QUINAZOLINONE DERIVATIVE

• Main Authors: HATTORI, KOUJI, ISHIDA, JUNYA, KIDO, YOSHIYUKI
• Format: Patent
• Language: English; French
• Published: 10.07.2003
• Edition: 7
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

A quinazolinone derivatives having poly (adenosine 5'−diphospho−ribose) polymerase (PARP) inhibitory activity represented by the formula (I): wherein R1 is substituted cyclic amino groups or optionally substituted amino group, R2 is substituent, n means an integer of 0 to 4, and L1is (1) cyclo (lower) alkylene, (2) cyclo (lower) alkenylene, (3) diradical of saturated− or unsaturated monocyclic group with one or more nitrogen atom(s), which is obtained after removal of one hydrogen atom from said monocyclic group, or (4) −N (R3) −L2− (wherein R3 is hydrogen or lower alkyl, and L2 is lower alkylene or lower alkenylene), or its prodrug, or a salt thereof. A quinazolinone derivatives having poly adenosine 5'-diphospho-ribose polymerase PARP inhibitory activity represented by the formula I: wherein R1 is substituted cyclic amino groups or optionally substituted amino group, R2 is substituent, n means an integer of 0 to 4, and L1is 1 cyclo lower alkylene, 2 cyclo lower alkenylene, 3 diradical of saturated- or unsaturated monocyclic group with one or more nitrogen atoms, which is obtained after removal of one hydrogen atom from said monocyclic group, or 4 -N R3 -L2- wherein R3 is hydrogen or lower alkyl, and L2 is lower alkylene or lower alkenylene, or its prodrug, or a salt thereof. Cette invention concerne des dérivés de quinazolinone présentant une activité inhibitrice de la poly (adénosine 5'-diphospho-ribose) polymérase (PARP) qui sont représentés par la formule (I). Dans cette formule R1 représente des groupes amino cycliques substitués ou un groupe amino éventuellement substitué, R2 est un substituant, n est un entier compris entre 0 et 4, et L1est (1) un cyclo (inférieur) alkylène, (2) un cyclo (inférieur) alkènylène, (3) un groupe monocyclique saturé ou insaturé avec un ou plusieurs atomes d'azote, qui s'obtient après retrait d'un atome d'hydrogène dudit groupe monocyclique, ou bien (4) -N (R3) -L2- (dans lequel R3 est un hydrogène ou un alkyle inférieur, et L2 est un alkylène inférieur ou un alkènylène inférieur). L'invention porte également sur des promédicaments et des sels de ces dérivés.