seleccionados de C1-3 alcoxi, C1-3 tioalcoxi y CN; cada R11 es independientemente -H, C1-3 alquilo o R22; o R10 y R11, cuando están unidos al mismo átomo, junto a dicho átomo forman; un anillo saturado de 5 a 7 miembros, opcionalmente sustituido por 1 a 2 grupos independientemente seleccionados de C1-3 alquilo, OH y C1-3 alcoxi; o un anillo de 5 a 7 miembros que contiene 1 o 2 heteroátomos, opcionalmente sustituido por 1 a 2 grupos independientemente seleccionados de C1-3 alquilo, OH y C1-3 alcoxi; cada R12 es independientemente -H, o C1-3 alquilo; cada R13 es independientemente -H, o C1-3 alquilo; cada R14 y R15 es, independientemente, C1-7 alquilo, C3-8 cicloalquilo, C2-7 alquenilo, C2-7 alquinilo, -OH, -F, C7-14 arilalquilo, en donde dicho arilalquilo está opcionalmente sustituido con 1 a 3 grupos independientemente seleccionados de NO2, C1-6 alquilo, C1-3 perhaloalquilo, halogeno, CH2CO2R11, fenilo y C1-3 alcoxi, o R14 y R15 junto con el átomo al cual ellos están unidos pueden formar un alilo saturado de 3 a 7 miembros; cada R16 y R17 es, independientemente, hidrogeno, C1-3 alquilo, C1-3 alquenilo, C1-3 alquinilo, fenilo, bencilo o C3-8 cicloalquilo, en donde dicho C1-3 alquilo está opcionalmente sustituido con un grupo OH, y en donde dicho bencilo está opcionalmente sustituido con 1 a 3 grupos seleccionados de C1-3 alquilo y C1-3 alcoxi; o R16 y 17, junto con el átomo al cual ellos están unidos, pueden formar un heterociclo de 3 a 8 miembros el cual está opcionalmente sustituido con uno o dos sustituyentes independientemente seleccionados del grupo que consiste de C1-3 alquilo, -OH, CH2OH, -CH2OCH3, -CO2CH3, y -CONH2; cada R18 y R19 es, independientemente, C1-3 alquilo; cada R20 es independientemente H, fenilo, o la cadena lateral de un alfa aminoácido que existe de manera natural; cada R22 es independientemente arilalquilo opcionalmente sustituido con CH2COOH; y cada R23 es fenilo; o una sal farmacéuticamente aceptable de lo mismo.
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