| 摘要 |
<p>Thienopyridines of formulae (I) and (II) and their acid addition salts are new: In the formulae, R1 is H or halo; R2=H or OH; and R3 and R4 are each H, 1-6C alkyl or phenyl-(1-6C)alkyl opt. substd. on the ring by >=1 halo, 1-6c alkyl or alkoxy, OH, NO2, CN or CF3. (I) and (II) are prepd. by reacting thiophenes having a -CHR2. CH(NH2).COOH substit. with HCHO, then opt. modifying the COOH and/or ring N. (I) and (II) inhibit thomboycte aggregation and have anti-sludging and antithrombotic activities. They are useful in human and veterinary medicine and suitable dosage forms contain 0.01-0.3g. Their 24-'r. Ld50 in mice is >350 mg/kg orally and typically 118-325 mg/kg intravenously.</p> |
