MC GOWAN, David, Craig,EMBRECHTS, Werner, Constant, Johan,GUILLEMONT, Jérôme, Émile, Georges,COOYMANS, Ludwig, Paul,JONCKERS, Tim, Hugo, Maria,RABOISSON, Pierre, Jean-Marie, Bernard
申请号:
EPEP2019/054941
公开号:
WO2019/166532A1
申请日:
2019.02.28
申请国别(地区):
EP
年份:
2019
代理人:
摘要:
This application relates to quinazoline derivatives of formula (I), pharmaceutical compositions comprising the compounds of formula (I), and the use of the compounds of formula (I) in the treatment or prevention of a viral infection, of a virus-induced disease, of cancer or of an allergy. In formula (I), R1 is a C3-8alkyl, optionally substituted by one or more substituents independently selected from fluorine, hydroxyl, amino, nitrile, ester, amide, C1-3 alkyl, or C1-3 alkoxy, the carbon of R1 bonded to the amine in the 4-position of the quinazoline is in (R)-configuration, R2 is hydrogen, deuterium, fluorine, chlorine, methyl, methoxy, cyclopropyl, trifluoromethyl, or carboxylic amide, wherein each of methyl, methoxy and cyclopropyl is optionally substituted by one or more substituents independently selected from fluorine and nitrile, R3 is hydrogen or deuterium, R4 is hydrogen, deuterium, fluorine, methyl, carboxylic ester, carboxylic amide, nitrile, cyclopropyl, C4-7 heterocycle, or 5-membered heteroaryl group, wherein each of methyl, cyclopropyl, C4-7 heterocycle and 5-membered heteroaryl group is optionally substituted by one or more substituents independently selected from fluorine, hydroxyl, or methyl, R5 is hydrogen, deuterium, fluorine, chlorine, methyl, or methoxy, provided that at least one of R2, R3, R4 and R5 is not hydrogen.La présente invention concerne des dérivés de quinazoline de formule (I), des compositions pharmaceutiques comprenant les composés de formule (I), et l'utilisation des composés de formule (I) dans le traitement ou la prévention d'une infection virale, d'une maladie induite par un virus, du cancer ou d'une allergie. Dans la formule (I), R1 représente un alkyle en C3-8, éventuellement substitué par un ou plusieurs substituants choisis indépendamment parmi le fluor, hydroxyle, amino, nitrile, ester, amide, alkyle en C1-3, ou alcoxy en C1-3, le carbone de R1 lié à l'amine en position 4 de la quinazoline est dans la configuration (R), R2