| 摘要 |
<p>PROBLEM TO BE SOLVED: To obtain a novel compound which antagonizes fibrinogen receptor and has high platelet coagulation-inhibitory action and high in vivo stability. SOLUTION: This novel fibrinogen receptor-antagonistic substance is a compound represented by formula I (R1 , R2 and R3 are each H, a low alkyl, amino group-protecting group; R1 and R2 may incorporate together with a N-atom to form 21 cyclic tertiary amine; X is a bridge moiety of 3-6 carbon atoms) and its salt, typically 2-aminodiphenyl-5-(3'-carboxypropoxy)-2,3-dihydro-3- oxyisoindole. The compound of formula I is obtained by starting with a compound of formula II, treating the arylmethyl group with bromine, followed by cyclization and condensation to a compound of formula III and deprotection or amidination. This preparation is useful during or after the thrombolytic treatment, platelet thrombosis and thromboembolism after the aorto-coronary artery bypass graft and for prevention of reinfarction and prevention of myocardial infarction. In addition, this substance is also useful as an inhibitor of coagulation of the blood circulating in vivo.</p> |
