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Benzodiazepine Bromodomain Inhibitor
专利权人:
GlaxoSmithKline LLC
发明人:
BAILEY, James,GOSMINI, Romain Luc Marie,MIRGUET, Olivier,WITHERINGTON, Jason
申请号:
ES10773325
公开号:
ES2564318T3
申请日:
2010.11.03
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
A compound of formula (Ic) or a pharmaceutically acceptable salt thereof: ** Formula ** where R 1 is C 1-3 alkyl; R2 is -NR2aR2a 'or -OR2b; wherein one of R2a or R2'a is H and R2b or the other of R2a or R2'a is selected from C1-6 alkyl, C1-6 haloalkyl, R2cR2'cN-C1-6 alkyl, carbocyclyl, C1- carbocyclylalkyl 4, heterocyclyl and heterocyclylC 1-4 alkyl, wherein one of the carbocyclyl or heterocyclyl groups is optionally substituted with one or more groups selected from halogen, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, C1-6 haloalkoxy , carbonyl, -CO-carbocyclyl, azido, nitro and cyano, in which the -CO-carbocyclyl group may also be optionally substituted by one or more groups selected from halogen, C1-6 alkyl, C1-6 haloalkyl, C1- alkoxy 6, C1-6 haloalkoxy, azido, nitro and cyano; or two adjacent groups in any of the carbocyclyl or heterocyclyl groups together with the interconnecting atoms form a 5 or 6 membered ring, a ring that may contain 1 or 2 heteroatoms independently selected from O, S and N; or R2a and R2'a together with the nitrogen atom to which they are attached form a ring of 5, 6 or 7 members which can optionally confer 1 or 2 heteroatoms independently selected from O, S and N; wherein the 5, 6 or 7 member ring may be optionally substituted by C1-6 alkyl, R2c and R2'c are independently H and C1-6 alkyl; each R3 is independently selected from H, hydroxy, halo, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, C1-6 haloalkoxy, nitro, cyano, CF3, -OCF3 and -COOR5; R4 is hydroxy, halo, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, C1-6 haloalkoxy, nitro, cyano, CF3, -OCF3; -COOR5 or -OS (O) 2 C1-4alkyl; R5 is C1-3 alkyl; and n is an integer from 1 to 5 for use in the treatment of cancer.Un compuesto de fórmula (Ic) o una sal farmacéuticamente aceptable del mismo:**Fórmula** donde R1 es alquilo C1-3; R2 es -NR2aR2a' u -OR2b; en el que uno de R2a o R2'a es H y R2b o el otro de R2a o R2'a es seleccionado de alquilo C1-6, haloalquilo C1-6, R2cR2'cN-alquilo C1-6, carbociclilo, c
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