| 摘要 |
PROBLEM TO BE SOLVED: To obtain a pharmaceutical composition having excellent cGMP- specific phosphodiesterase inhibitory activity (PDE V-inhibiting activity) by compounding a specific isoquinoline derivative. SOLUTION: This pharmaceutical composition contains a compound of formula I rings A and B are each a (substituted) benzene ring; R1 is H, a (substituted) lower alkyl, a (substituted) lower cycloalkyl, a (substituted) aryl, a (substituted) heterocyclic group or a (substituted) amino; R2 is a group of the formula: COOR3 (R3 is H or an ester residue) or the formula: CON(R4)(R5) [the group expressed by N(R4)(R5) is a (substituted) nitrogen-containing aliphatic heterocyclic group or a (substituted) amino group]} [e.g. 6-methoxy-3-methoxycarbonyl-2- morpholino-7-(4-pyridylmethyloxy)-4-(3,4,5-trimethoxyphenyl)-1(2H)-iso quinoline]. The compound of formula I is obtained by reacting an isocoumarin derivative of formula II with an amine compound of the formula: R1NH2.
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