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Triazolopyrazines as inhibitors of BRD4 for use in cancer treatment
专利权人:
Boehringer Ingelheim International GmbH
发明人:
ENGELHARDT, Harald,SMETHURST, Christian,GIANNI, Davide
申请号:
ES13789833
公开号:
ES2641465T3
申请日:
2013.11.15
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound of formula (I) ** (See formula) ** in which, R 1 is -C 1-3 alkyl or -C 1-3 alkyl; R2 is selected from -NHR4, -C1-5 alkyl, C1-5 haloalkyl, halogen and -S-C1-3 alkyl; R3 is a 5-12 membered heteroaryl, a group that is substituted with -X-R10 and optionally further substituted with one or more groups independently selected from R9; R4 is selected from -C1-5 alkyl and 5-12 membered heterocycloalkyl, heterocycloalkyl which may be optionally substituted with one or more groups independently selected from R5; R5 is selected from -C1-5 alkyl, -C1-5 haloalkyl and -C1-3 alkylene-O-C1-3 alkyl; R9 is selected from -C1-5 alkyl, -O-C1-5 alkyl, -N (C1-5 alkyl) 2, halogen, C1-3 alkylene-O-C1-3 alkyl, - C1-5 alkylene (-C1-5 alkyl, -C1-5 alkyl), 5-12 membered heterocycloalkyl, in which the heterocycloalkyl group may be optionally substituted with one or more groups independently selected from>; = O, -C1-3 alkyl, or R9 is selected from C6-10 -aryl and 5-12 membered heteroaryl, in which the aryl and heteroaryl groups may be optionally and independently substituted with one or more groups selected from halogen, - C1-3 alkyl, -O-alkyl C1-3, -C1-3 haloalkyl, -O-C1-3 haloalkyl, -N (C1-5 alkyl, C1-5 alkyl) and -NH-C1-5 alkyl; X is -C 1-3 alkylene- or -O-; R10 is -C6-10 aryl or a 5-12 membered heteroaryl, each of which groups may be optionally substituted with one or more groups selected from halogen, -C1-3alkyl, -O-C1-3alkyl, -haloalkyl C1-3, -Ohaloalkyl C1-3; wherein the compounds of formula (I) may optionally be present in the form of salts.Un compuesto de fórmula (I) **(Ver fórmula)** en la que, R1 es -alquilo C1-3 o -haloalquilo C1-3; R2 se selecciona entre -NHR4, -alquilo C1- 5, -haloalquilo C1-5, halógeno y -S-alquilo C1-3; R3 es un heteroarilo de 5-12 miembros, grupo que está sustituido con -X-R10 y opcionalmente adicionalmente sustituido con uno o más grupos seleccionados independientemente entre R9; R4 se selecciona entre -alquilo C1-5 y heterocicloalquilo de 5-12 miemb
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