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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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Application number
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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    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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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) JP4969443B2 (es)
KR (2) KR101286969B1 (es)
CN (2) CN1980899B (es)
AR (2) AR049656A1 (es)
AT (2) ATE498613T1 (es)
AU (2) AU2005259188B2 (es)
BR (2) BRPI0512797A (es)
CA (2) CA2568835C (es)
DE (1) DE602005026391D1 (es)
EA (2) EA012837B1 (es)
ES (2) ES2380702T3 (es)
IL (2) IL180382A (es)
MX (2) MXPA06014933A (es)
MY (2) MY140572A (es)
NO (2) NO339883B1 (es)
NZ (2) NZ551680A (es)
SG (2) SG154435A1 (es)
TW (2) TWI361689B (es)
UA (2) UA86237C2 (es)
WO (2) WO2006003146A1 (es)
ZA (2) ZA200610772B (es)

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AU2004295058B9 (en) 2003-11-20 2011-06-30 Janssen Pharmaceutica N.V. 6-alkenyl and 6-phenylalkyl substituted 2-quinolinones and 2-quinoxalinones as poly(ADP-ribose) polymerase inhibitors
MXPA06014933A (es) 2004-06-30 2007-02-28 Janssen Pharmaceutica Nv Derivados de 2-alquil quinazolinona sustituidos como inhibidores de poli(adp-ribosa) polimerasa-1.
EA011552B1 (ru) 2004-06-30 2009-04-28 Янссен Фармацевтика Н.В. Производные хиназолиндиона в качестве ингибиторов parp
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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
RU2447889C2 (ru) 2005-07-18 2012-04-20 Бипар Сайенсиз, Инк. Способ лечения рака (варианты)
CA2662337A1 (en) 2006-09-05 2008-03-13 Bipar Sciences, Inc. Inhibition of fatty acid synthesis by parp inhibitors and methods of treatment thereof
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EP2134691B1 (en) 2007-03-08 2012-01-25 Janssen Pharmaceutica, N.V. Quinolinone derivatives as parp and tank inhibitors
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