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Pyrimidine macrocyclic derivatives
专利权人:
Janssen Pharmaceutica NV
发明人:
DIELS, Gaston,SCHOENTJES, Bruno,VERSELE, Matthias,BERTHELOT, Didier,WILLEMS, Marc,VIELLEVOYE, Marcel,EMBRECHTS, Werner,WROBLOWSKI, Berthold,MEERPOEL, Lieven
申请号:
ES15713522
公开号:
ES2667723T3
申请日:
2015.04.02
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
A compound of Formula (I) ** Formula ** a tautomer or a stereoisomeric form, wherein each of Xa, Xb and Xc independently represents CH or N; -X1- represents - (CHR12) s-NR1-Xe-alkanediylC1-4- (SO2) p3- or - (CH2) s-O-Xe-alkanediylC1-4- (SO2) p3-; wherein each of said C1-4 alkanediyl moieties are optionally substituted with hydroxy or C1-4 hydroxyalkyl; -Xe- represents -C (R2) 2- or -C (>; = O) -; a represents -NR4-C (>; = O) - [C (R5b) 2] r- or -NR4-C (R5b) 2-C (>; = O) - or -C (>; = O) -NR4-C (R5b) 2-; b represents ** Formula ** where said ring b may contain extra bonds to form a bridged ring system selected from 2,5-diazabicyclo [2.2.2] octanyl, 3,8-diazabicyclo [3.2.1] octanyl, 3 , 6- diazabicyclo [3.1.1] heptanyl, 3,9-diazabicyclo [3.3.1] nonyl; Xd1 represents CH or N; Xd2 represents CH2 or NH; with the proviso that at least one of Xd1 and Xd2 represents nitrogen; c represents a bond, - [C (R5a) 2] m-, -C (>; = O) -, -O-, -NR5a'-, -SO2-, or -SO-; ** Formula ** the ring ** Formula ** represents phenyl or pyridyl; R 1 represents hydrogen, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, C 1-4 cyanoalkyl, -C (>; = O) -C 1-4 alkyl, -C (>; = O) -C 1-4 haloalkyl, C 1-4 hydroxyalkyl, C 1-4 haloalkyl, C 1-4 alkyloxyC 1-4 alkyl, C 1-4 haloalkyloxyC 1-4 alkyl, -C (>; = O) NR7R8, -SO2-NR7R8, -SO2-R9, R11, alkyl C1-4 substituted with R11, -C (>; = O) -R11, or -C (>; = O) -C1-4-R11 alkyl; each R2 independently represents hydrogen, C1-4 alkyl, C1-4 alkyl substituted with C3-6 cycloalkyl, C1-4 hydroxyalkyl, C1-4 alkyloxy C1-4 alkyl, carboxyl, -C (>; = O) -O-C1-alkyl -4 where C1-4 alkyl is optionally substituted with C1-4 alkyloxy, -C (>; = O) -NH2, -C (>; = O) -NH (C1-4 alkyl) where C1-4 alkyl is optionally substituted with C1-4 alkyloxy, or -C (>; = O) -N (C1-4 alkyl) 2 where each C1-4 alkyl is optionally substituted with C1-4 alkyloxy; or R1 and R2 are taken together to form C1-4 alkanediyl or C2-4 alkenodiyl, each of said C1-4 alkanediyl and C2-4 alken
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