AR057987A1 - Compuestos agonistas de cb1 (receptor cannabinoide) - Google Patents

Compuestos agonistas de cb1 (receptor cannabinoide)

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Publication number
AR057987A1
AR057987A1 ARP060105092A ARP060105092A AR057987A1 AR 057987 A1 AR057987 A1 AR 057987A1 AR P060105092 A ARP060105092 A AR P060105092A AR P060105092 A ARP060105092 A AR P060105092A AR 057987 A1 AR057987 A1 AR 057987A1
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AR
Argentina
Prior art keywords
alkyl
cycloalkyl
aryl
heteroaryl
haloalkoxy
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ARP060105092A
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English (en)
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Astrazeneca Ab
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Publication of AR057987A1 publication Critical patent/AR057987A1/es

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Abstract

Los compuestos de la formula (1) son utiles en tratamientos del trastorno gastrointestinal funcional, dispepsia, intestino irritable, dolor. Reivindicacion 1: Un compuesto de la formula (1), donde por lo menos uno de A1 y A2 es N, y si ambos no son N, entonces el otro es CH; R1 se selecciona de hidrogeno, ciano, halogeno, hidroxi, NR6R7, alquenilo C2-6, alquinilo C2-6, alquilo C1-9, cicloalquilo C3-6 y haloalcoxi C1-6, donde dichos alquenilo C2-6, alquinilo C2-6, alquilo C1-9, cicloalquilo C3- 6 o haloalcoxi C1-6 están opcionalmente sustituidos con hidroxi, NR6aR7a, cicloalquilo C3-6, arilo y heteroarilo; R2 se selecciona de hidrogeno, ciano, halogeno, hidroxi, NR6R7, alquenilo C2-6, alquinilo C2-6, alquilo C1-6, cicloalquilo C3-6 y haloalcoxi C1-6, donde dichos alquenilo C2-6, alquinilo C2-6, alquilo C1-6, cicloalquilo C3-6 o haloalcoxi C1-6 están opcionalmente sustituidos con hidroxi, NR6aR7a, cicloalquilo C3-6, arilo y heteroarilo; R3 se selecciona del grupo de formulas (2), y donde R3 está opcionalmente sustituido con halogeno, ciano, nitro, NR6R7, alquilo C1-6, cicloalquilo C3-6, alcoxi C1-6, haloalcoxi C1-6, arilo o heteroarilo, donde dichos alquilo C1-6, cicloalquilo C3-6, arilo o heteroarilo están opcionalmente sustituidos con halogeno, ciano, nitro, NR6R7, alquilo C1-6, cicloalquilo C3-6, alcoxi C1-6, haloalcoxi C1-6, arilo, heteroarilo o un sistema de anillo saturado que consiste en 4 a 7 átomos seleccionados de C, N y O, y donde dichos alquilo C1-6, cicloalquilo C3-6, arilo, heteroarilo o sistema de anillo están opcionalmente sustituidos con alquilo C1-4, y donde dicho alquilo C1-4 está opcionalmente sustituido con NR6R7, arilo, hidroxi o alcoxi C1-4; R4 se selecciona de hidrogeno y alquilo C1- 6; R5 se selecciona de alquilo C1-6, cicloalquilo C3-6, alcoxi C1-6, haloalcoxi C1-6 heteroarilo y arilo, donde dichos alquilo C1-6, cicloalquilo C3-6, heteroarilo o arilo están opcionalmente sustituidos con halogeno, ciano, nitro, NR6R7, alquilo C1- 6, cicloalquilo C3-6, alcoxi C1-6, haloalcoxi C1-6, arilo o heteroarilo; n se selecciona de 0, 1, 2, 3, 4 y 5; o R4 y R5 juntos forman un sistema de anillo saturado, insaturado o parcialmente saturado que consiste en 3 a 7 átomos seleccionados de C, O y N; o R4 y R5 juntos forman un sistema de anillo condensado saturado, insaturado o parcialmente saturado que consiste en 7 a 13 átomos seleccionados de C, O y N; donde dicho sistema de anillo está opcionalmente sustituido con halogeno, ciano, nitro, NR6R7, alquilo C1-6, cicloalquilo C3-6, alcoxi C1-6, haloalcoxi C1-6, arilo o heteroarilo, y donde dichos alquilo C1-6, cicloalquilo C3-6, arilo o heteroarilo están opcionalmente sustituidos con halogeno, ciano, nitro, NR6R7, alquilo C1-6, cicloalquilo C3-6, alcoxi C1-6, haloalcoxi C1-6, arilo o heteroarilo; R6, R6a, R7 y R7a se seleccionan de manera independiente de hidrogeno, alquilo C1-6, cicloalquilo C3-6, alcoxi C1-6, haloalcoxi C1-6, alquenilo C2-6, alquinilo C2-6, arilo y heteroarilo; o R6 y R7 juntos pueden formar un sistema de anillo saturado que consiste en 4 a 7 átomos seleccionados de C, O y N, donde el sistema de anillo está opcionalmente sustituido con alquilo C1-6, alcoxi C1-6, halogeno o hidroxi; donde uno o más átomos de carbono de cada grupo alquilo o cicloalquilo definido para R1 pueden estar sustituidos con O, NH, C(O), SO o SO2, donde ningun N u O está en una posicion adyacente a cualquier otro O o N, y donde ningun SO o SO2 está en una posicion adyacente a cualquier otro SO o SO2; donde uno o más átomos de carbono de cada grupo alquilo o cicloalquilo definido para R2, R3, R4, R5, R6, R6a, R7 y R7a pueden estar sustituidos con O, NH, C(O) o SO2, donde ningun N u O está en una posicion adyacente a cualquier otro O o N; donde uno o más átomos de carbono de cada grupo alquilo o cicloalquilo definido para R1, R2, R3, R4, R5, R6, R6a, R7 y R7a pueden estar sustituidos con fluor; y con la condicion de que R1 no sea hidrogeno, halogeno, ciano, acetilamino, hidroxi, alcoxi C1-6, alquilo C1-6, haloalcoxi C1-6, alquenilo C2-6, haloalquilo C1-6, haloalquenilo C2-6 o NR6R7; al mismo tiempo que R2 es hidrogeno, halogeno, ciano, acetilamino, hidroxi, alcoxi C1-6, alquilo C1-6, haloalcoxi C1-6, alquenilo C2-6, haloalquilo C1-6, haloalquenilo C2-6 o NR6R7; a menos que R3 esté sustituido con un alquilo C1-4, donde dicho alquilo C1-4 está sustituido con un heteroarilo, cicloalquilo C3-6, arilo o un sistema de anillo saturado que consiste en 4 a 7 átomos seleccionados de C, O y N, donde dicho heteroarilo, cicloalquilo C3-6 o arilo está adicionalmente sustituido con alquilo C1-4 o halogeno, donde dicho alquilo C1-4 está opcionalmente sustituido con NR6R7, arilo, hidroxi o alcoxi C1-4, y donde dicho sistema de anillo está opcionalmente sustituido con alquilo C1-4, donde dicho alquilo C1-4 está opcionalmente sustituido con NR6R7, arilo, hidroxi o alcoxi C1-4; o a menos que R3 se seleccione entre el grupo de formulas (3), opcionalmente sustituidos con halogeno, ciano, nitro, NR6R7, alquilo C1-6, cicloalquilo C3-6, alcoxi C1-6, haloalcoxi C1-6, arilo o heteroarilo; o una de sus sales aceptables para uso farmacéutico, o diastereomeros, enantiomeros o sus mezclas.
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