AR048346A1 - Piridonas sustituidas como inhibidores de poli(adp-ribosa)-polimerasa (parp), composiciones farmaceuticas que las contienen y el uso de las mismas para el tratamiento de trastornos cardiovasculares y del sistema nervioso central. - Google Patents

Piridonas sustituidas como inhibidores de poli(adp-ribosa)-polimerasa (parp), composiciones farmaceuticas que las contienen y el uso de las mismas para el tratamiento de trastornos cardiovasculares y del sistema nervioso central.

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AR048346A1
AR048346A1 ARP050101225A ARP050101225A AR048346A1 AR 048346 A1 AR048346 A1 AR 048346A1 AR P050101225 A ARP050101225 A AR P050101225A AR P050101225 A ARP050101225 A AR P050101225A AR 048346 A1 AR048346 A1 AR 048346A1
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alkyl
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heterocycle
heteroaryl
aryl
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Aventis Pharma Inc
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Abstract

Piridonas sustituidas como inhibidores de poli-(ADP-Ribosa)-polimerasa PARP), estos compuestos son inhibidores de la poli(adenosina 5'-difosfato ribosa)-polimerasa (PARP) y, por tanto son utiles para preparar composiciones farmacéuticas para tratamiento y/o prevencion de una diversidad de enfermedades, incluyendo enfermedades asociadas con el sistema nervioso central, y trastornos cardiovasculares. Reivindicacion 1: Un compuesto, incluyendo los enantiomeros, estereoisomeros y tautomeros de dicho compuesto y sus sales farmacéuticamente aceptables, solvatos o derivados, teniendo dicho compuesto la estructura general que aparece en la formula (1) en a que: R es H o alquilo C1-6; R1 es alquilo C1-4, alquenilo C1-4, fluoroalquilo o fluoroalcoxi de formula CnHxFy u OCnHxFy, en las que n es un numero entero desde 1 a 4, x es un numero entero desde 0 a 8, y es un numero entero desde 1 a 9, y la suma de x e y es 2n+1, en la que dicho alquilo o alquenilo está opcionalmente sustituido con uno o más hidroxi o cloro; R2 es Ar-Y, en el que Ar es arilo, ariloílo o heteroarilo sustituidos o no sustituidos, en los que dichos sustituyentes se seleccionan del grupo que consiste en alquilo C1-4, alcoxi C1-4, alquenilo C1-4, fluoroalquilo o fluoroalcoxi de formula CnHxFy u OCnHxFy, en las que n es un numero entero desde 1 a 4, x es un numero entero desde 0 a 8, y es un numero entero desde 1 a 9, y la suma de x e y es 2n+1, -NO2, -CH2NH2, -NH2, - NH(alquilo C1-4, -N(alquilo C1-4)2, -CN, -C(O)R11, -NHC(O)(alquilo C1-4), -SO2Cl, -SO2(alquilo C1-4), halogeno e hidroxi e Y es H, -SO2NR5R6, -(CH2)nNR7R8, -CH=N-OR9, -C(O)NR7R8, -C(O)R9, -CH(OH)R9, -(CH2)nNHC(O)R9, -NHC(O)R9, -NHSO2R9 y - (CH2)nNHSO2R9; R3 es H, alquilo C1-4, alquenilo C1-4, fluoroalquilo o fluoroalcoxi de formula CnHxFy u OCnHxFy, en las que n es un numero entero desde 1 a 4, x es un numero entero desde 0 a 8, y es un numero entero desde 1 a 9, y la suma de x e y es 2n+1, en la que dicho alquilo o alquenilo está opcionalmente sustituido con uno o más hidroxi o Cl; R4 es alquilo C1-6, alquenilo C1-6, cicloalquilo C3-8, fluoroalquilo o fluoroalcoxi de formula CnHxFy u OCnHxFy, en las que n es un numero entero desde 1 a 4, x es un numero entero desde 0 a 8, y es un numero entero desde 1 a 9, y la suma de x e y es 2n+1, o R3 y R4 tomados conjuntamente con los átomos de C a los cuales están unidos forman un anillo cicloalquilo C4-8 o un anillo de benceno; R5, R6, R7 y R8 son los mismos o diferentes, y se seleccionan independientemente entre sí del grupo que consiste en H, alquilo C1-10 no sustituido y al menos monosustituido, cicloalquilo C3-8, (alcoxi C1-4)-alquilo C1-6, fluoroalquilo o fluoroalcoxi de formula