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Makrocykliczne pochodne chinazoliny jako środki przeciwproliferacyjne
专利权人:
Janssen Pharmaceutica NV
发明人:
FREYNE, EDDY JEAN EDGARD,PERERA, TIMOTHY PIETRO SUREN,BUIJNSTERS, PETER JACOBUS JOHANNES ANTONIUS,WILLEMS, MARC,DIELS, GASTON STANISLAS MARCELLA,EMBRECHTS, WERNER CONSTANT JOHAN,TEN HOLTE, PETER,ROMBO,FREYNE EDDY JEAN EDGARD,PERERA TIMOTHY PIETRO SUREN,BUIJNSTERS PETER JACOBUS JOHANNES ANTONIUS,WILLEMS MA
申请号:
PL04739341
公开号:
PL1633365T3
申请日:
2004.05.25
申请国别(地区):
PL
年份:
2012
代理人:
摘要:
The present invention concerns the compounds of formula the N -oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents NH; Y represents -C 3-9 alkyl-, -C 2-9 alkenyl-, -C 3-7 alkyl-CO-NH optionally substituted with amino, mono - or di(C 1-4 alkyl)amino or C 1-4 alkyloxycarbonylamino-, -C 3-7 alkenyl-CO-NH- optionally substituted with amino, mono- or di(C 1- 4 alkyl)amino- or C 1-4 alkyloxycarbonylamino-, C 1-5 alkyl-NR 13 -C 1-5 alkyl-, -C 1-5 alkyl-NR 14 -CO-C 1-5 alkyl-, -C 1-6 alkyl-CO-NH-, -C 1-5 alkyl-CO NR 15 -C 1-5 alkyl-, -C 1-3 alkyl-NH-CO-Het 20 -, -C 1-2 alkyl-CO-Het 21 -CO-, -C 1-2 alkyl-NH-CO-CR 16 R 17 -NH-, -C 1-2 alkyl-CO-NH-CR 18 R 19 -CO-, -C 1-2 alkyl-CO-NR 20 -C 1-3 alkyl-CO-, or -NR 22 -CO-C 1-3 alkyl-NH-; X 1 represents a direct bond, O or-O-C 1-2 alkyl-; X 2 represents a direct bond, -CO-C 1- 2 alkyl-, NR 12 , -NR 12 -C 1-2 alkyl-, -O-N=CH- or -C 1-2 alkyl-; R 1 and R 2 each independently represents hydrogen or halo; R 3 represents hydrogen; R 4 represents hydrogen or C 1-4 alkyloxy; R 12 and R 13 each independently represents hydrogen or C 1-4 alkyl; R 14 and R 15 represents hydrogen; R 16 and R 17 each independently represent hydrogen or C 1-4 alkyl; R 18 and R 19 each independently represent hydrogen or C 1-4 alkyl optionally substituted with phenyl or hydroxy; R 20 and R 21 each independently represent hydrogen or C 1-4 alkyl optionally substituted with C 1-4 alkyloxy; Het 20 , Het 21 and Het 22 each independently represent a heterocycle selected from the group consisting pyrrolidinyl, 2-pyrrolidinonyl or piperidinyl optionally substituted with hydroxy.
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