| 摘要 |
<p>Tetracyclic derivatives of formula (I) in which: R0 represents hydrogen, halogen or C1-6alkyl; R1 represents hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, haloC1-6alkyl, C3-8cycloalkyl, C3-8cycloalkyl C1-3alkyl, arylC1-3alkyl or heteroaryl C1-3alkyl; R2 represents an optionally substituted monocyclic aromatic ring selected from benzene, thiophene, furan and pyridine or an optionally substituted bicyclic ring (a), wherein the fused ring (A) is a 5- or 6-membered ring which may be saturated or partially or fully unsaturated and comprises carbon atoms and optionally one or two heteroatoms selected from oxygen, sulphur and nitrogen; and R3 represents hydrogen or C1-3 alkyl, or R1 and R3 together represent a 3- or 4-membered alkyl or alkenyl chain. A compound of formula (I) is a potent and selective inhibitor of cyclic guanosine 3',5'-monophosphate specific phosphodiesterase (cGMP specific PDE) having a utility in a variety of therapeutic areas where such inhibition is beneficial, including the treatment of cardiovascular disorders. Also disclosed is a method of preparing said derivatives and pharmaceutical compositions based thereon.</p> |
