Quinazolinone derivatives as PARP inhibitors

摘要

Compounds of the formula I;
in which R1, R2, R3, X1, X2 and Y have the meanings indicated in Claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.

主权项

1. A compound, which is one of the following compoundsNo.Name“A1”6-fluoro-2-[4-(1-hydroxy-1-methyl-ethyl)-phenyl]-3H-quinazolin-4-one“A2”2-[4-(1-hydroxy-1-methyl-ethyl)-phenyl]-8-methoxy-3H-quinazolin-4-one“A3”8-fluoro-2-[4-(1-hydroxy-1-methyl-ethyl)-phenyl]-3H-quinazolin-4-one“A4”5-fluoro-2-[4-(1-hydroxy-1-methyl-ethyl)-phenyl]-3H-quinazolin-4-one“A5”6-chloro-2-[4-(1-hydroxy-1-methyl-ethyl)-phenyl]-3H-quinazolin-4-one“A6”8-chloro-2-[4-(1-hydroxy-1-methyl-ethyl)-phenyl]-3H-quinazolin-4-one“A7”6-fluoro-2-{4-[1-(2-hydroxy-ethoxy)-1-methyl-ethyl]-phenyl}-3H-quinazolin-4-one“A8”6-fluoro-2-{4-[1-(2-methoxy-ethoxy)-1-methyl-ethyl]-phenyl}-3H-quinazolin-4-one“A9”2-(4-tert-butyl-phenyl)-6-fluoro-3H-quinazolin-4-one“A10”6-fluoro-2-[4-(4-methyl-piperazin-1-yl)-phenyl]-3H-quinazolin-4-one“A11”6,8-difluoro-2-[4-(1-hydroxy-1-methyl-ethyl)phenyl]-3H-quinazolin-4-one“A12”5,6-difluoro-2-[4-(1-hydroxy-1-methyl-ethyl)phenyl]-3H-quinazolin-4-one“A13”6-fluoro-2-[5-(1-hydroxy-1-methyl-ethyl)-2-pyridyl]-3H-quinazolin-4-one“A14”2-[4-(1-ethyl-1-hydroxy-propyl)phenyl]-6-fluoro-3H-quinazolin-4-one“A15”6-fluoro-2-[4-(2-methyltetrahydrofuran-2-yl)phenyl]-3H-quinazolin-4-one“A16”6-fluoro-2-[4-(1-hydroxycyclopentyl)phenyl]-3H-quinazolin-4-one“A17”6-fluoro-2-[4-(3-hydroxyoxetan-3-yl)phenyl]-3H-quinazolin-4-one“A18”2-[4-[1-(2-aminoethoxy)-1-methyl-ethyl]phenyl]-6-fluoro-3H-quinazolin-4-one“A19”6-fluoro-2-[4-(4-piperidyl)phenyl]-3H-quinazolin-4-one“A20”6-fluoro-2-[4-(1-methyl-4-piperidyl)phenyl]-3H-quinazolin-4-one“A21”6-fluoro-2-{4-[1-(2-hydroxy-ethoxy)-1-methyl-ethyl]-phenyl}-8-methyl-3H-quinazolin-4-one“A22”6-fluoro-2-(4-isopropyl-phenyl)-3H-quinazolin-4-one“A23”5-chloro-2-[4-(1-hydroxy-1-methyl-ethyl)-phenyl]-3H-quinazolin-4-one“A24”2-[4-(1-hydroxy-1-methyl-ethyl)-phenyl]-8-methyl-3H-quinazolin-4-one“A25”6-fluoro-2-[4-(1-hydroxy-1-methyl-ethyl)-phenyl]-8-methyl-3H-quinazolin-4-one“A26”5,6,8-trifluoro-2-[4-(1-hydroxy-1-methyl-ethyl)-phenyl]-3H-quinazolin-4-one“A27”5,8-difluoro-2-[4-(1-hydroxy-1-methyl-ethyl)-phenyl]-3H-quinazolin-4-one“A28”fluoro-8-methyl-2-[4-(4-methyl-piperazin-1-yl)-phenyl]-3H-quinazolin-4-one“A29”6-fluoro-2-[4-(4-hydroxy-piperidin-1-yl)-phenyl]-8-methyl-3H-quinazolin-4-one“A30”2-[4-(1,1-dioxo-1l6-thiomorpholin-4-yl)-phenyl]-6-fluoro-8-methyl-3H-quinazolin-4-one“A31”6-fluoro-2-[4-(4-hydroxymethyl-piperidin-1-yl)-phenyl]-8-methyl-3H-quinazolin-4-one“A32”6-fluoro-8-methyl-2-[4-(4-methyl-[1,4]diazepan-1-yl)-phenyl]-3H-quinazolin-4-one“A33”6-fluoro-8-methyl-2-(4-piperidin-4-yl-phenyl)-3H-quinazolin-4-one“A34”6,8-difluoro-2-(4-piperidin-4-yl-phenyl)-3H-quinazolin-4-onehydrochloride“A35”6,8-difluoro-2-[4-(1-methyl-piperidin-4-yl)-phenyl]-3H-quinazolin-4-oneor a pharmaceutically acceptable salt, tautomer or stereoisomer thereof.