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AR049335A1 - Compuestos de morfolina sustituida para el tratamiento de trastornos del sistema nervioso central - Google Patents

Compuestos de morfolina sustituida para el tratamiento de trastornos del sistema nervioso central

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Publication number
AR049335A1
AR049335A1 ARP050101667A ARP050101667A AR049335A1 AR 049335 A1 AR049335 A1 AR 049335A1 AR P050101667 A ARP050101667 A AR P050101667A AR P050101667 A ARP050101667 A AR P050101667A AR 049335 A1 AR049335 A1 AR 049335A1
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Argentina
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alkyl
alkoxy
aryl
con
heterocycle
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Warner Lambert Co
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Application filed by Warner Lambert Co filed Critical Warner Lambert Co
Publication of AR049335A1 publication Critical patent/AR049335A1/es

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Abstract

Reivindicacion 1: Un compuesto de formula (1), y sales o derivados farmacéuticamente aceptables del mismo, donde: A es O o S; X es arilo, un heterociclo biciclo benzocondensado, -alquiloC1-10, -alqueniloC2-8, -cicloalquiloC5-8, -(CH2)n- cicloalquiloC3-9, cicloalquilo condensado, H, SCF3, hidroxi-alquiloC1-6, -alcoxiC1-6, -alcoxiC1-6-alcoxiC1-6, -(CH2)nS-alquiloC1-6, -(CH2)nSO2-alquiloC1-6; donde cada grupo está opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente entre -alquiloC1-6, -cicloalquiloC3-8, -alcoxiC1-6, arilo, heterociclo, OH, halo, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, -O(CH2)nCF3, -CN, -CONH2, -CON(H)alquiloC1-6, -CON(alquiloC1-6)2, hidroxi-alquiloC1-6, -alcoxiC1-4, - SCF3, SO2, -alquilC1-4-S-alquiloC1-4, -alquilC1-4-S-, -alquilC1-4-NR'R'', NR'R'', con la condicion de que cuando X sea fenilo, fenilo sustituido, alquilo C1-4 no sustituido, alquilo C1-4 sustituido con halo, cicloalquilo C3-8 no sustituido o cicloalquilo C3-8 sustituido con halo, entonces * y @ sean (R,S) o (S,R); R1-R5 se seleccionan independientemente entre H, -alquiloC1-6, arilo, -cicloalquiloC3-8, -alqueniloC1-6, cicloalquenilo C5-8, -(CH2)ncicloalquiloC3-8, -alcoxiC1-6, -O-arilo, heterociclo, SO2, OH, halo, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, -O(CH2)nCF3, -CN, -CONH2, -CON(H)alquiloC1-6, -CON(alquiloC1-6)2, hidroxi-alquiloC1-6, -alcoxiC1-4-alquiloC1-6, -SCF3, -alquilC1-6-SO2, -alquilC1-4-S-alquiloC1-4, -alquilC1-4-S-, alquilC1-4-NR'R'' y NR'R'' y cuando dos de los grupos R1-R5 se unen al anillo pueden formar un anillo bicíclico benzocondensado que comprende un grupo fenilo condensado con un anillo carbocíclico de 5 o 6 miembros o un grupo fenilo condensado con un grupo heterocíclico de 5 o 6 miembros que contiene al menos un heteroátomo N, O o S y donde cada uno de los grupos -alquiloC1-6, arilo, -cicloalquiloC3-8, -alqueniloC2-8, -cicloalquenilo C5-8, -alcoxiC1-6, -heterociclo puede estar opcionalmente sustituido con uno o más de los siguientes grupos: arilo, heterociclo, OH, halo, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, -O(CH2)nCF3, -CN, -CONH2, -CON(H)alquiloC1-6, -CON(alquilC1-6)2, hidroxi-alquiloC1-6, alcoxi C1-6, alquilo C1-6, -SCF3, - alquilC1-6-SO2, -alquilC1-4-S-alquiloC1-4-, -alquilC1-4-S-, -alquilC1-4-NR'R'' y NR'R''; R' y R'' son independientemente alquilo C1-6 o H; n es de 1 a 5; * indica un primer centro quiral; y @ indica un segundo centro quiral. Reivindicacion 5: Un compuesto de formula (2), y sales o derivados farmacéuticamente aceptables del mismo, donde: R1 y R6, R7 y R8 se seleccionan independientemente entre H, -alquiloC1-6, arilo, -cicloalquiloC3-8, -alqueniloC2-6, -cicloalquenilo C5-8, - (CH2)ncicloalquiloC3-9, -alcoxiC1-6, -O-arilo, heterociclo, -SO2, OH, halo, -CF3, -CHF2, -CH2F, OCF3, -OCHF2, -OCH2F, -O(CH2)nCF3, -CN, -CONH2, -CON(H)alquiloC1-6, -CON(alquiloC1-6)2, hidroxi-alquiloC1-6, -alcoxiC1-4-alquiloC1-6, -SCF3, -alquilC1-6- SO2, -alquilC1-4-S-alquiloC1-4, -alquilC1-4-S-, alquilC1-4-NR'R'' y NR'R'' y donde cada uno de los grupos -alquiloC1-6, arilo, -cicloalqueniloC3-8, -alqueniloC2-8; -cicloalquenilo C5-8, -alcoxiC1-6, arilo, heterociclo puede estar opcionalmente sustituidos con uno o más de los siguientes grupos: -alquiloC1-6, arilo, heterociclo, OH, halo, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, -O(CH2)nCF3, -CN, -CONH2, -CON(H)alquiloC1-6, -CON(alquilC1-6)2, hidroxi-alquiloC1-6, -alcoxi C1-6-alquilo C1- 6, -alcoxiC1-6, -SCF3, -alquilC1-6-SO2, -alquilC1-4-S-alquiloC1-4, -alquilC1-4-S-, -alquilC1-4-NR'R'' y NR'R''; R' y R'' son independientemente -alquiloC1-6 o H; n es de 1 a 5; R3 es H o F; R4 es H o F, sin embargo, cuando R3 es F, R4 no es F; R5 es H, halogeno, alquilo C1-6, alcoxi C1-6, -S-alquiloC1-6, -(CH2)n-O-(CH2)n-, -OCF3 o -SCF3; y * indica un primer centro quiral; y @ indica un segundo centro quiral con la condicion de que cuando R1 sea metilo, -O-metilo, -O-etilo, Cl y R3-R8 sea H, entonces * y @ sean (S,R) o (R,S) y además, cuando R1 es -O-metilo y R6-R8 son H, -O-metilo, Cl o metilo entonces * y @ son (S,R) o (R,S). Reivindicacion 9: Un compuesto de formula (1), y sales o derivados farmacéutica y/o veterinariamente aceptables del mismo, donde: A es O; Z es heteroarilo no fenilo seleccionado entre piridina, furano, tiofeno, naftaleno, naftiridina, pirazol, pirazina, pirimidina, tiazol, oxazol, isoxazol, triazol, tetrazol; o un anillo de fenilo condensado con un heterociclo que contiene N, O o S; donde cada uno de los heteroarilo puede estar opcionalmente sustituido con uno o más de los sustituyentes seleccionados independientemente entre heterociclo, -cicloalquiloC3-8, fenilo, -alqueniloC2-8, - cicloalqueniloC5-8, -(CH2)ncicloalquiloC3-9, -cicloalquiloC5-9 condensado, arilo, H, -SCF3, hidroxi-alquiloC1-6, -alcoxiC1-6, -O-arilo, -(CH2)nS-alquiloC1-6, -alquilC1-6-SO2, -(CH2)nSO2-alquiloC1-6, -alquilC1-6-S-, -alquilC1-4-NR'R'' o NR'R'', donde cualquiera de los grupos anteriores está opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente entre -alquiloC1-6, -cicloalquiloC3-8, -alcoxiC1-6, arilo sustituido o no sustituido, heterociclo, OH, halo, -CF3, -CHF2, - CH2F, -OCF3, -OCHF2, -OCH2F, -O(CH2)nCF3, -CN, -CONH2, -CON(H)alquiloC1-6, -CON(alquiloC1-6)2, hidroxi-alquiloC1-6, -SCF3, -alquilC1-6-SO2, -alquilC1-4-S-alquiloC1-4, -alquilC1-4-S-, alquilC1-4-NR'R'' y NR'R''; X es heterociclo, arilo, alquilo C1-8, -alqueniloC2-8, -cicloalquiloC5-8, biciclo benzocndensado, -cicloalquiloC3-8, -(CH2)n-cicloalquiloC3-8, -cicloalquiloC5-9 condensado, H, -SCF3, hidroxi-alquiloC1-6, -alcoxiC1-6, alquiloC1-6, -(CH2)nS-alquiloC1-6, -(CH2)nSO2-alquiloC1-6, donde cada grupo está opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente entre -alquiloC1-6, cicloalquilo C3-8, -alcoxiC1-6, arilo, heterociclo, OH, halo, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, -OCH2F, -O(CH2)nCF3, -CN, -CONH2, - CON(H)alquiloC1-6, -CON(alquiloC1-6)2, hidroxi-alquiloC1-6, -SCF3, -alquilC1-6-SO2, -alquilC1-4-S-alquiloC1-4, -alquilC1-4-S-, -alquilC1-4-NR'R'', NR'R''; R' y R'' son independientemente alquilo C16 o H; n es de 1 a 5; * indica un primer centro quiral; y @ indica un segundo centro quiral.
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BRPI0510453A (pt) 2007-10-30
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AU2005238296A1 (en) 2005-11-10
ZA200608628B (en) 2009-01-28
CA2564994A1 (en) 2005-11-10
PA8631301A1 (es) 2006-05-16
PE20060680A1 (es) 2006-08-11
KR100943555B1 (ko) 2010-02-22
MXPA06012505A (es) 2006-12-15
UY28876A1 (es) 2005-11-30
JP4185154B2 (ja) 2008-11-26
US7659394B2 (en) 2010-02-09
JP2008019267A (ja) 2008-01-31
JP2007535530A (ja) 2007-12-06
TNSN06348A1 (fr) 2008-02-22
GEP20084550B (en) 2008-11-25
US20050245519A1 (en) 2005-11-03
MA28555B1 (fr) 2007-04-03
TW200600506A (en) 2006-01-01
CN1950348A (zh) 2007-04-18
ECSP066962A (es) 2006-12-20
NL1028924C2 (nl) 2006-04-27
KR20070006881A (ko) 2007-01-11
CR8718A (es) 2007-07-24
EP1745029A1 (en) 2007-01-24
SV2006002098A (es) 2006-02-15
EA200601798A1 (ru) 2007-04-27
NO20065456L (no) 2007-01-04
AP2006003771A0 (en) 2006-10-31
IL178648A0 (en) 2007-02-11
GT200500097A (es) 2005-12-12

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