| 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 NR13-, -C1-5alkyl-, -C1-5 alkyl-NR14-CO-C1-5alkyl-, -C1-5alkyl-CO NR 15-C1-5alkyl-, -C1-6alkyl-CO-NH-, -C1-6 alkyl-NH-CO-, -C1-3alkyl-NH-CS-Het20-, -C1-3 alkyl-NH-CO-Het20-, -C1-2alkyl-CO-Het21-CO-, - Het22-CH2-CO-NH-C1-3alkyl-, -CO-NH-C1- 6alkyl-, -NH-CO-C1-6alkyl-, -CO-C1-7alkyl-, -C 1-7alkyl-CO-, -C1-6alkyl-CO-C1-6alkyl-, -C1- 2alkyl-NH-CO-CR16R17-NH-, -C1-2alkyl-CO- NH-CR18R19-CO-, -C1-2alkyl-CO-NR20- C1-3alkyl-CO-, C1-2alkyl-NR21-CH2-CO- NH-C1-3alkyl-, or -NR22-CO-C1-3alkyl-NH-; X 1 represents a direct bond, O or -O-C1-2alkyl-, CO, -CO- C1-2alkyl-, NR11, -NR11-C1-2alkyl-, CH2-, -O-N=CH- or -C1-2alkyl-; X2 represents a direct bond, O, -O-C1-2alkyl-, CO, -CO-C1-2alkyl-, NR12, -NR12-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. |
