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Phthalazine derivatives as PARP inhibitors
专利权人:
Janssen Pharmaceutica NV
发明人:
MEVELLEC, Laurence Anne,KENNIS, Ludo Edmond Josephine,MERTENS, Josephus Carolus,VAN DUN, Jacobus Alphonsus Josephus,SOMERS, Maria Victorina Francisca,WOUTERS, Walter Boudewijn Leopold
申请号:
ES05761151
公开号:
ES2563954T3
申请日:
2005.06.28
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
A compound of formula (I), ** Formula ** an N-oxide form, a pharmaceutically acceptable addition salt or a stereochemically isomeric form thereof, in which n is 0, 1, 2 or 3, and when n is 0, then a direct link is planned; Q is -C (>; = O) -; X is -CH <;and Y is -N <;or -NH-; or X is -N <;and Y is -CH <;or -CH2-; L1 is a direct link or -NH-; L2 is a direct bond or a bivalent radical selected from -C 1-6 alkanediyl-, C2-6 alkanediyl-, carbonyl or -C 1-6 alkanediyl- substituted with a substituent selected from hydroxy or aryl; R1 is hydrogen, nitro, halo or amino; R2 is hydrogen, C1-6 alkyl or aryl-C1-6 alkyl; the central rest can also be bridged (that is, forming a bicyclic moiety) with an ethylene bridge; Z is hydrogen, hydroxy, C1-6 alkyl, C1-6 alkyl-oxy, aryloxy, amino, cyano, aryl-C1-6-amino alkyl or benzothiazolyl (C1-6 alkyl) amino or an annular system selected from ** Formula ** in which R4 and R5 are each independently selected from hydrogen, halo, C1-6 alkyl, C1-6-oxy alkyl or trihalomethyl; aryl is phenyl, or phenyl substituted with one or two substituents each independently selected from halo, C1-6 alkyl or C1-6 alkyl; with the proviso that when Q is -C (>; = O) - and X is -N <;and Y is -CH <;or -CH2- and L1 is a direct link and L2 is a direct link, or the bivalent radical - C 1-6 alkanediyl or C 1-6 alkanediyl substituted with hydroxy, and R 1 is hydrogen, and R 2 is hydrogen or C 1-6 alkyl, then Z is other than hydrogen, hydroxy or C 1-6 alkyl; and with the proviso that the following compounds are excluded ** Formula **Un compuesto de fórmula (I),**Fórmula** una forma de N-óxido, una sal de adición farmacéuticamente aceptable o una forma estereoquímicamente isomérica del mismo, en la que n es 0, 1, 2 o 3, y cuando n es 0, entonces está previsto un enlace directo; Q es -C(>;=O)-; X es -CH<; e Y es -N<; o -NH-; o X es -N<; e Y es -CH<; o -CH2-; L1 es un enlace directo o -NH-; L2 es un enlace directo o un radical bivalente seleccio
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中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/
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