Quinazolindiona derivatives as PARP Inhibitors, Methods for their preparation, Pharmaceutical compositions containing as the active ingredient and Use thereof in medicaments for the Treatment or prevention of cancer.

摘要

Pentachloronitrobenzene derivatives as PARP inhibitors, pharmaceutical ingredients containing these substances and drugs for cancer prevention or treatment. Item 1: a formula compound (1)N-oxidation form, drug acceptable addictive salt, and stereochemical isomerization form of each x independent and That's what it means!When x is with GT, then with GT, N,Comment more than a month agoThat's what it means!Unless x is gt, then gt, N -;L1 is a direct link or selected bivalent radical link of C1-6 alkane; L2 is a direct link or selected bivalent radical link of carbide, C1-6 alkane, c1-6-alkane, c1-6-alkane or c1-6-c (o) alkane;R1 is H or hydroxy; and Z is H or a radical selected from the group of formulas (2) where R2 is independently selected from H, halo or C1-6 alkyl with the proviso that 1- [1 - [(2S) -2 - [(2R) -3,4- dihydro-2H-1-benzopyran-2-yl] -2-hydroxyethyl] -4-piperidinyl] -2,4- (1H, 3H) -quinazolindione, 1- [2- [4- (4 -fluorbenzoyl) -1-piperidinyl] ethyl] -2,4- (1H, 3H) -quinazolindione, 1- [3- [4- (4-fluorbenzoyl) -1-piperidinyl] propyl] -2,4- (1H , 3H) -quinazolindione,3 - [2 - [4 - [4 - [4 - (4-chlorobenzodiazo) - 1-pyridine] ethyl] - 2, 4 - (1H, 3H) - quinolyl and 3 - [2 - [4 - [(4-fluorophenyl) hydroxy] ethyl] - 1-pyridine-ethyl] - 2, 4 - (1H, 3H) - quinediol are not included. Item 13: a process for preparing a compound, as claimed in Item 1, characterized by (a) reaction to a formula intermediate (3) and a formula intermediate (4),Where W is an appropriate output group to form a formula compound (5),Where x is with GTIn an inert reaction solvent, and an appropriate basis is added, or (b) reaction with a formula intermediate (6) (7),Where W is an appropriate output group to form a formula compound (8),Where and whereIn an inert reaction solvent and add a suitable base.