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(AZA-)ISOQUINOLINE DERIVATIVES
专利权人:
MERK PATENT GMBKH
发明人:
DORSH Diter (DE),ДОРШ Дитер (DE),BUKHSHTALLER Khans-Peter (DE),БУХШТАЛЛЕР Ханс-Петер (DE),DORSH Diter,ДОРШ Дитер,BUKHSHTALLER Khans-Peter,БУХШТАЛЛЕР Ханс-Петер
申请号:
RU2015107702
公开号:
RU0002654216C2
申请日:
2013.07.12
申请国别(地区):
RU
年份:
2018
代理人:
摘要:
FIELD: chemistry.SUBSTANCE: invention relates to the field of organic chemistry, namely to a heterocyclic compound selected from the group 3-[4-(1-hydroxy-1-methyl-ethyl)-phenyl]-2H-isoquinolin-1-one ("A3"), 6-fluoro-3-[4-(1-hydroxy-1-methyl-ethyl)-phenyl]-2H-isoquinolin-1-one ("A5"), 7-fluoro-3-[4-(1-hydroxy-1-methyl-ethyl)-phenyl]-2H-isoquinolin-1-one ("A6"), 3-[4-(1-hydroxy-1-methyl-ethyl)-phenyl]-7-methyl-2H-isoquinolin-1-one ("A7"), 3-(4-hydroxymethyl-phenyl)-2H-isoquinolin-1-one ("A8"), 7-fluoro-3-{4-[1-(2-hydroxy-ethoxy)-1-methyl-ethyl]-phenyl}-2H-isoquinolin-1-one ("A16"), 3-[4-(1-hydroxy-1-methyl-ethyl)phenyl]-2H-2,6-naphthyridin-1-one ("A23"), 3-[4-(1-hydroxy-1-methyl-ethyl) phenyl]-2H-2,7-naphthyridin-1-one ("A24"), 7-chloro-3-[4-(1-hydroxy-1-methyl-ethyl) phenyl]-2H-isoquinolin-1-one ("A25"), 8-fluoro-3-[4-(1-hydroxy-1-methyl-ethyl)phenyl]-2H-isoquinolin-1-one ("A27"), 5-fluoro-3-[4-(1-hydroxy-1-methyl-ethyl)phenyl]-2H-isoquinolin-1-one ("A28"), 5,7-difluoro-3-[4-(1-hydroxy-1-methyl-ethyl)-phenyl]-2H-isoquinolin-1-one ("A33"). Invention also relates to a medicament based on the above compound.EFFECT: technical result: new derivatives of isoquinoline and naphthyridine having inhibitory activity of tankyrase (TANK) and the activity of poly (ADP-ribose) polymerase PARP-1 and useful in the treatment of cancer have been obtained.4 cl, 3 tbl, 22 exИзобретение относится к области органической химии, а именно к гетероциклическому соединению, выбранному из группы 3-[4-(1-гидрокси-1-метил-этил)-фенил]-2H-изохинолин-1-она ("A3"), 6-фтор-3-[4-(1-гидрокси-1-метил-этил)-фенил]-2H-изохинолин-1-она ("A5"), 7-фтор-3-[4-(1-гидрокси-1-метил-этил)-фенил]-2H-изохинолин-1-она ("A6"), 3-[4-(1-гидрокси-1-метил-этил)-фенил]-7-метил-2H-изохинолин-1-она ("A7"), 3-(4-гидроксиметил-фенил)-2H-изохинолин-1-она ("A8"), 7-фтор-3-{4-[1-(2-гидрокси-этокси)-1-метил-этил]-фенил}-2H-изохинолин-1-она ("A16"), 3-[4-(1-гидрокси-1-метил-этил)фенил]-2H-2,6-нафтиридин-1-она ("A23"), 3-[4-(1-гидрок
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