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Quinazoline derivatives such as MTKI
专利权人:
JANSSEN PHARMACEUTICA NV
发明人:
PAPANIKOS, Alexandra,FREYNE, Eddy Jean Edgard,TEN HOLTE, Peter,WILLEMS, Marc,EMBRECHTS, Werner Constant Johan,MEVELLEC, Laurence Anne,STORCK, Pierre Henri
申请号:
ES07787471
公开号:
ES2569428T3
申请日:
2007.07.12
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
A compound with the formula: ** Formula ** N-oxide forms, pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, in which: Y represents -C3-9- alkyl, -C1 alkyl- 5-O-C1-5 alkyl-, C1-5 alkyl-NR6-C1-5 alkyl-, C1-5 alkyl-NR7-CO-C1-5 alkyl-, C1-6 alkyl -NR7-CO- , -NR7-CO- C1-6 alkyl -, -C1-3 alkyl -NR7-CO-Het1-, -C1-6 alkyl -NR8-Het2-, C1-6 alkyl -CO- C1-6 alkyl -, - C1-6 alkyl -CO-NR7- or -CO-NR7- C1-6 alkyl -; X1 represents -O-, -O-C1-2 alkyl- or -NR4-C1-2 alkyl; X2 represents a direct bond, - C1-2 alkyl-, -O-, -O- C1-2 alkyl- or -NR5- C1-2 alkyl; R1 represents hydrogen, cyano, halo, hydroxy, C1-4 alkyl, Het3, Ar1, Het3-O- or Ar1-O-; R 2 represents hydrogen, cyano, halo, C 2-6 alkenyl, C 2-6 alkynyl, C 3-7 cycloalkyl or C 1-6 alkyl in which said C 2-6 alkenyl, C 2-6 alkynyl, C 3-7 cycloalkyl or C 1-6 alkyl two or more substituents selected from hydroxy or halo are optionally substituted with one or whenever possible; R3 represents hydroxy; C1-4 alkyloxy or C1-4 alkyloxy - substituted with one or whenever possible two or more substituents each independently selected from: Het4, hydroxy, C1-4- alkyloxy, halo, NR9R10, C1-4-OC alkyl (>; = O) -O-, Ar2, NR11R12-carbonyl, Het5-carbonyl and oxyranyl; R4 represents hydrogen, Ar3-S (>; = O) 2-, Ar3-S (>; = O) -, C1-4 alkyl, C2-4 alkenyl, C3-7 cycloalkyl, C2-4 alkynyl, C1-4 alkyl - carbonyl or C 1-4 alkyloxy -carbonyl- wherein said C 1-4 alkyl, C 2-4 alkenyl, C 3-7 cycloalkyl, C 2-4 alkynyl, C 1-4 alkylcarbonyl or C 1-4 alkyloxycarbonyl- is optionally substituted with C1-4 alkyloxy, Het6 or phenyl; R5 represents hydrogen, Ar3-S (>; = O) 2-, Ar3-S (>; = O) -, C1-4 alkyl, C2-4 alkenyl, C3-7 cycloalkyl, C2-4 alkynyl, C1-4 alkyl - carbonyl or C 1-4 alkyloxy -carbonyl- wherein said: C 1-4 alkyl, C 2-4 alkenyl, C 3-7 cycloalkyl, C 2-4 alkynyl, C 1-4 alkylcarbonyl or C 1-4 alkyloxycarbonyl- is optionally substituted with C1-4- alkyloxy, Het6 or phenyl; R6 represents hydrogen, Ar4-S (>; = O) 2
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