| 摘要 |
PROBLEM TO BE SOLVED: To obtain a new compound having a cGMP-specific phosphodiesterase- inhibiting action and useful as a medicine for preventing and treating hypertension, angina, etc. SOLUTION: A compound of formula I the ring A is a group of formula II [A1 is OH group, (substituted) phenyl group or the like; the ring B is a (substituted) benzene ring; R1 is (substituted) pyridyl, a (substituted) alkyl or the like; R2 is COOR3 (R3 is H, an ester residue or the like) or the like}, for example, 7-benzyloxy-2-(3hydroxypropyl)-3-methoxycarbonyl-4-(3,4,5- trimethoxyphenyl)-1-(2H)isoquinolinone. The above compound is obtained by reacting an isocoumarin derivative of formula III or its salt with an amine compound of the formula: R1-NH2 or its salt in a solvent such as dimethylformamide or in the absence of a solvent at a reaction temperature of 20-150 deg.C. The compound of formula I is preferably administered at a daily does of about 0.00001-0.5 mg/kg.
|
