AR053109A1 - DERIVADOS DE PIPERIDINA Y PIPERAZINA, UN METODO PARA SU PREPARACION, COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN Y SU USO EN LA ELABORACIoN DE MEDICAMENTOS PARA EL TRATAMIENTO DE ENFERMEDADES MEDIADAS POR EL RECEPTOR DE QUIMIOQUINA CCR2. - Google Patents

DERIVADOS DE PIPERIDINA Y PIPERAZINA, UN METODO PARA SU PREPARACION, COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN Y SU USO EN LA ELABORACIoN DE MEDICAMENTOS PARA EL TRATAMIENTO DE ENFERMEDADES MEDIADAS POR EL RECEPTOR DE QUIMIOQUINA CCR2.

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AR053109A1
AR053109A1 ARP050105527A ARP050105527A AR053109A1 AR 053109 A1 AR053109 A1 AR 053109A1 AR P050105527 A ARP050105527 A AR P050105527A AR P050105527 A ARP050105527 A AR P050105527A AR 053109 A1 AR053109 A1 AR 053109A1
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Argentina
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ring
alkyl
heterocyclyl
atoms
group
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ARP050105527A
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Justin F Bowers
Jeffrey P Poyser
Paul Turner
David Waterson
Jon Winter
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Astrazeneca Ab
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=36084353&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR053109(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from GB0428327A external-priority patent/GB0428327D0/en
Priority claimed from GB0520325A external-priority patent/GB0520325D0/en
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR053109A1 publication Critical patent/AR053109A1/es

