| 摘要 |
The present invention concerns the compounds of formula (I) the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents O, CH2, NH or S; in particular Z represents NH; Y represents -C3-9alkyl-, -C3-9alkenyl-, -C3-9alkynyl-, -C3-7alkyl-CO-NH- optionally substituted with amino, mono- or di(C1-4alkyl)amino or C1-4 alkyloxycarbonylamino-, -C3-7alkenyl-CO-NH- optionally substituted with amino, mono- or di(C1-4alkyl)amino- or C1-4alkyloxycarbonylamino-, C1-5alkyl-oxy-C1-5alkyl-, -C1-5alkyl NR<13>-, -C1-5alkyl-, -C1-5alkyl-NR<14>-CO-C1-5alkyl-, -C1-5alkyl-CO NR<15>-C1-5alkyl-, -C1-6alkyl-CO-NH-, -C1-6alkyl-NH-CO-, -C1-3alkyl-NH-CS-Het<20>-, -C1-3alkyl-NH-CO-Het<20>-, -C1-2alkyl-CO-Het<21>-CO-, -Het<22>-CH2-CO-NH-C1-3alkyl-, -CO-NH-C1-6alkyl-, -NH-CO-C1-6alkyl-, -CO-C1-7alkyl-, -C1-7alkyl-CO-, -C1-6alkyl-CO-C1-6alkyl-, -C1-2alkyl-NH-CO-CR<16>R<17>-NH-, -C1-2alkyl-CO-NH-CR<18>R<19>-CO-, -C1-2alkyl-CO-NR<20>-C1-3alkyl-CO-, C1-2alkyl-NR<21>-CH2-CO-NH-C1-3alkyl-, or -NR<22>-CO-C1-3alkyl-NH-; X<1> represents a direct bond, O or -O-C1-2alkyl-, CO, -CO-C1-2alkyl-, NR<11>, -NR<11>-C1-2alkyl-, CH2-, -O-N=CH- or -C1-2alkyl-; X<2> represents a direct bond, O, -O-C1-2alkyl-, CO, -CO-C1-2alkyl-, NR<12>, -NR<12>-C1-2alkyl-, -CH2-, -O-N=CH- or -C1-2alkyl-. The growth inhibitory effect anti-tumour activity of the present compounds has been demonstrated in vitro, in enzymatic assays on the receptor tyrosine kinase EGFR. |
