4-((3-Chloro-2-fluorophenyl)-amino)-6-(4-(optionally N-substituted or N,N-disubstituted amino)-cyclohexyloxy)-7-methoxy-quinazoline derivatives (I) are new. 4-((3-Chloro-2-fluorophenyl)-amino)-6-cyclohexyloxy-7-methoxy-quinazoline derivatives of formula (I) (including tautomers and tautomer mixtures) and their acid addition salts, solvates and hydrates are new. R : cis- or trans-4-(NR 1R 2)-cyclohexyl； R 1H, Me, COOMe, COOEt, COOtBu, COMe, COCH 2OMe, CONMe 2, morpholinocarbonyl, piperazin-1-ylcarbonyl, 4-methyl-piperazin-1-ylcarbonyl or SO 2Me； R 2H or Me, provided that R 2 = H if R 1 = Me； or NR 1R 2phthalimido. Independent claims are included for the preparation of (I) [Image] ACTIVITY : Cytostatic； Antiinflammatory； Antiasthmatic； Antiallergic； Antitussive； Antiulcer； Dermatological； Ophthalmological； Antirheumatic； Antiarthritic； Neuroprotective； Antipsoriatic； Immunomodulator. MECHANISM OF ACTION : Epidermal growth factor receptor (EGFR)-mediated signal transduction inhibitor； Tyrosine kinase inhibitor. (I) inhibit EGFR)-mediated signal transduction by inhibiting ligand bonding, receptor dimerization or the tyrosine kinase itself, and may also inhibit signal transfer to other downstream components. Some unspecified compounds (I) show IC 50 values of less than 1 mu M for inhibition of human EGR receptor kinase in a maculovirus expression system.
