AR049656A1 - Derivados de 2-alquil quinazolinona sustituidos como inhibidores de parp - Google Patents

Derivados de 2-alquil quinazolinona sustituidos como inhibidores de parp

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Publication number
AR049656A1
AR049656A1 ARP050102688A ARP050102688A AR049656A1 AR 049656 A1 AR049656 A1 AR 049656A1 AR P050102688 A ARP050102688 A AR P050102688A AR P050102688 A ARP050102688 A AR P050102688A AR 049656 A1 AR049656 A1 AR 049656A1
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AR
Argentina
Prior art keywords
radical
hydrogen
formula
alkanediyl
alkyloxy
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ARP050102688A
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English (en)
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Janssen Pharmaceutica Nv
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Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR049656A1 publication Critical patent/AR049656A1/es

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    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
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Abstract

Reivindicacion 1: Un compuesto de formula (1), sus formas de N-oxido, sales de adicion farmacéuticamente aceptables y formas estereoquímicamente isoméricas, donde: las líneas de puntos representan enlaces opcionales; X es >N-, >CH- o >CR2- donde R2 es aminocarbonilo; o cuando X es >CR2-, entonces R2 tomado junto con L-Z puede formar un radical bivalente de formula: -C(O)-NH-CH2NR10-; donde R10 es fenilo; -N==Y- es -N-C(O)- o -N=CR4-, donde R4 es hidroxi; R1 es hidrogeno, halo, alquiloxi C1-6 o alquilo C1-6; R3 es hidrogeno o alquiloxi C1-6; Z es un radical seleccionado de un resto de grupo de formulas (2) a (12), donde cada R5, R6, R7 y R8 está seleccionado, de manera independiente, a partir de hidrogeno, halo, amino, alquilo C1-6 o alquiloxi C1-6; o R7 y R8 tomados juntos pueden formar un radical bivalente de formulas: -CH2-CR92-O-; -(CH2)3-O-; -O-(CH2)2-O-; -CH=CH-CH=CH-; donde cada R9 está seleccionado de manera independiente a partir de hidrogeno o alquilo C1-6; y L es un radical bivalente seleccionado de -C(O)-, -C(O)-NH-, -C(O)-alcanodiilo C1-6- o -C(O)-O-alcanodiilo C1-6-; o L puede ser un enlace directo cuando X es >CR2- o cuando Z es un radical de formula (12); con la condicion de que cuando X es >CH-, -N==Y- es -N-C(O)-, la segunda línea de puntos no es un enlace, Z es un radical de formula (3) y L es -C(O)-, entonces -alcanodiilo C1-6- no es -CH2-CH2-.
ARP050102688A 2004-06-30 2005-06-29 Derivados de 2-alquil quinazolinona sustituidos como inhibidores de parp AR049656A1 (es)

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US (5) US8623872B2 (es)
EP (2) EP1763518B1 (es)
JP (2) JP4836946B2 (es)
KR (2) KR101184036B1 (es)
CN (2) CN1980899B (es)
AR (2) AR049656A1 (es)
AT (2) ATE498613T1 (es)
AU (2) AU2005259188B2 (es)
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SG (2) SG154435A1 (es)
TW (2) TWI361689B (es)
UA (2) UA86237C2 (es)
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AU2004295057B2 (en) 2003-11-20 2010-11-25 Janssen Pharmaceutica N.V. 7-phenylalkyl substituted 2-quinolinones and 2 quinoxalinones as poly(ADP-ribose) polymerase inhibitors
NZ551801A (en) 2004-06-30 2009-11-27 Janssen Pharmaceutica Nv Quinazolinedione derivatives as PARP inhibitors
US8623872B2 (en) 2004-06-30 2014-01-07 Janssen Pharmaceutica, Nv Quinazolinone derivatives as PARP inhibitors
ES2563954T3 (es) 2004-06-30 2016-03-16 Janssen Pharmaceutica Nv Derivados de ftalazina como inhibidores de PARP
WO2006047022A1 (en) 2004-10-25 2006-05-04 Virginia Commonwealth University Nuclear sulfated oxysterol, potent regulator of cholesterol homeostasis, for therapy of hypercholesterolemia, hyperlipidemia, and atherosclerosis
ZA200800907B (en) 2005-07-18 2010-04-28 Bipar Sciences Inc Treatment of cancer
CN101534836B (zh) 2006-09-05 2011-09-28 彼帕科学公司 Parp抑制剂在制备治疗肥胖症的药物中的用途
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