QUINAZOLINONE DERIVATIVES AS PARP INHIBITORS Russian patent published in 2018 - IPC C07D239/91 A61K31/517 A61P35/00 A61P29/00 A61P25/28 A61P9/00 

FIELD: chemistry.

SUBSTANCE: invention relates to novel quinazolinone derivatives selected from the group of compounds indicated below or pharmaceutically acceptable salts thereof. Compounds possess the properties of an inhibitor of Tankyrase (TANK) and can be used to treat diseases selected from a group consisting of cancer of the head, neck, eye, mouth, throat, esophagus, bronchus, larynx, pharynx, chest, bone, lung, colon, rectum, stomach, prostate, urinary bladder, uterine, cervix, breast, ovaries, testicles or other reproductive organs, skin, thyroid, blood, lymph nodes, kidney, liver, pancreas, brain, central nervous system, solid tumors and malignant transformation of blood.

No. Name "A1" 6-fluoro-2-[4-(1-hydroxy-1-methylethyl)-phenyl]-3H-quinazolin-4-one "A2" 2-[4-(1-hydroxy-1-methylethyl)-phenyl] -8-methoxy-3H-quinazolin-4-one "A3" 8-fluoro-2-[4-(1-hydroxy-1-methylethyl)-phenyl]-3H-quinazolin-4-one "A4" 5-fluoro-2- [4-(1-hydroxy-1-methylethyl)-phenyl]-3H-quinazolin-4-one "A5" 6-chloro-2-[4-(1-hydroxy-1-methylethyl)-phenyl]-3H-quinazolin-4-one "A6" 8-chloro-2-[4-(1-hydroxy-1-methylethyl)-phenyl]-3H-quinazolin-4-one "A7" 6-fluoro-2-{4-[1- (2-hydroxyethoxy)-1-methylethyl]-phenyl}-3H-quinazolin-4-one "A11" 6,8-difluoro-2-[4-(1-hydroxy-1-methylethyl)phenyl]-3H-quinazolin-4-one "A12" 5,6-difluoro-2-[4- (1-hydroxy-1-methylethyl)phenyl]-3H-quinazolin-4-one "A13" 6-fluoro-2-[5-(1-hydroxy-1-methylethyl)-2-pyridyl]-3H-quinazolin-4-one "A14" 2-[4-(1-ethyl-1-hydroxypropyl)phenyl]-6-fluoro-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-methylethyl]phenyl]-6-fluoro-3H-quinazolin-4-one "A19" 6-fluoro-2-[4-(4-piperidyl)phenyl]-3H-quinazolin-4-one "A21" 6-fluoro-2-{4-[1-(2-hydroxyethoxy)-1-methylethyl]-phenyl}-8-methyl-3H-quinazolin-4-one "A23" 5-chloro-2-[4-(1-hydroxy-1-methylethyl)-phenyl]-3H-quinazolin-4-one "A24" 2-[4-(1-hydroxy-1-methylethyl)-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-methylethyl)-phenyl]-3H-quinazolin-4-one "A27" 5,8-difluoro-2-[4-(1-hydroxy-1-methylethyl)-phenyl]-3H-quinazolin-4-one "A29" 6-fluoro-2-[4-(4-hydroxypiperidin-1-yl)-phenyl]-8-methyl-3H-quinazolin-4-one "A31" 6-fluoro-2-[4-(4-hydroxymethylpiperidin-1-yl)phenyl]-8-methyl-3H-quinazolin-4-one "A33" 6-fluoro-8-methyl-2-(4-piperidin-4-ylphenyl)-3H-quinazolin-4-one "A34" hydrochloride 6,8-difluoro-2- (4-piperidin-4-yl-phenyl)-3H-quinazolin-4-one

Compounds of the present invention are selected from the table above.

EFFECT: compounds can be used to treat and / or prevent malignant neoplasm, multiple sclerosis, cardiovascular diseases, central nervous system lesions, and various forms of inflammation mediated by tankyrase activity (TANK).

4 cl, 3 tbl, 19 ex