| 摘要 |
<p>Dihydrothienopyrimidine derivatives (I) are new. Dihydrothienopyrimidine derivatives of formula (I) and their salts, diastereomers, enantiomers, racemates, hydrates or solvates are new. X : O, S, SO or SO 2; either R 1>H, 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl, 6-10C aryl or 6-10C aryl-1-6C-alkylene, 5-10C heteroaryl-1-6C-alkylene; and R 2>1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl (all optionally substituted), optionally one or more bridged mono- or bicyclic 3-10C cycloalkyl, 6-10C aryl, aromatic or non-aromatic, 3-10C heterocyclic ring, a bicyclic ring or 3-10C heterocycle condensed 6-10C aryl, or H; or NR 1>R 2>heterocyclic ring, optionally with one or more of 1-4C-alkyl, 2-6C-alkenyl, 2-6C-alkynyl, 1-6C alkanol or oxo; R 3>6-10C heterocyclic ring, 3-7C cycloalkyl, 6-10C aryl-1-6C alkylene, 5-10C heteroaryl-1-6C-alkylene, a condensed bicyclic ring (optionally containing 1-4 heteroatoms of N, O or S), optionally substituted phenyl, COR 37>, COCH 2R 38>, CONHR 38> or SO 2R 38>; R 37>H, 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl or 6-10C aryl; R 38>1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl, 3-7C cycloalkyl, 6-10C aryl, 3-10C heterocyclic ring and a bicyclic ring, optionally substituted with one or more of 1-6C-alkyl, 2-6C alkenyl, 2-6C alkynyl, halo, NR-38aR-38b, 6-10C aryl or 3-10C heterocyclic ring; R-38a, R-38b : H, 1-6C alkyl, 2-6C alkenyl or 2-6C alkynyl; R 4>H, 1-4C alkyl, 2-4C alkenyl, 2-4C alkynyl or oxo; R 5>, R 6>H, 1-4C alkyl, 2-4C alkenyl or 2-4C alkynyl; and either R 7>, R 8>H, 1-4C alkyl, 2-4C alkenyl, 2-4C alkynyl, 6-10C aryl or OH; or R 7>+R 8>oxo. An independent claim is included for 50 intermediate compounds e.g. pyrimidine derivatives of formula (VIII), (IV) or (V). [Image] [Image] - ACTIVITY : Respiratory-Gen.; Gastrointestinal-Gen.; Antiinflammatory; Cytostatic; CNS-Gen.; Antiasthmatic; Antiulcer.Antidepressant; Neuroleptic; Antimanic; Neuroprotective; Nootropic; Antiparkinsonian; Cerebroprotective; Vasotropic; Tranquilizer. - MECHANISM OF ACTION : Phosphodiesterase-4 enzyme inhibitor.</p> |
