AR051565A1 - DERIVADOS DE IMIDAZO[1, 2 - A]PIRIDINA; MÉTODOS PARA SU PREPARACIoN; COMPOSICIONES FARMACÉUTICAS QUE LOS CONTIENEN Y SU USO EN LA ELABORACIoN DE MEDICAMENTOS PARA EL TRATAMIENTO DE ENFERMEDADES E INFECCIONES POR VIH MEDIADAS POR CXCR4. - Google Patents

DERIVADOS DE IMIDAZO[1, 2 - A]PIRIDINA; MÉTODOS PARA SU PREPARACIoN; COMPOSICIONES FARMACÉUTICAS QUE LOS CONTIENEN Y SU USO EN LA ELABORACIoN DE MEDICAMENTOS PARA EL TRATAMIENTO DE ENFERMEDADES E INFECCIONES POR VIH MEDIADAS POR CXCR4.

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AR051565A1
AR051565A1 ARP050103666A ARP050103666A AR051565A1 AR 051565 A1 AR051565 A1 AR 051565A1 AR P050103666 A ARP050103666 A AR P050103666A AR P050103666 A ARP050103666 A AR P050103666A AR 051565 A1 AR051565 A1 AR 051565A1
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alkyl
independently
het
alkynyl
cycloalkyl
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Smithkline Beecham Corp
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Abstract