CnHxFy u OCnHxFy, en las que n es un numero entero desde 1 a 4, x es un numero entero desde 0 a 8, y es un numero entero desde 1 a 9, y la suma de x e y es 2n+1,alquenilo C1-6, alquinilo C1-6, arilo, heteroarilo y heterociclo; en los que dichos sustituyentes se seleccionan del grupo que consiste en arilo, heteroarilo, heterociclo, -O-arilo, F, Cl, Br, -CF3, -OCF3, -NO2, -CN, -C(O)R11, -NHC(O)(alquilo C1-3), -NH2, hidroxi, alquilo C1-6, alcoxi C1-3, -NH(alquilo C1-3), -N(alquilo C1- 3)2, -SO2NH2, -SO2(alquilo C1-3) y -NH-SO2(alquilo C1-3); y el arilo, heterociclo y heteroarilo puede estar opcionalmente al menos monosustituido con F, Cl, Br, oxo, -CF3, -OCF3, -NO2, -CN, heteroarilo, -NHC(O)(alquilo 1-3), -COOH, hidroxi, alquilo C1-3, alcoxi C1-3, -SO2NH2, -SO2NH(alquilo C1-3), -SO2N(alquilo C1-3)2, -C(O)NH2, -C(O)NH(alquilo C1-3), -C(O)N(alquilo C1-3)2, -SO2(alquilo C1-3), -NH2, -NH(alquilo C1-3) o -N(alquilo C1-3)2; o R5 y R6 tomados conjuntamente con el átomo de N al que están unidos forman un heterociclo no sustituido o al menos monosustituido, o R7 y R8 tomados conjuntamente con el átomo de N al que están unidos forman un heterociclo no sustituido o al menos monosustituido, en los que dichos sustituyentes se seleccionan de arilo, heteroarilo, heterociclo, oxo, F, Cl, Br, -CF3, -OCFR3, -NO2, -CN, -C(O)R11, -NHC(O)(alquilo C1-3), -NH2, hidroxi,. alquilo C1-3, alcoxi C1-3, -NH(alquilo C1-3), -N(alquilo C1-3)2, -SO2NH2, -SO2(alquilo C1-3) y-NH-SO2(alquilo C1-3), y el arilo, heterociclo y heteroarilo puede estar opcionalmente al menos monosustituido con F, Cl, Br, hidroxi, alquilo C1-3 o alcoxi C1-3; R9 es H, alquilo C1-6, fenilo, heteroarilo o heterociclo no sustituidos o al menos monosustituidos; en los que dichos sustituyentes se seleccionan del grupo que consiste en F, Cl, Br, arilo, heterociclo, heteroarilo, -CF3, -OCF3, -NO2, -CN, -C(O)R11, -NHC(O)(alquilo C1-3), -NH2, hidroxi, alquilo C1-3, alcoxi C1-3, -N(alquilo C1-3), -N(alquilo C1-3)2, -SO2NH2, -SO2(alquilo C1-3) y -NH-SO2(alquilo C1-3); y el arilo, heterociclo y heteroarilo puede estar opcionalmente al menos monosustituido con F, Cl, Br, hidroxi, alquilo C1-3 o alcoxi C1-3; R11 es hidroxi, alcoxi C1-3, -O-fenilo, -NH2, - NH(alquilo C1-3), -N(alquilo C1-3)2 o fenilo; n es un numero entero desde 1 a 4; y en la que heteroarilo es un heterociclo mono- o bicíclico, aromático, de 5 a 10 miembros, que contiene uno o más heteroátomos seleccionados del grupo que consiste en N, O y S: arilo es un anillo mono- o bicíclico aromático de 6 a 10 miembros, y heterociclo es un heterociclo mono- o bicíclico, no aromático, de 3 a 10 miembros, que contiene uno o más heteroátomos seleccionados del grupo que consiste en N, O y S; y con la condicion de que: cuando Y y R son H, R3 y R4 son H o metilo, y R1 es metilo. Ar no es 4-metoxifenilo o 4-piridinilo; y cuando Y y R son H, R3 y R4 tomados conjuntamente con los átomos de C a los cuales están unidos forman un anillo de benceno, y R1 es metilo. Ar no es fenilo.
ARP050101225A 2004-03-30 2005-03-30 Piridonas sustituidas como inhibidores de poli(adp-ribosa)-polimerasa (parp), composiciones farmaceuticas que las contienen y el uso de las mismas para el tratamiento de trastornos cardiovasculares y del sistema nervioso central. AR048346A1 (es)

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US8173682B2 (en) 2012-05-08
PE20060285A1 (es) 2006-05-08
EP1732896B1 (en) 2012-12-12
CN1960975A (zh) 2007-05-09
JP2007531752A (ja) 2007-11-08
JP4913724B2 (ja) 2012-04-11
AU2005230901A1 (en) 2005-10-20
US20120202795A1 (en) 2012-08-09
IL178058A0 (en) 2006-12-31
KR20070010157A (ko) 2007-01-22
EP1732896A1 (en) 2006-12-20
US20070032489A1 (en) 2007-02-08
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