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Abstract

Un método de preparacion, composiciones farmacéuticas y usos en medicamentos de utilidad en el tratamiento de afecciones mediadas por quimioquinas C-C. Reivindicacion 1: Un compuesto de la formula (1) Q-L-W-C(=X)-Z-P caracterizado porque Q es una amina de la formula -N(R1)(R2) donde R1 y R2 se seleccionan independientemente entre H (con la condicion que R1 y R2 no sean ambos H), C1-6 alquilo, C3-7 cicloalquilo, C2-6 alquenilo, C2-6 alquinilo, cicloalquil-alquilo de hasta 14 átomos de anillos y cadenas, heterociclilo de hasta 7 átomos de anillos, heterociclilalquilo de hasta 14 átomos de anillos y cadenas, heterociclil-cicloalquilo de hasta 14 átomos de anillos, heterociclil-heterociclialquilo de hasta 20 átomos de anillos y cadenas, heterociclil-arlalquilo de hasta 20 átomos de anillos y cadenas, heterociclil-arilo de hasta 20 átomos de anillo; aril-alquilo de hasta 14 átomos de anillos y cadenas, aril-heterociclil-alquilo de hasta 20 átomos de anillos y cadenas, aril-oxi- alquilo de hasta 14 átomos de anillos y cadenas, aril-cicloalquilo de hasta 14 átomos de anillos, aril-arilalquilo de hasta 20 átomos de anillos y cadenas, donde cada cadena o anillo está, independientemente entre sí, sustituido opcionalmente con hasta 3 sustituyentes cada uno seleccionado independientemente entre halogeno, hidroxi, C1-6 alquilo, C1-4 alcoxi sustituido opcionalmente con C1-4 alcoxi, ciano, C1-4 alquilsulfonilo, trifluorometilo, carboxi, C1-4 alcoxicarbonilo, C1-2 alquiloxicarbonilfenilo, fenilo, NH2, NO2, =O, C1-4 alquilcarbonilo, C3-7 cicloalquil-heteroarilo de hasta 10 átomos de anillos y un átomo de N de un anillo heteroaromático puede estar sustituido con un grupo oxido, o R1 y R2 tomados juntos co el átomo de N de Q representan un anillo saturado de 4-7 miembros que comprende otro heteroátomo opcional seleccionado entre O, N o S y opcionalmente sustituido con hasta 3 sustituyentes cada uno de los cuales se selecciona independientemente entre los sustituyentes enumerados precedentemente; L es un ligador que comprende C1-6 alquilo, C1-6 alquilo-C4-10 cicloalquilo o C4-10 cicloalquil-C1-6-alquilo donde en cada caso el grupo alquilo y/o cicloalquilo puede comprender además 1, 2 o 3 heteroátomos seleccionados independientemente entre N, O S y/o un grupo =O; o tomados juntos con el átomo de N de la amina Q y R2, L representa un grupo heterociclilo o heterociclil-C1-6 alquilo, donde el grupo heterociclilo es de hasta 10 átomos de anillos y donde, además del átomo de N de la amina Q el grupo heterociclilo y/o alquilo puede comprender opcionalmente 1 o 2 heteroátomos adicionales seleccionados independientemente entre N, O S y/o un grupo =O; y donde cada cadena o anillo está independientemente entre sí, sustituido opcionalmente con hidroxi, halogeno o C1-4 alquilo; con la condicion que (i) cuando L es un grupo C5-7 cicloalquil-C1-6 alquilo definido precedentemente, entonces Q no es un anillo heterocíclico saturado que tiene dos heteroátomos de N y está sustituido o no sustituido sobre un heteroátomo de N del anillo con un grupo protector, y (ii) cuando L representa un grupo heterociclil C1-6 alquilo, definido precedentemente, y el grupo heterociclilo no comprende heteroátomos adicionales, entonces R1 no representa un heteroanillo saturado que tiene un solo heteroátomo de N y dicho anillo no está sustituido o posee un grupo protector sobre el heteroátomo de N; W es un anillo alifático de6 o 7 miembros que comprende los átomos de anillos Y1 y Y2 está ligado por Y1 e Y2 a los grupos L y C(=X), respectivamente, Y1 y Y2 se seleccionan independientemente entre N y C, y cuando Y1 e Y2 son ambos N o ambos C entonces W está sustituido opcionalmente en cualquier átomo del anillo con 1, 2 o 3 grupos R1 seleccionados independientemente entre sí o con un puente C2 entre dos átomos de C del anillo; y cuando Y1 es C e Y2 es N entonces Y1 está sustituido opcionalmente con hidroxi o halogeno, X es O, N, N-CN o S; Z es NR3, donde R3 es H o alquilo C1-4, o cuando Y2 es N entonces Z también puede ser O; P es un grupo arilo o heteroarilo C5-10 monocíclico o bicíclico de hasta 20 átomos de anillos, cada uno de los cuales está sustituido opcionalmente con 1, 2 o 3 sustituyentes seleccionados independientemente entre halogeno, C1-4alquilo, C2-4 alquenilo, C2-4 alquinilo, cano, trifluorometilo, trifluorometoxi, C1-4alcoxi, C1-4 alquiltio, trifluorometiltio, carboxi C1-4-alquilo y NO2; o P está sustituido opcionalmente con fenilo, fenoxi o aralquiloxi de hasta 10 átomos de C cada uno sustituido opcionalmente con 1 o 2 de cualquier otro sustituyente enumerado precedentemente para P; o una sal o solvato aceptable para uso farmacéutico del mismo. Reivindicacion 18:Un proceso para preparar un compuesto de acuerdo con la cláusula 1, o una sal o solvato aceptable para uso farmacéutico del mismo, caracterizado porque dicho proceso comprende: (i) hacer reaccionar un compuesto de la formula (2) (X)C-Z-P con un compuesto de la formula (3) Q-L-W o (ii) hacer reaccionar un compuesto de la formula (4) Q-L-W-C(X)-Z-P con un compuesto de la formula (5) Q donde Q, P, Z, -C(X), W y L(n) son como se definieron con relacion a la formula (1), excepto Q que es como se definio para la formula (4) donde comprende un grupo amino libre para su reaccion con Q' como una arte sustituyente de Q; y después, opcionalmente, comprende uno o más de los pasos (i), (ii) o (iii) en cualquier orden: (i) eliminar todos los grupos protectores; (ii) convertir el compuesto de la formula (1) en otro compuesto de la formula (1); (iii) formar una sal.
ARP050105527A 2004-12-24 2005-12-26 DERIVADOS DE PIPERIDINA Y PIPERAZINA, UN METODO PARA SU PREPARACION, COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN Y SU USO EN LA ELABORACIoN DE MEDICAMENTOS PARA EL TRATAMIENTO DE ENFERMEDADES MEDIADAS POR EL RECEPTOR DE QUIMIOQUINA CCR2. AR053109A1 (es)

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