Compuestos que demuestran efectos protectores en las células objetivo de la infeccion de VIH en una manera a fin de unirse específicamente al receptor de quimioquina, y los cuales afectan la union del ligante natural o quimioquina a un receptor tal como CXCR4 y/o CCR5 de una célula objetivo. Métodos de preparacion y composiciones farmacéuticas que los contienen y su uso para la fabricacion de medicamentos para el tratamiento de la infeccion por VIH y otras patologías. Reivindicacion 1: Un compuesto de la formula (1), en donde: t es 0, 1 o 2; cada R independientemente es H, alquil, alquenil, alquinil, haloalquil, cicloalquil, -RaAy, -RaOR10, o -RaS(O)qR10; cada R1 independientemente es halogeno, haloalquil, alquil, alquenil, alquinil, cicloalquil, cicloalquenil, -Ay, -NHAy, -Het, -NHHet, -OR10, -OAy, -OHet, -RaOR10, -NR6R7, -RaNR6R7, -RaC(O)R10, -C(O)R10, -CO2R10, -RaCO2R10, -C(O)NR6R7, -C(O)Ay, -C(O)Het, -S(O)2NR6R7, -S(O)qR10, -S(O)qAy, ciano, nitro, o azido; n es 0, 1 o 2; R2 se selecciona de un grupo que consiste de H, alquil, haloalquil, cicloalquil, alquenil, alquinil, -RaAy, -RaOR5, -RaS(O)qR5, o -Racicloalquil, y en donde R2 no se sustituye con amina o alquilamina; cada R4 independientemente es halogeno, haloalquil, alquil, alquenil, alquinil, cicloalquil, cicloalquenil, -Ay, -NHAy, -Het, -NHHet, -OR10, -OAy, -OHet, -RaOR10, -NR6R7, -RaNR6R7, -RaC(O)R10, -C(O)R10, -CO2R10, -RaCO2R10, -C(O)NR6R7, -C(O)Ay, -C(O)Het, -S(O)2NR6R7, -S(O)qR10, -S(O)qAy, ciano, nitro, o azido; m es 0, 1 o 2; cada R5 independientemente es H, alquil, alquenil, alquinil, cicloalquil, o -Ay; p es 0 o 1; Y es -NR10-, -O-, -C(O)NR10-, -NR10C(O)-, -C(O)-, -C(O)O-, -NR10C(O)N(R10)-, -S(O)q-, -S(O)qNR10-, o -NR10S(O)q-; X es -N(R10)2, - RaN(R10)2, -AyN(R10)2, -RaAyN(R10)2, -AyRaN(R10)2, -RaAyRaN(R10)2, -Het, -RaHet, -HetN(R10)2, -RaHetN(R10)2, -HetRaN(R10)2, -RaHetRaN(R10)2, -HetRaAy, o HetRaHet; cada Ra independientemente es alquileno opcionalmente sustituido con uno o más de alquil, oxo o hidroxil, cicloalquileno opcionalmente sustituido con uno o más de alquil, oxo o hidroxil, alquenileno, cicloalquenileno o alquinileno; cada R10 independientemente es H, alquil, cicloalquil, alquenil, alquinil, cicloalquenil, - Racicloalquil, -RaOH, -RaOR5, -RaNR6R7, o -RaHet; cada uno de R6 y R7 independientemente se seleccionan de H, alquil, alquenil, alquinil, cicloalquil, cicloalquenil, -Racicloalquil, -RaOH, -RaOR5, -RaNR8R9, -Ay, -Het, -RaAy, -RaHet, o -S(O)qR5; cada uno de R8 y R9 independientemente se seleccionan de H o alquil; cada q independientemente es 0, 1 o 2; cada Ay independientemente representa un grupo aril opcionalmente sustituido; y cada Het independientemente representa un grupo heteroaril o heterociclil opcionalmente sustituido; o ésteres o sales farmacéuticamente aceptables de los mismos. Reivindicacion 58: El proceso para preparar un compuesto de la formula (1), en donde t es 1; cada R es H; cada R1 independientemente es halogeno, haloalquil, alquil, alquenil, alquinil, cicloalquil, cicloalquenil, -Ay, -NHAy, -Het, -NHHet, -OR10, -OAy, -OHet, -RaOR10, -NR6R7, -RaNR6R7, -RaC(O)R10, -C(O)R10, -CO2R10, -RaCO2R10, -C(O)NR6R7, -C(O)Ay, -C(O)Het, -S(O)2NR6R7, -S(O)qR10, -S(O)qAy, ciano, nitro, o azido; n es 0, 1 o 2; R2 se selecciona de un grupo que consiste de H, alquil, haloalquil, cicloalquil, alquenil, alquinil, -RaAy, -RaOR5, -RaS(O)qR5 o Racicloalquil; cada R4 independientemente es halogeno, haloalquil, alquil, alquenil, alquinil, cicloalquil, cicloalquenil, -Ay, -NHAy, -Het, -NHHet, -OR10, -OAy, -OHet, -RaOR10, -NR6R7, -RaNR6R7, -RaC(O)R10, -C(O)R10, -CO2R10, -RaCO2R10, -C(O)NR6R7, -C(O)Ay, -C(O)Het, -S(O)2NR6R7, -S(O)qR10, -S(O)qAy, ciano, nitro, o azido; m es 0, 1, o 2; cada R5 independientemente es H, alquil, alquenil, alquinil, cicloalquil, o -Ay; p es 0 o 1; Y es -NR10-, -O-, -C(O)NR10-, -NR10C(O)-, -C(O)-, -C(O)O-, -NR10C(O)N(R10)-, -S(O)q-, -S(O)qNR10-, o -NR10S(O)q-; X es -N(R10)2, - RaN(R10)2, -AyN(R10)2, -RaAyN(R10)2, -AyRaN(R10)2, -RaAyRaN(R10)2, -Het, -RaHet, -HetN(R10)2, -RaHetN(R10)2, -HetRaN(R10)2, -RaHetRaN(R10)2, -HetRaAy, o HetRaHet, cada Ra independientemente es alquileno opcionalmente sustituido con uno o más de alquil, oxo o hidroxil, cicloalquileno opcionalmente sustituido con uno o más de alquil, oxo o hidoxil, alquenileno, cicloalquenileno, o alquileno; cada R10 independientemente es H, alquil, cicloalquil, alquenil, alquinil, cicloalquenil, - Racicloalquil, -RaOH, -RaOR5, -RaNR6R7, o -RaHet; cada uno de R6 y R7 independientemente se seleccionan de H, alquil, alquenil, alquinil, cicloalquil, cicloalquenil, -Racicloalquil, -RaOH, -RaOR5, -RaNR8R9, -Ay, -Het, -RaAy, -RaHet, o -S(O)qR5; cada uno de R8 y R9 independientemente se seleccionan de H o alquil; cada q independientemente es 0, 1 o 2; cada Ay independientemente representa un grupo aril opcionalmente sustituido; y cada Het independientemente representa un grupo heteroaril o heterociclil opcionalmente sustituido; comprendiendo la etapa de reaccionar un compuesto de formula (2), en donde R1 y n es segun se define con respecto a la formula (1) con el compuesto de la formula (3), en donde R2, Ra, R4, R5, Y, X, p y m son segun se define con respecto a la formula (1) bajo condiciones de aminacion reductiva para formar un compuesto de la formula (1).
ARP050103666A 2004-09-02 2005-09-01 DERIVADOS DE IMIDAZO[1, 2 - A]PIRIDINA; MÉTODOS PARA SU PREPARACIoN; COMPOSICIONES FARMACÉUTICAS QUE LOS CONTIENEN Y SU USO EN LA ELABORACIoN DE MEDICAMENTOS PARA EL TRATAMIENTO DE ENFERMEDADES E INFECCIONES POR VIH MEDIADAS POR CXCR4. AR051565A1 (es)

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