New substituted pteridine compounds, useful as phosphodiesterase 4 inhibitors for treating e.g. inflammatory diseases, cancer, asthma, ulcerative colitis, depression and schizophrenia

摘要

Substituted pteridine compounds (I) and their salts are new. Substituted pteridine compounds of formula (I) and their salt are new. R 1heterocyclic ring which contains a nitrogen atom; R 2aryl, het or hetaryl (all optionally substituted by 1-6C alkyl, O-1-6C alkyl, 3-6C cycloalkyl, 7-11C aralkyl or N(1-4C alkyl) 2), halo, OR 2a, SR 2aor NR 2aR 2b; R 2a, R 2bH, 1-4C alkyl, aryl or 7-11C aralkyl; R 3aryl, het, hetaryl or -X-Y-A-(R 3a) m; A : aryl or hetaryl; X : NR 3b, S or O; Y : 1-4C alkylene (optionally substituted by at least one R 3c; m : 0 - 3; R 3a1-6C alkyl, 1-6C haloalkyl, 1-6C alkyl-CONR 3dR 3e, -1-6C alkyl-NR 3dR 3e, OR 3d, O-1-16C haloalkyl, NHCOR 3d, SO 2R 3d, aryl, halo, CN, OH or CONR 3dR 3e; R 3a+two atoms of A : 5- or 6-membered carbocyclic or heterocyclic ring (which may contain at least one of O or N atoms); R 3b, R 3d, R 3eH or 1-6C alkyl; R 3c1-6C alkyl, 1-6C alkyl-OH, 3-6C cycloalkyl-OH, COOR 3dor CONR 3dR 3e; R 3c+one or two carbon atoms of Y : 3-6C carbocyclic ring; R 4aryl, het or hetaryl (all optionally substituted by at least one of 1-6C alkyl, 1-6C haloalkyl, CN, O-1-16C alkyl or halo), 1-6C alkyl, 2-6 alkenyl, 2-4C alkynyl, 3-6C cycloalkyl, 3-6C cycloalkenyl, OR 4a, SR 4a, 1-6C haloalkyl or NR 4aR 4b; R 4aH, 1-6C alkyl, aryl or 7-11C aralkyl; R 4bH, 1-6C alkyl, aryl or 7-11C aralkyl. [Image] ACTIVITY : Respiratory-Gen.; Gastrointestinal-Gen.; Antiinflammatory; Cytostatic; CNS-Gen.; Antiasthmatic; Antiulcer; Antidepressant; Neuroleptic; Antimanic; Tranquilizer; Nootropic; Neuroprotective; Antiparkinsonian; Analgesic; Vulnerary; Antitussive; Antiallergic; Antirheumatic; Antiarthritic. MECHANISM OF ACTION : Phosphodiesterase 4 (PDE4) inhibitors. No activity data given.