AR042085A1 - Compuestos de pirazina como moduladores de crf - Google Patents

Compuestos de pirazina como moduladores de crf

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Publication number
AR042085A1
AR042085A1 ARP030104275A ARP030104275A AR042085A1 AR 042085 A1 AR042085 A1 AR 042085A1 AR P030104275 A ARP030104275 A AR P030104275A AR P030104275 A ARP030104275 A AR P030104275A AR 042085 A1 AR042085 A1 AR 042085A1
Authority
AR
Argentina
Prior art keywords
heteroaryl
nrara
substituted
heterocycloalkyl
nrac
Prior art date
Application number
ARP030104275A
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English (en)
Original Assignee
Upjohn Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Application filed by Upjohn Co filed Critical Upjohn Co
Publication of AR042085A1 publication Critical patent/AR042085A1/es

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    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/12—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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Abstract

Se describen derivados de pirazina, composiciones farmacéuticas que los contienen y procedimientos para utilizarlos para tratar un trastorno o afección cuyo tratamiento puede efectuarse o facilitarse antagonizando un receptor de CRF, tal como un trastorno relacionado con la ansiedad o un trastorno afectivo. Reivindicación 1: Un compuesto de fórmula (1) o formas estereoisoméricas del mismo, o mezclas de formas estereoisoméricas del mismo, fármacos farmacéuticamente aceptables del mismo o formas de sal farmacéuticamente aceptables del mismo, en la que en la fórmula (1) X se selecciona de un grupo monocíclico modificado, arilcicloalquilo, arilcicloalquilo sustituido, heteroarilcicloalquilo, heteroarilcicloalquilo sustituido, arilheterocicloalquilo, arilheterocicloalquilo sustituido, heteroarilheterocicloalquilo o heteroarilheterocicloalquilo sustituido ( siendo el punto de unión N o C); el grupo monocíclico modificado se selecciona de cicloalquilo, arilo, heterocicloalquilo, heteroarilo que está sustituido con Y o (CRbRb)nZ, en la que Y se selecciona de -CN, -NO2, -C(O)Ra, -C(S)Ra, -C(O)ORa, -C(S)ORa, -C(O)NRaRa, -C(S)NRaRa, NRaC(O)Ra, NRaC(S)Ra, NRaC(O)NRaRa, NRaC(S)NRaRa, NRaC(O)ORa, -OC(O)Ra, -OC(S)Ra, -OC(O)NRaRa, -OC(S)NRaRa, S(O)mNRaRa, NRaS(O)mRa, arilo, arilo sustituido, heteroarilo, heteroarilo sustituido, heterocicloalquilo, heterocicloalquilo sustituido, cicloalquilo, cicloalquilo sustituido, ORc y NHRc; Z se selecciona de Y, ORa, NRaRa y S(O)mRa; Rb se selecciona independientemente de H, alquilo, arilo, heteroarilo, heterocicloalquilo o cicloalquilo opcionalmente sustituido con 1-5Rt; Rc se selecciona de arilo, heteroarilo, heterocicloalquilo o cicloalquilo opcionalmente sustituido con 1 a 5 Rt; n se selecciona de 1-6; y m se selecciona de 0, 1, y 2; Ar se selecciona de arilo, arilo sustituido, heteroarilo, heteroarilo sustituido; R1, R2 se seleccionan independientemente de H, halógeno, -NO2, -CN,-ORa, NRaRa, -C(O)Ra, -C(O)NRaRa, -C(S)NRaRa, -C(O)ORa, -C(S)ORa, S(O)mNRaRa, NRaS(O)mRa, NRaC(O)ORa, NRaC(O)Ra, NRaC(O)NRaRa, NRaC(S)NRaRa, y -OC(O)NRaRa, OC(O)Ra, OC(O)ORa, CRbRbZRf; Ra se selecciona independientemente de H, alquilo, cicloalquilo, haloalquilo, arilo, heteroarilo o heterocicloalquilo opcionalmente sustituido con 1 a 5 de Rt, oxo (=O), tiona (=S), fenilo, heteroarilo o heterocicloalquilo, estando opcionalmente sustituidos fenilo, heteroarilo y heterocicloalquilo con 1 a 5 independientemente tomados de Rt; Rf se selecciona independientemente de etilo, propilo, butilo, pentilo, cicloalquilo, haloalquilo, arilo, heteroarilo o heterocicloalquilo opcionalmente sustituido con 1 a 5 de Rt, oxo (=O), tiona (=S), fenilo, heteroarilo o heterocicloalquilo, estando opcionalmente sustituidos fenilo, heteroarilo y heterocicloalquilo con 1 a 5 independientemente tomados de Rt; Rt se selecciona independientemente de Rw, halógeno, -NO2, NRwRw, -ORw, -SRw, -CN, -C(O)NRwRw, -C(O)Rw, -OC(O)NRwRw, -OC(O)Rw, NRwC(O)Rw, NRwC(O)NRwRw, NRwC(O)ORw, S(O)mRwRw, NRwS(O)mRw, -S(O)2NRwRw, -NRwS(O)2NRwRw, y Rw se selecciona independientemente de H, alquilo, cicloalquilo, fenilo, bencilo, heteroarilo o heterociclo, estando opcionalmente sustituidos fenilo, bencilo, heteroarilo y heterocicloalquilo con alquilo o halógeno.
ARP030104275A 2002-11-21 2003-11-19 Compuestos de pirazina como moduladores de crf AR042085A1 (es)

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