New quinazoline compounds are tyrosin-kinase inhibitors e.g. to treat cancer, hematologic or solid tumors, non-Hodgkin tumors or T-cell lymphoma; and for the modulation of the cell cycle, cell differentiation, apoptosis or angiogenesis

摘要

Quinazoline compounds (I) and their salts with counter ions are new. Quinazoline compounds of formula (I) and their salts with counter ions are new. R 1, R 2H, OH, halo, CN, NO 2, one or more times saturated 1-10C-alkyl (which is optionally 1-3 times substituted by OH, halo or 1-5C-alkoxy, and interrupted by one or more O, S, N, carbonyl or sulfonyl group, aliphatic or aromatic 5-7 membered homo or heterocyclic ring system), one or more times saturated 1-10C-alkoxy (which is optionally 1-3 times substituted by OH, halo or 1-5C-alkoxy, and interrupted by one or more O, S, N, carbonyl or sulfonyl group, aliphatic or aromatic 5-7 membered homo or heterocyclic ring system), one or more times saturated 1-10C-alkylthio (which is optionally 1-3 times substituted by OH, halo or 1-5C-alkoxy, and interrupted by one or more O, S, N, carbonyl or sulfonyl group, aliphatic or aromatic 5-7 membered homo or heterocyclic ring system), or 1-5C-perfluoroalkyl (optionally one or more times unsaturated); R 3, R 4H, halo, CN, NO 2, CF 3or 1-4C-alkyl; R 5an aliphatic or aromatic 5-7 membered homo- or heterocyclic ring system, which can be condensed with 1 or 2 further aliphatic or aromatic 5-7 membered homo- or heterocyclic ring systems, which is optionally substituted by halo, CN or NO 2, or 1-4C-alkyl or 1-4C-alkoxyl, 2-4C-alkenyl, 2-4C-alkynyl (all optionally one or more times saturated and substituted by phenyl or halogenated phenyl group); L : N(R 6), O, C(=O)-, -O-C(=O)- or -C(=O)-O-, -N(R 6)-C(=O)- or -C(=O)-N(R 6)-, -N(R 6)-O- or -N(R 6)-O-, -O-N(R 6)-C(=O)- or -C(=O)-N(R 6)-O-, -N(R 6)-C(=O)-O- or -O-C(=O)-N(R 6)-; and R 6H or 1-4C-alkyl. Provided that: at least one residue of R 1or R 2is not H. An independent claim is included for the preparation of (I). [Image] ACTIVITY : Cytostatic; Angiogenesis Modulator; Antiinflammatory; Antiasthmatic; Antiallergic; Ophthalmological; Dermatological; Antiarthritic; Osteopathic; Antirheumatic; Gastrointestinal-Gen.; Antibacterial; Immunosuppressive; Antidiabetic; Hemostatic; Neuroprotective; Muscular-Gen.; Antipsoriatic; Nephrotropic; Respiratory-Gen.; Anabolic; Anorectic; Cardiant; Antiapoptotic. MECHANISM OF ACTION : Tyrosin-kinase inhibitor.