AR072318A1 - Compuestos de diarilo, composiciones farmaceuticas que los comprenden y su uso en el tratamiento de enfermedades mediadas por el antagonismo del receptor opioide kappa. - Google Patents

Compuestos de diarilo, composiciones farmaceuticas que los comprenden y su uso en el tratamiento de enfermedades mediadas por el antagonismo del receptor opioide kappa.

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Publication number
AR072318A1
AR072318A1 ARP090102359A ARP090102359A AR072318A1 AR 072318 A1 AR072318 A1 AR 072318A1 AR P090102359 A ARP090102359 A AR P090102359A AR P090102359 A ARP090102359 A AR P090102359A AR 072318 A1 AR072318 A1 AR 072318A1
Authority
AR
Argentina
Prior art keywords
alkyl
ring
halogen
substituted
membered
Prior art date
Application number
ARP090102359A
Other languages
English (en)
Inventor
Hayardy
Mchardy
Mclean
Parikh
Verhoest
Original Assignee
Pfizer
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Filing date
Publication date
Application filed by Pfizer filed Critical Pfizer
Publication of AR072318A1 publication Critical patent/AR072318A1/es

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    • C07D211/10—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
    • C07D211/14—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
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Abstract

Su uso para tratamiento de enfermedades, afecciones y/o trastornos mediados por receptores opioides k (KOR), se proveen además, composiciones farmacéuticas que comprenden a estos compuestos. Reivindicacion 1: Un compuesto caracterizado porque es de formula (1) o una sal farmacéuticamente aceptable del mismo, en la que R1 es alquilo C1-6, alquil C2-4-O-alquilo C1-2, un anillo carbocíclico bicíclico puenteado de 7, 8 o 9 miembros, un anillo carbocíclico bicíclico condensado, fenilo-(CH2)a, heteroarilo-(CH2)a o heterocicloalquilo-(CH2)a, en el que el anillo puenteado, el anillo condensado, fenilo, heteroarilo o heterocicloalquilo está no sustituido o sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente de halogeno, OH, alquilo C1-3, O-alquilo C1-3, NH2, NH-alquilo C1-3, o N(alquilo C1-3)2; R2 es H o alquilo C1-4; o R1 y R2 se toman conjuntamente con el nitrogeno al que están unidos para formar un anillo de N mono o bicíclico, en el que dicho anillo de N es un anillo heterocicloalquilo mono-cíclico de 4 a 7 miembros; un anillo heterocíclico bicíclico condensado; o un anillo heterocíclico bicíclico puenteado de 7, 8 o 9 miembros, en el que dicho anillo de N está no sustituido o sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente de halogeno, OH, -CN, alquilo C1-3, alquil C1-3-OH, O-alquilo C1-3, alquil C1-3-O-alquilo C1-3, NH2, NH-alquilo C1-3, o N(alquilo C1-3)2; a es 0, 1 o 2; R3 es H, o alquilo C1-3 o cuando X1 o X3 es >(C(R8))-, R3 se puede tomar conjuntamente con R8 de uno de X1 o X3 y los átomos de carbono a los que están unidos forman un anillo de 5 o 6 miembros saturado, o parcialmente saturado, en el que un átomo de carbono en dicho anillo de 5 o 6 miembros pueden ser un heteroátomo seleccionado de -O-, -N(H)-, -N(alquilo C1-3)-, y >N-, y en el que dicho anillo está no sustituido o sustituido donde la valencia permite 1 sustituyente seleccionado de halogeno, -CN o alquilo C1-3; R4 es H, halogeno, CN, alquilo C1-3, o O-alquilo C1-3; R5 es H, halogeno, CN, alquilo C1-3, o O-alquilo C1-3; R6 es alquilo C1-4, o alquil C2-4-O-alquilo C1-2; R7 es H, o alquilo C1-4; o R6 y R7 se toman conjuntamente con el nitrogeno al que están unidos para formar un anillo de SN mono- o bicíclico, en el que dicho anillo de SN es un anillo heterocíclico mono-cíclico de 4 a 7 miembros que contiene 0 o 1 heteroátomo adicional seleccionado de O, NH, o N-alquilo C1-3, o un anillo heterocíclico bicíclico puenteado de 7, 8 o 9 miembros, en el que dicho anillo de SN está no sustituido o sustituido con 1 o 2 sustituyentes seleccionados independientemente de halogeno, OH, -CN, alquilo C1-3, alquil C1-3-OH, O-alquilo C1-3, alquil C1-3-O-alquilo C1-3, NH2, NH-alquilo C1-3, o N(alquil C1-3)2; X1, X2, X3, X4, X5 y X6 son independientemente >(C(R8))- o >N-; y cada R8 es independientemente H, halogeno, -CN, -alquilo C1-3, -O-alquilo C1-3, a condicion de que cuando X1 o X3 es >(C(R8))-, un R8 de X1 o X3 puede tomarse conjuntamente con R3 y los átomos de carbono a los que están unidos forman dicho anillo de 5 o 6 miembros saturado, o parcialmente saturado.
ARP090102359A 2008-06-25 2009-06-25 Compuestos de diarilo, composiciones farmaceuticas que los comprenden y su uso en el tratamiento de enfermedades mediadas por el antagonismo del receptor opioide kappa. AR072318A1 (es)

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EP2321011A1 (en) 2011-05-18
US20100035873A1 (en) 2010-02-11
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